The present invention provides a pharmaceutical composition comprising: a biodegradable multi-branched copolymer comprising at least three polyester arms attached to a central core which comprises a polyether, and wherein the multi-branched copolymer is substantially insoluble in aqueous solution, further comprising at least one pharmaceutically active ingredient.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
2.
METHOD FOR MORSELIZING AND/OR TARGETING PHARMACEUTICALLY ACTIVE PRINCIPLES TO SYNOVIAL TISSUE
A method of targeting to the synovial tissue biodegradable drug delivery compositions or morselizing biodegradable drug delivery compositions are described. The biodegradable drug composition comprises a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as at least one pharmaceutically active principle is disclosed.
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
An optical measurement apparatus has a microfluidic conduit having an inlet and an outlet for fluid flow through the apparatus, and a light emitter and light detector arranged such that the light path between the light emitter and the light detector coincides with the conduit. The apparatus is operable between a calibration mode and a fluid assessment mode. A reaction vessel has a chamber to contain an aqueous liquid or a gel, an injection port, and an inlet and outlet.
G01N 21/27 - ColourSpectral properties, i.e. comparison of effect of material on the light at two or more different wavelengths or wavelength bands using photo-electric detection
B01L 3/00 - Containers or dishes for laboratory use, e.g. laboratory glasswareDroppers
A method of treating or managing pain or inflammation in a patient following a total knee replacement (TKR) by administering to the knee joint of said patient biodegradable drug delivery compositions. The biodegradable drug composition comprises a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as an NSAID.
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention is directed to methods of treating psychiatric diseases and disorders comprising administering to a subject in need thereof an injectable formulation comprising risperidone, triblock and diblock copolymers wherein the concentration of the risperidone is 250-400 mg/ml and injection volume is 1 mL or less.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE (France)
UNIVERSITE DE MONTPELLIER (France)
INSTITUT REGIONAL DU CANCER DE MONTPELLIER - VAL D'AURELLE (France)
Inventor
Grizot, Sylvestre
Liu, Fang
Gros, Laurent
Bonnefoy, Nathalie
Abstract
Antineoplastic Combinations The present disclosure provides a combination comprising: (a) a first composition comprising at least one antineoplastic antibody or an antigen-binding fragment thereof; and (b) a second composition comprising at least one small-molecule antineoplastic agent; wherein at least one of the first composition and the second composition further comprises: (c) at least one polyether-polyester copolymer, wherein the copolymer has the formula: B(A)n wherein B represents a polyether and comprises polyethylene glycol (PEG), each A represents a polyester arm and n is an integer from 1 to 8; and (d) at least one organic solvent. Therapeutic methods/uses for treating solid tumors are also provided as are products and kits of parts comprising the combinations/compositions of the present disclosure.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The present invention provides a pharmaceutical composition comprising or consisting of at least one polyether-polyester copolymer, wherein the copolymer has the formula: B(A)n wherein B represents a polyether and comprises polyethylene glycol (PEG), each A represents a polyester arm and n is an integer from 1 to 8; at least one nucleophilic compound; at least one organic solvent; and up to 10% (w/w) of at least one acidic compound having a pKa(H2O) of less than 3.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention generally relates to an injectable formulation for sustained release of etonogestrel, a pharmaceutical dosage and an application device comprising such formulation, methods for preparing thereof, and use thereof for contraception.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
10.
Long acting injectable formulation comprising risperidone and biodegradable polymers
The present invention is directed to methods of treating psychiatric diseases and disorders comprising administering to a subject in need thereof at a frequency of no more than once every 28 days an injectable formulation comprising risperidone, triblock and diblock copolymers wherein the concentration of the risperidone is 250-400 mg/mL and injection volume is 1 mL or less.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
The disclosure provides pharmaceutical compositions for subcutaneous administration comprising olanzapine, and organic solvent, and a triblock copolymer, and a diblock copolymer, as well as methods of treating psychiatric diseases and disorders using such compositions.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
a biodegradable multi-branched copolymer comprising at least three polyester arms attached to a central core which comprises a polyether, and wherein the multi-branched copolymer is substantially insoluble in aqueous solution, further comprising at least one pharmaceutically active ingredient.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The disclosure provides pharmaceutical compositions for subcutaneous administration comprising olanzapine, and organic solvent, and a triblock copolymer, and a diblock copolymer, as well as methods of treating psychiatric diseases and disorders using such compositions.
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The disclosure provides pharmaceutical compositions for subcutaneous administration comprising olanzapine, and organic solvent, and a triblock copolymer, and a diblock copolymer, as well as methods of treating psychiatric diseases and disorders using such compositions.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
The present invention provides a pharmaceutical composition comprising
(a) a triblock copolymer having the formula:
The present invention provides a pharmaceutical composition comprising
(a) a triblock copolymer having the formula:
Av-Bw-Ax
wherein A is a polyester, B is polyethylene glycol, v and x are the number of repeat units ranging from 1 to 3,000 and w is the number of repeat units ranging from 3 to 300 and v=x or v≠x in an amount of from about 3 to 25 w/w % of the total composition;
(b) a diblock copolymer having the formula:
The present invention provides a pharmaceutical composition comprising
(a) a triblock copolymer having the formula:
Av-Bw-Ax
wherein A is a polyester, B is polyethylene glycol, v and x are the number of repeat units ranging from 1 to 3,000 and w is the number of repeat units ranging from 3 to 300 and v=x or v≠x in an amount of from about 3 to 25 w/w % of the total composition;
(b) a diblock copolymer having the formula:
Cy-Az
Wherein A is a polyester, C is an end-capped polyethylene glycol and y and z are the number of repeat units with y ranging from 2 to 250 and z ranging from 1 to 3,000 in an amount of from about 3 to 35 w/w % of the total composition;
(c) a therapeutic protein which is an Interleukin-1 antagonist in an amount of from about 0.5 to 25 w/w % of the total composition;
(d) optionally one or more stabilizer compounds in an amount of from about 0.25 to 15 w/w % of the total composition; and
(e) organic solvent in an amount of from about 50 to 80 w/w % of the total composition.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A device for controlling flow of a fluid, comprising: a first valve comprising: a selectively openable inlet; an opening; a selectively openable outlet, arranged such that fluid may enter the first valve through the inlet, exit the first valve through the opening, enter the first valve through the opening and exit the first valve through the outlet; a first sensor for detecting a fluid; a second sensor for detecting a fluid, the first sensor and second sensor in fluid communication with the first valve via the opening; a controller for receiving signals from the first sensor and second sensor and for controlling opening and closing of the inlet and outlet in response to receiving said signals, arranged to allow, in use, a fluid to flow through the device by flowing: —into the first valve through the inlet of the first valve; —out of the first valve through the opening of the first valve; —past the first sensor for detecting a fluid; —to the second sensor for detecting a fluid; —into the first valve through the opening of the first valve; —out of the first valve through the outlet of the first valve.
The present invention is directed to methods of treating psychiatric diseases and disorders comprising administering to a subject in need thereof an injectable formulation comprising risperidone, triblock and diblock copolymers wherein the concentration of the risperidone is 250-400 mg/mL and injection volume is 1 mL or less.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
19.
Long Acting Injectable Formulation Comprising Risperidone and Biodegradable Polymers
The present invention is directed to methods of treating psychiatric diseases and disorders comprising administering to a subject in need thereof at a frequency of no more than once every 28 days an injectable formulation comprising risperidone, triblock and diblock copolymers wherein the concentration of the risperidone is 250-400 mg/mL and injection volume is 1 mL or less.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
The present invention provides a pharmaceutical composition comprising
(a) a triblock copolymer having the formula:
The present invention provides a pharmaceutical composition comprising
(a) a triblock copolymer having the formula:
PLAv-PEGw-PLAx
wherein v and x are the number of repeat units ranging from 1 to 3,000 and w is the number of repeat units ranging from 3 to 300 and v=x or v≠x in an amount of 22 to 34 w/w % of the total composition;
(b) a diblock copolymer having the formula:
The present invention provides a pharmaceutical composition comprising
(a) a triblock copolymer having the formula:
PLAv-PEGw-PLAx
wherein v and x are the number of repeat units ranging from 1 to 3,000 and w is the number of repeat units ranging from 3 to 300 and v=x or v≠x in an amount of 22 to 34 w/w % of the total composition;
(b) a diblock copolymer having the formula:
mPEGy-PLAz
wherein y and z are the number of repeat units with y ranging from 2 to 250 and z ranging from 1 to 3,000 in an amount of 5 to 9 w/w % of the total composition;
(c) tacrolimus or a pharmaceutically acceptable salt, hydrate or solvate thereof in an amount of 8 to 32 w/w % of the total composition; and
(d) organic solvent in an amount of 30 to 62 w/w % of the total composition.
A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
21.
Methods and Compositions for the Prophylactic Treatment of SARS-CoV-2 virus (COVID-19)
A method of prophylactically treating COVID-19 in subject who is at high risk for exposure to SARS-CoV-2 virus or who is been recently exposed to SARS-CoV-2, but who tests negative for the virus, by administering to said subject an effective dose of ivermectin to inhibit one or symptoms of SARS-CoV-2 virus.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
UNIVERSITÉ DE MONTPELLIER (France)
Inventor
Dawson, Harry
Delamare, Romain
Etienne, Pascal
Calas-Etienne, Sylvie
Abstract
The invention provides a silica aerogel comprising one or more channels, each channel having a surface roughness of from about 0.1 to about 10 µm, an internal diameter in the range of from about 100 µm to about 2900 µm and a length of from about 5mm to about 200 mm.
B01J 13/00 - Colloid chemistry, e.g. the production of colloidal materials or their solutions, not otherwise provided forMaking microcapsules or microballoons
23.
Method for morselizing and/or targeting pharmaceutically active principles to synovial tissue
A method of targeting to the synovial tissue biodegradable drug delivery compositions or morselizing biodegradable drug delivery compositions are described. The biodegradable drug composition comprises a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as at least one pharmaceutically active principle is disclosed.
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
The present invention provides a pharmaceutical composition comprising:
a multi-branched copolymer comprising at least three polyester arms, wherein the polyester is poly(ε-caprolactone-co-lactic acid), attached to a central core which comprises a polyether, and wherein the multi-branched copolymer is substantially insoluble in aqueous solution, further comprising at least one pharmaceutically active ingredient, and a pharmaceutically acceptable organic solvent in an amount of at least 20% (w/w %) of the total composition.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A biodegradable drug delivery compositions comprising a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as a pharmaceutically active principle is disclosed.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
C08L 67/04 - Polyesters derived from hydroxy carboxylic acids, e.g. lactones
C08G 63/66 - Polyesters containing oxygen in the form of ether groups
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 31/00 - Medicinal preparations containing organic active ingredients
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention provides a pharmaceutical composition comprising or consisting of at least one polyether-polyester copolymer, wherein the copolymer has the formula: B(A)n wherein B represents a polyether and comprises polyethylene glycol (PEG), each A represents a polyester arm and n is an integer from 1 to 8; at least one nucleophilic compound; at least one organic solvent; and up to 10% (w/w) of at least one acidic compound having a pKa(H2O) of less than 3.
A61K 31/00 - Medicinal preparations containing organic active ingredients
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
28.
BIODEGRADABLE DRUG DELIVERY FOR HYDROPHOBIC COMPOSITIONS
A biodegradable drug delivery compositions comprising a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as at least one pharmaceutically active principle or hydrophobic active principle such as medroxyprogesterone acetate, levonorgestrel, cyclosporine, progesterone or bupivacaine is disclosed.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
The present invention generally relates to an injectable formulation for sustained release of etonogestrel, a pharmaceutical dosage and an application device comprising such formulation, methods for preparing thereof, and use thereof for contraception.
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 9/00 - Medicinal preparations characterised by special physical form
The present invention generally relates to an injectable formulation for sustained release of etonogestrel, a pharmaceutical dosage and an application device comprising such formulation, methods for preparing thereof, and use thereof for contraception.
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention is directed to methods of treating psychiatric diseases and disorders comprising administering to a subject in need thereof an injectable formulation comprising risperidone, triblock and diblock copolymers wherein the concentration of the risperidone is 250-400 mg/mL and injection volume is 1 mL or less.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
A device for controlling flow of a fluid, comprising: a first valve comprising: a selectively openable inlet; an opening; a selectively openable outlet, arranged such that fluid may enter the first valve through the inlet, exit the first valve through the opening, enter the first valve through the opening and exit the first valve through the outlet; a first sensor for detecting a fluid; a second sensor for detecting a fluid, the first sensor and second sensor in fluid communication with the first valve via the opening; a controller for receiving signals from the first sensor and second sensor and for controlling opening and closing of the inlet and outlet in response to receiving said signals, arranged to allow, in use, a fluid to flow through the device by flowing: - into the first valve through the inlet of the first valve; - out of the first valve through the opening of the first valve; - past the first sensor for detecting a fluid; - to the second sensor for detecting a fluid; - into the first valve through the opening of the first valve; - out of the first valve through the outlet of the first valve
vwxyzz Wherein A is a polyester, C is an end-capped polyethylene glycol and y and z are the number of repeat units with y ranging from 2 to 250 and z ranging from 1 to 3,000 in an amount of from about 3 to 35 w/w% of the total composition; (c) a therapeutic protein which is an lnterleukin-1 antagonist in an amount of from about 0.5 to 25 w/w % of the total composition; (d) optionally one or more stabilizer compounds in an amount of from about 0.25 to 15 w/w % of the total composition; and (e) organic solvent in an amount of from about 50 to 80 w/w % of the total composition.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
34.
LONG ACTING INJECTABLE FORMULATION COMPRISING RISPERIDONE AND BIODEGRADABLE POLYMERS
The present invention is directed to methods of treating psychiatric diseases and disorders comprising administering to a subject in need thereof at a frequency of no more than once every 28 days an injectable formulation comprising risperidone, triblock and diblock copolymers wherein the concentration of the risperidone is 250-400 mg/mL and injection volume is 1 ml or less.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
The present invention provides a pharmaceutical composition comprising (a) a triblock copolymer having the formula: PLAv-PEGw-PLAx wherein v and x are the number of repeat units ranging from 1 to 3,000 and w is the number of repeat units ranging from 3 to 300 and v=x or v≠x in an amount of 22 to 34 w/w % of the total composition; (b) a diblock copolymer having the formula: mPEGy-PLAz wherein y and z are the number of repeat units with y ranging from 2 to 250 and z ranging from 1 to 3,000 in an amount of 5 to 9 w/w% of the total composition; (c) tacrolimus or a pharmaceutically acceptable salt, hydrate or solvate thereof in an amount of 8 to 32 w/w % of the total composition; and (d) organic solvent in an amount of 30 to 62 w/w % of the total composition.
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C08G 63/664 - Polyesters containing oxygen in the form of ether groups derived from hydroxycarboxylic acids
C08L 67/04 - Polyesters derived from hydroxy carboxylic acids, e.g. lactones
36.
METHODS AND COMPOSITIONS FOR THE PROPHYLACTIC TREATMENT OF SARS-COV-2 VIRUS (COVID-19)
A method of prophylactically treating COVID-19 in subject who is at high risk for exposure to SARS-CoV-2 virus or who is been recently exposed to SARS-CoV-2, but who tests negative for the virus, by administering to said subject an effective dose of ivermectin to inhibit one or symptoms of SARS-CoV-2 virus.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 31/00 - Medicinal preparations containing organic active ingredients
The present invention provides a pharmaceutical composition comprising: a biodegradable multi-branched copolymer comprising at least three polyester arms attached to a central core which comprises a polyether, and wherein the multi-branched copolymer is substantially insoluble in aqueous solution, further comprising at least one pharmaceutically active ingredient.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention provides a pharmaceutical composition comprising: a multi-branched copolymer comprising at least three polyester arms, wherein the polyester is poly(ε-caprolactone-co-lactic acid), attached to a central core which comprises a polyether, and wherein the multi-branched copolymer is substantially insoluble in aqueous solution, further comprising at least one pharmaceutically active ingredient, and a pharmaceutically acceptable organic solvent in an amount of at least 20% (w/w%) of the total composition.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
C08G 63/664 - Polyesters containing oxygen in the form of ether groups derived from hydroxycarboxylic acids
C08L 67/00 - Compositions of polyesters obtained by reactions forming a carboxylic ester link in the main chainCompositions of derivatives of such polymers
39.
Method for morselizing and/or targeting pharmaceutically active principles to synovial tissue
A method of targeting to the synovial tissue biodegradable drug delivery compositions or morselizing biodegradable drug delivery compositions are described. The biodegradable drug composition comprises a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as at least one pharmaceutically active principle is disclosed.
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention is directed to methods of treating psychiatric diseases and disorders comprising administering to a subject in need thereof an injectable formulation comprising risperidone, triblock and diblock copolymers wherein the concentration of the risperidone is 250-400 mg/mL and injection volume is 1 mL or less.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
The present invention is directed to methods of treating psychiatric diseases and disorders comprising administering to a subject in need thereof an injectable formulation comprising risperidone, triblock and diblock copolymers wherein the concentration of the risperidone is 250-400 mg/mL and injection volume is 1 mL or less.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/00 - Drugs for disorders of the nervous system
The present invention provides a pharmaceutical composition comprising: a biodegradable multi-branched copolymer comprising at least three polyester arms attached to a central core which comprises a polyether, and wherein the multi-branched copolymer is substantially insoluble in aqueous solution, further comprising at least one pharmaceutically active ingredient.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention provides a pharmaceutical composition comprising: a biodegradable multi-branched copolymer comprising at least three polyester arms attached to a central core which comprises a polyether, and wherein the multi-branched copolymer is substantially insoluble in aqueous solution, further comprising at least one pharmaceutically active ingredient.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
44.
Biodegradable block copolymer drug delivery composition
z wherein A is a polyester and C is an end-capped polyethylene glycol and y=2 to 250 and z=1 to 3,000; and wherein the mixture comprises at least one (a) and at least one (b); and the weight ratio between (a) and (b) is 1:19 to 5:1; and for at least one of the copolymers according to (a) or (b) A is poly(lactic-co-glycolic acid) (PLGA); and (ii) at least one pharmaceutically active ingredient.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
C08G 63/664 - Polyesters containing oxygen in the form of ether groups derived from hydroxycarboxylic acids
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
z wherein A is a polyester and C is an end-capped polyethylene glycol and y and z are the number of repeat units with y=2 to 250 and z=1 to 3,000; wherein the weight ratio between (a) and (b) is 1:19 to 5:1; and for at least one of the copolymers according to (a) or (b) A is poly(ε-caprolactone-co-lactide); and (c) at least one pharmaceutically active ingredient.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
C08G 63/664 - Polyesters containing oxygen in the form of ether groups derived from hydroxycarboxylic acids
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
z wherein A is a polyester and C is an end-capped polyethylene glycol and y and z are the number of repeat units with y=2 to 250 and z=1 to 3,000; and wherein the mixture comprises at least one (a) and at least one (b); and the weight ratio between (a) and (b) is 1:19 to 5:1; and (ii) at least one pharmaceutically active ingredient.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
C08G 63/664 - Polyesters containing oxygen in the form of ether groups derived from hydroxycarboxylic acids
C08L 67/04 - Polyesters derived from hydroxy carboxylic acids, e.g. lactones
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
The present invention provides a biodegradable drug delivery composition comprising: (i) a mixture of at least three different block copolymers, wherein each block copolymer is: (a) a biodegradable triblock copolymer having the formula: A v-B w-A x wherein A is a polyester and B is polyethylene glycol and v and x are the number of repeat units from 1 to 3,000 and w is the number of repeat units from 3 to 300 and v=x or v.noteq.x; or (b) a biodegradable diblock copolymer having the formula: C y-A z wherein A is a polyester and C is an end-capped polyethylene glycol and y and z are the number of repeat units with y = 2 to 250 and z = 1 to 3,000; and wherein the mixture comprises at least one (a) and at least one (b); and the weight ratio between (a) and (b) is 1:19 to 5:1; and (ii) at least one pharmaceutically active ingredient. [Continued on next page]
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
C08G 63/00 - Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
C08L 67/04 - Polyesters derived from hydroxy carboxylic acids, e.g. lactones
vwxyzz wherein A is a polyester and C is an end-capped polyethylene glycol and y and z are the number of repeat units with y = 2 to 250 and z = 1 to 3,000; and wherein the mixture comprises at least one (a) and at least one (b); and the weight ratio between (a) and (b) is 1:19 to 5:1; and (ii) at least one pharmaceutically active ingredient.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
C08G 63/00 - Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
C08L 67/04 - Polyesters derived from hydroxy carboxylic acids, e.g. lactones
vwxyzz wherein A is a polyester and C is an end-capped polyethylene glycol and y and z are the number of repeat units with y =2 to 250 and z =1 to 3,000; wherein the weight ratio between (a) and (b) is 1:19 to 5:1; and for at least one of the copolymers according to (a) or (b) A is poly(ε-caprolactone-co-lactide); and (c) at least one pharmaceutically active ingredient.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
C08G 63/00 - Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
C08L 67/04 - Polyesters derived from hydroxy carboxylic acids, e.g. lactones
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
vwxyzz wherein A is a polyester and C is an end-capped polyethylene glycol and y = 2 to 250 and z =1 to 3,000; and wherein the mixture comprises at least one (a) and at least one (b); and the weight ratio between (a) and (b) is 1:19 to 5:1; and for at least one of the copolymers according to (a) or (b) A is poly(lactic-co-glycolic acid) (PLGA); and (ii) at least one pharmaceutically active ingredient.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
C08G 63/00 - Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
C08L 67/04 - Polyesters derived from hydroxy carboxylic acids, e.g. lactones
A method of targeting to the synovial tissue biodegradable drug delivery compositions or morselizing biodegradable drug delivery compositions are described. The biodegradable drug composition comprises a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as at least one pharmaceutically active principle is disclosed.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
52.
A METHOD FOR MORSELIZING AND/OR TARGETING PHARMACEUTICALLY ACTIVE PRINCIPLES TO SYNOVIAL TISSUE
A method of targeting to the synovial tissue biodegradable drug delivery compositions or morselizing biodegradable drug delivery compositions are described. The biodegradable drug composition comprises a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as at least one pharmaceutically active principle is disclosed.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
Inventor
Gaudriault, Georges
Heurteaux, Catherine
Mazella, Jean
Borsotto, Marc
Moha Ou Maati, Hamid
Veyssiere, Julie
Abstract
Compositions, pharmaceutical compositions and biodegradable pharmaceutical compositions containing at least one analog of spadin or at least one analog of a propeptides of spadin or mixtures thereof are described. Methods for treating depression using the analogs of spadin or analogs of propeptides of spadin or mixtures thereof, as well as methods for blocking TREK-1 channel activity are also disclosed.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
54.
BIODEGRADABLE DRUG DELIVERY FOR HYDROPHOBIC COMPOSITIONS
A biodegradable drug delivery compositions comprising a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as at least one pharmaceutically active principle or hydrophobic active principle such as medroxyprogesterone acetate, levonorgestrel, cyclosporine, progesterone or bupivacaine is disclosed.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
55.
BIODEGRADABLE DRUG DELIVERY FOR HYDROPHOBIC COMPOSITIONS
A biodegradable drug delivery compositions comprising a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as at least one pharmaceutically active principle or hydrophobic active principle such as medroxyprogesterone acetate, levonorgestrel, cyclosporine, progesterone or bupivacaine is disclosed.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A biodegradable drug delivery compositions comprising a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as at least one pharmaceutically active principle or hydrophobic active principle such as medroxyprogesterone acetate, levonorgestrel, cyclosporine, progesterone or bupivacaine is disclosed.
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A biodegradable drug delivery compositions comprising a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as a pharmaceutically active principle is disclosed.
A biodegradable drug delivery compositions comprising a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as a pharmaceutically active principle is disclosed.
A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A biodegradable drug delivery compositions comprising a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as a pharmaceutically active principle is disclosed.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers