The present invention provides stable pharmaceutical antibody formulations, including liquid formulations and lyophilized formulations, comprising an anti-IL-4/anti-IL-13 bispecific antibody, a polyaminoacid consisting of glutamic acid or aspartic acid or both randomly grafted with Vitamin E, and a cryoprotectant, wherein the formulation has a salt concentration of 50 m M or less. The present invention also provides stable pharmaceutical antibody formulations, including liquid formulations and lyophilized formulations, comprising an anti-IL-4/anti-IL-13 bispecific antibody, a polyaminoacid consisting of glutamic acid or aspartic acid or both randomly grafted with Vitamin E, a cryoprotectant, and a buffering system, wherein the pH of the formulation is about pH 7, and wherein the formulation has a salt concentration of 50 mM or less. The formulations may, optionally, further comprise a surfactant, or a stabilizing agent, or both. The present invention includes methods for making such formulations. The formulations can be used in the treatment of various diseases.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
2.
COMPOSITION FOR CONTROLLED RELEASE OF BUPRENORPHINE
The present invention relates to a novel aqueous liquid pharmaceutical composition for controlled release of buprenorphine or of a buprenorphine analogue, comprising at least one low-water-solubility prodrug of said buprenorphine or of a buprenorphine analogue, and at least one polymer which has a linear backbone, chosen from polyglutamates, polyaspartates, poly(meth)acrylates and polysaccharides, onto which one or more hydrophobic groups are grafted.
The present invention relates to a novel solid composition, useful for treating hepatitis, in particular hepatitis C, comprising at least one interferon alpha and at least one grafted poly(glutamic acid) having an average molar mass ranging from 26,000 to 40,000g/mol, preferably approximately 33,000g/mol and carrying grafts of alpha- tocopherol at an average molar grafting rate ranging from 4.5 to 5.5%, preferably approximately 5%, the interferon alpha and said grafted poly(glutamic acid) being present in a grafted poly(glutamic acid)/interferon alpha weight ratio ranging from 21 to 125. It also relates to the use of such a solid composition for the preparation of a liquid composition by the addition of an aqueous liquid.
The present invention relates to a novel process for preparing nanoparticles having a diameter of less than or equal to 500 nm, which comprises bringing a solution (1) comprising nanoparticles of a first polyelectrolyte in the charged state, bearing hydrophobic side groups, into contact with (2) at least a second polyelectrolyte which has a polarity opposite to that of the first polyelectrolyte, characterized in that the ratio Z of the number of cationic groups to the number of anionic groups in the mixture of the two polyelectrolytes is between 0.1 and 0.75 or between 1.3 and 2, and the total concentration by weight C of polyelectrolytes is strictly less than 2 mg/g of the mixture.
A61K 31/00 - Medicinal preparations containing organic active ingredients
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 39/00 - Medicinal preparations containing antigens or antibodies
B82Y 5/00 - Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
The present invention relates to novel nanoparticles consisting of at least one active agent and at least two polyelectrolytes having opposite polarities, characterised in particular in that at least one of the two polyelectrolytes has hydrophobic lateral groupings and at least one of the two polyelectrolytes has polyalkylene glycol lateral groupings, said nanoparticles having a mean diameter of 10 to 100 nm and including an amount of polyalkylene glycol groupings such that the weight ratio (w PAG) of polyalkylene glycol relative to the total polymer is no lower than 0.05.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
B82Y 5/00 - Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
The present invention relates to novel amphiphilic polymers comprising hydrophobic groups and methionine groups. The invention also relates to compositions with a regulated release profile comprising said polymers, combined in a non-covalent manner with an active agent, in particular an active agent such as a peptide or a protein comprising at least one oxidation-sensitive amino acid in the sequence thereof.
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
C08B 15/00 - Preparation of other cellulose derivatives or modified cellulose
C08B 31/00 - Preparation of chemical derivatives of starch
C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof
The present invention relates to a novel family of acrylic and/or methacrylic polymers, including alpha-tocopherol grafts, suitable for forming nanoparticles in an aqueous medium with neutral pH. The invention also relates to the use of such nanoparticles, associated in a non-covalent manner with an active agent, in particular an active agent with low or medium solubility in water, in order to convey, make soluble and/or increase the solubility in water of said active agent.
C08F 220/30 - Esters containing oxygen in addition to the carboxy oxygen containing aromatic rings in the alcohol moiety
C08F 220/58 - Amides containing oxygen in addition to the carbonamido oxygen
A61K 8/81 - Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
8.
ANTI-MISUSE SOLID ORAL DOSAGE FORM PROVIDED HAVING A MODIFIED SPECIFIC RELEASE PROFILE
The present invention relates to a solid oral dosage form, enabling the modified release of at least one active principle, containing at least microparticles containing said active agent and at least one viscosifying agent in a form that is isolated from said microparticles of the active agent, characterised in that said microparticles have an average diameter of 100 to 600 μm, and are made up of a core containing at least said active principle and coated with at least one coating layer, said core being made up of a supporting particle covered by a layer including at least said active agent, and said coating layer being made of a material made up of at least 25 to 70 wt % of at least one water-insoluble polymer A relative to the total weight of said coating layer, 30 to 75 wt % of at least one polymer B that is not soluble in water with a pH of less than 5 but is soluble in water with a pH of more than 7 relative to the total weight of said coating layer, and 0 to 25 wt % of at least one plasticiser relative to the total weight of said coating layer, said polymers A and B having a weighted ratio of polymer(s) B/polymer(s) A of 0.25 to 4, said coating layer accounting for at least 35 wt % relative to the total weight of said microparticle.
The present invention provides N-phosphonomethylglycine guanidine salts. The N-phosphonomethylglycine guanidine salts have improved herbicidal efficacy over glyphosate alone. The present invention also provides guanidine compounds and salts thereof.
A01N 57/20 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-carbon bonds containing acyclic or cycloaliphatic radicals
C07C 279/04 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
C07C 279/12 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 279/20 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups containing any of the groups X being a hetero atom, Y being any atom, e.g. acylguanidines
The present invention provides N-phosphonomethylglycine guanidine salts. The N-phosphonomethylglycine guanidine salts have improved herbicidal efficacy over glyphosate alone. The present invention also provides guanidine compounds and salts thereof.
A01N 57/20 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-carbon bonds containing acyclic or cycloaliphatic radicals
C07C 279/04 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
C07C 279/12 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 279/20 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups containing any of the groups X being a hetero atom, Y being any atom, e.g. acylguanidines
11.
METHOD FOR PREPARING HOLLOW PARTICLES, AND USES THEREOF
The invention relates to a method for preparing hollow particles, including: 1) spray-depositing, in particular in a fluidized air bed and onto a substrate that is partially soluble in a liquid medium M, a coating containing: 40 to 100 wt % of at least one compound that is insoluble in water having a pH of less than 5 and that comprises at least one polymer; and 60 to 0 % of at least one water-soluble compound; 2) extracting a portion of the substrate in the medium M; and 3) drying the particles obtained in step 2. The invention also relates to the resulting hollow particles and to the uses thereof, in particular in floating pharmaceutical compositions.
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
The invention relates to a pharmaceutical composition that includes a plurality of controlled-release coated microparticles, each comprising a floating core, at the surface of which a layer containing at least one active principle is deposited, said layer being covered by a controlled-release coating, characterized in that said floating core consists of cellulose phthalate acetate and has a bulk density of less than or equal to 0.6 g/mL, and in that said coated microparticles have a density of less than or equal to 0.7 g/mL.
The present invention relates to a composition including at least one active agent with low water solubility, said active agent being present in a form non-covalently in combination with nanoparticles made of at least one polymer POM of formula (I), and in which said active agent is present at a rate of at least 5 μmol/g of POM. The invention also relates to the use of such nanoparticles, non-covalently in combination with an active agent, with a view to increasing the water solubility of said active agent.
The present invention aims to provide novel micropariculate oral drug forms for the modified release of active principle(s), particularly of the protein or peptide nature. The invention also relates to the particularly therapeutic or cosmetic uses of said microparticulate oral drug forms.
The invention relates to a solid form intended for the oral administration of at least one active agent and capable of ensuring a dual mechanism for the release of said active agent, whereby the first release is conditioned by time and the second release is conditioned by pH. The invention is characterised in that the active agent is present in the form of a microparticulate system, the microparticulates of which include a core which is made up entirely or partly of said active agent and coated with at least one layer which conditions the release profile of the active agent and which is formed by a material containing at least: (i) 25% to 75% by weight, relative to the total weight of the coating, of at least a polymer A that is insoluble in the gastrointestinal fluids, (ii) 25% to 75% by weight, relative to the total weight of the coating, of at least a polymer B that has a solubilisation pH value in the pH range of from 5 to 7, and (iii) 0 to 25% by weight, relative to the total weight of the coating, of at least one plasticiser, said polymers A and B being present in a polymer(s) B/polymer(s) A weight ratio that is at least equal to 0.25. The invention also relates to a method for preparing this solid form and the corresponding microparticulates.
The present invention relates to novel polyelectrolyte polymer particles for transporting an active principle (AP), in particular a protein and peptide active principle, and also to novel modified-release pharmaceutical formulations containing said AP microparticles. These novel AP-loaded particles release the AP over a prolonged duration of several days, or even several weeks. The invention relates, in a first aspect, to particles comprising: a) a first polyelectrolyte polymer (PE1) in the charged state, bearing side hydrophobic groups (HG), said first polyelectrolyte polymer (PE1) spontaneously forming, in water, a colloidal solution of particles at at least a value pHm of the pH between 3 and 8; b) a second polyelectrolyte polymer (PE2) of opposite polarity to that of the first polyelectrolyte polymer (PE1), said second polyelectrolyte polymer (PE2) forming, in water, a solution or a colloidal solution at at least said pHm value of the pH; c) at least one active principle (AP) combined non-covalently with the particles of the colloidal solution of the first polyelectrolyte polymer (PE1); said particles being obtained by mixing, at a pH equal to pHm, of the first polyelectrolyte polymer (PE1) in the form of a colloidal solution of particles combined with the active principle (AP) with the second polyelectrolyte polymer (PE2) in the form of a solution or a colloidal solution. The invention also relates to the process for preparing these particles, a pharmaceutical formulation comprising such particles and a process for preparing medications.
The present invention relates to novel pharmaceutical formulations for the prolonged release of active principle (AP), which make it possible to release the AP over a prolonged duration of several days, or even several weeks. The invention relates, in a first aspect, to a liquid formulation, comprising at least one active principle (AP) and an aqueous suspension, based on colloidal particles of a polymer (PO), characterized in that it satisfies the following four conditions: (a) the polymer (PO) is a polyamino acid comprising glutamic residues, - certain glutamic residues bearing a pendant cationic group (CG), the cationic groups being identical to or different from one another, - other glutamic residues bearing a pendant hydrophobic group (HG), said hydrophobic groups (HG) being identical to or different from one another; (b) the value pHf of the pH of said formulation is between 3.0 and 6.5; (c) for the value pHf of the pH, the polymer (PO) forms a colloidal solution which combines spontaneously and non-covalently with the active principle (AP); (d) 1 ml of said formulation precipitates during mixing with a volume of 1 ml of a test buffer solution Tp. The invention also relates to the process for preparing this formulation and a process for preparing medications.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
18.
POLYGLUTAMIC ACIDS FUNCTIONALIZED BY CATIONIC GROUPS AND HYDROPHOBIC GROUPS AND APPLICATIONS THEREOF, IN PARTICULAR THERAPEUTIC APPLICATIONS THEREOF
The present invention relates to novel biodegradable materials based on modified polyamino acids that can be used, in particular, for the vectorization of active principle(s) (PA). The invention also relates to novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on these polyamino acids. The objective of the invention is to provide a novel polymer starting material that is capable of being used for the AP vectorization and that makes it possible to optimally satisfy all the specifications required in the case in point: biocompatibility, biodegradability, ability to associate easily with numerous active principles or to dissolve them, and to release these active principles in vivo. This objective is achieved by the present invention, which relates to novel polyglutamates modified by cationic groups that, if they can be deprotonated, have a pKa greater than or equal to 7, and by hydrophobic groups comprising from 8 to 30 carbon atoms. These polyglutamates modified by cationic groups are capable of being easily and economically converted into particles for the vectorization of active principles, these particles being themselves capable of forming stable aqueous colloidal suspensions. These modified polyglutamates have the advantage of being less viscous than other similar polymers, while retaining an ability to associate proteins such as insulin. Some are soluble in water at acid pH and become insoluble at physiological pH (7.4) and should therefore, during a subcutaneous injection, precipitate at the injection site.
C08G 69/48 - Polymers modified by chemical after-treatment
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
19.
DISPERSION OF POLYAMINO ACIDS IN A CONTINUOUS LIPID PHASE
The invention relates to injectable pharmaceutical compositions featuring sustained release of at least one active principle, and comprising at least one active principle in an aqueous phase of amphiphilic polymer, in disperse form in a continuous lipid phase. The composition takes the form of a water-in-oil emulsion comprising: a pharmaceutically acceptable lipid continuous phase; an aqueous disperse phase containing at least one amphiphilic polymer and at least one active principle which is not covalently bonded to said amphiphilic polymer; and at least one pharmaceutically acceptable surfactant.
A61K 47/30 - Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
20.
MICROPARTICLES BASED ON AN AMPHIPHILIC COPOLYMER AND ON ACTIVE INGREDIENT(S) WITH MODIFIED RELEASE AND PHARMACEUTICAL FORMULATIONS CONTAINING SAME
The present invention relates to novel microparticles of amphiphilic polyamino acids that transport active ingredient(s) - AI(s) -, in particular protein and peptide active ingredient(s), and also to novel modified-release pharmaceutical formulations containing said microparticles of AI. The objective of the invention is to develop novel microparticles loaded with AI, obtained by aggregation of nanoparticles of amphiphilic polyamino acids, and having improved properties, in particular in dry solid form, with regard to their capacity for dispersion and, as regards the reconstituted suspension, with regard to its stability and its ability to be readily handled and injected. In a first aspect, the invention relates to microparticles of amphiphilic polyamino acid (PO) containing at least one AI (associated noncovalently), spontaneously forming a colloidal suspension of nanoparticles in water, at pH 7.0, under isotonic conditions; wherein said microparticles are characterized a. in that they are obtained by atomization of a colloidal suspension or solution of PO comprising at least one AI, b. by a size of between 0.5 and 100 쎽m, and c. in that they are dispersible in a colloidal suspension. The invention also relates to the method for preparing these microparticles, to a liquid formulation comprising a suspension of these PO/AI microparticles, to a method and a kit for reconstituting this formulation, and to a dry form of this formulation.
The present invention concerns new pharmaceutical formulations based on aqueous colloidal suspensions for sustained release of active ingredient(s) -AI - in particular, protein(s) and peptide(s), as well as the applications, especially therapeutic, of these formulations. This formulation comprises an aqueous colloidal suspension with low viscosity based on micrometric particles of amphiphilic polymer PO that is biodegradable, hydrosoluble and carrying hydrophobic groups (HG) - alpha-tocopherol- and ionizable hydrophilic groups (IG) -Glu -, ionized at least in part, said particles being suitable for spontaneously combining non-covalently with an AI at pH = 7.0 under isotonic conditions; and with a size between 0.5 and 100 쎽m. This suspension contains multivalent ions (Mg++) with a polarity opposite that of IH groups of the PO, the ratio r fulfilling the formula (A) where n is the valence of said multivalent ions, [MI] is the molar of multivalent ions, [IG] is the molar concentration of ionizable groups IG, is between 0.3 and 10.
Modified-release multimicroparticulate pharmaceutical form capable of maintaining the modified release of the active ingredient in an alcoholic solution and of withstanding attempts at misuse.
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 9/52 - Sustained or differential release type
A61P 25/04 - Centrally acting analgesics, e.g. opioids
23.
MICROPARTICULATE PHARMACEUTICAL FORMS RESISTANT TO IMMEDIATE RELEASE OF THE ACTIVE PRINCIPLE IN THE PRESENCE OF ALCOHOL
The invention aims at minimizing the risks of release of the dose associated with the concurrent consumption of alcohol and certain pharmaceutical or dietary forms with modified release. The invention concerns an oral form comprising reservoir-type microparticles, with modified release of at least one active principle. The invention is characterized in that it is resistant to the immediate release of the dose of active principle in the presence of alcohol. In particular, the inventive oral form is characterized in that the releasing time of 50% of the active principle, in an alcohol-containing solution is not reduced by more than 3 times compared to the releasing time of 50% of the active principle in an alcohol-free aqueous medium. The form comprises an agent D which is a pharmaceutically acceptable compound of which the hydrating or solvating speed and capacity is higher in an alcohol-free aqueous medium than in an alcohol-containing solution.
The invention relates to injectable long-acting insulin formulations for the treatment of type I and II diabetes in humans and animals. The essential objective of the invention is to provide a long-acting insulin formulation in the form of a colloidal suspension: which makes it possible to readily fill a syringe through a small-diameter needle (for example, of 29G, 30G or 31G gauge) and/or which is readily injectable through a small-diameter needle (for example, of 29G, 30G or 31G gauge), without harming the therapeutic efficacy of the insulin. To achieve this objective, the invention relates to an aqueous and stable colloidal formulation of nanoparticles of at least one poly(Leu-bloc-Glu), loaded with insulin, in which the pH is such that: 6.0 ≤ pH ≤ 7.0, characterized in that it comprises at least one magnesium salt in an amount such that: the osmolarity Osm (in mOsmol) is such that: 270 ≤ Osm ≤ 600, the viscosity v (in mPa.s), measured according to a procedure Mv, is such that: v ≤ 15, preferably v ≤ 10, and even more preferably v ≤ 5; the concentration (in mg/ml) of poly(Leu-bloc-Glu) is between 30 and 70, preferably between 38 and 65.
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 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
25.
ANTI-MISUSE MICROPARTICULATE ORAL PHARMACEUTICAL FORM
The present invention relates to solid microparticulate oral pharmaceutical forms which have a composition and a structure that prevents the misuse of the active pharmaceutical ingredient (API) contained therein. The aim of the present invention is to prevent the improper use of solid oral drugs for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. In other words, it is a question of preventing the voluntary or involuntary misuse of solid oral drugs. The invention relates to a solid oral pharmaceutical form, characterized in that it comprises anti-misuse means, in that at least part of the API that it contains is contained in coated microparticles for modified API release, and in that the coated API microparticles comprise a coating layer (Ra), which ensures modified release of the API and which, simultaneously, confers resistance to crushing on the coated API microparticles, so as to prevent misuse.
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
A61P 25/04 - Centrally acting analgesics, e.g. opioids
The invention relates to novel biodegradable materials based on modified polyomino acids and suitable, in particular, for vectoring active substance(s) (AS). Said invention also relates to novel pharmaceutical, cosmetic, dietary or plant protective compositions which are based on said polyamino acids. The aim of said invention is to provide a novel polymer raw material usable for vectoring the AS and capable to optimally meet all specification in this area: biocompatibility, biodegradability, ability to become easily associated with many active substances or to solubilise them and to release said active substances in vivo. The aim is attained by the invention which relates to novel polyglutomates modified by histidine derivatives and hydrophobic groups containing from 8 to 30 carbon atoms. Said polyglutomates modified by histidine derivatives are soluble with pH lower than 5 and are easily and economically convertible into active substance vectorisation particles which are able to form stable aqueous colloidal suspensions. On the contrary, said modified polyglutamates are insoluble in water with a physiological pH (7, 4), and thereby have to be precipitated on an injection site in the case of a subcutaneous injection.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
27.
MICROPARTICLES WITH MODIFIED RELEASE OF AT LEAST ONE ACTIVE PRINCIPLE AND ORAL GALENIC FORM COMPRISING SAME
The invention concerns microparticulate systems with modified release of oral active principle(s). The invention aims at providing a novel multimicroparticulate galenic system operating in accordance with a dual time-dependent and pH-dependent release mechanism, which enables the following three parameters to be adjusted independently of one another: a) the latent period preceding the release of the active principle in the stomach; b) the pH triggering the release of the active principle in the intestine; c) the release speed of the active principle. This is achieved through the use of coated microparticles made from particles of active principle each coated with two coating films A and B. A comprises: film-forming (co)polymer (A1) insoluble in fluids of the gastrointestinal tract; ethylcellulose (co)polymer (A2) soluble in fluids of the gastrointestinal tract; plasticizing polyvinylpyrrolidone (A3); castor oil/optionally a surfactant and/or magnesium stearate lubricant (A4). B comprises a hydrophilic polymer (B1) bearing ionized groups with neutral pH (EUDRAGITꡞ L100-55) and a hydrophobic compound (B2) (LUBRITABꡞ).The invention also concerns medicines based on said microparticules.
patents
