The present invention relates to a solid oral pharmaceutical composition that include: (a) an active pharmaceutical ingredient; (b) a co‑processed additive that includes a nitrosamine inhibitor and microcrystalline cellulose; and (c) optionally a pharmaceutically acceptable excipient. With the solid oral pharmaceutical compositions, at least one of: (i) the active pharmaceutical ingredient includes at least one covalently bonded amine group that is subject to conversion to nitrosamine; and/or (ii) the solid oral pharmaceutical composition includes at least one amine, that is other than the amine group covalently bonded to/within the active pharmaceutical ingredient, and which is subject to conversion to nitrosamine. The nitrosamine inhibitor is present in an amount at least sufficient to reduce the amount of nitrosamine formed in the solid oral pharmaceutical composition, compared to the amount of nitrosamine formed in a comparative solid oral pharmaceutical composition that is free of the nitrosamine inhibitor.
A61K 31/24 - Esters, p. ex. nitroglycérine, sélénocyanates d'acides carboxyliques ayant un noyau aromatique lié au groupe carboxyle ayant un groupe amino ou nitro
The present invention relates to a solid oral pharmaceutical composition that includes: (a) an active pharmaceutical ingredient; (b) a nitrosamine inhibitor comprising mannitol; and (c) a pharmaceutically acceptable excipient. With the solid oral pharmaceutical compositions, at least one of: (i) the active pharmaceutical ingredient includes at least one covalently bonded amine group that is subject to conversion to nitrosamine; or (ii) the solid oral pharmaceutical composition includes at least one amine, that is other than the amine group covalently bonded to/within the active pharmaceutical ingredient, and which is subject to conversion to nitrosamine. The nitrosamine inhibitor is present in an amount at least sufficient to reduce the amount of nitrosamine formed in the solid oral pharmaceutical composition, compared to the amount of nitrosamine formed in a comparative solid oral pharmaceutical composition that is free of the nitrosamine inhibitor.
C07C 291/02 - Composés contenant du carbone et de l'azote et comportant des groupes fonctionnels non couverts par les groupes contenant des liaisons oxyde d'azote
C07C 291/04 - Composés contenant du carbone et de l'azote et comportant des groupes fonctionnels non couverts par les groupes contenant des liaisons oxyde d'azote contenant des liaisons oxyde d'amine
The present invention relates to a solid oral pharmaceutical composition that includes: (a) an active pharmaceutical ingredient; (b) a nitrosamine inhibitor that includes linear or branched C1-C10 alkyl 3,4,5-trihydroxybenzoate; and (c) a pharmaceutically acceptable excipient. At least one of: (i) the active pharmaceutical ingredient includes at least one covalently bonded amine group that is subject to conversion to nitrosamine; or (ii) the solid oral pharmaceutical composition includes at least one amine, that is other than the amine group covalently bonded to/within the active pharmaceutical ingredient, and which is subject to conversion to nitrosamine. The nitrosamine inhibitor is present in an amount at least sufficient to reduce the amount of nitrosamine formed in the solid oral pharmaceutical composition, compared to the amount of nitrosamine formed in a comparative solid oral pharmaceutical composition that is free of the nitrosamine inhibitor.
11010 alkyl 3,4,5‑trihydroxybenzoate; and (c) a pharmaceutically acceptable excipient. At least one of: (i) the active pharmaceutical ingredient includes at least one covalently bonded amine group that is subject to conversion to nitrosamine; or (ii) the solid oral pharmaceutical composition includes at least one amine, that is other than the amine group covalently bonded to/within the active pharmaceutical ingredient, and which is subject to conversion to nitrosamine. The nitrosamine inhibitor is present in an amount at least sufficient to reduce the amount of nitrosamine formed in the solid oral pharmaceutical composition, compared to the amount of nitrosamine formed in a comparative solid oral pharmaceutical composition that is free of the nitrosamine inhibitor.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of multiple sclerosis; pharmaceutical preparations for the treatment of neurological disorders; pharmaceuticals for the treatment of diseases and disorders of the central nervous system; pharmaceuticals; pharmaceutical preparations.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of multiple sclerosis; pharmaceutical preparations for the treatment of neurological disorders; pharmaceuticals for the treatment of diseases and disorders of the central nervous system; pharmaceuticals; pharmaceutical preparations; medical preparations.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of multiple sclerosis; pharmaceutical preparations for the treatment of neurological disorders; pharmaceuticals for the treatment of diseases and disorders of the central nervous system; pharmaceuticals; pharmaceutical preparations; medicine; medical preparations.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of asthma in patients 6 years of age and older and maintenance treatment of airflow obstruction and reducing exacerbations in patients with chronic obstructive pulmonary disease (COPD) including chronic bronchitis and/or emphysema; Anti-inflammatories
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of multiple sclerosis; pharmaceutical preparations for the treatment of neurological disorders; pharmaceuticals for the treatment of diseases and disorders of the central nervous system.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of multiple sclerosis; pharmaceutical preparations for the treatment of neurological disorders; pharmaceuticals for the treatment of diseases and disorders of the central nervous system; pharmaceuticals; pharmaceutical preparations; medicine; medical preparations.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of asthma in patients 6 years of age and older and maintenance treatment of airflow obstruction and reducing exacerbations in patients with chronic obstructive pulmonary disease (COPD) including chronic bronchitis and/or emphysema; Anti-inflammatories
Novel processes for making the N-pyrrazole substituted 2-adenosine derivative regadenoson and a novel polymorph thereof. The novel polymorph of regadenoson designated form H and drug substances and pharmaceutical compositions including the novel polymorph H are disclosed.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of Non Hodgkin's Lymphoma (NHL) and Chronic Lymphocytic Leukemia (CLL); pharmaceutical preparations for the treatment of rheumatoid arthritis, chronic plaque psoriasis, Crohn's disease, ankylosing spondylitis, psoriatic arthritis, and polyarticular juvenile idiopathic arthritis.
Processes are disclosed for making vortioxetine and pharmaceutically acceptable salts thereof. A propylene glycol solvate of vortioxetine hydrobromide is disclosed. A novel crystalline form of vortioxetine hydrobromide propylene glycol solvate, designated form AC1, is disclosed along with a method for making same. Form AC1 may be characterized by an x-ray powder diffraction pattern with peaks at about 19.64, 22.85, 25.51, 29.57, 30.18±0.2 degrees 2-theta.
C07D 295/096 - Composés hétérocycliques contenant des cycles polyméthylène imine d'au moins cinq chaînons, des cycles aza-3 bicyclo [3.2.2] nonane, piperazine, morpholine ou thiomorpholine, ne comportant que des atomes d'hydrogène liés directement aux atomes de carbone du cycle avec des radicaux hydrocarbonés substitués liés aux atomes d'azote du cycle substitués par des atomes d'oxygène ou de soufre liés par des liaisons simples avec les atomes d'azote du cycle et les atomes d'oxygène ou de soufre séparés par des carbocycles ou par des chaînes carbonées interrompues par des carbocycles
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Patient support services, namely, providing information to patients relating to diagnostic, prophylactic, and therapeutic properties of pharmaceuticals
Novel crystalline ponatinib hydrochloride forms designated Form alpha and Form beta are disclosed. Form alpha is characterized by data selected from an XRPD pattern with peaks at about 6.5, 9.0, 12.25, 14.4, 16.70, 19.6, 22.2, 24.5, 28.2±0.2 degrees 2-theta; an XRPD pattern substantially as depicted in FIG. 1; and/or a combination thereof. Form beta is characterized by data selected from an XRPD pattern with peaks at about 10.7, 15.2, 15.8, 16.4 23.1, 25.0, 27.8±0.2 degrees 2-theta; an XRPD pattern substantially as depicted in FIG. 3; and/or combinations thereof. Processes for making Form alpha and Form beta are disclosed.
Processes are provided for the preparation of a stable polymorphic form C of regadenoson, the process involving steps of a) obtaining a solution of regadenoson in benzyl alcohol solvent, b) maintaining the reaction mixture of step a) to about 10° C. to about 90° C., and c) isolating the stable polymorphic form C of regadenoson. Polymorphic form C may be characterized by an x-ray powder diffraction pattern with peaks at about 6.1, 10.2, 10.6, 19.0 and 25.4.±0.2 degrees 2-theta.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Injectable pharmaceuticals for treatment of multiple sclerosis; syringes sold filled with injectable pharmaceuticals for treatment of multiple sclerosis
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Injectable pharmaceuticals for treatment of multiple sclerosis; Syringes sold filled with injectable pharmaceuticals for treatment of multiple sclerosis
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Providing information to patients relating to diagnostic, prophylactic, and therapeutic properties of pharmaceuticals for the treatment of multiple sclerosis.
Novel processes for making the N-pyrrazole substituted 2-adenosine derivative regadenoson and a novel polymorph thereof. The novel polymorph of regadenoson designated form H and drug substances and pharmaceutical compositions including the novel polymorph H are disclosed.
Novel synthetic approaches to make 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide, intermediates and pharmaceutically acceptable salts thereof are provided.
C07D 209/48 - Iso-indolesIso-indoles hydrogénés avec des atomes d'oxygène en positions 1 et 3, p. ex. phtalimide
C07C 233/80 - Amides d'acides carboxyliques ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons ayant l'atome d'azote d'au moins un des groupes carboxamide lié à un atome de carbone d'un radical hydrocarboné substitué par des groupes amino avec le radical hydrocarboné substitué lié à l'atome d'azote du groupe carboxamide par un atome de carbone d'un cycle aromatique à six chaînons
C07C 233/75 - Amides d'acides carboxyliques ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons ayant l'atome d'azote d'au moins un des groupes carboxamide lié à un atome de carbone d'un radical hydrocarboné substitué par des atomes d'oxygène liés par des liaisons simples avec le radical hydrocarboné substitué lié à l'atome d'azote du groupe carboxamide par un atome de carbone d'un cycle aromatique à six chaînons
C07C 233/76 - Amides d'acides carboxyliques ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons ayant l'atome d'azote d'au moins un des groupes carboxamide lié à un atome de carbone d'un radical hydrocarboné substitué par des atomes d'oxygène liés par des liaisons doubles
C07D 233/80 - Deux atomes d'oxygène, p. ex. hydantoïne avec des hétéro-atomes ou des radicaux acyle liés directement aux atomes d'azote du cycle
C07D 233/76 - Deux atomes d'oxygène, p. ex. hydantoïne avec des radicaux hydrocarbonés substitués liés au troisième atome de carbone du cycle
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Injectable pharmaceuticals for treatment of multiple sclerosis; syringes sold filled with injectable pharmaceuticals for treatment of multiple sclerosis.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, ophthalmic, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders
Embodiments of a controlled release minitablet comprise an extended release core and an optional pH dependent delayed release coating thereon, wherein the extended release core comprises budesonide, a carrier, an extended release polymer, and an acid. The budesonide may be embedded in the extended release polymer to facilitate extended release of the budesonide upon administration.
A61K 9/28 - DragéesPilules ou comprimés avec revêtements
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes contenant des hétérocycles, p. ex. danazol, stanozolol, pancuronium ou digitogénine
Embodiments of a controlled release minitablet comprise an extended release core and an optional pH dependent delayed release coating thereon, wherein the extended release core comprises budesonide, a carrier, and an extended release polymer. The budesonide may be embedded in the extended release polymer to facilitate extended release of the budesonide upon administration.
A61K 9/28 - DragéesPilules ou comprimés avec revêtements
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes contenant des hétérocycles, p. ex. danazol, stanozolol, pancuronium ou digitogénine
80.
TRANSDERMAL SYSTEMS CONTAINING MULTILAYER ADHESIVE MATRICES TO MODIFY DRUG DELIVERY
A transdermal drug-containing dosage unit comprises: a backing layer substantially impervious to the drug to be delivered transdermally; a first polymeric adhesive matrix, in contact with the backing layer, having dispersed therein the drug and having a first delivery profile of the drug; a second polymeric adhesive matrix, in contact with said first polymeric adhesive matrix, having dispersed therein the drug and having a second delivery profile of the drug, wherein said second delivery profile is different from said first delivery profile; and a release liner in contact with the second polymeric adhesive matrix. The first polymeric adhesive matrix can release the drug more quickly or more slowly than the second polymeric adhesive matrix. Through the selection of the two matrices, the delivery profile of the drug through the skin can be selectively modified and controlled.
Extended release pharmaceutical formulations are disclosed wherein the formulations contain an extended release portion and an immediate release portion, the extended release portion comprising an active pharmaceutical ingredient and a wax. Methods of making such extended release pharmaceutical formulations are also disclosed.
A pharmaceutical composition contains tolterodine L-tartrate stabilized against degradation with an acid. Acid-stabilized tolterodine L-tartrate may be used to make various types of immediate release and controlled release dosage forms.
A drug composition comprising a coated bead is used in the manufacture of immediate release and/or controlled release drug compositions. In a specific embodiment, the bead includes an inert core of a water-soluble or water-swellable material, which has been coated with a seal layer formed from a non-polymeric hydrophobic material. The immediate and/or controlled release beads may be used to form tablets or capsules. A method of making the beads by sequential deposition of multiple layers on the inert cores is also described.
A61K 9/54 - Préparations en capsules, p. ex. de gélatine, de chocolat du type à libération prolongée ou discontinue contenant des particules distinctes avec des revêtements de différentes épaisseurs ou de différents matériaux
A drug composition comprising a coated bead is used in the manufacture of immediate release and/or controlled release drug compositions. In a specific embodiment, the bead includes an inert core of a water-soluble or water-swellable material, which has been coated with a seal layer formed from a non-polymeric hydrophobic material. The immediate and/or controlled release beads may be used to form tablets or capsules. A method of making the beads by sequential deposition of multiple layers on the inert cores is also described.
A pharmaceutical composition contains tolterodine L-tartrate stabilized against degradation with an acid. Acid-stabilized tolterodine L-tartrate may be used to make various types of immediate release and controlled release dosage forms.
Provided are pharmaceutical formulations comprising sustained release particles each having an inner core bead comprising an active pharmaceutical ingredient an intermediate coating substantially surrounding the inner core bead, and an outer coating substantially surrounding the intermediate coating comprising a pH independent polymer. Also provided is a pharmaceutical formulation comprising two bead populations wherein each of the first and second bead populations have a different drug release profile. Also provided is a method of preparing an extended release dosage composition comprising one or more bead populations.
