Solid Pharmaceutical Compositions Containing Pregabalin

• US 20150094371A1
• Filed: 12/15/2014
• Published: 04/02/2015
• Est. Priority Date: 11/02/2005
• Status: Active Grant

• Current Assignee: Viatris Specialty LLC
• Original Assignee: Warner-Lambert Company LLC (Pfizer Inc.)
• Inventors: Bockbrader, Howard N., Cho, Yun Hyung, Diaz Santiago, Steven, Mahjour, Majid, Reynolds, Thomas Daniel, Shao, Pushpa Ganapathi, Shao, Zezhi Jesse, Wan, Jiansheng
• Granted Patent: US 9,144,559 B2
• Time in Patent Office: Days
• US Class Current: 514/561
• CPC Class Codes: A61K 2039/542 oral/gastrointestinal
• CPC Class Codes: A61K 31/197 the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid carnitine A61K31/205
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: 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 A61K47/10 takes precedence
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/0065 Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
• CPC Class Codes: A61K 9/141 Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers (co) spray-dried products A61K9/16, (co) lyophilised products A61K9/19; the carrier being chemically bound to the active ingredient A61K47/50
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/32 Alcohol-abuse
• CPC Class Codes: A61P 25/36 : Opioid-abuse
• CPC Class Codes: A61P 29/00 : Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

A solid pharmaceutical composition containing pregabalin is described. The composition includes a matrix forming agent and a swelling agent and is suitable for once daily oral administration. Exemplary matrix forming agents include mixtures of polyvinyl acetate and polyvinylpyrrolidone, and exemplary swelling agents include cross-linked polymers of polyvinylpyrrolidone.

Claims

1-15. -15. (canceled)

16. A pharmaceutical composition comprising an active pharmaceutical ingredient and excipients, the active pharmaceutical ingredient comprising pregabalin, or a pharmaceutically acceptable complex, salt, solvate or hydrate thereof, and the excipients comprising a matrix forming agent and a swelling agent, the matrix forming agent comprising polyvinyl acetate and polyvinylpyrrolidone, and the swelling agent comprising crosslinked polyvinylpyrrolidone, wherein the pharmaceutical composition is adapted for once-daily oral dosing;

wherein the pregabalin comprises from about 5% to about 60% of the pharmaceutical composition by weight;

the matrix forming agent comprises from about 5% to about 45% of the pharmaceutical composition by weight, and the swelling agent comprises from about 15% to about 70% of the pharmaceutical composition by weight.

17. The pharmaceutical composition according to claim 16 in which:

a) said matrix forming agent comprises about 20% to about 35% of the pharmaceutical composition by weight, and;

b) said swelling agent comprises about 20% to about 55% of the pharmaceutical composition by weight.

18. The formulation according to claim 16 in which the polyvinyl acetate is present in the quantity of about 60% to about 90% by weight based on the total weight of the polyvinyl acetate and polyvinylpyrrolidone.

19. The formulation according to claim 16 in which the polyvinyl acetate is present in the quantity of about 70% to about 90% by weight based on the total weight of the polyvinyl acetate and polyvinylpyrrolidone.

20. A pharmaceutical formulation suitable for once-a-day administration comprising:

a) pregabalin, or a pharmaceutically acceptable complex, salt, solvate or hydrate thereof, present in the quantity of from about 5% to about 60%, based on the total weight of the formulation;

b) a matrix of polyvinyl acetate and polyvinylpyrrolidone, in which the polyvinyl acetate is present in the quantity of about 70% to about 90% based on the total weight of the polyvinyl acetate and polyvinylpyrrolidine and the matrix is present in the quantity of about 20% to 35% by weight, based on the total weight of the formulation, and;

c) cross linked polyvinylpyrrolidone, present in the quantity of about 10% to about 35% by weight, based on the total weight of the formulation.

21. The formulation according to claim 20 in which the cross linked polyvinylpyrrolidone is present in the quantity of from about 20% to about 30% by weight, based on the total weight of the formulation.