Solid pharmaceutical compositions containing pregabalin

• US 9,144,559 B2
• Filed: 12/15/2014
• Issued: 09/29/2015
• 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
• Primary Examiner(s): DICKINSON, PAUL W
• Application Number:
  US14/570,115
• Publication Number:
  US 20150094371A1
• Time in Patent Office: 288 Days
• Field of Search: None
• US Class Current: 1/1
• 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. 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.

2. The pharmaceutical composition according to claim 1 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.

3. The pharmaceutical composition according to claim 1 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.

4. The pharmaceutical composition according to claim 1 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.

5. 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.

6. The formulation according to claim 5 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.