Pharmaceutical formulation

• US 8,367,101 B2
• Filed: 01/30/2002
• Issued: 02/05/2013
• Est. Priority Date: 01/30/2001
• Status: Expired due to Fees

• Current Assignee: Capsugel Belgium NV (Lonza Group AG)
• Original Assignee: Capsugel Belgium NV (Lonza Group AG)
• Inventors: McAllister, Stephen Mark, Raby, Ronald K. Jr., Brown, Adrian, Clarke, Allan J., Margetson, Daniel N., Matthews, Wayne
• Primary Examiner(s): TRAN, SUSAN T
• Application Number:
  US10/060,849
• Publication Number:
  US 20030068369A1
• Time in Patent Office: 4,024 Days
• Field of Search: 424/451, 424/472, 424/400
• US Class Current: 424/451
• CPC Class Codes: A61K 9/4808 characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• CPC Class Codes: A61K 9/4816 Wall or shell material
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The present invention is directed to pharmaceutically acceptable polymeric compositions suitable for injection molding of single or multi-component pharmaceutical dosage forms comprising a plurality of drug substance containing sub-units, being capsule compartments and/or solid sub-units comprising a solid matrix of a polymer which contains a drug substance, the sub-units being connected together in the assembled dosage form by a weld between parts of the assembled dosage form.

Claims

1. An extruded, injection molded capsule shell comprising a composition comprising:

a copolymer of methyl acrylate, methyl methacrylate, and methacrylic acid, present in an amount ranging from about 42% to about 72% w/w, with a molar ratio of monomer units of 7;

3;

1 and a ratio of free carboxyl groups to ester groups of 1;

10;

Stearyl alcohol is present in an amount of about 12% w/w;

a surfactant selected from the group consisting of sodium dodecyl sulphate and a block copolymer of ethylene oxide and propylene oxide present in an amount ranging from about 0.1% to about 5% w/w;

a swellable solid present in an amount ranging from about 5% to about 70% w/w selected from the group consisting of, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, hydroxypropylmethyl cellulose phthalate, and combinations thereof; and

a dissolution modifying excipient present in an amount ranging from about 5% to about 40% w/w selected from the group consisting of sodium starch glycollate, croscarmellose sodium, Lactose, and combinations thereof.

2. The capsule shell according to claim 1, wherein the composition is selected from the group consisting of:

Copolymer 62.9%, Crosscarmellose sodium 10%, Sodium starch glycollate 10%, Stearyl alcohol 12%, Hydroxypropyl methylcellulose 5%, Sodium dodecyl sulphate 0.1%;

Copolymer 62.75%, Crosscarmellose sodium 10%, Sodium starch glycollate 10%, Stearyl alcohol 12%, Hydroxypropyl methylcellulose 5%, Sodium dodecyl sulphate 0.25%;

Copolymer 52%, Crosscarmellose sodium 15%, Sodium starch glycollate 15%, Stearyl alcohol 12%, Hydroxypropyl methylcellulose 5%, Sodium dodecyl sulphate 1%;

Copolymer 42%, Crosscarmellose sodium 20%, Sodium starch glycollate 20%, Stearyl alcohol 12%, Hydroxypropyl methylcellulose 5%, Sodium dodecyl sulphate 1%;

and

Copolymer 62%, Crosscarmellose sodium 5%, Sodium starch glycollate 5%, Stearyl alcohol 12%, Hydroxypropyl methylcellulose 15%, Sodium dodecyl sulphate 1%.

3. The capsule shell according to claim 1, wherein the composition is selected from the group consisting of:

Copolymer 68%, Hydroxypropylmethyl cellulose 10%, Lactose (regular) 5%, Sodium dodecyl sulphate 5%, Stearyl alcohol 12%;

Copolymer 72%, Hydroxypropylmethyl cellulose 10%, Lactose (regular) 5%, Sodium dodecyl sulphate 1%, Stearyl alcohol 12%;

Copolymer 71%, Hydroxypropylmethyl cellulose 10%, Lactose (regular) 5%, Sodium dodecyl sulphate 2%, Stearyl alcohol 12%;

Copolymer 62%, Sodium starch glycollate 20%, Hydroxypropylmethyl cellulose 5%, Sodium dodecyl sulphate 1%, Stearyl alcohol 12%;

Copolymer 62.5%, Sodium starch glycollate 20%, Hydroxypropylmethyl cellulose 5%, Sodium dodecyl sulphate 0.5%, Stearyl alcohol 12%;

Copolymer 62%, Croscarmellose sodium 10%, Sodium starch glycollate 10%, Hydroxypropylmethyl cellulose 5%, Sodium dodecyl sulphate 1%, Stearyl alcohol 12%;

Copolymer 67%, Croscarmellose sodium 15%, Hydroxypropylmethyl cellulose 5%, Sodium dodecyl sulphate 1%, Stearyl alcohol 12%;

Copolymer 72%, Croscarmellose sodium 10%, Hydroxypropylmethyl cellulose 5%, Sodium dodecyl sulphate 1%, Stearyl alcohol 12%;

Copolymer 52%, Croscarmellose sodium 15%, Sodium starch glycollate 15%, Hydroxypropylmethyl cellulose 5%, Sodium dodecyl sulphate 1%, Stearyl alcohol 12%;

Copolymer 62.9%, Croscarmellose sodium 10%, Sodium starch glycollate 10%, Hydroxypropylmethyl cellulose 5%, Sodium dodecyl sulphate 0.1%, Stearyl alcohol 12%;

Copolymer 62%, Sodium dodecyl sulphate 1%, Croscarmellose sodium 10%, Sodium starch glycollate 10%, Stearyl alcohol 12%, Hydroxypropylmethyl cellulose 5%;

Copolymer 52%, Sodium dodecyl sulphate 1%, Croscarmellose sodium 15%, Sodium starch glycollate 15%, Stearyl alcohol 12%, Hydroxypropylmethyl cellulose 5%;

Copolymer 62%, Polyoxypropylene-polyoxyethylene block copolymer 1%, Sodium starch glycollate 20%, Stearyl alcohol 12%, Hydroxypropylmethyl cellulose 5%;

and

Copolymer 47%, Stearyl alcohol 12%, Sodium starch glycollate 10%, Hydroxypropylmethyl cellulose 30%, Sodium dodecyl sulphate 1%.

4. An extruded, injection molded capsule shell comprising a composition selected from the group consisting of:

Copolymer 62%, Hydroxypropylmethyl cellulose phthalate 20%, Hydroxypropylmethyl cellulose 5%, Sodium dodecyl sulphate 1%, Stearyl alcohol 12%;

Copolymer 77%, Croscarmellose sodium 5%, Hydroxypropylmethyl cellulose 5%, Sodium dodecyl sulphate 1%, Stearyl alcohol 12%; and

Copolymer 63%, Croscarmellose sodium 10%, Sodium starch glycollate 10%, Hydroxypropylmethyl cellulose 5%, Stearyl alcohol 12%;

wherein the copolymer is a copolymer of methyl acrylate, methyl methacrylate, and methacrylic acid with a molar ratio of monomer units of 7;

3;

1, and a ratio of free carboxyl groups to esters groups of 1;

10.