Pharmaceutical formulation
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.
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.