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US 2004/0166153 A1Published application
Pharmaceutical formulation
AssigneeSmithKline Beecham Corporation
InventorsStephen Mark McAllister, Ronald K Raby JR., Adrian Brown, Allan J Clarke, Wayne Matthews, Daniel N Margetson
Life of this patent
Estimating the term…
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.
Claims70
A pharmaceutical composition for moulded capsules comprising Eudragit 4135F present in an amount of about 20 to 90% w/w;
- a lubricant present in an amount of 0 to about 30% w/w;
- a dissolution modifying excipient present in an amount of about 2.5 to about 70% w/w, and optionally a surfactant present in an amount of 0 to 10%, a plasticizer present in an amount of 0 to 10% w/w and/or a processing agent present in an amount of 0 to about 10% w/w.
12 A pharmaceutical composition for molded capsule shells comprising:
- (1) (2) (3) (4) (5) (6) (7) 4135F 45% 35% 25% 15% 75% 65% 55% Stearyl Alcohol 10% 10% 10% 10% 10% 10% 10% Lactose 5% 5% 5% 5% 5% 5% 5% Klucel LF 40% 50% 60% 70% 10% 20% 30% Total 100% 100% 100% 100% 100% 100% 100%
13 A pharmaceutical composition for molded capsule shells comprising:
- (1) (2) (3) (4) (5) (6) 4135F 63% 62.9% 62.75% 52% 42% 62% Croscarmellose 10% 10% 10% 15% 20% 5% sodium Sodium starch 10% 10% 10% 15% 20% 5% glycollate Stearyl alcohol 12% 12% 12% 12% 12% 12% Hydroxypropyl- 5% 5% 5% 5% 5% 15% methylcellulose SDS 0% 0.1% 0.25% 1% 1% 1%
14 A pharmaceutical composition for molded capsule shells comprising:
- #(1) (2) (3) (4) (5) (6) (7) 4135F 45% 35% 25% 15% 75% 65% 55% Stearyl Alcohol 10% 10% 10% 10% 10% 10% 10% Lactose 5% 5% 5% 5% 5% 5% 5% Klucel LF 40% 50% 60% 70% 10% 20% 30% Total 100% 100% 100% 100% 100% 100% 100%
15 A pharmaceutical composition for molded capsule shells comprising:
- Formulation % w/w Eudragit 4135F 73.0 Hydroxypropylmethyl cellulose 10.0 Lactose (regular) 5.0 Glyceryl monostearate 12.0 Eudragit 4135F 53.0 Hydroxypropylmethyl cellulose 10.0 Lactose (regular) 5.0 Hydroxypropylmethyl cellulose phthallate 20.0 Stearyl alcohol 12.0 Eudragit 4135F 20.0 Hydroxypropylmethyl cellulose 10.0 Hydroxypropylmethyl cellulose phthallate 20.0 Stearyl alcohol 12.0 Eudragit 4135F 68.0 Hydroxypropylmethyl cellulose 10.0 Lactose (regular) 5.0 Sodium dodecyl sulphate 5.0 Stearyl alcohol 12.0 Eudragit 4135F 72.0 Hydroxypropylmethyl cellulose 10.0 Lactose (regular) 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 71.0 Hydroxypropylmethyl cellulose 10.0 Lactose (regular) 5.0 Sodium dodecyl sulphate 2.0 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Sodium starch glycollate 20.0 Lactose (regular) 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Sodium starch glycollate 20.0 Lactose (regular) 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 72.0 Sodium starch glycollate 10.0 Lactose (regular) 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Croscarmellose sodium 20.0 Lactose (regular) 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Sodium starch glycollate 20.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Hydroxypropylmethyl cellulose phthallate 20.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.5 Sodium starch glycollate 20.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 0.5 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Croscarmellose sodium 10.0 Sodium starch glycollate 10.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 72.0 Sodium starch glycollate 10.0 Lactose (regular) 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Croscarmellose sodium 20.0 Lactose (regular) 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Sodium starch glycollate 20.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Hydroxypropylmethyl cellulose phthallate 20.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.5 Sodium starch glycollate 20.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 0.5 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Croscarmellose sodium 10.0 Sodium starch glycollate 10.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 67.0 Croscarmellose sodium 15.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 72.0 Croscarmellose sodium 10.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 77.0 Croscarmellose sodium 5.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 52.0 Croscarmellose sodium 15.0 Sodium starch glycollate 15.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 42.0 Croscarmellose sodium 20.0 Sodium starch glycollate 20.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 42.0 Croscarmellose sodium 20.0 Sodium starch glycollate 20.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.0 Croscarmellose sodium 5.0 Sodium starch glycollate 5.0 Hydroxypropylmethyl cellulose 15.0 Sodium dodecyl sulphate 1.0 Stearyl alcohol 12.0 Eudragit 4135F 62.9 Croscarmellose sodium 10.0 Sodium starch glycollate 10.0 Hydroxypropylmethyl cellulose 5.0 Sodium dodecyl sulphate 0.1 Stearyl alcohol 12.0
A multi-component pharmaceutical dosage form which comprises a plurality of sub-units, each sub-unit being selected from
- a) a drug substance-containing capsule compartment which is soluble or disintegrable in a patient's gastrointestinal environment for release of the drug substance contained in the capsule compartment, and
- b) a solid matrix comprising a polymer and containing a drug substance, the polymer being soluble, dispersible or disintegrable in a patient's gastro-intestinal environment for release of the drug substance contained in the solid matrix, and in which, at least prior to administration to a patient, the sub-units are welded together in an assembled dosage form.
A set of multi-component dosage forms, each comprising a plurality of sub-units each sub-unit being selected from:
- a) a drug substance-containing capsule compartment which is soluble or disintegrable in a patient's gastro-intestinal environment for release of the drug substance contained in the capsule compartment, and
- b) a solid matrix comprising a polymer and containing a drug substance, the polymer being soluble, dispersible or disintegrable in a patient's gastro-intestinal environment for release of the drug substance contained in the solid matrix, in which at least one of the dosage forms of the set comprises at least one said drug substance-containing capsule compartment and at least one other dosage form of the set comprises at least one said solid matrix, and in which the drug substance-containing capsule compartment of said at least one of the dosage forms is interchangeable with said solid matrix of said at least one other dosage form, and in which at least prior to administration to a patient, the sub-units of each dosage form are welded together to provide an assembled dosage form.
A process for making a pharmaceutical dosage form comprising the steps of:
- a) introducing Eudragit 4135F and an excipient composition simultaneously, and at substantially the same location, into an elongated hot melt extruder;
- b) mixing said Eudragit 4135F and said excipient composition in the hot melt extruder to form a homogeneous composition therein and ejecting the homogeneous composition in the form of a strand from the hot melt extruder though a die at a location remote from said same location at which the Eudragit 4135F and said excipient composition are introduced;
- c) cutting the strand into pellets;
- d) introducing said pellets into an injection molder and forming thin-walled capsule compartments from said pellets by injection molding.
1 more element
Dependencies are inferred from the claim text.