Pharmaceutical formulation
First Claim
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1. A process for making a pharmaceutical dosage form comprising the steps of:
- a) introducing simultaneously, and at substantially the same location, into an elongated hot melt extrudera copolymer of methyl acrylate, methyl methacrylate and methacrylic acid, with a ratio of free carboxyl groups to esters groups of 1;
10, and an average molecular weight of approximately 220,000, present in an amount of about 20 to 90% w/w, andan excipient composition comprising;
i) a lubricant present in an amount of about 10 to about 25% w/w;
ii) at least one dissolution-modifying excipient selected from the group consisting of a swellable solid, disintegrant, non-reducing sugar, water soluble filler, wicking agent, and an inorganic salt present in an amount of about 2.5 to about 70% w/w; and
iii) a surfactant present in an amount of less than 5% w/w, and wherein the surfactant is selected from a block copolymer of ethylene oxide and propylene oxide, lecithin, sodium dioctyl sulfosuccinate, sodium dodecyl sulphate, polyoxyl 40 hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, sorbitan fatty acid ester, polyethylene glycol, d-alpha-tocopheryl polyethylene glycol 1000 succinate, or a sucrose fatty acid ester, or combinations and mixtures thereof; and
optionally a plasticizer present in an amount of 0 to 10% w/w, and/or optionally a processing agent present in an amount of 0 to about 10% w/w;
b) mixing said copolymer and said excipient composition in the hot melt extruder to form a homogeneous composition, 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 copolymer and said excipient composition are introduced;
c) cutting the strand into pellets;
d) introducing said pellets into an injection molder and forming capsule shells by injection molding.
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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.
149 Citations
15 Claims
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1. A process for making a pharmaceutical dosage form comprising the steps of:
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a) introducing simultaneously, and at substantially the same location, into an elongated hot melt extruder a copolymer of methyl acrylate, methyl methacrylate and methacrylic acid, with a ratio of free carboxyl groups to esters groups of 1;
10, and an average molecular weight of approximately 220,000, present in an amount of about 20 to 90% w/w, andan excipient composition comprising; i) a lubricant present in an amount of about 10 to about 25% w/w; ii) at least one dissolution-modifying excipient selected from the group consisting of a swellable solid, disintegrant, non-reducing sugar, water soluble filler, wicking agent, and an inorganic salt present in an amount of about 2.5 to about 70% w/w; and iii) a surfactant present in an amount of less than 5% w/w, and wherein the surfactant is selected from a block copolymer of ethylene oxide and propylene oxide, lecithin, sodium dioctyl sulfosuccinate, sodium dodecyl sulphate, polyoxyl 40 hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, sorbitan fatty acid ester, polyethylene glycol, d-alpha-tocopheryl polyethylene glycol 1000 succinate, or a sucrose fatty acid ester, or combinations and mixtures thereof; and optionally a plasticizer present in an amount of 0 to 10% w/w, and/or optionally a processing agent present in an amount of 0 to about 10% w/w; b) mixing said copolymer and said excipient composition in the hot melt extruder to form a homogeneous composition, 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 copolymer and said excipient composition are introduced; c) cutting the strand into pellets; d) introducing said pellets into an injection molder and forming capsule shells by injection molding. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
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Specification