Controlled release formulation
AssigneeE. R. Squibb & Sons, Inc.
InventorsJoseph D. Drost, George E. Reier, Nemichand B. Jain
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AssigneeE. R. Squibb & Sons, Inc.
InventorsJoseph D. Drost, George E. Reier, Nemichand B. Jain
Estimating the term…
A controlled release pharmaceutical formulation which undergoes substantially or approaches zero order release of active drug is provided, preferably in the form of a coated tablet, containing a core portion from which medicament, such as procainamide hydrochloride, is slowly released over a controlled length of time. The core also includes one or more primary hydrocolloid gelling agents which is a hydropropylmethyl cellulose having a viscosity of within the range of from about 1,000 to about 6,000 centipoises in 2% solution at 20.degree. C., and a methoxyl content of 28-30%, optionally a secondary hydrocarbon gelling agent, such as hydroxypropyl cellulose and/or methyl cellulose, one or more non-swellable binders and/or wax binders (where the medicament and/or hydrocolloid gelling agents are non-compressible), one or more inert fillers or excipients, one or more lubricants, and optionally one or more anti-adherents such as silicon dioxide and water. The above-described core is coated with a pharmaceutical coating composition containing a hydrophobic polymer and a hydrophilic polymer.
In a controlled release procainamide hydrochloride formulation in the form of a tablet which is adapted to approach zero order release of procainamide hydrochloride over an 8 to 12 hour or more period, which tablet is comprised of a core and a pharmaceutically acceptable coating therefor, said core comprising more than about 70% by weight of procainamide hydrochloride, the improvement which consists essentially of incorporating in said core, from at least about 5 to not more than 15% by weight of one or more primary hydrocolloid gelling agent composed of hydroxypropylmethyl cellulose having a methoxyl content of 28 to 30% having a viscosity of within the range of from about 1,000 to about 6,000 centipoises in 2% solution of 20.degree. C., from 0 to about 7.5% by weight of a secondary hydrocolloid gelling agent which is hydroxypropyl cellulose, from 0 to about 8% by weight of one or more non-swellable binders and/or from 0 to about 8% by weight of one or more wax binders, said non-swellable binder or wax binder being present when said medicament and hydrocolloid gelling agent are non-compressible and from about 1.1 to less than about 4% by weight water, all of said % being based on the weight of said core, and said coating permitting entry of water and hydration of the core, so that there is not a large initial surge in the release of medicament and essentially comprising as film formers a mixture of at least one hydrophobic polymer and at least one hydrophilic polymer in a weight ratio to each other of from about 4:1 to about 1:4.
Dependencies are inferred from the claim text.