United States Patent:  5,980,944

Assignee:  McNeil-PPC, Inc. (Skillman, NJ)

Filed:  November 25, 1997

A solid oral dosage form for the treatment of gastrointestinal disorders comprising a therapeutically effective amount of a pharmaceutical suitable for the treatment of gastric disorders selected from the group consisting of granules of diphenoxylate, loperamide, loperamide-N-oxide, pharmaceutically acceptable salts thereof and combinations thereof; and a therapeutically effective amount of simethicone wherein the pharmaceutical and simethicone are separated by a barrier coat on the granules which is substantially impermeable to simethicone.

SUMMARY OF THE INVENTION

In accordance with the present invention, we have discovered a solid oral dosage form for the treatment of gastrointestinal disorders comprising a therapeutically effective amount of a pharmaceutical suitable for the treatment of gastric disorders selected from the group consisting of cimetidine, ranitidine, famotidine, diphenoxylate, loperamide, loperamide-N-oxide, pharmaceutically acceptable salts thereof and combinations thereof; and a therapeutically effective amount of simethicone wherein the oral dosage form has a first portion containing the simethicone and a second portion containing the pharmaceutical suitable for the treatment of gastric disorders wherein the first and second portions are in contact with and separated by a barrier which is substantially impermeable to simethicone.

In an another embodiment of the present invention, we have further discovered a solid oral dosage form for the treatment of gastrointestinal disorders comprising a therapeutically effective amount of a pharmaceutical suitable for the treatment of gastric disorders selected from the group consisting of cimetidine, ranitidine, famotidine, diphenoxylate, loperamide, loperamide-N-oxide, pharmaceutically acceptable salts thereof and combinations thereof wherein the pharmaceutical suitable for the treatment of gastric disorders is provided in the form of coated granules which are coated with a nonenteric coating impermeable to simethicone; a therapeutically effective amount of simethicone; and pharmaceutically acceptable excipients.

In a further embodiment of the invention we have discovered a method for manufacturing the multilayered solid dosage form having one layer containing simethicone and one layer containing a pharmaceutical suitable for treating gastric disorders with a barrier sandwiched between the two layers comprising pressing one of two granulations, each containing pharmaceutically acceptable excipients with either a therapeutic amount of simethicone or a therapeutic amount of a pharmaceutical suitable for the treatment of a gastric disorder therein, to form a first layer with one exposed surface; then coating the exposed surface with a material which is substantially impermeable to simethicone to form a coated layer with a coated surface; contacting the coated surface with the remaining granulation; then pressing the granulation and coated layer to form a multilayered solid oral dosage form wherein the simethicone and the pharmaceutical are separated by the material substantially impermeable to simethicone.

Claim 1 of 12 Claims

1. A solid oral dosage form for the treatment of gastrointestinal distress comprising simethicone and a pharmaceutical having an enhanced dissolution profile, comprising a therapeutically effective amount of a pharmaceutical for the treatment of gastric disorders selected from the group consisting of diphenoxylate, loperamide and loperamide-N-oxide, pharmaceutically acceptable salts thereof, and combinations thereof; wherein the pharmaceutical is provided in the form of coated granules which are coated with a nonenteric polymer coating impermeable to simethicone; a therapeutically effective amount of simethicone free of said nonenteric coating; and pharmaceutically acceptable excipients.

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