Stable oral pharmaceutical dosage forms
AssigneeSage Pharmaceuticals, Inc.
InventorJivn-Ren Chen
Life of this patent
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Abstract
The present invention relates to new stable enteric coated pharmaceutical dosage forms for oral use containing Omeprazole or Lansoprazole, to a formulation and a method for the manufacture of such a dosage forms, and to a method of gastric acid pump inhibition and providing gastrointestinal cytoprotective benefit by using them.
Claims14
A pharmaceutical dosage form for oral administration to human being or animal host which consists essentially of:
- (a) a core granulation formed by dry mixing, without using an aqueous granulation solution, an acid-unstable drug with an alkaline substance and a pharmaceutical excipient or excipients, wherein the core granulation is capable of being quantitatively filled into an empty hard gelatin capsule shell having an outer surface and an inner surface, wherein the hard gelatine capsule shell separates the core granulation from an enteric coating, and wherein the acid-unstable drug is a benzimidazole derivative;
- and
- (b) the enteric coating being disposed on the outer surface of the hard gelatin capsule shell to prevent the release of the acid-unstable drug in the gastric environment and to deliver the acid-unstable drug in the intestinal environment, wherein the pharmaceutical dosage form has more than about 95% of the drug remaining after 11 months in ambient room temperature conditions.
A pharmaceutical dosage form for oral administration to human being or animal host which consists essentially of:
- (a) a core tablet formed by dry mixing, without using an aqueous solution, an acid-unstable drug with an alkaline substance and a pharmaceutical excipient or excipients and then by direct compression, wherein the core tablet is capable of being filled into an empty hard gelatin capsule shell having an outer surface and an inner surface, wherein the hard gelatin capsule shell separates the core tablet from an enteric coating, and wherein the acid-unstable drug is a benzimidazole derivative;
- and
- (b) the enteric coating being disposed on the outer surface of the hard gelatin capsule shell to protect the acid-unstable drug in the gastric environment and to deliver the acid-unstable drug in the intestinal environment, wherein the pharmaceutical dosage form has more than about 95% of the drug remaining after 11 months in ambient room temperature conditions.
A pharmaceutical dosage form for oral administration to human being or animal host which consists essentially of:
- (a) a core tablet formed by dry mixing, without using an aqueous solution, an acid-unstable drug with an alkaline substance and a pharmaceutical excipient or excipients and then by direct compression, wherein the acid-unstable drug is a benzimidazole derivative, and wherein the core tablet is subcoated with a protective layer as a barrier to:
- (i) separate the acid-unstable active drug in the core tablet from an enteric coating;
- and
- (ii) protect the enteric coating from the permeation of alkaline solution formed in the core tablet;
- and
- (b) the enteric coating being disposed on the protectively subcoated tablet to protect the coated tablet from releasing the acid-unstable drug in the stomach and to deliver the acid-unstable drug to the small intestine, wherein the pharmaceutical dosage form has more than about 95% of the drug remaining after 11 months in ambient room temperature conditions.
An oral pharmaceutical preparation consisting essentially of:
- (a) a core formulation comprising an acid-unstable drug and an alkaline substance, formed by dry mixing without using an aqueous granulating solution, wherein the acid-unstable drug is a benzimidazole derivative;
- (b) a hard gelatin capsule shell housing the core formulation, wherein the gelatin capsule shell has an outer surface and an inner surface;
- and
- (c) an enteric coating disposed on the outer surface of the hard gelatin capsule, wherein the enteric coating is separated from the core formulation by the hard gelatin capsule shell without a protective coating.
Dependencies are inferred from the claim text.