Substituted benzimidazole dosage forms and method of using same
AssigneeThe Curators of the University of Missouri
InventorJeffrey O. Phillips
Life of this patent
Estimating the term…
Abstract
The present invention relates to pharmaceutical preparations comprising substituted benzimidazole proton pump inhibitors. There is provided a liquid or solid pharmaceutical dosage form that is not enteric coated or delayed released containing a proton pump inhibitor and a Primary Essential Buffer. When the dosage form is placed in a liquid phase the Primary Essential Buffer maintains the pH of the environment at a value greater than the pKa of the proton pump inhibitor for a time sufficient to substantially avoid acid degradation of the proton pump inhibitor in the environment. Also provided is a method for treating acid-related gastrointestinal disorders by administering a solid pharmaceutical dosage form; and a kit for the preparation of a liquid oral pharmaceutical composition.
Claims29
A solid oral pharmaceutical dosage form that is not enteric-coated, comprising:
- active ingredients consisting essentially of:
- (a) at least one proton pump inhibitor (PPI) selected from the group consisting of omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, and an enantiomer, isomer, free base, or salt thereof, in an amount of approximately 5 mg to approximately 300 mg;
- and
- (b) at least one Primary Essential Buffer and at least one optional Secondary Essential Buffer in a total amount of approximately 0.1 mEq to approximately 2.5 mEq per mg of proton pump inhibitor;
- and
- a pharmaceutically-acceptable excipient;
- wherein the dosage form is selected from the group consisting of a suspension tablet, chewable tablet, two-part tablet, effervescent powder, and effervescent tablet.
A solid oral pharmaceutical dosage form that is not enteric-coated, comprising:
- an outer layer and an inner core;
- the outer layer comprising active ingredients consisting essentially of at least one Primary Essential Buffer;
- and
- the inner core comprising active ingredients consisting essentially of at least one proton pump inhibitor selected from the group consisting of omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, or an enantiomer, isomer, free base, or salt thereof, and at least one buffering agent selected from the group consisting of a Primary Essential Buffer and a Secondary Essential Buffer;
- wherein the total amount of the proton pump inhibitor is approximately 5 mg to approximately 300 mg;
- and the total amount of the buffering agent is approximately 0.1 mEq to approximately 2.5 mEq per mg of proton pump inhibitor.
A non-enteric coated solid oral pharmaceutical dosage form, comprising:
- (a) active ingredients consisting essentially of:
- (i) a proton pump inhibitor (PPI) selected from the group consisting of omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, and an enantiomer, isomer, free base, and salt thereof, in an amount of approximately 5 mg to approximately 300 mg;
- and
- (ii) at least one Primary Essential Buffer and at least one optional Secondary Essential Buffer in a total amount of approximately 0.1 mEq to approximately 2.5 mEq per mg of proton pump inhibitor;
- and
- (b) a pharmaceutically-acceptable excipient;
- wherein the dosage form is created by a method comprising:
- i) blending the proton pump inhibitor, the Primary Essential Buffer, the optional Secondary Essential Buffer, and the pharmaceutically-acceptable excipient;
- and
- ii) formulating the proton pump inhibitor, the Primary Essential Buffer, the optional Secondary Essential Buffer, and the pharmaceutically-acceptable excipient into a powder, tablet, suspension tablet, chewable tablet, capsule, two-part tablet, two-part capsule, effervescent powder, pellet, granule or effervescent tablet.
Dependencies are inferred from the claim text.