Film coated tablet for improved upper gastrointestinal tract safety

Abstract

A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines / antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

Description

CROSS REFERENCE [0001] This application is a continuation of prior U.S. application Ser. No. 10 / 401,352 filed on Mar. 28, 2003 and which claims priority to application Ser. No. 09 / 694,799 filed Oct. 23, 2000, allowed on Jan. 2, 2003, now U.S. Pat. No. 6,569,460, issued May 27, 2003, which is a Continuation of U.S. application Ser. No. 09 / 095,322 filed Jun. 10, 1998, now U.S. Pat. No. 6,165,513, issued Dec. 26, 2000 which claims the benefit of U.S. Provisional Application Ser. No. 60 / 049,306 filed Jun. 11, 1997.TECHNICAL FIELD [0002] The present invention relates to novel oral dosage forms that protect the epithelial and mucosal tissues of the mouth and the buccal cavity, the pharynx, the larynx, and the esophagus from erosion, ulceration, or other like irritation suffered by direct contact of these tissues with the active ingredient. The tablet is a modified oval shape and is film coated. This invention further relates to a method of treating or preventing diseases characterized by ...

AI Technical Summary

Benefits of technology

[0006] The present invention is directed to a pharmaceutical formulation in an oral generally oval shaped, including but not limited to oval, modified oval and caplet shaped form. The dosage form is film coated and comprised of a safe and effective amount of an active ingredient and pharmaceutically-acceptable excipients. Said dosage forms facilitate rapid esophageal transit time thereby avoiding the release of active ingredient in the buccal cavity, pharynx, and esophagus and protecting the epithelial and mucosal tissues thereof from erosion, ulceration or other like irritation.

[0007] Accordingly, the novel dosage forms described herein effect the delivery to the stomach of said human or other mammal of a safe and effective amount of active ingredient, and substantially alleviates esophagitis or esophageal irritation which sometimes accompanies the oral administration of certain active ingredients.

Problems solved by technology

It is hypothesized that said irritation results from the active ingredient coming in direct contact with those epithelial and mucosal tissues, resulting in the topical irritation thereof.

Particularly problematic drugs are those which when dissolved have a pH below 2-3, drugs with cytotoxic activity (caustic) and / or the local development of a hyperosmolar solution which causes mucosal desiccation.

But, in certain instances its is undesirable or unnecessary for a medicant to be in a delayed release dosage form.

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