Sublingual buccal effervescent

Abstract

A pharmaceutical dosage form adapted to supply a medicament to the oral cavity for buccal, sublingual or gingival absorption of the medicament which contains an orally administrable medicament in combination with an effervescent for use in promoting absorption of the medicament in the oral cavity. The use of an additional pH adjusting substance in combination with the effervescent for promoting the absorption drugs is also disclosed.

Description

[0001] The present application is a divisional application of U.S. patent application Ser. No. 09 / 661,693, filed Sep. 14, 2000, which is a continuation application of U.S. patent application Ser. No. 09 / 327,814 filed Jun. 8, 1999, which is a continuation application of U.S. patent application Ser. No. 09 / 277,424, filed Mar. 26, 1999, which claims the benefit of U.S. Provisional Application No. 60 / 079,652 filed on Mar. 27, 1998, the benefit of which is claimed under 35 U.S.C. .sctn.120 and the disclosure of which is incorporated by reference herein.[0002] The present invention relates to pharmaceutical compositions, and more particularly to pharmaceutical compositions for oral administration of a medicament, which contain an effervescent agent for enhancing oral drug absorption across the buccal, sublingual, and gingival mucosa.DESCRIPTION OF PRIOR ART[0003] Effervescents have been shown to be useful and advantageous for oral administration. See Pharmaceutical Dosage Forms: Tablets V...

AI Technical Summary

Benefits of technology

[0031] The dosage form may be administered to a human or other mammalian subject by placing the dosage form in the subject's mouth and holding it in the mouth, either adjacent a cheek (for buccal administration), beneath the tongue (for sublingual administration) and between the upper lip and gum (for gingival administration). The dosage form spontaneously begins to disintegrate due to the moisture in the mouth. The disintegration, and particularly the effervescence, stimulates additional salivation which further enhances disintegration.

Problems solved by technology

However, many compounds do not rapidly penetrate the oral mucosa.

The compounds which may be well absorbed per-orally (through the gastrointestinal tract) may not be well absorbed through the mucosa of the mouth because the oral mucosa is less permeable than the intestinal mucosa and it does not offer as big a surface area as the small intestine.

Despite these and other efforts toward increasing the permeation of medicaments across the oral mucosa, there have been unmet needs for improved methods of administrating medicaments across the oral mucosa.

Effervescent agents can be used alone or in combination with other penetration enhancers, which leads to an increase in the rate and extent of absorption of an active drug.

Such water-activated materials must be kept in a generally anhydrous state and with little or no absorbed moisture or in a stable hydrated form, since exposure to water will prematurely disintegrate the tablet.