Sublingual buccal effervescent

a buccal effervescent, sublingual technology, applied in the direction of organic active ingredients, pharmaceutical active ingredients, pharmaceutical delivery mechanisms, etc., can solve the problems of unsatisfactory needs for improving the method of administration, many compounds do not rapidly penetrate the oral mucosa, and are not well absorbed per-orally (through the gastrointestinal tract)

Inactive Publication Date: 2003-05-15
CIMA LABS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 2

[0034] The dosage form included prochlorperazine (pKa=8.1), an effervescent and pH adjusting substance so that a slightly higher pH is produced to facilitate the permeation enhancement.

[0035] With respect to prochlorperazine, an anti-emetic drug, two formulations, buccal and sublingual, were developed. The buccal tablets were compressed as quarter inch diameter biconvex tablets, whereas the sublingual tablets were three-eighths inch diameter biconvex tablets. These dimensions were chosen to give a comfortable fit in the respective part of the oral cavity for which they were designed. The formulae for these tablets are as follows:

3 QUANTITY FORMULATION COMPONENT NAME (MG) BUCCAL Prochlorperazine 5.00 Sodium Bicarbonate 15.52 Citric Acid, Anhydrous 11.08 Sodium Bicarbonate 45.78 HPMC K4M Prem 5.00 Dicalcium phosphate 5.00 dihydrate Mannitol 11.67 Magnesium Stearate 0.95 Total 100.00 SUBLINGUAL Prochlorperazine 5.00 Sodium Bicarbonate 61.25 Citric Acid, Anhydrous 43.75 Sodium Bicarbona...

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/46A61K31/4468A61K31/5415
CPCA61K9/0007A61K9/0056A61K31/5415A61K31/4468A61K9/006
Inventor PATHER, S. INDIRANKHANKARI, RAJENDRA K.EICHMAN, JONATHAN D.ROBINSON, JOSEPH R.HONTZ, JOHN
Owner CIMA LABS
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