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Formulations for therapeutic agents absorbed through mucous membranes

a technology of therapeutic agents and mucous membranes, applied in the field of formulations for therapeutic agents absorbed through mucous membranes, can solve the problems of difficult technical problems, ineffective interaction, and mucous membranes

Inactive Publication Date: 2003-03-20
ELAN PHRMA INT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The development of appropriate surface active stabilizers that will enable mucous membranes to be utilized to enhance bioavailability represents a difficult technical problem.
The primary difficulty with previously reported mucoadhesive stabilizers is that they do not interact effectively with both the particles of the therapeutic agent and mucous membrane uniformly so that, e.g., both the upper and lower GI tract can be used as sites to increase bioavailability.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

Paclitaxol 10 g Pluronic F108 5.0 g Benzoate Sodium 0.2 g Saccharin Sodium 0.1 g FD&C Red No. 40 0.03 g Water, qs 100 ml Example 2 Naproxen 5.0 g Pluronic F68 3.0 g Benzoate Sodium 0.2 g Sorbate Potassium 0.15 g Saccharin Sodium 0.1 g FD&C Red No. 40 0.03 g Water, qs 100 ml Example 3 Griseofulvin 5.0 g Pluronic F127 2.5 g Benzoate Sodium 0.2 g Saccharin Sodium 0.1 g FD&C Red No. 3 0.03 g Water, qs 100 ml Example 4 Paclitaxol 0.5 g Sucrose 10 g Pluronic F87 .25 g Dioctylsulfosuccinate 0.1 g Methylparabens 0.2 g Propylparabens 0.07 g FD&C Yellow No. 5 0.03 g Water, qs 100 ml Example 5 Phenytoin 5.0 g Pluronic F108 2, 5 g Sorbitol 5 g Benzoate Sodium 0.2 g Water, qs 100 ml

[0055] The following Table 2 is a listing of formulations comprised of particles of therapeutic agents produced by wet grinding in the presence of the poloxamer listed which resulted in the particles having the poloxamer absorbed on the surface thereof. The weight average particle size of the resulting particles is al...

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Abstract

Particulate crystalline therapeutic substances are formulated with stabilizers to enhance contact between the crystalline therapeutic substances and the mucosal membranes to provide extended therapeutic effect.

Description

RELATIONSHIP TO OTHER APPLICATIONS[0001] This is a continuation-in-part of copending application Ser. No. 08 / 366,841, filed Dec. 30, 1994.[0002] 1. Field of the Invention[0003] This invention relates to improved formulations of poorly soluble crystalline therapeutic agents which are absorbed through mucous membranes.[0004] 2. Background of the Invention[0005] There is a constant need in the pharmaceutical industry for improved pharmaceutical formations which enhance the efficacy of poorly soluble therapeutic agents. There is especially a need for formulations that (1) enhance the adsorption of poorly soluble therapeutic agents across mucous membranes or (2) extend the period of time that poorly soluble therapeutic agents useful for treating of a site have contact with the mucosa of the site.[0006] Since most poorly soluble crystalline therapeutic agents do not inherently adhere to mucosal surfaces, there is a need to provide in such formulations, primary surface active stabilizers w...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/14A61K9/51A61K49/04A61M36/14
CPCA61K9/146A61K9/5146A61K49/0423A61K49/049B82Y5/00Y10S977/906Y10S514/975
Inventor LIVERSIDGE, GARY G.EICKHOFF, W. MARKILLIG, KATHLEEN J.SARPOTDAR, PRAMODRUDDY, STEPHEN B.
Owner ELAN PHRMA INT LTD