Transnasal anticonvulsive pharmaceutical composition

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S785000

Reexamination Certificate

active

07745430

ABSTRACT:
Disclosed herein is a transnasal anticonvulsive pharmaceutical composition comprising diazepam as an active ingredient, water, a fatty acid ester, diethylene glycol monoethyl ether, ethanol and sodium glycocholate, wherein the weight of the fatty acid ester is at least 2-fold higher than that of water and is at least 2-fold higher than that of ethanol.The anticonvulsive pharmaceutical composition for transmucosal delivery of diazepam according to the present invention includes a minimized content of water and ethanol, a fatty acid ester as a main ingredient and no use of a polar solvent, e.g. glycol, and, exhibits improved diazepam solubility and transmucosal permeability due to using a small amount of water and ethanol. The present invention also includes treatment of convulsions by transnasally administering to a patient in need thereof a therapeutically effective amount of the disclosed compositions.

REFERENCES:
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patent: 6627211 (2003-09-01), Choi et al.
patent: 2002/0032171 (2002-03-01), Chen et al.
patent: 2005/0002987 (2005-01-01), Choi et al.
Bechgaard et al. Solubilization of various benzodiazepines for intranasal administration, a pilot study. Pharm. Dev. Tech. 2 (3), 293-96 (1997).
Moolenaar, et al., International Journal of Pharmaceutics, 5 (1980) 127-137.
Lau and Slatterery (Lau et al., Int. J. Pharm, 54:171-174 (1989).
Li et al. (International Journal of Pharmaceuticals vol. 237, pp. 77-85, 2002.

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