Highly active, rapidly absorbable formulations of glibenclamide,

Details Highly active, rapidly absorbable formulations of glibenclamide, Highly active, rapidly absorbable formulations of glibenclamide,

1991-08-19

1993-11-02

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Matrices

424439, 424452, 424465, 424451, 424464, 424474, 424489, 424499, 424488, 514866, 514960, A61K 4710, A61K 4726, A61K 908, A61K 914

Patent

active

052581853

ABSTRACT:
This invention relates to highly active and solid pharmaceutical preparations rapidly releasing the active substance for the treatment of diabetes, particularly: 1. liquid formulations of glibenclamide consisting of 1 part of glibenclamide and 4 to 1500 parts of liquid sugar alcohols such as 70% sorbitol solution or glycol such as propylene glycol, hexylene glycol, di-, tri- or polyethylene glycol having a molecular weight from 76 to 600, optionally 0.5 to 2 moles of an alkaline reacting substance and other drug additives; 2. solid formulations of glibenclamide consisting of 1 part of glibenclamide, 4 to 30 parts of sugar alcohols, preferably 70% sorbitol solution, optionally dilute in alcohol, 30 to 150 parts of pharmacologically safe excipients, carrier mterials or other drug additives; and this invention also relates to a process for the production of a molecularly disperse solution or active substance alloy of glibenclamide or another sparingly soluble substance selected from the group consisting of sulfonyl ureas or substances and/or compounds having similar chemico-physical properties.

REFERENCES:
patent: 3979520 (1976-09-01), Rothe et al.
patent: 4696815 (1987-09-01), Schepky et al.
patent: 4708868 (1987-11-01), Brickl et al.
patent: 4727109 (1988-02-01), Schmidt et al.
Martindale, 28th Ed., No. 14038-q, "Isomalt".
ERSTE Internationale ZL-Qualitatsvergleichstudie, "Erhebliche Qualitatsunterschiede bei Glibenclamide-Arzneimitteln", Apotheker Zeitung Nr. 50, Dec. 9, 1991 (with translation).
Blume, Henning et al., "Untersuchungen Zur Therapeutischen Relevanz Der Bioaquivalenz . . . Glibenclamidhaltiger Fertigarzneimittel", Pharmazeutiache Zeitung, 132, Jahrgang Nr. 39-24, Sep. 1987, p. 2352/101.
H. Schiweck, "Alimenta 19", p. 15 (1980).

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