Extended release formulations of erythromycin derivatives

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills

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424468, 424480, A61K 920, A61K 922, A61K 936

Patent

active

060107189

ABSTRACT:
Disclosed is a pharmaceutical composition for extended release of an erythromycin derivative in the gastrointestinal environment. The composition comprises an erythromycin derivative and a pharmaceutically acceptable polymer so that, when ingested orally, the composition induces statistically significantly lower C.sub.max in the plasma than an immediate release composition of the erythromycin derivative while maintaining bioavailability and minimum concentration substantially equivalent to that of the immediate release composition of the erythromycin derivative upon multiple dosing. The compositions of the invention have an improved taste profile and reduced gastrointestinal side effects as compared to those for the immediate release composition.

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patent: 4226849 (1980-10-01), Schor
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patent: 4808411 (1989-02-01), Lu et al.
patent: 4842866 (1989-06-01), Horder et al.
patent: 5393765 (1995-02-01), Infeld et al.
Die Pharmazie, vol. 50, No. 4 (Feb. 1995), pp. 154-155, J. Rak et al., "Matrixtabletten aus Niedrigviskoser Hydropromellose".
Journal of Controlled Release, vol. 12 (1990), pp. 133-141, K.V. Ranga Rao et al., "Influence of Molecular Size and Water Solubility of the Solute on Its Release from Swelling and Erosion Controlled Polymeric Matrices".

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