Merck Patent Gesellschaft MIT

Merck Patent Gesellschaft

Olivier Saslawski

Philippe Giet

Dominique Michel

Thierry Holot

Laurence Orlando

The present invention relates to an orally administrable galenic formulation allowing improved absorption by the transmembrane or paracellular route in the gastrointestinal tract of active ingredients which are hydrophilic or ionizable in physiological media. The galenic formulation comprises at least one active ingredient, an absorption-promoting agent, and one or more pharmaceutically acceptable excipients.

Orally administerable immediate-release and prolonged-release galenic form comprising an absorption-promoting agent and use of this absorption-promoting agent

The present invention relates to an orally administrable galenic form allowing improved absorption by the transmembrane or paracellular route in the gastrointestinal tract of active ingredients which are hydrophilic or ionizable in physiol. media, comprising at least one such active ingredient, an absorption-promoting agent having an HLB>8, the the absorption-promoting agent consisting of one or more lipid substances chosen from: polysorbates; polyoxyethylene ethers; esters of polyoxyethylene and fatty acids; fatty acids; fatty alcs.; bile acids and their salts with pharmaceutically acceptable cations; esters of C1-C6 alkanol with fatty acids; esters of polyol with fatty acids, the polyol comprising from 2 to 6 hydroxyl functional groups; and polyglycolyzed glycerides; in combination with one or more pharmaceutically acceptable excipients, the pharmaceutical forms comprising captopril being excluded. A controlled-release tablet contained (1) cores contg. calcium acamprosate 50, Gelucire 44/14 10, Compritol 10, microcryst. cellulose 19, Povidone 10, and Mg stearate 1% and (2) a film-coating compn. contg. HPMC 64, PEG-4000 15, and talc 21%.

Orally administrable immediate-release and prolonged-release galenic form comprising an absorption-promoting agent and use of this absorption-promoting agent

A multi-layer tablet for the instant and prolonged release of active substances comprises at least two layers where the first outer layer comprises a mixture of excipients and an active substance, allowing for the immediate release of the active substance within the first layer, and a second layer, arranged in contact with the first layer. The second layer comprises a nonbiodegradable inert porous polymeric matrix in which an active substance is dispersed, allowing for the prolonged release of the active substance within the second layer.

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Lyons, France

Olivier Saslawski