A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 9/52 (2006.01) A61K 9/50 (2006.01)
Patent
CA 2463134
The invention concerns a microparticulate system for delayed and controlled release of active principles whereof the in vivo absorption window is essentially limited to the high parts of the gastrointestinal tract, said system being designed for oral administration. The invention aims at providing a system for reliably releasing active principles through a double time-dependent and pH-dependent mechanism. Therefor, the invention proposes a multiple microcapsule galenic oral formulation designed so as to guarantee its therapeutic efficacy, and wherein the release of active principles is controlled by a double release-triggering mechanism: time-triggering and pH-triggering. Said system consists of microcapsules (200 to 600 mu m) comprising a core of active principles coated with a coating film (not more than 40 wt. %) including a hydrophilic polymer A (Eudradigit3L) and a hydrophobic compound B (vegetable wax with melting point between 40 to 90 DEG C), B/A ranging between 0.2 and 1.5. Said microcapsules have a dissolving behaviour in vitro such that at constant pH 1.4, a latent period ranging between 1 and 5 hours is observed followed by a release of active principles and such that the shift from pH 1.4 to of pH 6.8 results in a release of active principles without latent time in vitro.
L'invention conceme un système microparticulaire à libération retardée controlée de principes actifs (PA) dont la fenêtre d'absorption in vivo est essentiellement limitée aux parties hautes du tractus gastro-intestinal, ce système étant destiné à une administration par voie orale. Le but de l'invention est de foumir un système assurant la libération du PA de fasçon certaine grâce à un double mécanisme de libération "temps dépendant" et "pH dépendant".Pour atteindre ce but, l'invention proposé une forme galénique orale multimicrocapsulaire conçue de telle sorte que son efficacité thérapeutique soit garantie, et dans laquelle la libération du PA est régie par un double mécanisme de déclenchement de la libération: "temps déclenchant" et "pH déclenchant" Ce système est constitue de microcapsules (200 a 600 ~m) comprenant un coeur en PA recouvert d'une pellicule d'enrobage (maximum 40% en poids) comprenant un polymère hydrophile A (Eudragit® L) et un composé B hydrophobe (cire végétale température de fusion = 40-90~C), avec B/A compris entre 0,2 et 1,5. Ces microcapsules ont un comportement de dissolution in vitro tel qu'a pH 1,4 constant, on observe une phase de latence comprise entre 1 et 5 heures suivie d'une libération du PA et tel que le passage de pH 1,4 à pH 6,8 entraîne une libération du PA sans temps de latence in vitro.
Castan Catherine
Legrand Valerie
Meyrueix Remi
Soula Gerard
Flamel Technologies
Robic
LandOfFree
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