Multiparticulate pulsatile drug delivery system

A - Human Necessities – 61 – K

Patent

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A61K 9/56 (2006.01) A61K 9/50 (2006.01) A61K 31/55 (2006.01)

Patent

CA 2163433

A unit dosage form of capsule or tablet composed of a large number of pellets made up of two or more populations of pellets/particles. Each pellet containing a core containing the therapeutic drug and water soluble osmotic agent, which enclose a water-insoluble polymer. The film coating of each population of pellets differs from the coating of every other population of pellets in a dosage form in the rate at which water passes through to the core and the rate at which drug diffuses out of the core. The osmotic agent dissolves in the water causing the pellet to swell and regulating the rate of diffusion of drug into the environment of use. As each population of pellets releases its drugs into the environment sequentially, the effect is to provide a series of pulsatile administrations of the drug from a single dosage form.

Forme galénique individuelle en capsules (4) ou comprimés ou analogue constituée d'un grand nombre de billes (6, 7, 5) elles-mêmes formées de deux populations ou plus de billes/particules. Chaque bille présente un noyau (3) contenant le principe actif et l'agent osmotique soluble dans l'eau, lequel contient un polymère insoluble dans l'eau. L'enrobage de chaque population de billes diffère de celui des autres populations de billes présentes dans la forme galénique pour ce qui concerne la vitess à laquelle l'eau arrive jusqu'au noyau et la vitesse à laquelle le médicament est diffusé à l'extérieur du noyau. L'agent osmotique se dissout dans l'eau, ce qui fait gonfler la bille et régule la vitesse à laquelle le médicament est diffusé dans l'environnement dans lequel il est utilisé. Chaque population de billes libére son médicament dans l'environnement de manière séquentielle, ce qui permet d'assurer une administration pulsatoire du médicament à partir d'une seule forme galénique.

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