Sustained release porous microparticles for inhalation

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/72 (2006.01) A61K 9/12 (2006.01) A61K 9/16 (2006.01) A61K 31/00 (2006.01) A61K 31/56 (2006.01) A61K 31/58 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2500065

Pharmaceutical formulations and methods are provided for the sustained delivery of a pharmaceutical agent to the lungs of a patient by inhalation. The formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein upon inhalation of the formulation a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles in the lungs for at least 2 hours. Preferably, a majority of the pharmaceutical agent is released from the microparticles by 24 hours following inhalation, for example where a majority of the pharmaceutical agent is released no earlier than about 2 hours and no later than about 24 hours following inhalation. Methods for delivering a pharmaceutical agent, such as a corticosteroid, to the lungs of a patient are also provided. For example, the method includes having the patient inhale a dry powder blend comprising the present microparticles and a pharmaceutically acceptable bulking agent.

L'invention concerne des formulations pharmaceutiques et des procédés destinés à l'administration régulière d'un agent pharmaceutique dans les poumons d'un patient par inhalation. Cette formulation comprend des microparticules poreuses qui contiennent un agent pharmaceutique et un matériau de base. Lors de l'inhalation de la formulation, un quantité efficace d'un point de vue thérapeutique ou prophylactique de l'agent pharmaceutique est libérée des microparticules dans les poumons pendant au moins 2 heures. De préférence, une grande partie de l'agent thérapeutique est libérée des microparticules dans les 24 heures qui suivent l'inhalation, par exemple une grande partie de l'agent thérapeutique est libérée depuis pas moins de 2 heures et pas plus de 24 heures après l'inhalation. L'invention porte aussi sur des procédés d'administration d'un agent thérapeutique, tel un corticostéroïde, dans les poumons d'un patient. Par exemple le procédé consiste à faire inhaler au patient un mélange de poudre sèche contenant ces microparticules et un agent gonflant pharmaceutiquement acceptable.

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