Multiparticulate bisoprolol formulation

Details Multiparticulate bisoprolol formulation Multiparticulate bisoprolol formulation

A - Human Necessities

61

K

A61K 31/135 (2006.01) A61K 9/50 (2006.01) A61K 31/138 (2006.01)

Patent

CA 2359709

A multiparticulate bisoprolol formulation for once-daily oral administration, each particle of which comprises a core of bisoprolol or a pharmaceutically acceptable salt thereof surrounded by a polymeric coating, the polymeric coating being effective to achieve an initial lag of bisoprolol release in vivo of at least 4-6 hours following administration and thereafter maintaining therapeutic concentrations of bisoprolol for the remainder of the twenty-four hour period. The formulation can be used for night-time dosing so as to minimise the likelihood of acute cardiovascular occurrences in the well- documented high risk period in the morning.

Cette invention a trait à une formulation de bisoprolol multiparticulaire à administrer oralement une fois par jour. Chaque particule de cette formulation comporte un noyau bisoprolol ou un sel de celui-ci acceptable du point de vue pharmaceutique recouvert d'un enrobage polymère, lequel enrobage permettant un décalage initial de la libération du bisoprolol in vivo d'au moins 4 à 6 heures après administration et permettant de conserver à l'organisme, par la suite, des concentrations thérapeutiques de bisoprolol pendant les vingt-quatre heures qui suivent. Il est possible d'utiliser cette formulation pour un dosage nocturne de manière à éviter une éventuelle survenue de manifestations cardio-vasculaires aiguës durant la période matinale à haut risque bien connu.

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