Pharmaceutical formulation of carboxamide hiv integrase...

A - Human Necessities – 61 – K

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A61K 31/513 (2006.01) A61K 9/20 (2006.01) A61K 31/517 (2006.01)

Patent

CA 2588445

Pharmaceutical formulations suitable for oral administration in solid dosage forms are described. The compositions comprise an effective amount of a base salt of a compound of Formula (I) and a release rate controlling composition comprising a solubilizing agent, a gelling agent, and a water soluble filler; wherein R1, R2, R3 and R4 are defined herein. The formulations are suitable for use in the inhibition of HIV integrase, the treatment and prophylaxis of HIV infection, and the treatment, prophylaxis and delay in the onset of AIDS.

L'invention concerne des préparations pharmaceutiques appropriées à une administration orale sous formes dosifiées solides. Ces compositions contiennent une quantité efficace d'un sel de base d'un composé de formule (I) et une composition de contrôle du taux de libération qui renferme un agent solubilisant, un agent gélifiant et une charge soluble dans l'eau. Dans la formule (I), R1, R2, R3 et R4 sont définis tels que mentionnés. Lesdites préparations sont appropriées dans l'inhibition de l'intégrase du VIH, le traitement et la prophylaxie d'une infection au VIH, ainsi que dans le traitement, la prophylaxie et le retard de l'apparition du sida.

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