Pharmaceutical formulation containing a release rate controlling composition

摘要

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.

主权项

1. A pharmaceutical formulation for oral administration as a solid dose, which comprises an effective amount of a potassium salt of Compound A and a release rate controlling composition comprising a solubilizing agent, a gelling agent, and optionally a water soluble filler, wherein Compound A is:the solubilizing agent comprises a poloxamer, the gelling agent comprises a high-viscosity hydroxypropylmethylcellulose; and the optional water soluble filler comprises lactose,and wherein:
the potassium salt of Compound A is employed in an amount in a range of from about 25 to about 75 wt. % on a free phenol basis; the poloxamer is employed in an amount in a range of from about 10 to about 20 wt. %; the high-viscosity hydroxypropylmethylcellulose is employed in an amount in a range of from about 3 to about 9 wt. %; and the lactose is employed in an amount in a range of from 3 to about 9 wt. %.