Pharmaceutical compositions of adsorbates of amorphous drugs and lipophilic microphase-forming materials

摘要

A pharmaceutical composition comprises a solid adsorbate comprising a drug adsorbed onto a substrate and a lipophilic microphase-forming material. The solid adsorbate may also be co-administered with a lipophilic microphase-forming material to an in vivo use environment. The compositions of the present invention enhance the concentration of drug in a use environment.

主权项

1. A composition comprising:
(a) a spray-dried solid dispersion adsorbate comprising a completely amorphous drug and a concentration enhancing polymer adsorbed onto an inorganic oxide substrate, and wherein said drug in said adsorbate is substantially completely amorphous and (b) a lipophilic microphase-forming material selected from the group consisting of medium-chain glyceryl mono-, di-, and tri-alkylates, sorbitan esters, fatty acid esters, polyoxyethylene sorbitan fatty acid esters, alpha tocopheryl polyethylene glycol 1000 succinate (TPGS), and mixtures thereof; said composition having a mass ratio of said lipophilic microphase-forming material to said drug of from 0.1 to 500, and wherein said lipophilic microphase forming material is co-adsorbed with said drug onto said substrate of the spray-dried solid dispersion adsorbate; wherein said lipophilic microphase-forming material is water immiscible and said drug has a partition coefficient Kp between a use environment.