Pharmaceutical compositions of adsorbates of amorphous drugs and lipophilic microphase-forming materials
First Claim
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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, sorbitan 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 and said lipophilic microphase-forming material of about 10 or more.
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Abstract
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.
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Citations
16 Claims
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1. A composition comprising:
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(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, sorbitan 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 and said lipophilic microphase-forming material of about 10 or more. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)
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Specification