Cyclosporin analog formulations
The present invention relates to formulations containing cyclosporin analogs that are structurally similar to cyclosporin A, in particular isomeric mixtures of cyclosporin analogs that are structurally similar to cyclosporin A. The formulations form stable microemulsion preconcentrates and may provide superior drug bioavailability and/or may reduce one or more adverse effects associated with the administration of cyclosporin. Also disclosed are methods for using and preparing the formulations.
1. A pharmaceutical composition comprising:
a) a pharmaceutically effective amount of ISA Tx 247;
b) triacetin;
c) MCT oil;
d) an emulsifier; and
e) ethanol;
wherein the pharmaceutical composition forms a clear microemulsion upon contact with an aqueous medium.
2. The pharmaceutical composition of claim 1 wherein the emulsifier is selected from the group consisting of: polyoxyethylene(20)sorbitanmonopalmitate and polyoxyethylene(20)sorbitanmonooleate.
3. The pharmaceutical composition of claim 1 , wherein the ratio by weight of ISA Tx 247 : MCT oil:emulsifier:triacetin:ethanol is about 0.5-1:5:3:1:1.