초록 ▼

Stable solutions of lipophilic drugs, such as cyclosporin, forming a polar lipid self-emulsifying drug delivery system. The solutions can include lipophilic drugs, such as cyclosporin, dissolved in a polar lipid, such as having a C6-C12 fatty acid monoglyceride content of at least about 50%, surfact

Stable solutions of lipophilic drugs, such as cyclosporin, forming a polar lipid self-emulsifying drug delivery system. The solutions can include lipophilic drugs, such as cyclosporin, dissolved in a polar lipid, such as having a C6-C12 fatty acid monoglyceride content of at least about 50%, surfactants and triglycerides. The composition forms a fine emulsion on exposure to water. The encapsulated dosage form of this composition needs neither a hydrophilic component nor air-tight blister packaging, and is particularly suitable for oral administration.

대표청구항 ▼

What is claimed is: 1. A composition for oral administration comprising: 1) a cyclosporin and a carrier medium comprising 2) polyethylene glycol glyceryl fatty acid ester, 3) a monoglyceride, diglyceride, medium-chain triglyceride, or mixtures thereof, and 4) a surfactant in addition to 2) and 3

What is claimed is: 1. A composition for oral administration comprising: 1) a cyclosporin and a carrier medium comprising 2) polyethylene glycol glyceryl fatty acid ester, 3) a monoglyceride, diglyceride, medium-chain triglyceride, or mixtures thereof, and 4) a surfactant in addition to 2) and 3) wherein the composition, on contact with an aqueous phase, is capable of spontaneously forming a clear, fine emulsion. 2. The composition of claim 1 wherein the polyethylene glycol glyceryl fatty acid ester comprises PEG(8) caprylic/capric glyceride. 3. The composition of claim 1 wherein the surfactant comprises PEG castor oil. 4. The composition of claim 3 wherein the polyethylene glycol glyceryl fatty acid ester comprises PEG(8) caprylic/capric glyceride. 5. The composition of claim 1 comprising a medium-chain monoglyceride. 6. The composition of claim 5 wherein the polyethylene glycol glyceryl fatty acid ester comprises PEG(8) caprylic/capric glyceride. 7. The composition of claim 5 wherein the surfactant comprises PEG castor oil. 8. The composition of claim 7 wherein the polyethylene glycol glyceryl fatty acid ester comprises PEG(8) caprylic/capric glyceride. 9. The composition of claim 1 wherein the surfactant comprises polysorbate 80. 10. The composition of claim 1 wherein the surfactant comprises polysorbate 20. 11. The composition of claim 7 comprising medium chain triglyceride. 12. The composition of claim 5 comprising monoglyceride and polysorbate 80. 13. The composition of claim 1 wherein the polyethylene glycol glyceryl fatty acid ester comprises polyglycolyzed glycerides. 14. The composition of claim 13 wherein the polyglycolyzed glycerides comprises polyglycolyzed C8-C10 glycerides. 15. The composition of claim 13 wherein the polyglycolyzed glycerides comprise a surfactant having HLB from about 10 to 16. 16. The composition of claim 1 wherein upon contact with an aqueous phase, the composition forms an emulsion of mean particle size of less than about 50 nm. 17. The composition of claim 16 wherein upon contact with an aqueous phase, the composition forms and emulsion of mean particle size of less than about 30 nm.