| 摘要 |
A pharmaceutical composition comprising cyclosporine is provided to be able to increase bioavailability after being administered into gastrointestine, and be able to control the administration amount by adding small amount of carrier such as a hydrophilic solvent, a hydrophobic surfactant and an amphiphilic surfactant into an insoluble cyclosporine so as to obtain an uniform and transparent nano-emulsion concentrate solution. The nano-emulsion concentrate solution composition comprising cyclosporine is characterized in that it consists of 2-35 parts by weight of cyclosporine powder having a size of 0.01-0.1 micrometer, 5-35 parts by weight of a hydrophilic solvent selected from the group consisting of propyleneglycol, ethyleneglycol monoethylether and a mixture thereof, 10-50 parts by weight of a hydrophobic surfactant selected from the group consisting of polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester and a mixture thereof, and 10-50 parts by weight of an amphiphilic surfactant of polyoxyethylene-polyoxypropylene copolymer. The cyclosporine powder is obtained by quick freezing molten cyclosporine at a temperature of more than 148-151 deg.C using liquid nitrogen to obtain amorphous cyclosporine and crushing it with a high energy plantary ball mill.
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