| 摘要 |
PURPOSE:To enable formation of stable liposome containing a substance unstable at a high temperature, at a temperature lower than a phase-transition temperature (Tc), by hydrating a liposome membrane component substance containing phospholipid and cholesterol at >=Tc. CONSTITUTION:Water is added to a liposome membrane component substance containing phospholipid (preferably hydrogenated natural lecithin or synthetic lecithin composed of saturated fatty acid composition) and cholesterol and preferably further a negatively charged substance (e.g. phosphatidic acid and dicetyl phosphate) as an anticoagulant, and the membrane is completely hydrated at >=Tc. The amounts of cholesterol and the negatively charged substance are 0.2-1.0pt.wt. and 0.1-0.3pt.wt. per 1pt.wt. of the phospholipid, respectively. The hydrated product is cooled to <=Tc, maintained at a temperature to keep a compounding drug component from deactivation, mixed with an aqueous solution of a drug and vigorously agitated to form liposome. |
