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目的:优化丹皮酚阳离子脂质体凝胶剂的制备工艺。方法:采用薄膜分散-探头超声法结合研磨法制备丹皮酚阳离子脂质体凝胶,以包封率、粒径大小及ξ电位为考察指标,以中性脂材/带电脂材摩尔比、药脂比、水化时间和超声条件因素,每因素采取3个水平,利用正交试验优化制备工艺。结果:最佳制备工艺为DC-Chol 160 mg,Chol 300 mg,HSPC 500 mg,溶于40 mg丹皮酚三氯甲烷液(15 mL)中,40℃水浴减压蒸发除去有机溶剂,形成均匀薄膜,加入pH 6.5磷酸盐缓冲液(PBS,0.05 mol.L-1)10 mL水化2 h,探头式超声3 min,再依次过0.8,0.45μm的微孔滤膜,得脂质体溶液。另取卡波姆1.0 g,加入脂质体溶液中,溶胀完全后,加入甘油0.3 g,研磨均匀,即得。结论:薄膜分散-探头超声法结合研磨法制备脂质体凝胶,脂质体包封率较高、粒径分布均匀、ξ电位适宜,制剂黏度佳,刺激性小。
Objective: To optimize the preparation of paeonol cationic liposome gel. Methods: The paeonol cationic liposome gel was prepared by thin film dispersion-probe ultrasonic method and grinding method. The entrapment efficiency, particle size and zeta potential were taken as the investigation indexes. The molar ratio of neutral fat / Lipid ratio, hydration time and ultrasonic conditions, each factor to take three levels, the use of orthogonal test to optimize the preparation process. Results: The optimal preparation conditions were as follows: DC-Chol 160 mg, Chol 300 mg, HSPC 500 mg, dissolved in 40 mg paeonol chloroform solution (15 mL). The organic solvent was removed by evaporation under reduced pressure in a 40 ° C water bath to form a uniform The membrane was hydrated by adding 10 mL of PBS (0.05 mol·L-1) pH 6.5 for 2 h. The probe was ultrasonically sonicated for 3 min and then filtered through a 0.8, 0.45 μm microporous membrane to obtain a liposome solution . Another take carbomer 1.0 g, added to the liposome solution, after swelling completely, adding glycerin 0.3 g, grinding evenly, that is, too. CONCLUSION: The liposome gel prepared by the membrane dispersion-probe ultrasonic method combined with grinding method has the advantages of high encapsulation efficiency, uniform particle size distribution, suitable zeta potential, good viscosity and less irritation.