主动载药方式石斛碱脂质体的制备研究

Study on Preparation of Active Drug Loaded Liposome

目的:石斛碱具有退热、止痛作用,还可降低心率、血压,减慢呼吸,使血糖中度升高,同时还可解巴比妥中毒。但石斛碱难溶于水、生物利用度低,限制了其在临床方面的应用。脂质体有靶向性,缓释性,降低药物毒性和提高药物稳定性等特点,运用主动载药方式将提高脂质体的稳定性、包封率。本次试验旨在探究石斛碱脂质体的制备,为石斛碱制备脂质体剂型提供参考依据。方法:乙醇加热回流提取石斛碱,经减压蒸馏浓缩,冷冻干燥、重结晶得到石斛碱。乙醇注入-超声分散法制备空白脂质体,pH梯度法主动载药方式包封药物。结果:柱分离度为0.72,包封率为96.7%,在透射电镜下观察其形态粒径,为分布均匀的圆球形,平均粒径约为20~50 nm。结论:在制备石斛碱脂质体时,采用主动载药方式能得到质粒均一,包封率较高,稳定性较好地脂质体。

Objective: Dendrobine has analgesic, antipyretic effect, reduce heart rate, blood pressure, slow breathing, blood glucose were moderately elevated, with strong effect and solution of barbiturate poisoning. But Dendrobium alkali insoluble in water, low bioavailability, limiting its application in clinic. Liposome target to, sustained release, reduce drug toxicity and improve drug stability characteristics, will improve the stability of liposomes by active loading method, encapsulation efficiency. This experiment aims to explore dendrobine liposome preparation, Dendrobium alkali preparing liposomal formulations provide a reference basis. Methods: Ethanol reflux extraction of dendrobine, decompression distillation and concentration, freeze drying, recrystallization of dendrobine. By ethanol injection ultrasonic dispersing method to prepare blank liposome, pH gradient active loading drug delivery the drug entrapment. Result: The optimal technology extraction conditions were soaking 3 h, extraction 5 h, liquid material ratio 1︰12. Under these conditions, the average mass of volatile oil was 0.3184 g with a small deviation(10.18 %) between the predicted value(0.3545 g). The relative standard deviation(RSD) was 3.67 %. Conclusion: The active loading method can get uniform plasmid, high entrapment efficiency, stability better liposome in the preparation of dendrobium stem alkaloids liposomes.