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目的:为了提高口服黄体酮后的生物利用度,开发黄体酮口服制剂,制备了一种新型黄体酮前体脂质体口服制剂,并测定了其水合后的包封率。方法:采用一种新型前体脂质体制备方法将黄体酮制成前体脂质体,开发新型前体脂质体口服制剂。采用葡聚糖Sephadex G-50凝胶柱对黄体酮脂质体进行柱分离,测定其包封率。结果:包封率与稀释倍数和药脂比有关。当药脂比为1∶20、稀释倍数为1∶10时,黄体酮前体脂质体包封率可达(72.36±11.69)%。结论:利用前体脂质体制备技术可将黄体酮包裹成脂质体,所形成的脂质体包封率较高,可为黄体酮前体脂质体口服制剂的开发奠定基础。
OBJECTIVE: To improve the bioavailability of progesterone after oral administration of progesterone, a new oral progestin preparation was prepared and its entrapment efficiency after hydration was determined. Methods: A new pro-liposome preparation method was used to make progesterone into pro-liposome and to develop a novel pro-liposome formulation. The progesterone liposomes were separated by Sephadex G-50 gel column and the encapsulation efficiency was determined. Results: The entrapment efficiency was related to dilution ratio and drug-lipid ratio. When the ratio of lipid to lipid was 1:20 and the dilution ratio was 1:10, the entrapment efficiency of progesterone liposomes reached 72.36 ± 11.69%. CONCLUSION: Prolactin can be encapsulated into liposomes by using liposome preparation technique. The entrapment efficiency of liposomes is high, which lays a foundation for the development of progestins.