天然蜂毒多肽口服结肠定位释药系统设计及其评价
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陈大为1，刘 星1，邹艳霜1，张荣庆2，张汝华1
(1. 沈阳药科大学药学院，辽宁 沈阳 110016；2. 清华大学生物系，北京 100084)
摘要：目的 制备天然蜂毒多肽口服结肠定位释药系统并对其进行体内评价。方法 将天然蜂毒包封于脂质体内并均匀混悬于高浓度的海藻酸钠溶液中，然后将其滴入含有固凝剂的氯化钙溶液中交联固化并干燥，制成海藻酸钙凝胶小球。将凝胶小球中蜂毒多肽0~8 h内的释放量按Weibull分布进行拟合，以包胶丸率及速度常数、相关系数为判定指标，经正交设计L9(33)试验，筛选出最佳处方。通过流化床包衣技术，采用肠溶性材料Eudragit S 100水分散体包衣，制备天然蜂毒多肽口服结肠定位释药系统。通过测定大鼠单剂量静脉注射及口服给药后的血药浓度，对蜂毒多肽海藻酸钙凝胶小球包衣微丸体内过程进行科学评价。结果 凝胶小球中蜂毒多肽的释药动力学符合Weibull分布模型，相关系数为0.952 9。其在体内的绝对生物利用度为79.88%，而口服蜂毒冻干粉在体内的绝对生物利用度仅为5.23%。结论 该结肠定位释药系统为多肽类药物的口服给药奠定了基础。
关键词：药剂学；蜂毒多肽；脂质体；海藻酸钙凝胶；结肠定位释药；体内外评价
中图分类号：R94 文献标识码：A
Design and evaluation of bee venom oral colon delivery system
CHEN Da-wei1, LIU Xing1, ZOU Yan-shuang1, ZHANG Rong-qing2, ZHANG Ru-hua1
(1. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China; 2. Department of Biology, Tsinghua University, Beijing 100084, China)
Abstract: Objective To prepare oral colon delivery system of bee venom and evaluate pharmacokinetics by ELISA. Methods Alginate gel beads (approximately 1 mm in diameter) were prepared by dripping concentrated sodium alginate solution containing bee venom liposome into concentrated calcium chloride solution including a hardening agent and followed by frozen drying. The release rates of total venom peptides from the gel beads were determined over an 8 h time period and the release model was simulated according to the Weibull’s distribution equation ......
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