【摘要】 目的将从新疆民族药蒺藜科植物骆驼蓬种子中提取的抗肿瘤活性生物碱成分———盐酸去氢骆驼蓬碱(HM),制成可供肝动脉栓塞的微球新剂型,对其处方设计及制备工艺进行研究。方法选择具有生物可降解性、无毒、价廉的明胶为载体,采用乳化分散法制备盐酸去氢骆驼蓬碱明胶微球,以外观、粒径、载药量、包封率等为考察指标,采用均匀设计确定了盐酸去氢骆驼蓬碱微球的制备工艺。结果含药微球为淡黄色粉末,光镜及电镜观察微球球形圆整,表面附有少量药物结晶。平均产率为86.63%,载药量为(34.45±0.35)%(g/g);包封率为63.00%(g/g)。平均算术径为63.0μm,平均体积径为69.6μm,粒径分布基本属正态,跨度Span为0.769。HM-GMS体外释药规律可用R itger-peppas方程表示,具有一定的缓释特性。结论所研制微球符合肝动脉栓塞微球剂的要求。更多还原

【Abstract】 OBJECTIVE To extract Harmine(HM) hydrochloride,an effective anticancer alkaloid ingredient in Preganum harmala seeds which was used by Uygur and Mongolian as a traditional medicine as microspheres(HM-GMS) for hepatic arterial embolization.METHODS Gelatin was chosen as carrier of microspheres because of its characters of biodegradationable,low toxicity and no interaction between drugs.In preparation technology for HM-GMS,the pharmaceutical investigation was performed using uniform design. RESULTS HM-GMS showed light yellow color,spherical with a rough surface.The mean percent of yield of three batches HM-GMS was 86.63%,the drug loading was 34.45%,and the embedding ratio was 63.00%.Release profile in vitro could be described by the Ritger-peppas equation.HM-GMS had the property of sustained release.CONCLUSION HM-GMS may be suitable for hepatic arterial embolization.更多还原