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目的制备鸦胆子油(BFO)交联环糊精(CDP)包合物(BFO-CDP-IC),并通过急性毒性实验比较BFO-CDP-IC与市售BFO乳剂的安全性。方法提取BFO及合成CDP;采用均质法制备BFO-CDP-IC,通过单因素试验及正交试验设计优化BFO-CDP-IC处方及制备工艺;通过扫描电镜(SEM)法、红外光谱(FTIR)法、核磁共振(1H-NMR)法验证CDP及BFO-CDP-IC的形成;HPLC法测定BFO-CDP-IC中BFO的包封率;通过小鼠急性毒性实验并与市售BFO乳剂进行比较,考察其安全性。结果 BFO得率为17.3%;CDP产率49.26%,交联度8.47;BFO-CDP-IC最佳包合工艺为BFO与CDP投料比1∶10,包合温度20℃,均质时间6 min,稀释BFO的乙醚用量0.5 g;经SEM、FTIR和1H-NMR表明了CDP及BFO-CDPIC形成;HPLC法测得BFO包封率达80%,载药量为7.1%。BFO-CDP-IC的半数致死量(LD_(50))未测出,安全性显著高于市售BFO乳剂(LD_(50)为9.780 g/kg)。结论制备的BFO-CDP-IC包封率高,且与市售BFO乳剂相比毒性降低,安全性高。
OBJECTIVE To prepare BFO-CDP inclusion complex (BFO-CDP-IC) and compare the safety of BFO-CDP-IC and commercially available BFO emulsion through acute toxicity test. Methods The BFO-CDP-IC was prepared by homogeneous method. The formulation and preparation of BFO-CDP-IC were optimized by single factor test and orthogonal design. The scanning electron microscopy (SEM), FTIR ) Method was used to confirm the formation of CDP and BFO-CDP-IC by 1H-NMR. The entrapment efficiency of BFO in BFO-CDP-IC was determined by HPLC. The toxicity of BFO was evaluated by acute toxicity test in mice and commercial BFO emulsion Compare and examine its safety. Results BFO yield was 17.3%, yield of CDP was 49.26%, and degree of cross-linking was 8.47. The best inclusion process of BFO-CDP-IC was the ratio of BFO to CDP was 1:10. Inclusion temperature was 20 ℃ and homogenization time was 6 min . The amount of diethyl ether diluted with BFO was 0.5 g. The formation of CDP and BFO-CDPIC was confirmed by SEM, FTIR and 1H-NMR. The entrapment efficiency of BFO was 80% and the drug loading was 7.1% by HPLC. The median lethal dose (LD_ (50)) of BFO-CDP-IC was not detected, and its safety was significantly higher than that of commercially available BFO emulsion (LD_ (50) was 9.780 g / kg). Conclusions The prepared BFO-CDP-IC has high entrapment efficiency and lower toxicity compared with the commercially available BFO emulsion, with high safety.