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-CDP- IC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（LD₅₀）未测出，安全性显著高于市售BFO乳剂（LD₅₀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 Bruceae Fructus oil (BFO) β-cyclodextrin polymer (CDP) inclusion complexes (BFO-CDP-IC), and investigate its safety by acute toxicity test. Methods BFO was extracted and CDP was prepared according to the literature, the IC of BFO with CDP (BFO-CDP) was prepared by homogenizing method and characterized by SEM, ¹H-NMR, and FT-IR. The optimum preparation process was determined by single factor test and L₉(3⁴) orthogonal test. Entrapment efficiency (EE) was determined by HPLC. Acute toxicity of BFO-CDP-IC was assessed by determining the number of deaths of ICR mice over gavage treatment for 2 weeks. The commercial emulsion of BFO (BFOE) was used as a reference. Results The extraction rate of BFO was 17.3%, the yield of CDP was 49.26%, and the degree of crosslinking was 8.47. The optimal conditions for preparation were as follows, ratio of BFO and CDP was 1:10, preparation temperature and time was 20 ℃ and 6 min, the amount of ether was 0.5 g. Additionally, the HPLC data showed that drug loading of complexes was 7.1%, and EE was 80%. In the acute toxicity test, the median lethal dose (LD₅₀) of BFOE was 9.78 g/kg. In contrast, all mice treated with IC survived even at the highest dosage (15.36 g/kg). Conclusion The prepared BFO-IC has high EE compared with commercially available BFOE, BFO-CDP polymer significantly decreased toxicity of BFO.

研究生创新工程项目（CXLX_1441）