阿苯达唑-甲基-β环糊精包合物的制备和物像鉴定  

Synthesis and Characterization of the Albendazole-methyl-β-cyclodextrin Inclusion Complex

作　　者：张志远 徐淑凤 马艳芝 聂结华 廖洁丹 ZHZNG Zhi-yuan;XU Shu-feng;MA Yan-zhi;NIE Jie-hua;LIAO Jie-dan(Collegeof Life Science and Engineering,Foshan University,Foshan,Guangdong,528225,China)

机构地区：[1]佛山科学技术学院生命科学与工程学院,广东佛山528225

出　　处：《动物医学进展》2024年第8期65-70,共6页Progress In Veterinary Medicine

基　　金：广东省研究生教育创新计划资助项目(2022JGXM129,2022JGXM128,2023ANLK-080);佛山市自筹经费类科技计划项目(2220001005797);佛山市社科规划项目(2024GJ037);2024年佛山科学技术学院学生学术基金项目。

摘　　要：为提高难溶性药物阿苯达唑(ABZ)的水溶性,制备阿苯达唑-甲基-β-环糊精包合物(ABZ-Me-β-CD)。通过单因素试验和正交试验,以包合物的包合率和回收率为指标,探索了包合物的最佳制备工艺。通过相溶解度试验,确定最佳包合材料。用高效液相色谱法(HPLC)对包合物的溶解度、包合率以及体外溶出度进行了检测。最后用粉末X-射线衍射(XRD)和扫描电镜(SEM)对包合物的物象结构进行鉴定。结果表明,包合物的最佳制备工艺为超声法、时间60min、功率60%(360W)、主客摩尔比1:3;最佳包合材料为甲基-β-环糊精。包合物在水中的溶解度为(22.3±0.66)mg/mL,是阿苯达唑原药(0.2μg/mL)的11万倍。包合物的体外溶出度是阿苯达唑原药的8倍。包合物的平均回收率、包合率分别为95%和16.5%,经X-射线衍射和扫描电镜鉴定,证实了阿苯达唑和环糊精处于非晶体结构的包合状态。研究制备的阿苯达唑环糊精包合物,大幅提升了难溶性药物阿苯达唑的水溶性和溶出度,且制备方法简单易行,适用于工业生产。To enhance albendazole's water solubility,we synthesized albendazole-methyl-β-cyclodextrin(ABZ-ME-β-CD).Through systematic experiments,we optimized the inclusion complex preparation method,focusing on inclusion and recovery rates.The ideal inclusion material was determined via a phase solubility test.High-performance liquid chromatography(HPLC)assessed the solubility,inclusion rates,and dissolution.Optimal conditions were as follows:ultrasonic method,60 minutes,60%power(360 W),and a 1:3 molar ratio(subject to guest).Methyl-β-cyclodextrin proved the most effective inclusion material.The resulting complex exhibited impressive water solubility,reaching(22.3±0.66)mg/mL,a remarkable 110000-fold increase over albendazole(0.2μg/mL).In vitro dissolution was eight times faster than albendazole.Average recovery and inclusion rates were 95%and 16.5%,respectively.X-ray diffraction and scanning electron microscopy confirmed albendazole's amorphous inclusion within the cyclodextrin.In conclusion,this study significantly improved albendazole's water solubility and dissolution via cyclodextrin inclusion.The method's simplicity and scalability make it suitable for industrial production.

关 键 词：阿苯达唑 包合物 超声法 环糊精 水溶性 

分 类 号：S859.1[农业科学—临床兽医学]