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引用本文:王彦竹,赵亚绘,张赫然,孙立章,宋丽明,董欣,王杏林.TM-4000磺丁基醚-β-环糊精包合物的制备及增溶效果研究[J].中国现代应用药学,2019,36(5):545-550.
WANG Yanzhu,ZHAO Yahui,ZHANG Heran,SUN Lizhang,SONG Liming,DONG Xin,WANG Xinglin.Preparation of TM-4000 Sulfobutyl Ether-β-Cyclodextrin Inclusion Complex and Study on Its Solubilization Effect[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(5):545-550.
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TM-4000磺丁基醚-β-环糊精包合物的制备及增溶效果研究
王彦竹1, 赵亚绘2, 张赫然1, 孙立章3, 宋丽明1, 董欣1, 王杏林1
1.天津药物研究院, 释药技术与药代动力学国家重点实验室, 天津 300193;2.中南大学湘雅医院药学部, 长沙 410008;3.正大天晴药业集团股份有限公司, 南京 210000
摘要:
目的 制备TM-4000磺丁基醚-β-环糊精包合物并考察其增溶效果。方法 初步考察磺丁基醚-β-环糊精对TM-4000的增溶效果,并测定不同温度下包合反应的表观稳定常数。通过工艺筛选,确定合理的制备方法和最佳的工艺参数,制备TM-4000的磺丁基醚-β-环糊精包合物,并对其进行表征和溶出度测定。结果 在pH为2.0的盐酸溶液中,磺丁基醚-β-环糊精对TM-4000的增溶效果较好,采用饱和溶液法,水浴温度为50℃,转速为60 r·min-1,反应时间为6 h,TM-4000和磺丁基醚-β-环糊精的重量比为1:5时,能够制备出稳定性较好的包合物。TM-4000的磺丁基醚-β-环糊精包合物在pH 2.0介质中1 h内的累积溶出量可以达到80%。结论 以简便可行的方法制备的TM-4000磺丁基醚-β-环糊精包合物能够显著提高TM-4000的溶出水平。
关键词:  磺丁基醚-β-环糊精  TM-4000  包合物  增溶效果
DOI:10.13748/j.cnki.issn1007-7693.2019.05.007
分类号:R943
基金项目:
Preparation of TM-4000 Sulfobutyl Ether-β-Cyclodextrin Inclusion Complex and Study on Its Solubilization Effect
WANG Yanzhu1, ZHAO Yahui2, ZHANG Heran1, SUN Lizhang3, SONG Liming1, DONG Xin1, WANG Xinglin1
1.Tianjin Institute of Pharmaceutical Research, Tianjin State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin 300193, China;2.Department of Pharmacy, Xiangya Hospital, Central South University, Changsha 410008, China;3.Tianjin Chase Sun Pharmaceutical Co., Ltd., Nanjing 210000, China
Abstract:
OBJECTIVE To prepare TM-4000 sulfobutyl ether-β-cyclodextrin inclusion complex and investigate the solubilization effect. METHODS The solubilization effect of sulfobutyl ether-β-cyclodextrin on TM-4000 was preliminary investigated, and the apparent stability constant of the inclusion reaction at different temperatures was determined. The sulfobutyl ether-β-cyclodextrin inclusion complex of TM-4000 was prepared through process screening. A reasonable preparation method and optimal reaction parameters were determined. The sulfobutyl ether-β-cyclodextrin inclusion complex of TM-4000 was prepared, characterized and tested for dissolution. RESULTS In pH 2.0 hydrochloric acid solution, sulfobutyl ether-β-cyclodextrin solubilization effect of TM-4000 was the best. Inclusion compound with a better stability could be prepared through saturated solution method at 50℃ with 60 r·min-1 stirring in 6 h. The weight ratio of TM-4000 to sulfobutyl ether-β-cyclodextrin was 1:5. The accumulative dissolution of TM-4000-sulfobutyl ether-β-cyclodextrin inclusion complex within 1 h in pH 2.0 medium could reach 80%. CONCLUSION The TM-4000 sulfobutyl ether-β-cyclodextrin inclusion complex prepared in a simple and feasible way can significantly increase the dissolution level of TM-4000.
Key words:  sulfobutyl ether-β-cyclodextrin  TM-4000  inclusion complex  solubilization
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