| 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 |
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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
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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
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| 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: |
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| Preparation of TM-4000 Sulfobutyl Ether-β-Cyclodextrin Inclusion Complex and Study on Its Solubilization Effect |
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WANG Yanzhu1, ZHAO Yahui2, ZHANG Heran1, SUN Lizhang3, SONG Liming1, DONG Xin1, WANG Xinglin1
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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
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| 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 |
