摘要
以β-环糊精为药物载体,采用饱和水溶液法制备了吡嗪酰胺-β-环糊精包合物、异烟肼-β-环糊精包合物、异烟肼利福霉素腙-β-环糊精包合物,采用冷冻干燥法制备了胸腺五肽-β-环糊精包合物。吡嗪酰胺与β-环糊精的最佳包合工艺条件为:吡嗪酰胺与β-环糊精物质的量比1.5∶1、包合温度70℃、包合时间1.03 h,此条件下的综合评价为96.18%。异烟肼与β-环糊精的最佳包合工艺条件为:异烟肼与β-环糊精物质的量比1.5∶1、包合温度30℃、包合时间0.5 h,此条件下的综合评价为87.80%。异烟肼利福霉素腙与β-环糊精的最佳包合工艺条件为:异烟肼利福霉素腙与β-环糊精物质的量比1.5∶1、包合温度70℃、包合时间1.08 h,此条件下的综合评价为90.83%。胸腺五肽与β-环糊精的最佳包合工艺条件为:胸腺五肽与β-环糊精物质的量比1.5∶1、包合温度70℃、包合时间1.15 h,此条件下的综合评价为90.03%。包合后药物的水溶解性和热稳定性得到明显改善,具有较好的抗结核杆菌活性。
Using β-cyclodextrin as a drug carrier,we prepared pyrazinamide-β-cyclodextrin inclusion complex,isoniazid-β-cyclodextrin inclusion complex,isoniazid Rifamycin-β-cyclodextrin inclusion complex by a saturated solution method,and prepared thymopentin-β-cyclodextrin inclusion complex by a freeze-drying method.The comprehensive index of assessment is 96.18% under the optimum inclusion conditions of pyrazinamide and β-cyclodextrin as follows:the molar ratio of pyrazinamide and β-cyclodextrin is 1.5∶1,the inclusion temperature is 70 ℃,and the inclusion time is 1.03 h.The comprehensive index of assessment is 87.80% under the optimum inclusion conditions of isoniazid and β-cyclodextrin as follows:the molar ratio of isoniazid and β-cyclodextrin is 1.5∶1,the inclusion temperature is 30 ℃,and the inclusion time is 0.5 h.The comprehensive index of assessment is 90.83% under the optimum inclusion conditions of isoniazid Rifamycin and β-cyclodextrin as follows:the molar ratio of isoniazid Rifamycin and β-cyclodextrin is 1.5∶1,the inclusion temperature is 70 ℃,and the inclusion time is 1.08 h.The comprehensive index of assessment is 90.03% under the optimum inclusion conditions of thymopentin and β-cyclodextrin as follows:the molar ratio of thymopentin and β-cyclodextrin is 1.5∶1,the inclusion temperature is 70 ℃,and the inclusion time is 1.15 h.The water solubility and thermal stability of drug after inclusion improve obviously,and the inclusion complex has good anti-Mycobacterium tuberculosis activity.
作者
祝宏
丁娇
彭薇
马峻
ZHU Hong;DING Jiao;PENG Wei;MA Jun(School of Chemical Engineering and Pharmacy,Key Laboratory for Green Chemical Process of Ministry of Education,Wuhan Institute of Technology,Wuhan 430073,China;Wuhan Jinyintan Hospital,Wuhan 430023,China)
出处
《化学与生物工程》
CAS
2019年第5期46-50,65,共6页
Chemistry & Bioengineering
基金
武汉工程大学研究生教育创新基金项目(CX2017138)
