| 氯化钠强化硫酸吗啡缓释液体栓制备及其性能 |
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| 引用本文： | 丁明和,娄杰,洪春雪,耿琴,曹宇,李星,束家有.氯化钠强化硫酸吗啡缓释液体栓制备及其性能[J].武汉大学学报(理学版),2011,57(4):277-282. |
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| 作者姓名： | 丁明和 娄杰 洪春雪 耿琴 曹宇 李星 束家有 |
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| 作者单位： | 武汉大学药学院,湖北武汉,430072 |
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| 基金项目： | 国家火炬计划项目(2010GH021397)资助 |
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| 摘 要： | 根据温敏原位凝胶的特性制备了以泊洛沙姆407/188为主要基质,卡波姆、氯化钠、氮酮和2,6-二叔丁基-4-甲基苯酚为添加剂的硫酸吗啡缓释液体栓,测定了其凝胶温度、凝胶强度和生物黏附力,研究了其体外溶出和在Beagle犬体内的药物吸收.用3p97程序计算药物代谢动力学参数,进行体外释放和体内吸收的相关性研究.结果表明,一定量的氯化钠与卡波姆产生协同作用,使凝胶温度下降,凝胶强度增加.该缓释液体栓在体外释药符合零级模式,在Beagle犬体内释药过程符合一室模型.其中,经氯化钠强化的处方（卡波姆为0.8%,氯化钠为1.0%）相关药物代谢动力学参数为：峰浓度为409.7 ng.mL-1,血药浓度-时间曲线下面积（AUC）为5 708 ng.h.mL-1,体内平均滞留时间（MRT）为10.92 h,体外释药时间为7~10 h,体内缓释时限达9~18 h,显示出良好的缓控释特征.
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| 关 键 词： | 硫酸吗啡缓释液体栓 卡波姆 泊洛沙姆 水凝胶 药物代谢动力学 |
Preparation and Property of Morphine Sulfate Sustained-Release Liquid Suppository Reinforced by Sodium Chloride |
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| DING Minghe,LOU Jie,HONG Chunxue,GENG Qin,CAO Yu,LI Xing,SHU Jiayou.Preparation and Property of Morphine Sulfate Sustained-Release Liquid Suppository Reinforced by Sodium Chloride[J].JOurnal of Wuhan University:Natural Science Edition,2011,57(4):277-282. |
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| Authors: | DING Minghe LOU Jie HONG Chunxue GENG Qin CAO Yu LI Xing SHU Jiayou |
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| Institution: | DING Minghe,LOU Jie,HONG Chunxue,GENG Qin,CAO Yu,LI Xing,SHU Jiayou(College of Pharmaceutical,Wuhan University,Wuhan 430072,Hubei,China) |
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| Abstract: | Morphine sulfate sustained-release liquid suppositories were prepared by morphine sulfate sustained-release liquid suppositories with poloxamer 407/188,cabopol,sodium chloride,azone,2,6-di-tert-butyl-4-methylphenol according to the properties of in situ gel.The physicochemical properties such as gelation temperature,gel strength,bioadhesive force were studied.The drug released from the morphine sulfate sustained-release liquid suppository was studied with new device,and the drug absorption was performed in ... |
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| Keywords: | morphine sulfate sustained-release liquid suppository cabopol poloxamer hydroxylgel pharmacokinetics |
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