| 紫杉醇透明质酸冻干制剂的制备和药动学研究 |
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| 引用本文： | 殷殿书,葛志强,刘昌孝,元英进.紫杉醇透明质酸冻干制剂的制备和药动学研究[J].中草药,2005,36(2):192-195. |
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| 作者姓名： | 殷殿书 葛志强 刘昌孝 元英进 |
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| 作者单位： | 1. 天津大学化工学院,制药工程系,天津,300072
2. 天津大学化工学院,制药工程系,天津,300072;天津药物研究院,天津药代动力学与药效学动力学省部共建国家重点实验室,天津,300193 |
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| 摘 要： | 目的以透明质酸为载体材料制备紫杉醇透明质酸冻干制剂,并考察冻干制剂在大鼠体内的药动学。方法采用乳匀-冻干法制备冻干制剂;以透射电子显微镜观察其粒子形态;建立冻干制剂及其在血浆中紫杉醇的HPLC分析方法;以紫杉醇注射剂为对照,测定冻干制剂10mg/kgiv给药后,大鼠体内的药动学参数。结果在冻干制剂中,紫杉醇以球形包覆于透明质酸基质中;在溶液中,分散成平均粒径为80nm的包覆微球;大鼠iv冻干制剂和紫杉醇注射剂的药物浓度-时间曲线符合二室模型,其药动学参数AUC分别为(37.68±6.36μg·h/mL和(27.54±5.88)μg·h/mL;CL分别为(0.26±0.04)h-1和(0.38±0.07)h-1。结论透明质酸可能成为一种新的抗癌药物载体。
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| 关 键 词： | 紫杉醇 透明质酸 冻干制剂 药动学 |
| 文章编号： | 0253-2670(2005)02-0192-04 |
| 收稿时间： | 7/8/2004 12:00:00 AM |
Paclitaxel lyophilized preparation with hyaluronic acid as a carrier and its pharmacokinetics |
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| YIN Dian-shu,GE Zhi-qiang,LIU Chang-xiao and YUAN Ying-jin.Paclitaxel lyophilized preparation with hyaluronic acid as a carrier and its pharmacokinetics[J].Chinese Traditional and Herbal Drugs,2005,36(2):192-195. |
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| Authors: | YIN Dian-shu GE Zhi-qiang LIU Chang-xiao and YUAN Ying-jin |
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| Affiliation: | Department of Pharmaceutical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China;Department of Pharmaceutical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China;Department of Pharmaceutical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China;Tianjin State Key Laboratories of Pharmacokinetics and Phartnacodynamicsatat Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China;Department of Pharmaceutical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China |
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| Abstract: | Objective To prepare paclitaxellyophilized preparation with hyaluronic acid as a carrier and investigate its pharmacokinetics in rats in vivo.Methods The preparation was prepared by emulsion-homogenous lyophilization.The particle morphology was observed by transmission electron microscope and the HPLC analysis for the paclitaxel in lyophilized preparation and in plasma was established.Taking paclitaxel injection as control,the in vivo pharmackinetics of lyophilized preparation by iv to rats at a dose of 10 mg/kg was studied.Results In lyophilized preparation the paclitaxel particles were wrapped spherically in hyaluronic acid matrix and were dispersed in wrapped-mierosphere in mean diameter of 80 nm in solution.The concentration-time curve of lyophilized preparation and paclitaxel injection by iv to rats was identical with the two-compartment model and the pharmacokinetie parameters of AUC were(37.68±6.36)and(27.54±5.88)µg·h/mL and CL were(0.26±0.04)and(0.38±0.07)h-1,respectively.Conclusion Hyaluronic acid may be used as a novel and specific carrier of anti-tumor drug in the future. |
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| Keywords: | paclitaxel hyaluronic acid lyophilized preparation pharmacokinetics |
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