| 摘要: |
| [目的]制备氯氰碘柳胺缓释剂,比较其与氯氰碘柳胺注射液的药动学过程,为氯氰碘柳胺缓释剂的研制奠定基础.[方法]以蓖麻油、单硬脂酸铝和N-甲基-吡咯烷酮为溶剂,制备出氯氰碘柳胺缓释剂,将其与氯氰碘柳胺注射液分别以5 mg/kg的剂量皮下注射家兔,于注射后不同时间(0.5,1,3,5,7,10,17,24,31,38,45,52,59,66,73,80 d)采血,测定血药浓度,分析药动学参数.[结果]氯氰碘柳胺注射液与氯氰碘柳胺缓释剂的药-时曲线均符合一级吸收一室模型,缓释剂达到最大血药浓度的时间比注射液延长了2.513 d,吸收半衰期比注射液有明显的延长,消除半衰期比注射液延长了9.918 d.[结论]与氯氰碘柳胺注射液相比,氯氰碘柳胺缓释剂皮下注射后吸收缓慢,消除半衰期延长. |
| 关键词: 氯氰碘柳胺 高效液相色谱法 家兔 药动学 |
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| 基金项目:国家科技支撑计划 |
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| Pharmacokinetics of closantel sustain-released injection in rabbits |
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| Abstract: |
| 【Objective】 The research prepared preparative Closantel sustain released injection and compared Pharmacokinetics procedure with Closantel injection to lay a foundation for trituration Closantel sustain released injection.【Methed】 Castor oil,N methyl ketopyrrolidine and aluminum monostearate were used for preparative Closantel sustain released injection.The rabbits were injected Closantel injection and Closantel sustain released injection subcutaneously at a dose of 5 mg/kg.After 0.5,1,3,5，7，10，17，24，31，38，45，52，59，66，73，80 d,blood concentrations were tested and Pharmacokinetics parameters analysed.【Result】 The pharmacokinetics of Closantel injection and Closantel sustain released injection fitted one compartment model with an equation.Sustain released injection’s blood concentration time extended 2.513 d than Closantel injection.Absorption half life extended obviously and elimination half life extended 9.918 d than Closantel injection.【Conclusion】 Results suggested that the Closantel sustain released injection is absorbed slowly and half life period prolonged. |
| Key words: Closantel HPLC rabbit pharmacokinetics |
