| 肝素钠肌醇烟酸酯乳膏中肌醇烟酸酯皮肤药动学研究 |
| 投稿时间：2024-04-02 修订日期：2024-07-10 点此下载全文 |
| 引用本文：崔亚玲,吴琼,马良煜,胡北,姚东,许子华.肝素钠肌醇烟酸酯乳膏中肌醇烟酸酯皮肤药动学研究[J].药学实践杂志,2025,43(1):6~9,21 |
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| 基金项目:国家科技重大新药创制专项（2013ZX09J13109-03B） |
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| 中文摘要:目的 建立HPLC法测定大鼠皮肤中肌醇烟酸酯（IN）的浓度，并研究肝素钠肌醇烟酸酯乳膏在大鼠经皮给药后IN的药动学特征。方法 采用HPLC法建立简便快速的测定给药后不同时间点大鼠皮肤中IN浓度的分析方法，并用建立的方法开展肝素钠肌醇烟酸酯乳膏在大鼠经皮给药后IN的药动学研究，采用DAS软件拟合药物动力学参数。结果 该分析方法在0.25 ~ 20 μg/ml浓度范围内线性良好，定量限为0.25 μg/ml，平均加样回收率为96.18%。肝素钠肌醇烟酸酯乳膏皮肤给药后IN的药动学参数t1/2 为（4.555±2.054） h、Tmax为（6±0） h、Cmax为（16.929±2.153） mg/L、AUC0-t为（150.665±16.568） mg·h /L、AUC0-∞为（161.074±23.917） mg·h /L、MRT（0-t）为（9.044±0.618） h、MRT（0-∞）为（10.444±1.91） h、CLz/F 为（0.19±0.03） L/（h·kg）、Vz/F 为（1.190±0.437） L/（h·kg）。结论 IN能迅速渗透进入皮肤，并能够长时间蓄积在皮肤局部，有利于IN在病变部位长时间发挥药效。该方法简便、快速、专属性强、重复性好，可应用于大鼠腹部皮肤给药后IN的药动学研究。 |
| 中文关键词:肝素钠肌醇烟酸酯乳膏 皮肤药动学 肌醇烟酸酯 |
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| Skin pharmacokinetics of inositol nicotinate in heparin sodium inositol nicotinate cream |
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| Abstract:Objective To establish an HPLC method to determine the concentration of inositol nicotinate（IN） in rat skin, and study the pharmacokinetic characteristics of IN after transdermal administration of heparin sodium inositol nicotinate cream in rats. Methods HPLC method was used to establish a simple and rapid analytical method for the determination of IN concentration in the skin of rats at different time points after administration. The established method was used to study the pharmacokinetics of IN after transdermal administration of heparin sodium inositol nicotinate cream in rats, and the pharmacokinetic parameters were fitted with DAS software. Results The linearity of the analytical method was good in the concentration range of 0.25-20 μg/ml, the quantitative limit was 0.25 μg/ml, and the average recovery rate was 96.18%. The pharmacokinetic parameters of IN after transdermal administration of heparin sodium inositol nicotinate cream in rats were as follows: t1/2 was （4.555±2.054） h, Tmax was （6±0）h, Cmax was （16.929±2.153）mg/L, AUC0-t was （150.665±16.568） mg·h /L ,AUC0-∞ was （161.074±23.917） mg·h /L, MRT（0-t） was （9.044±0.618）h, MRT（0-∞） was （10.444±1.91） h, CLz/F was （0.19±0.03） L/（h·kg）, and Vz/F was （1.19±0.437） L/（h·kg）. Conclusion IN could quickly penetrate the skin and accumulate in the skin for a long time, which was beneficial to the pharmacological action of drugs on the lesion site for a long time. The method is simple, rapid, specific and reproducible, which could be successfully applied to the pharmacokinetic study of IN after transdermal administration in rats. |
| keywords:heparin sodium inositol nicotinate cream skin pharmacokinetics inositol nicotinate |
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