| 引用本文: | 李小东,陈悦,李煜,洪利娅.采用GastroPlusTM软件评估甲磺酸多沙唑嗪缓释片的体内外溶出特征[J].中国现代应用药学,2016,33(1):71-75. |
| LI Xiaodong,CHEN Yue,LI Yu,HONG Liya.Evaluate in Vivo-in Vitro Dissolution Characteristics of Doxazosin Mesylate Sustained-release Tablets by GastroPlusTM[J].Chin J Mod Appl Pharm(中国现代应用药学),2016,33(1):71-75. |
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| 摘要: |
| 目的 通过甲磺酸多沙唑嗪缓释片药动学(pharmacokinetics，PK)模型的搭建和预测，为建立合理的体外溶出方法提供指导和依据。方法 采用GastroPlusTM软件搭建体内PK模型，去卷积得到体内溶出曲线，对比体外溶出实验结果进行评价。结果 建立了甲磺酸多沙唑嗪缓释片的体内PK模型，将体内与体外溶出曲线进行对比，发现后者的AUC和Cmax比实测值明显偏高。结论 现行体外溶出度检验方法不能准确反映体内过程，体内外相关性较差，溶出方法可进一步提高。 |
| 关键词: 甲磺酸多沙唑嗪 GastroPlusTM 溶出曲线 PK模型 体内外相关 |
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| Evaluate in Vivo-in Vitro Dissolution Characteristics of Doxazosin Mesylate Sustained-release Tablets by GastroPlusTM |
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LI Xiaodong1, CHEN Yue2, LI Yu2, HONG Liya2
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1.Zhejiang University of Technology, Hangzhou 310014, China;2.Zhejiang Institute for Food and Drug Control, Hangzhou 310051, China
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| Abstract: |
| OBJECTIVE To provide guidance and basis for establishing reasonable dissolution method by establishing and predicting of the doxazosin mesylate sustained-release tablets pharmacokinetic(PK) model. METHODS The PK model was established by GastroPlusTM, and the dissolution curves in vivo was obtained by deconvolution operation, which comparating the results of dissolution in vitro. RESULTS The PK model in vivo of doxazosin mesylate sustained release tablets was established. The AUC and Cmax of the dissolution curves in vitro was significantly higher than that of the measured value by comparing the dissolution curves in vivo and in vitro. CONCLUSION The current in vitro dissolution test method can not accurately reflect the in vivo process, in vivo-in vitro correlation is poor, and the method needs to be further improved. |
| Key words: doxazosin mesylate GastroPlussTM dissolution curves PK models in vivo-in vitro correlation |
