| 许彦 邹莉莉 但招陵 顾王文 曹海强.固体分散体提高普罗布考生物利用度的研究[J].,2016,16(29):5616-5619 |
| 固体分散体提高普罗布考生物利用度的研究 |
| Study on Enhancer of Bioavailability for Probucol by Solid Dispersion |
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| DOI： |
| 中文关键词: 固体分散体 普罗布考 生物利用度 药动学 |
| 英文关键词: Solid dispersion Probucol Bioavailability Pharmacokinetics |
| 基金项目:国家重大科学研究计划项目（2015CB932103） |
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| 中文摘要: |
| 目的：采用固体分散体技术（solid dispersion, SD）提高普罗布考的溶解度，从而提高其溶出速率及口服生物利用度。方法：选
用共聚维酮（S-630）为载体，采用喷雾干燥法制备普罗布考固体分散体，通过差示扫描热量法（differential scanning calorimetry，
DSC）、X- 射线粉末衍射分析（X-ray diffraction，XRD）对其进行物相鉴定，通过动力溶解度试验模拟固体分散体在体内胃肠道的
动态溶出过程，采用液相色谱- 质谱（LC-MS/MS）评价大鼠体内药动学行为。结果：差示扫描热量法和X-射线粉末衍射分析表明
药物以分子形式存在于固体分散体中；动力溶解度结果显示固体分散体在200 min 内的累积溶出度维持在80%以上，并且没有出
现药物析出现象。大鼠体内药动学研究表明，普罗布考固体分散体的Cmax 和AUC0→t分别是原料药的7.5 倍和6.3 倍。结论：将
药物制成固体分散体后，溶解度和溶出度得到了显著提高，生物利用度也随之增加。 |
| 英文摘要: |
| Objective:Solid dispersion technology was used to improve the solubility of probucol, so as to improve the dissolution
rate and oral bioavailability.Methods:The probucol solid dispersions were prepared with S-630 as the carrier by spray dry process. The
optimal prescription composition and preparation process of SD were determined by orthogonal design. The phase identification was determined
though differential scanning calorimetry and X-ray diffraction analysis. The dynamic dissolution process of SD in gastrointestinal
was simulated by the dynamic solubility test. The pharmacokinetics of rats was evaluated by liquid chromatography-mass spectrometry
(LC- MS/MS).Results:The results of differential scanning calorimetry and powder X-ray diffraction showed that probucol existed in
an amorphous state in the solid dispersion; The results of dynamic solubility showed that the cumulative dissolution fromthe solid dispersion
was more than 80% within 200 min, and there was no drug precipitation. The results of pharmacokinetic study in rats showed that
the Cmax and AUC0→t of probucol solid dispersions were 7.5 times and 6.3 times higher than those of bulk drug, respectively.Conclusion:The solubility and dissolution of the solid dispersion were significantly enhanced compared with the bulk drug, and the bioavailability
of the drug was increased accordingly. |
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