| 他克莫司固体分散体的制备及体外溶出度测定 |
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| 引用本文： | 方慧慧,郭健,桂双英,牛敏智.他克莫司固体分散体的制备及体外溶出度测定[J].中国医院药学杂志,2016,36(9):710-714. |
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| 作者姓名： | 方慧慧 郭健 桂双英 牛敏智 |
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| 作者单位： | 1. 安徽中医药大学, 安徽合肥 230012;
2. 安徽省中医药科学院药物制剂研究所, 安徽合肥 230012;
3. 安徽省中药制剂工程技术研究中心, 安徽合肥 230012 |
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| 基金项目： | 国家自然科学基金(编号:81274099) |
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| 摘 要： | 目的:制备他克莫司固体分散体,提高他克莫司的体外溶出度。方法:以体外溶出度为指标,从泊洛沙姆188(Poloxamer188)、聚维酮K30(PVP K30)、羟丙甲纤维素(HPMCE3)、聚乙二醇6000(PEG6000)中筛选最优载体及其比例。并采用差示热量扫描(DSC)、红外光谱(FTIR)、电子扫描电镜(SEM)等进行物相表征。结果:4种不同载体制成的固体分散体均能增加他克莫司体外溶出度,通过比较优选出HPMCE3为最佳载体。物相鉴定表明,他克莫司大部分以无定型状态分散于HPMCE3中。结论:制备他克莫司-HPMCE3固体分散体可以明显提高其体外溶出度,且制备方法简单可行。
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| 关 键 词： | 他克莫司 羟丙甲纤维素 固体分散体 溶出度 |
| 收稿时间： | 2015-11-02 |
Preparation and in vitro dissolution of tacrolimus solid dispersions |
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| FANG Hui-hui,GUO Jian,GUI Shuang-ying,NIU Min-zhi.Preparation and in vitro dissolution of tacrolimus solid dispersions[J].Chinese Journal of Hospital Pharmacy,2016,36(9):710-714. |
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| Authors: | FANG Hui-hui GUO Jian GUI Shuang-ying NIU Min-zhi |
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| Institution: | 1. Anhui University of Chinese Medicine, Anhui Hefei 230012, China;
2. Pharmaceutical Institute of Anhui Academy of TCM, Anhui Hefei 230012, China;
3. Engineering Research Center of Preparation Technology of TCM, Anhui Hefei 230012, China |
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| Abstract: | OBJECTIVE To prepare tacrolimus sodid dispersion by technology of solid dispersion improve in vitor release of eacrolimus. METHODS Solid dispersions of tacrolimus had been prepared with poloxamer188, HPMCE3, PVP K30 and PEG 6000, respectively. Optimal carrier was chosn from dissolution test. Existing forms of tacrolimus in dispersions were investigated by using differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM). RESULTS Dissolution of four solid dispersions was significantly improved. HPMCE3 was chosen as the best carrier. DSC, FTIR and SEM studies indicated that most tacrolimus existed at amorphous state in solid dispersions. CONCLUSION Solid dispersions can increase the in vitro dissolution rate, and the method is simple. |
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| Keywords: | tacrolimus HPMCE3 solid dispersion dissolution |
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