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白头翁皂苷D固体分散体制备及体内外评价

Preparation and in vivo and in vitro evaluation of Pulsatilla Saponin D Solid Dispersions

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【作者】 饶小勇; 尹姗; 何明珍; 罗晓健; 谢茵; 冯育林; 杨世林;

【Author】 RAO Xiao-yong;YIN Shan;HE Ming-zhen;LUO Xiao-jian;XIE Yin;FENG Yu-lin;YANG Shi-lin;Jiangxi University of Traditional Chinese Medicine;National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine;The Second Affiliated Hospital to Nanchang University;

【机构】 江西中医药大学; 中药固体制剂制造技术国家工程研究中心; 南昌大学第二附属医院;

【摘要】 目的制备白头翁皂苷D(PSD)固体分散体(PSD-SD),并评价其体内外释药行为。方法采用溶剂法考察了不同载体材料对PSD溶解度的影响,采用红外光谱法(IR)、差示扫描量热法(DSC)以及X射线衍射法(XRD)表征了PSD-SD,采用溶出度和大鼠血药浓度变化评价了固体分散体体内外释药行为。结果以PEG 6000为载体材料可使PSD在水中溶解度由2.39 mg/m L增大至7.06 mg/m L,制备的PSD-PEG 6000(1∶6)PSD-SD 60 min药物累积释放率达到了90%,大鼠给药PSD-SD后其AUC0~∞是原料药的2.24倍。结论以PEG 6000为载体材料制备的PSD-SD可以增加PSD溶解度,有效地提高PSD溶出速率,有利于提高PSD生物利用度。

【Abstract】 Objective To prepare the solid dispersion of Pulsatilla saponin D(PSD-SD) and evalution its in vivo and in vitro drug release behavior. Methods The PSD-SD was prepared by solvent method. Three carriers were used in the PSD-SD. Infrared spectroscopy(IR), differential thermal analysis(DSC), and X-ray diffraction(XRD) were used to determine the PSD-SD. Dissolution rates and pharmacokinetic parameters were evaluated in vitro and in vivo characteristics of the PSD-SD. Results When the PEG6000 was used as carrier, the solubility of PSD was increased from 2.39 to 7.06 mg/m L, and the cumulative release rate of PSD reached 90% in 60 min, and the bioavailability of PSD was increased to 2.24 times. Conclusion The solid dispersion prepared PSD can increase the solubility, dissolution rate, and bioavailability.

【基金】 江西省自然科学基金资助项目(20142BAB205082,20132BAB215031);江西省战略新型产业重点开发项目(2013AFC30031);江西中医药大学重点学科青年教师培养计划(2013jzzdxk045)
  • 【文献出处】 中草药 ,Chinese Traditional and Herbal Drugs , 编辑部邮箱 ,2015年21期
  • 【分类号】R283.6
  • 【被引频次】3
  • 【下载频次】288
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