SPG膜乳化制备汉防己甲素—丹参酮ⅡA—PLGA二元微球及其体外表征(1)
[摘要]该实验采用SPG膜乳化法制备了汉防己甲素-丹参酮ⅡA-PLGA二元微球，并对其进行了体外表征的研究。傅里叶红外光谱、DSC分析及X射线衍射分析表明，汉防己甲素和丹参酮ⅡA在二元微球中均是以非晶形式存在且高度分散在PLGA载体中;体外释放试验结果表明该二元微球中汉防己甲素在24 h内的累积释放量为6.44%，17 d内的累积释放量达到89.02%;丹参酮ⅡA在24 h内的累积释放量为3.60%，17 d内的累积释放量达到21.24%，体外释药过程符合Riger-Peppas模型。该二元微球具有一定的缓释作用，可明显降低突释，预期达到延长药效时间、减少给药次数的目的，并为中药复方制剂的研究提供新的思路和方法。
[关键词]SPG膜乳化技术; 汉防己甲素; 丹参酮ⅡA; 二元微球; 表征
Studies on preparation by SPG membrane emulsification method and in vitro
, 百拇医药
characterization of tetradrine-tashionone ⅡA -PLGA composite microspheres
LU Jin1，2， ZHANG Meng1，2， ZHU Hua-xu1，2*， GUO Li-wei1，2*， PAN Lin-mei1，2， FU Ting-ming1，2
(1.Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization， Nanjing University of
Chinese Medicine， Nanjing 210023， China;
2. Jiangsu Botanical Medicine Refinement Engineering Research Center， Nanjing University of Chinese
, 百拇医药
Medicine， Nanjing 210023， China)
[Abstract]Tetradrine-tashionone ⅡA-PLGA composite microspheres were prepared by the SPG membrane emulsification method， and the characterization of tetradrine-tashionone ⅡA-PLGA composite microspheres were studied in this experiment. The results of IR， DSC and XRD showed that teradrine and tashionone IIA in composite microspheres were highly dispersed in the PLGA with amorphous form. The results of tetradrine-tashionone ⅡA-PLGA composite microspheres in vitro release experiment showed that the cumulative release amounts of tetradrine and tashionone IIA were 6.44% and 3.60% in 24 h， and the cumulative release amounts of tetradrine and tashionone ⅡA were 89.02% and 21.24% in 17 d. The process of drug in vitro release accorded with the model of Riger-Peppas. Tetradrine-tashionone ⅡA-PLGA composite microspheres had slow-release effect， and it could significantly reduce the burst release， prolong the therapeutic time， decrease the dosage of drugs and provide a new idea and method to prepare traditional Chinese medicine compound.
, 百拇医药
[Key words]SPG membrane emulsification method; tetradrine; tanshinone ⅡA; composite microspheres; characterization
doi：10.4268/cjcmm20150620
研究报道，汉防己甲素有降低肺动压、抗肝纤维化、抗炎[1-4]等作用，临床上已广泛用于矽肺[5-9]各个阶段的治疗;丹参酮ⅡA可参与临床辅助治疗肺部疾病[10-14]，同时还可降低汉防己甲素引起的淤血、肝损伤等作用。本课题组利用SPG膜乳化技术已成功制备出粒径分布均一、高载药量及包封率且具有肺部靶向作用的汉防己甲素-聚乳酸微球[15]，在此基础上，本实验利用SPG膜乳化技术首次将汉防己甲素与丹参酮ⅡA构建于同一载体中并对其体外进行表征，旨在制备出具有缓释作用和肺部靶向趋势的汉防己甲素-丹参酮ⅡA二元微球，以期两者在发挥协同作用的同时，丹参酮ⅡA降低汉防己甲素的刺激性及毒副作用。, 百拇医药(陆瑾 张梦 朱华旭 郭立玮 潘林梅 付廷明)
[关键词]SPG膜乳化技术; 汉防己甲素; 丹参酮ⅡA; 二元微球; 表征
Studies on preparation by SPG membrane emulsification method and in vitro
, 百拇医药
characterization of tetradrine-tashionone ⅡA -PLGA composite microspheres
LU Jin1，2， ZHANG Meng1，2， ZHU Hua-xu1，2*， GUO Li-wei1，2*， PAN Lin-mei1，2， FU Ting-ming1，2
(1.Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization， Nanjing University of
Chinese Medicine， Nanjing 210023， China;
2. Jiangsu Botanical Medicine Refinement Engineering Research Center， Nanjing University of Chinese
, 百拇医药
Medicine， Nanjing 210023， China)
[Abstract]Tetradrine-tashionone ⅡA-PLGA composite microspheres were prepared by the SPG membrane emulsification method， and the characterization of tetradrine-tashionone ⅡA-PLGA composite microspheres were studied in this experiment. The results of IR， DSC and XRD showed that teradrine and tashionone IIA in composite microspheres were highly dispersed in the PLGA with amorphous form. The results of tetradrine-tashionone ⅡA-PLGA composite microspheres in vitro release experiment showed that the cumulative release amounts of tetradrine and tashionone IIA were 6.44% and 3.60% in 24 h， and the cumulative release amounts of tetradrine and tashionone ⅡA were 89.02% and 21.24% in 17 d. The process of drug in vitro release accorded with the model of Riger-Peppas. Tetradrine-tashionone ⅡA-PLGA composite microspheres had slow-release effect， and it could significantly reduce the burst release， prolong the therapeutic time， decrease the dosage of drugs and provide a new idea and method to prepare traditional Chinese medicine compound.
, 百拇医药
[Key words]SPG membrane emulsification method; tetradrine; tanshinone ⅡA; composite microspheres; characterization
doi：10.4268/cjcmm20150620
研究报道，汉防己甲素有降低肺动压、抗肝纤维化、抗炎[1-4]等作用，临床上已广泛用于矽肺[5-9]各个阶段的治疗;丹参酮ⅡA可参与临床辅助治疗肺部疾病[10-14]，同时还可降低汉防己甲素引起的淤血、肝损伤等作用。本课题组利用SPG膜乳化技术已成功制备出粒径分布均一、高载药量及包封率且具有肺部靶向作用的汉防己甲素-聚乳酸微球[15]，在此基础上，本实验利用SPG膜乳化技术首次将汉防己甲素与丹参酮ⅡA构建于同一载体中并对其体外进行表征，旨在制备出具有缓释作用和肺部靶向趋势的汉防己甲素-丹参酮ⅡA二元微球，以期两者在发挥协同作用的同时，丹参酮ⅡA降低汉防己甲素的刺激性及毒副作用。, 百拇医药(陆瑾 张梦 朱华旭 郭立玮 潘林梅 付廷明)