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目的:比较载体联用与单用对丹参酮ⅡA(TSⅡA)固体分散体溶出度的影响,以进一步提高TSⅡA溶出度。方法:分别以聚乙烯吡咯烷酮K30(PVPK30)、帕洛沙姆188(F68)及二者联用(PVPK30/F68)为载体,采用溶剂法制备TSⅡA固体分散体,对其物相特征、溶出行为及溶解度进行了研究。结果:经热差分析证实,药物在PVPK30与F68联合载体中以非晶型态分散;TSⅡA在3种不同载体中的Td(按Weibull分布累积溶出度达63.2%所需的时间)分别为(90.40±2.82),(204.5±8.20),(25.83±0.13)min;固体分散体PVPK30/F68-TSⅡA较F68-TSⅡA,PVPK30-TSⅡA可显著提高TSⅡA的溶解度(P<0.01)。结论:与单一载体相比,PVPK30与F68联用能显著增大TSⅡA的溶出度及溶解度(P<0.01);采用载体联用固体分散技术提高难溶性药物的溶出度将会受到广泛的关注。
OBJECTIVE: To compare the effect of carrier combination and single use on the dissolution of tanshinone IIA (TSIIA) solid dispersion to further increase the dissolution rate of TSIIA. Methods: The solid phase dispersions of TSIIA were prepared by solvent method with PVPK30, P68 and FPK and their combination, PVPK30/F68, respectively. Their phase characteristics and dissolution behavior were studied. And solubility was studied. RESULTS: After thermal analysis, it was confirmed that the drug was dispersed in the amorphous form in the PVPK30 and F68 combination carrier; the Td of TSIIA in 3 different carriers (the time required for cumulative dissolution according to the Weibull distribution reached 63.2%) was ( 90.40±2.82), (204.5±8.20), (25.83±0.13) min; Solid dispersion PVPK30/F68-TSIIA can significantly increase the solubility of TSIIA compared with F68-TSIIA and PVPK30-TSIIA (P<0.01). CONCLUSIONS: Compared with single vehicle, the combination of PVPK30 and F68 can significantly increase the dissolution and solubility of TSIIA (P<0.01). The use of carrier-based solid dispersion technology to increase the dissolution of insoluble drugs will receive widespread attention.