中国中药杂志

2015, v.40(24) 4840-4846

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液固压缩技术改善丹参酮Ⅱ_A释药的评价研究
Liquisolid technique for enhancement of dissolution prosperities of tanshinone Ⅱ_A

刘晓谦;孟庆举;徐雪林;赵洁;杨华;易红;
LIU Xiao-qian;MENG Qing-ju;XU Xue-lin;ZHAO Jie;YANG Hua;YI Hong;Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences;National Engineering Laboratory for Quality Control Technology of Chinese Herbal Medicines;Jiangsu Kanion Pharmaceutical Co.,Ltd.;

摘要(Abstract):

"液固压缩"技术是20世纪90年代新出现的能够显著改善难溶性药物溶解度的新技术,该文选择丹参中的难溶性有效成分——丹参酮Ⅱ_A及其脂溶性有效部位为研究对象,以不同的非挥发性液体为液相溶剂,微晶纤维素为载体材料,二氧化硅为涂层材料制备液固压缩片,并对其流动性(休止角,卡尔指数及豪森指数)、药物与辅料相互作用(DSC,XRPD)等进行研究。通过对比不同液固压缩片与普通片剂溶出曲线,探讨该技术在改善丹参酮Ⅱ_A溶出度方面的特性及其影响因素。结果表明,溶出度随液相溶剂的溶解度增高而增大,R及载药量对以丹参酮Ⅱ_A单体为模型药物的制剂影响较为明显,但对以丹参脂溶性有效部位为模型药物者影响较小。表明"液固压缩"技术能够显著改善丹参酮Ⅱ_A的溶出度,同时能够与丹参中的其他脂溶性成分发生协同作用,更好地促进丹参酮Ⅱ_A的释放,提示"液固压缩"技术在中药中具有较好的发展前景。
The technique of liquisolid compress is a new technique developed in 1990 s,which was considered to be the most promising technique to improve the dissolution of water-insoluble drugs. In this article,tanshinone Ⅱ_Aand the extracts of the ester-solubility fractions were chosen as the model drugs to evaluate the effects of the liquisolid technique for enhancement of dissolution properties of tanshinone Ⅱ_A. Several liquisolid tablets( LS) formulations containing different dosage of drugs and various liquid vehicle were prepared and for all the formulations,microcrystalline cellulose and silica were chosen as the carrier and coating materials to evaluate their flow properties,such as angle of repose,Carr's compressibility index and Hausner's ratio. The interaction between drug and excipients in prepared LS compacts were studied by differential scanning calorimetry( DSC) and X-ray powder diffraction( XRPD). The dissolution curves of tanshinone Ⅱ_Afrom liquisolid compacts were investigated to determine the technique's effect in improving the dissolution of tanshinone Ⅱ_Aand its impacting factors. According to the results,the dissolution increased with the rise in the dissolution of the liquid-phase solvent. The R-value and drug dosage can significantly affect the drug release,but with less impact on active fractions. This indicated that liquisolid technique is a promising alternative for improvement of dissolution property of water-soluble drugs,and can make a synergistic effect with other ester-soluble constituents and bettern improve the release of tanshinone Ⅱ_A. Therefore,the technique of liquisolid compress will have a better development prospect in traditional Chinese medicines.

关键词(KeyWords): 丹参酮ⅡA;液固压缩;溶出度;难溶性药物
tanshinone ⅡA;liquisolid compress;dissolution;water-insoluble drug

Abstract:

Keywords:

基金项目(Foundation): 国家“重大新药创制”科技重大专项(2012ZX09103201-009,2012ZX09103201-027);; 中国中医科学院客座研究员联合创新研究项目(ZZ070837)

作者(Author): 刘晓谦;孟庆举;徐雪林;赵洁;杨华;易红;
LIU Xiao-qian;MENG Qing-ju;XU Xue-lin;ZHAO Jie;YANG Hua;YI Hong;Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences;National Engineering Laboratory for Quality Control Technology of Chinese Herbal Medicines;Jiangsu Kanion Pharmaceutical Co.,Ltd.;

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