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“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。
Liquid-solid Compression technology is a new technology emerging in the 1990s that can significantly improve the solubility of poorly soluble drugs. In this paper, Tanshinone Ⅱ_A and its fat-soluble active components , Different non-volatile liquids as the liquid phase solvent, microcrystalline cellulose as the carrier material, silica as the coating material to prepare liquid-solid compressed tablets, and its fluidity (angle of repose, Karl index and the Haushausen index) , Drug-excipient interaction (DSC, XRPD) and so on. By comparing the dissolution curves of different liquid-solid compressed tablets and ordinary tablets, the characteristics of the technology in improving the dissolution of tanshinone Ⅱ_A and its influencing factors were discussed. The results showed that the dissolution rate increased with the increase of the solubility of liquid solvents, R and drug loading on the formulation of tanshinone Ⅱ_A monomer as a model drug more obvious impact, but the fat-soluble fraction of Salvia miltiorrhiza as a model drug small. The results showed that the “liquid-solid compression” technology can significantly improve the dissolution of tanshinone Ⅱ_A, at the same time, it can synergize with other lipid-soluble components in Salvia miltiorrhiza to promote the release of tanshinone Ⅱ_A, suggesting that “liquid-solid compression” In traditional Chinese medicine has a good development prospects.