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醋酸羟丙甲纤维素琥珀酸酯(HPMCAS)是羟丙甲纤维素的乙酸酯和琥珀酸酯的混合物,因此具有两亲性。HPMCAS的玻璃化转变温度约为120℃,因具有p H依赖性而常用作肠溶包衣材料。近年来,HPMCAS作为难溶性药物无定形固体分散体(SD)载体的应用研究日渐增多。HPMCAS不仅对常用的SD制备工艺[溶剂蒸发法、热熔挤出法、喷雾(冷冻)干燥法和球磨法]具有良好的适应性,而且可抑制SD在贮存、体外溶出和体内吸收过程中的药物重结晶现象,提高SD稳定性。本文综述了近年来HPMCAS在SD应用中的研究进展。
Hypromellose acetate succinate (HPMCAS) is a mixture of acetate and succinate of hypromellose and therefore has amphipathic properties. HPMCAS has a glass transition temperature of about 120 ° C and is commonly used as an enteric coating material because of its p H dependence. In recent years, HPMCAS as a poorly soluble drug amorphous solid dispersion (SD) carrier application research increasing. HPMCAS not only has good adaptability to the commonly used SD preparation process [solvent evaporation method, hot melt extrusion method, spray (freeze) drying method and ball milling method), but also inhibits SD in the storage, in vitro dissolution and in vivo absorption process Drug recrystallization, improve SD stability. This article summarizes the research progress of HPMCAS in SD applications in recent years.