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无定形与晶型紫杉醇(PTX)的理论溶解度之比为92.6(37℃时)。采用共溶剂骤冷法筛选得到适合作为PTX聚合物固体分散体(PSD)的基质材料为醋酸羟丙甲纤维素琥珀酸酯(HPMCAS)。多孔二氧化硅(又称白炭黑,WCB)可进一步调节溶出速率。因此,采用类乳化-溶剂扩散法(quasi-emulsion solvent diffusion method,QESDM)制备了3种处方的PSD,其中HPMCAS、PTX和WCB的质量比分别为4∶1∶0、8∶1∶0和4∶1∶4,记作F1、F2和F3。分别考察3种PSD的体外溶出度和大鼠口服给药后的生物利用度。结果表明,给
The theoretical solubility ratio of amorphous to paclitaxel (PTX) was 92.6 (at 37 ° C). A matrix material suitable for use as a PTX polymer solid dispersion (PSD) was screened using a co-solvent quench method as hypocrellose acetate succinate (HPMCAS). Porous silica (also known as white carbon black, WCB) can further adjust the dissolution rate. Therefore, three kinds of prescription PSDs were prepared by quasi-emulsion solvent diffusion method (QESDM), in which the mass ratios of HPMCAS, PTX and WCB were 4: 1: 0, 8: 1: 0 and 4: 1: 4, denoted F1, F2 and F3. The in vitro dissolution rates of three kinds of PSD and the bioavailability after oral administration of the rats were investigated. The results show that