Preparation and in vitro Dissolution of Sirolimus Self-microemulsifying Sustained-release Tablets
- 药学院－已发表论文 
目的制备并评价西罗莫司的自微乳缓释片。方法利用微晶纤维素吸附西罗莫司自微乳,再与羟丙甲纤维素混合压制缓释片;考察羟丙甲纤维素的型号和用量,以及缓释片的硬度对西罗莫司溶出的影响。结果随羟丙甲纤维素黏度的增大,西罗莫司的溶出逐渐减缓。分别制备羟丙甲纤维素K100lv和K4M的缓释片,均呈现随羟丙甲纤维素用量增大,西罗莫司溶出减缓的趋势,且在采用15%羟丙甲纤维素K100lv或10%羟丙甲纤维素K4M时溶出曲线相对较佳,但重现性差。调整缓释片的硬度为120N时,西罗莫司溶出符合Q2〈30%,45%90%,且3批样品溶出曲线的f2为67、61、72,均大于50,重复性良好,相比微晶纤维素片和市售纳米结晶片,可缓释12h。结论优选的西罗莫司自微乳缓释片具有良好的缓释性能。Objective To prepare sirolimus（SRL） self-microemulsifying tablets with sustained release behavior.Methods MCC was used to absorb the SRL self-microemulsifying delivery system,which was then mixed with HPMC to prepare the tablets. The type and percentage of HPMC, and the hardness of the tab lets were investigated and optimized. Results With the increase of the viscosity of HPMC, the release of SRL was decreased. Tablets with HPMC K1001v and K4M were prepared respectively. The release of SRL was reduced with the increase of the percentage of HPMC K1001v or K4M. 15 HPMC K100lv or 10 HPMC K4M led to favorable dissolution of SRL, but the reproducibility became poor.When the hardness of the tablets was optimized to be 120 N, the dissolution conformed to Q2 30 Y0,45 /00 Q6 65 /0, Qlz 90G.Moreover, the release curves of three batches of samples had f 2 values of 67, 61 and 72, indicating that the reproducibility was good. Compared to the MCC tablets and commercial tablets, the optimized tablets had a sustained release of 12 h.Conclusion The optimal SRL self-microemulsifying tablets possess favorable sustained-release property.