摘要
目的:制备他克莫司固体分散体,提高他克莫司的体外溶出度。方法:以体外溶出度为指标,从泊洛沙姆188(Poloxamer188)、聚维酮K30(PVP K30)、羟丙甲纤维素(HPMCE3)、聚乙二醇6000(PEG6000)中筛选最优载体及其比例。并采用差示热量扫描(DSC)、红外光谱(FTIR)、电子扫描电镜(SEM)等进行物相表征。结果:4种不同载体制成的固体分散体均能增加他克莫司体外溶出度,通过比较优选出HPMCE3为最佳载体。物相鉴定表明,他克莫司大部分以无定型状态分散于HPMCE3中。结论:制备他克莫司-HPMCE3固体分散体可以明显提高其体外溶出度,且制备方法简单可行。
OBJECTIVE To prepare tacrolimus sodid dispersion by technology of solid dispersion improve in vitor release of eacrolimus.METHODS Solid dispersions of tacrolimus had been prepared with poloxamer188,HPMCE3,PVP K30 and PEG6000,respectively.Optimal carrier was chosn from dissolution test.Existing forms of tacrolimus in dispersions were investigated by using differential scanning calorimetry（DSC）,fourier-transform infrared spectroscopy（FTIR）and scanning electron microscope（SEM）.RESULTS Dissolution of four solid dispersions was significantly improved.HPMCE3 was chosen as the best carrier.DSC,FTIR and SEM studies indicated that most tacrolimus existed at amorphous state in solid dispersions.CONCLUSION Solid dispersions can increase the in vitro dissolution rate,and the method is simple.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2016年第9期710-714,共5页
Chinese Journal of Hospital Pharmacy
基金
国家自然科学基金(编号:81274099)
