Solid dispersions technique was used to solidify buagafuran and improve buagafuran in vitro dissolution and stability.Buagafuran solid dispersions were prepared separately using PVPK30,PEG6000 and Poloxamer188 at various weight ratios as carriers.The status of buagafuran in solid dispersions was determined by using DSC and IR.The solubility,content and in vitro dissolution of pure drug and the solid dispersions were detected by using HPLC.When buagafuran/carrier was 1∶5 or less,the drug existed in a solid dispersion form.Three kinds of carriers all can improve buagafuran dispersibility and in vitro dissolution.Accelerating experiment showed that buagafuran/PVPK30≤1∶10 solid dispersions was ageing-resistant,and the aspect,content and in vitro dissolution did not change after storaged over 3 months,but PEG6000,Poloxamer188 and a lower ratio PVPK30 solid dispersions became aged.Buagafuran/PVPK30≤1∶10 solid dispersions can be developed as buagafuran oral drug delivery carrier.
目的:建立一种微柱离心方法测定紫杉醇脂肪乳包封率。方法:采用Sephadex G-50微柱,分别以适量体积的水及乙醇为洗脱液分离脂肪乳中的包封药物和游离药物。通过考察洗脱过程中紫杉醇及脂肪乳中油相成分大豆油的含量(紫杉醇的含量测定采用HPLC法,大豆油的含量测定采用HPLC-ELSD法),并以外加法制备的包封不完全的紫杉醇脂肪乳的洗脱曲线确立包封药物和游离药物的分界点,确定了最终的洗脱方式及洗脱液用量:以1 m L水,共洗3次将脂肪乳中包封药物完全洗脱,以3 m L乙醇,共洗2次将脂肪中游离药物完全洗脱。并以方法的回收率和重复性,对方法进行了验证。最终以建立的方法测定了3批紫杉醇脂肪乳样品的包封率。结果:微柱离心法能有效实现紫杉醇脂肪乳中包封药物和游离药物的分离。方法的回收率为100.4%,RSD为0.60%(n=9);重复性为99.4%,RSD为0.58%(n=5)。3批样品的包封率分别为99.2%、99.3%、99.5%。结论:该法操作简便,回收率高,重复性好,能区分不同包封情况的紫杉醇脂肪乳,测定结果准确可靠。
