论文部分内容阅读
乳剂可作为抗癌药的缓释制剂,但是人们很少注意乳剂中油相的含量对释药速度及毒性的影响。作者用司盘-80和聚氧乙烯氢化蓖麻油作乳化剂(HLB值=10)制备含橄榄油分别为35、50及65%的三种5-氟尿嘧啶(5-Fu)水包油型乳剂。三种乳剂的油滴平均直径均<1μm。体外释药试验表明:5-Fu乳剂中5-Fu释药速率明显低于5-Fu水溶液,不同油相含量的乳剂释药速率也不同,油相含量越高释药越慢。急性毒性试验表明:5-Fu水溶液及油相含量为35、50和65%的5-Fu乳剂的LD_(50)(mg/kg,小鼠)分别为231.4、408.2、417.2和434.5。表明乳剂油相含量
Emulsions can be used as slow-release preparations for anticancer drugs, but little attention has been paid to the effect of the oil phase in the emulsion on the drug release rate and toxicity. The authors prepared three 5-fluorouracil (5-Fu) oil-in-water emulsions containing 35, 50 and 65% olive oil with Span-80 and polyoxyethylene hydrogenated castor oil as emulsifiers . The average droplet diameter of all three emulsions was <1 μm. The in vitro drug release test showed that the release rate of 5-Fu in 5-Fu emulsion was significantly lower than that in 5-Fu aqueous solution. The emulsion release rates were also different in different oil phases. The higher the oil phase, the slower the drug release. Acute toxicity test showed that LD_ (50) (mg / kg, mice) of 5-Fu aqueous solution and 5-Fu emulsion with oil content 35, 50 and 65% were 231.4, 408.2, 417.2 and 434.5, respectively. Show the emulsion oil content