论文部分内容阅读
目的探讨三氧化二砷(Arsenictrioxide,As2O3)在40%的普通碘油和超液化碘油混悬剂和乳剂中的物理性状与缓释性能,以指导临床药物的应用。方法分别将40%的普通碘油(LIP)和超液化碘油(UFL)与As2O3用“泵法”制成几种不同的乳剂和混悬剂,肉眼与显微镜观察各种制剂的物理稳定性,并将各种制剂分别经透析带,在37℃±0.5℃恒温条件下,于磷酸盐缓冲液中进行透析,测定不同时间释放到透析液中As2O3的浓度,计算释放率。结果40%的普通碘油和超液化碘油As2O3混悬剂静置后出现As2O3的分离沉淀,超液化碘油As2O3混悬剂的分离速度更快;2种As2O3碘油普通乳剂静置后均立即出现油水分层,加乳化剂的乳剂稳定性好;As2O3在普通碘油和超液化碘油乳剂中,具有缓释性,加乳化剂的乳剂药物缓释效应更好,而在其混悬剂中释放较快。结论40%的普通碘油和超液化碘油均可作为肝癌等的化疗栓塞剂和As2O3的载体,使用其乳剂能更好地发挥其缓释效应,增加药物剂量而不至于增加其副作用。
Objective To investigate the physical properties and sustained-release properties of Arsenictrioxide (As2O3) in 40% ordinary lipiodol and ultra-liquified lipiodol suspensions and emulsions to guide the clinical application of drugs. Methods Several different emulsions and suspensions were prepared by pump method using 40% ordinary lipiodol (LIP) and ultra-liquefied lipiodol (UFL) and As2O3, respectively. The physical stability of various preparations was observed with naked eye and microscope , And the various preparations were dialyzed, respectively, at 37 ℃ ± 0.5 ℃ constant temperature conditions, in phosphate buffer dialysis, measured at different times released into the dialysate As2O3 concentration calculated release rate. Results After 40% of normal lipiodol and ultra-liquefied lipiodol As2O3 suspensions were allowed to stand for As2O3 separation and precipitation, ultra-liquefied lipiodol As2O3 suspensions were separated faster. Two kinds of As2O3 lipiodol common emulsions Immediately appear oil-water stratification, emulsifier emulsion stability; As2O3 in the ordinary lipiodol and ultra-liquefied lipiodol emulsion, with sustained release, emulsifier emulsion drug release effect is better, and in its suspension Release faster in the agent. Conclusion 40% of normal lipiodol and ultra-liquefied lipiodol can be used as chemoembolization agents and carrier of As2O3 for liver cancer. The use of the emulsion can better exert its sustained-release effect and increase the dosage without increasing its side effects.