吲哚美辛乳膏的制备及体外释放度考察

Preparation and Investigation of in Vitro Release of Indomethacin Cream

目的制备吲哚美辛乳膏,并考察其体外释放度。方法以吐温80、单硬脂酸甘油酯、液体石蜡、凡士林的用量为考察对象,以乳膏的外观性状及离心、耐热及耐寒试验是否分层为指标,采用L9(34)正交设计法优化乳膏处方,并采用高效液相色谱法测定乳膏在释放介质中的累积渗透量,通过小鼠热板法镇痛试验来观察乳膏的镇痛作用。结果最佳处方:吐温80为0.45 g,单硬脂酸甘油酯为0.9 g,液体石蜡为0.9 g,凡士林为0.6 g。吲哚美辛乳膏的累积渗透量几乎随时间呈等速率增加,且乳膏有明显的镇痛作用。结论正交试验法优选的吲哚美辛乳膏色泽均匀、质地细腻、渗透性良好、便于涂布,处方稳定。吲哚美辛乳膏的累积渗透量与时间呈良好的线性关系,方法简单可靠。

OBJECTIVE To prepare an O/W type indomethacin cream and to investigate of its in vitro release. METHODS With the mass of tween 80, glycerol monostearate, liquid paraffin, petroleum jelly as the research object, centrifugal, heat-resisting and cold-resisting tests whether stratified and cream appearance as an indicator, the L9（3^4） orthogonal design was used to select cream prescription. Then the cumulative permeation amount of cream was determined by HPLC in the release medium. The analgesic effect of cream was observed by the method of hot plate in mice analgesic experiment. RESULTS The best prescription was Tween-80 0.45 g, glycerin monostearate 0.9 g, liquid paraffin 0.9 g, petrolatum jelly 0.6 g. Cumulative permeation amount of indomethacin cream almost equal velocity increased with time. And cream had obvious analgesic effects. CONCLUSION The cream is uniform in color, homogeneous, exquisite and easy to spread. The prescription is stable. Cumulative permeation amount of indomethacin cream has a good linear relationship with time. The method is simple and reliable.