用药效学试验筛选尼美舒利新剂型

 目的通过比较尼美舒利栓剂、搽剂、口服水混悬液的药效学试验结果，为尼美舒利新制剂的开发和剂型选择提供依据。方法采用二甲苯引起小鼠耳壳肿胀炎症模型，观察尼美舒利新制剂的抗炎作用；采用醋酸扭体法，观察尼美舒利新制剂的镇痛作用；采用伤寒Vi多糖疫苗引起家兔发热模型，观察尼美舒利新制剂的解热作用；比较尼美舒利直肠栓剂和尼美舒利口服片剂的生物利用度；进行生物等效性分析。结果尼美舒利栓剂、搽剂、口服水混悬液均可明显减轻小鼠耳壳肿胀度、减少扭体次数、有明显的解热作用。尼美舒利栓剂的相对生物利用度为84.75%；尼美舒利栓剂与尼美舒利片剂生物不等效。结论尼美舒利栓剂具有良好的解热、镇痛、抗炎作用；尼美舒利栓剂的吸收速度快于片剂。

Screening for new dosage forms of nimesulide through pharmacodynamic study in animal models

OBJECTIVE To develop new preparations of nimesulide and screen for dosage forms by comparing the pharmacological effects of nimesulide supositories,liniments and oral suspentions in animal models.METHODS The anti inflammatory effects of nimesulide new drug forms in mouse ear edema induced by xylene were observed.The analgesic effects in mouse body twisting reaction induced by acetic acid were observed.The antipyretic effect were observed in rabbits of high temperature induced by Typhdod Vi polysaccharide vaccine.The relative bioavailibility of nimesulide suppositories to nimesulide tablets was investigated.Their bioequivalence was carried out.RESULTS Mouse ear edema was reduced by NIM S and NIM L.The incidence of mouse body twisting reaction was reduced.The high temperature of rabbits was dropped.The relative bioavailibility of nimesulide suppositories was 84.75% .Nimesulide suppositories and nimesulide tablets were not bioeqivalent.CONCLUSION Nimesulide suppositories manifested obvious anti inflammatory,analgesic and antipyretic effect and were absorbed more quickly than nimesulide tablets.