目的 研究维他昔布的抗炎镇痛作用。方法 采用对人全血、犬全血的环氧化酶-1、环氧化酶-2 活性抑制测试进行体外药效实验,继而采用角叉菜胶致大鼠足肿胀实验、小鼠耳廓巴豆油致炎实验探讨其抗炎作用,采用小鼠醋酸扭体疼痛实验研究其镇痛作用。结果 人全血、犬全血体外活性评价实验中,由IC₅₀(环氧化酶-1)/IC₅₀(环氧化酶-2)比值结果可见维他昔布为高选择性环氧化酶-2抑制剂。抗炎作用实验中,维他昔布对角叉菜胶致大鼠足肿胀具有显著的抑制活性(P<0.05),对小鼠耳廓巴豆油致炎具有极显著的抑制活性(P<0.01)。镇痛作用实验中,维他昔布对醋酸致小鼠疼痛扭体次数具有抑制活性(P<0.05)。结论 维他昔布具有良好的抗炎作用,对环氧化酶-2选择性高。

To study the anti-inflammatory and analgesic effects of vitacoxib. METHODS The in vitro COX-1 and COX-2 inhibitory activities of vitacoxib were tested in human whole blood assay as well as canine whole blood assay. The anti-inflammatory and analgesic effects of vitacoxib were evaluated in several in vivo models including croton oil induced mouse ear endema, carrageenan-induced rat paw swelling and mouse acetic acid writhing model. RESULTS In vitro assay, vitacoxib has potent inhibitory COX-2 activity and selectivity for COX-2 over COX-1. In vivo anti-inflammatory experiments, vitacoxib has significant inhibitory activities both in croton oil-induced mouse ear oedema model test(P<0.01)and the carrageenan-induced rat paw swelling test(P<0.05). In vivo analgesic effect experiments, vitacoxib has significant inhibitory activity on acetic acid-induced writhing pain in mice(P<0.05).CONCLUSION Vitacoxib, a selective COX-2 inhibitor, demonstrates excellent anti-inflammatory activity in both in vitro and in vivo models tested.