Hiramatsu Y, Akita S, Salamin P A, Maier R
Research Institute of Drug Safety, Setsunan University, Osaka, Japan.
Arzneimittelforschung. 1990 Oct;40(10):1117-24.
Four commercial gel preparations of topical anti-inflammatory agents have been assessed in six animal models commonly used to determine the biological activity of non-steroidal anti-inflammatory agents for systemic administration. Only UV-induced erythema of the skin, adjuvant induced arthritis and the measurement of vascular permeability proved suitable for differentiation of the potency of the four topical agents. Carrageenin-induced paw oedema, the cotton pellet test and the assessment of the pain threshold according to Randall and Selitto were of little value. The effects of the gel preparation of diclofenac (CAS 15307-86-5) diethylammonium (Voltaren Emulgel) were comparable to two preparations containing 1% and 5% active ingredient, respectively. Gel 4 showed low overall activity. The experiments demonstrated that some of the models used for the assessment of anti-inflammatory agent for systemic administration proved suitable for the testing of topical preparations and that percutaneous absorption was insufficient to elicit anti-inflammatory effect in the animals at sites remote from the site of application.
四种局部抗炎剂的商用凝胶制剂已在六种常用于确定全身给药非甾体抗炎剂生物活性的动物模型中进行了评估。只有紫外线诱导的皮肤红斑、佐剂诱导的关节炎以及血管通透性的测量被证明适用于区分这四种局部制剂的效力。角叉菜胶诱导的爪肿胀、棉球试验以及根据兰德尔和塞利托方法评估的疼痛阈值几乎没有价值。双氯芬酸（CAS 15307-86-5）二乙铵凝胶制剂（扶他林乳胶剂）的效果与另外两种分别含有1%和5%活性成分的制剂相当。凝胶4总体活性较低。实验表明，一些用于评估全身给药抗炎剂的模型被证明适用于局部制剂的测试，并且经皮吸收不足以在远离给药部位的动物部位引发抗炎作用。
