奥沙普秦凝胶剂的体外渗透性及药效学

目的:研究奥沙普秦凝胶剂体外经皮渗透性及体外释药情况,观察其抗炎镇痛作用。方法:采用Franz扩散池,进行奥沙普秦凝胶剂体外渗透性和释放度实验。采用角叉菜胶致大鼠足肿胀、二甲苯致小鼠耳肿胀、大鼠棉球肉芽肿、醋酸扭体法和甲醛致痛法模型,观察奥沙普秦凝胶剂的抗炎、镇痛作用,同时考察了奥沙普秦凝胶剂皮肤用药的急性毒性、致敏性和刺激性。结果:奥沙普秦凝胶剂对角叉菜胶致大鼠足肿胀、二甲苯致小鼠耳肿胀和大鼠棉球肉芽肿均有明显的抑制作用,对醋酸、甲醛所致小鼠炎症性疼痛有明显抑制作用。急性毒性、致敏性和刺激性实验结果表明奥沙普秦凝胶剂皮肤用药无明显的毒性、致敏性及刺激性。结论:皮肤是奥沙普秦凝胶剂透皮吸收的主要屏障。奥沙普秦凝胶剂具有抗炎镇痛作用,无明显的不良反应。

Study on pharmacodynamics and permeation of oxaprozin gel in vitro

AIM:To study the release and the percutaneous permeation of oxaprozin gel in vitro, together with the anti-inflammatory and analgesic effect. METHODS:The permeation and release of oxaprozin gel was measured by using Franz diffusion cell. The effects were observed on following models including carrageenim induced paw edema in rat, xylene induced swelling of mouse ear, granulation tissue hyerplasia induced by cotton, the writhing response induced by acetic acid and the pain response induced by formaldehyde; simultaneously to observe the effects of acute toxicity, hypersensitivity and irritancy caused by oxaprozin. RESULTS:Oxaprozin gel was found possessing the ability to inhibit paw edema induced by carrageenim in rat, suppress ear swelling induced by xylene in mice and restrain granulation tissue hyerplasia induced by cotton. The writhing response induced by acetic acid and the pain induced by formaldehyde were remarkably inhibited and decreased respectively by application of oxaprozin gel. Furthermore oxaprozin gel did not bring toxicity, hypersensitivity and irritancy. CONCLUSION:Oxaprozin gel can permeate through the skin barrier possessing significant anti-inflammatory and analgesic effects without remarkable adverse reactions.