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目的:制备酮基布洛芬(KTP)经皮吸收涂膜剂,研究其经皮吸收性能及抗炎作用。方法:采用双室渗透扩散装置,进行体外渗透试验;用大鼠为炎症模型,考察KTP涂膜剂的抗炎作用。结果:KTP涂膜剂体外透皮释药方程为:Q=0.4385t-0.1030(r=0.9998),8h累积渗透量为3.507mg·cm-2;本品对大鼠角叉莱胶性足趾肿胀,棉球性肉芽组织增生及大鼠佐剂性关节炎的原发病变和继发病变均有显著抑制作用。结论:涂膜剂使KTP以零级动力学透过皮肤,可以提供比口服制剂稳定的血药浓度;KTP具有显著抗炎作用。
Objective: To prepare ketoprofen (KTP) percutaneously absorptive coating and study its percutaneous absorption and anti-inflammatory effects. Methods: Double-chamber osmotic diffusion device was used for in vitro penetration test. The rat model of inflammation was used to investigate the anti-inflammatory effect of KTP coating agent. Results: The in vitro transdermal delivery equation of KTP was: Q = 0.4385t-0.1030 (r = 0.9998), and the cumulative permeation of 8-h was 3.507mg · cm-2 Fork Lai rubbery toe swelling, granulosa granulation tissue hyperplasia and primary adjuvant arthritis in rats with primary lesions and secondary lesions were significantly inhibited. CONCLUSION: The coating agent allows KTP to pass zero-order kinetics through the skin and provides a stable plasma concentration compared to the oral formulation; KTP has a significant anti-inflammatory effect.