复方痤疮凝胶的制备及皮肤安全性评价

Preparation of compound acne gel and safety evaluation on skin

目的优化复方痤疮凝胶剂的处方,通过家兔皮肤刺激性和豚鼠皮肤过敏性实验考察其对皮肤用药的安全性。方法通过正交试验优化处方,以克林霉素磷酸酯、维A酸、甲硝唑等为主药,卡波姆U21、甘油等为辅料制成复方制剂,并通过动物皮肤刺激性及过敏性实验初步评价制剂安全性。结果所制凝胶剂质地均匀,黏稠度适中,最佳处方为:甘油4%(w/w),卡波姆0.6%(w/w),三乙醇胺0.4%(v/w),2,6-二叔丁基对甲酚(BHT)0.05%(w/w),柠檬酸0.02%(w/w)。复方痤疮凝胶对家兔皮肤无明显干燥、脱屑等刺激性反应,对豚鼠皮肤均无明显红斑及水肿等过敏反应。结论该制剂性状良好,动物皮肤实验中无明显刺激过敏现象产生,与市售复方维A酸凝胶相比,一定程度上降低了维A酸的不良反应。

Objective To optimize the formulation of compound acne gel and evaluate its irritation and hypersensitivity on the skin of rabbits and guinea pigs respectively.Methods The formulation,optimized by orthogonal experiments was composed of clindamycin phosphate,tretinoin and metronidazole as active ingredients and carbomer U21 and glycerin as adjuvants.The safety of the formulation was evaluated through skin irritation test and hypersensitivity test.Results The gel was homogeneous with moderate viscosity.The optimal formulation was composed of glycerol 4%（w/w）,carbomer 0.6%（w/w）,triethanolamine 0.4%（v/w）,2,6-butylated hydroxy toluene（BHT）0.05%（w/w）and citric acid 0.02%（w/w）.The irritation test showed that there was no obvious aridity or desquamation on rabbits＇ skin.The hypersusceptibility test also showed that no erythema or dropsy on guinea pigs＇ skin was observed.Conclusion Compared with the traditional gel on sale,the acne gel causes no irritation on rabbits＇ skin and no hypersusceptibility on guinea pigs＇ skin.