吡罗昔康普朗尼克磷脂有机凝胶的体外评价和局部组织分布

In vitro evaluation and local tissue distribution of piroxicam Pluronic lecithin organogel

目的制备普朗尼克磷脂有机凝胶,以吡罗昔康为模型药物,评价其体外性能并考察其局部组织分布特征。方法应用椎-板模型流变仪测定普朗尼克磷脂有机凝胶的流变学参数,Franz扩散池法测试其体外释放和经皮通透性,考察大鼠局部给药的局部组织分布。结果普朗尼克磷脂有机凝胶具有典型的凝胶的流变学特征;48 h体外累积释放率和经皮通透率分别为(81.56±3.09)%和(3.80±1.59)%;皮肤和肌肉的药时曲线具有双峰特征,给药侧的组织药物浓度高于血药浓度和对侧相同组织的浓度,原因在于药物的直接通透和系统再分布。结论普朗尼克磷脂有机凝胶适用于皮肤局部给药的载体。

Objective To prepare Pluronic lecithin organogel （PLO）, evaluate its in vitro properties and investigate the tissue distribution with piroxicamn as the model drug. Methods The rheological parameters of PLO were obtained by cone-plate configuration rheometer, the in vitro release drug and transdermal permeability were tested by Franz cell method, and the pharmacokinetics and local tissues distribution were investigated after topical application of piroxicarn PLO to rat skin. Results It was demonstrated that PLO had typical rheological property. Percents of in vitro released drug and permeated through rat full-skin were（ 81.56 ± 3.09） % and（3.80 ± 1.59） % ,respectively. The drug concentration-time profiles of skin and muscle showed two peaks, and ρmax and AUC of various local tissues of applied side were higher than that of plasma and tissues of contralateral side which might be attributed to systemic redistribution and direct penetration. Conclusions PLO can be a potential carrier of piroxicam or other active drugs for topical administration.