尼索地平透皮贴片的制备及体外性质考察  

Preparation and in vitro characterization of a transdermal patch containing nisoldipine

作　　者：肖琰[1] 张文丽[1] 刘建平[1] 林芷艺[1] 汪铃[1] 于盼盼[1] 

机构地区：[1]中国药科大学药剂学教研室,南京210009

出　　处：《国际药学研究杂志》2013年第3期365-368,373,共5页Journal of International Pharmaceutical Research

基　　金：国家"重大新药创制"科技重大专项资助项目(2009ZX09310-004);中央高校基本科研业务费专项基金(JKY2011017)

摘　　要：目的制备处方优化的尼索地平透皮贴片并对其进行体外性质考察。方法采用流涎法制备处方优化的尼索地平透皮贴片,高效液相色谱(HPLC)法测定药物含量,改良的Franz扩散池评价制剂经大鼠皮肤的渗透性和释放度,差示扫描量热法对贴剂进行物相分析,选用家兔评价制剂的皮肤刺激性。结果所制备的尼索地平贴片含量均一,符合中国药典要求。72 h内药物的体外经皮渗透呈现稳态释药,药物的释放符合Weibull方程。药物在贴剂中以无定形存在,贴片对家兔的皮肤没有明显刺激性。结论尼索地平透皮贴片的体外质量符合要求,可能成为一种有效的抗高血压制剂。Objective To prepare an formulation-optimized nisoldipine transdermal patch and evaluate its in vitro properties.Methods The nisoldipine transdermal patch was prepared by solvent-diffusion technique.The HPLC was employed to determine the drug content in the patch.In vitro skin permeation and release behavior were studied by using modified Franz diffusion cells.The material phase of the patch was characterized by differential scanning calorimetry（DSC）.Rabbits were used to evaluate the skin irritation of the patch.Results The prepared patch met the requirements of the Chinese pharmacopoia.The drug permeation through the rat skin was a steady process during 72 h.The in vitro release profiles of nisoldipine from the patch were in accordance with Weibull equation.Nisoldipine in the patch existed in amorphous phase.No obvious skin irritations on the tested rabbits were observed.Conclusion The nisoldipine transdermal patch meets the in vitro requirements of Chinese Pharmacopoeia and can be used as an effective anti-hypertensive formulation.

关 键 词：尼索地平 透皮贴片 差示扫描量热法 皮肤刺激性 

分 类 号：R94[医药卫生—药剂学]