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可乐定为一种脂溶性的降血压药,分布容积高血浆药物有效治疗浓度低,因而适于制备一种间隔时间为7天的稳态释放经皮给药剂型。作者研究了商品可乐定贴膏的剂量直线性、敷贴部位的影响、稳态血浆药物浓度的持续时间以及药物更换时间的影响。受试者均为正常男性,年龄18～45岁。血药浓度的测定采用放射免疫法。对6名受试者在上臂外侧皮肤表面局部敷贴面积为3.5、7.0和10.5cm~2三种规格的可乐定贴膏后,测定结
Colamin, a lipid-soluble antihyperlipidemic drug, has a low concentration of high-volume, high-plasma drug and is therefore suitable for the preparation of a steady-state release transdermal dosage form with an interval of 7 days. The authors studied the dose linearity of the product clonidine patches, the effects of the application site, the duration of steady-state plasma drug concentration, and the time of drug change. Subjects were normal men, aged 18 to 45 years. Blood concentration was determined by radioimmunoassay. 6 subjects in the upper arm outside the skin surface of the local application area of 3.5, 7.0 and 10.5cm ~ 2 three kinds of clonidine paste, the measured knot