厄贝沙坦血浆蛋白结合率测定(1)
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[摘要] 目的：测定厄贝沙坦在人血浆中的蛋白结合率。方法：采用HPLC法测定厄贝沙坦的浓度。采用平衡透析法测定厄贝沙坦的人血浆蛋白结合率。结果：以Diamonsil C18(4.6 mm×250 mm，5 μm)为色谱柱，以乙腈-0.02 mol/L磷酸二氢钾水溶液(磷酸调pH至2.6)(45∶55)为流动相，检测波长为245 nm，血浆样品中其他成分不干扰厄贝沙坦的测定，厄贝沙坦的线性范围为0.10~10.40 μg/ml，定量下限为0.10 μg/ml。厄贝沙坦的低、中、高浓度的蛋白结合率分别为93.0%、91.5%、92.3%。结论：厄贝沙坦具有较强的蛋白结合率。
[关键词] 厄贝沙坦；血浆蛋白结合率；平衡透析法；HPLC
[中图分类号] R927.2 [文献标识码] A [文章编号] 1673-7210(2011)12(a)-027-03
Determination of human plasma protein binding rate of Irbesartan
LI Yin1, CHEN Fengyi1, ZHANG Guotian1, YANG Hui1, HUANG Yuling1, XIE Qingchun2, ZHONG Ming3
1.Panyu District Central Hospital of Guangzhou City, Guangdong Province, Guangzhou 511400, China; 2.Institute of Materia Medica, Guangdong Pharmaceutical University, Guangdong Province, Guangzhou 510006, China; 3.Guangzhou Hanfan Pharmaceutical Company Limited, Guangdong Province, Guangzhou 510240, China
[Abstract] Objective: To determine human plasma protein binding rate of Irbesartan. Methods: HPLC was applied to determine the content of Irbesartan. Human plasma protein binding rate of Irbesartan was estimated by equilibrium dialysis. Results: Diamonsil C18 (4.6 mm×250 mm, 5 μm) was selected as the fixed phase. The wavelength was 245 nm. The mobile phase was acetonitrile-0.02 mol/L potassium dihydrogen phosphate (pH was adjusted to 2.6 with phosphoric acid) (45∶55). The calibration curve of Irbesartan was in good linear correlation at the range of 0.10-10.40 μg/ml. Lower limit of quantitation was 0.10 μg/ml. The human plasma protein binding rate of Irbesartan low, medium and high concentrations was 93.0%, 91.5%, 92.3% respectively. Conclusion: The HPLC method for determination of Irbesartan is simple, fast, accurate and high sensitive. Irbesartan has a strong protein binding.
[Key words] Irbesartan; Human plasma protein binding rate; Equilibrium dialysis; HPLC
厄贝沙坦(Irbesartan)是血管紧张素Ⅱ(AngⅡ)受体拮抗剂，能特异性地拮抗血管紧张素Ⅱ受体(AT1)，通过特异性地拮抗AngⅡ与AT1受体的结合，抑制血管收缩和醛固酮的释放，产生降压作用，临床上主要用于高血压的治疗，同时厄贝沙坦在欧盟获准用于一个新的适应证，即治疗有高血压的2型糖尿病患者的肾脏病，是欧盟批准用于预防糖尿病早期及晚期肾脏疾病的第一个抗高血压药 ......
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