Zakeri-Milani Parvin, Valizadeh Hadi, Islambulchilar Ziba, Nemati Mahboob
Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Arzneimittelforschung. 2010;60(2):76-80. doi: 10.1055/s-0031-1296252.
Valsartan (CAS 137862-53-4) is an antihypertensive drug belonging to the family of angiotensin II receptor antagonists acting at the AT1 receptor, which mediates all known effects of angiotensin II on the cardiovascular system. In the present study, the pharmacokinetic parameters of two oral formulations of valsartan tablets were compared in a randomized, single oral dose, two-treatment crossover design in 24 healthy male volunteers under fasting conditions. After an overnight fast, the volunteers received 80 mg valsartan. Blood samples were collected up to 48 h and drug concentrations were determined by a reverse-phase HPLC method with fluorescence detection. Various pharmacokinetic parameters were determined from the plasma concentration-time curves of both formulations. The obtained values for test and reference products were 3067.7 +/- 1,281.7 and 3,304.3 +/- 1,196.4 ng/ml for Cmax; 17,834.4 +/- 7,083.8 and 18,319.1 +/- 7,800.7 ng x h/ml for AUC0-48; 18,825.7 +/- 7,553.2 and 19,172.2 +/- 8,307.2 ng x h/ml for AUC0-infinity, respectively. The 90% confidence intervals obtained by analysis of variance were 86.84-100.87% for Cmax and 93.43-115.54% for AUC0-t, which are within the acceptance range of 80-125%. Therefore it can be concluded that both products are bioequivalent in terms of rate and extent of drug absorption and therefore interchangeable.
缬沙坦（化学物质登记号137862-53-4）是一种抗高血压药物，属于作用于AT1受体的血管紧张素II受体拮抗剂家族，该受体介导血管紧张素II对心血管系统的所有已知作用。在本研究中，在24名健康男性志愿者禁食条件下，采用随机、单次口服剂量、双处理交叉设计，比较了两种缬沙坦片剂口服制剂的药代动力学参数。经过一夜禁食后，志愿者服用80毫克缬沙坦。采集血样长达48小时，并通过带有荧光检测的反相高效液相色谱法测定药物浓度。根据两种制剂的血浆浓度-时间曲线确定各种药代动力学参数。测试产品和参比产品的Cmax值分别为3067.7±1281.7和3304.3±1196.4纳克/毫升；AUC0-48分别为17834.4±7083.8和18319.1±7800.7纳克·小时/毫升；AUC0-∞分别为18825.7±7553.2和19172.2±8307.2纳克·小时/毫升。通过方差分析得到的90%置信区间，Cmax为86.84 - 100.87%，AUC0-t为93.43 - 115.54%，均在80 - 125%的可接受范围内。因此可以得出结论，两种产品在药物吸收的速率和程度方面具有生物等效性，因此可以互换使用。
