Nazir Shabnam, Iqbal Zafar, Shah Yasar, Ahmad Lateef, Khan Abad
Kohat University of Science and Technology, Kohat, Pakistan,
Eur J Drug Metab Pharmacokinet. 2015 Sep;40(3):313-8. doi: 10.1007/s13318-014-0211-z. Epub 2014 Jun 12.
Rosuvastatin is used to treat dyslipidemia and is metabolized by CYP2C9 that shows variable metabolic activity in males and females. Pharmacokinetics (PK) of drugs varies in males and females that may result in altered drug response and therapeutic efficacy. In current study, PK of rosuvastatin has been evaluated in males and females. A single oral dose (40 mg rosuvastatin), open-label and non-controlled PK study was arranged. A reversed phase HPLC method was applied for quantification of rosuvastatin in serum samples. PK parameters of rosuvastatin were compared in males and females by applying student t test at 95 % confidence interval. The C max, [Formula: see text]and [Formula: see text]of rosuvastatin was significantly higher (p < 0.05) in females compared with males. The Vd/F of rosuvastatin was insignificantly higher (p > 0.05) in males compared with females while CL/F was significantly (p < 0.05) faster in males when compared at 95 % confidence interval. Rosuvastatin plasma level was significantly high in females compared with males that may be a possible reason for higher incidence of cardiac myopathy and other side effects in females. The variation in PK of drugs in males and females may require dose adjustment for maximum therapeutic effectiveness and safety.
瑞舒伐他汀用于治疗血脂异常，且通过细胞色素P450 2C9（CYP2C9）代谢，而该酶在男性和女性中的代谢活性存在差异。药物的药代动力学（PK）在男性和女性中有所不同，这可能导致药物反应和治疗效果发生改变。在本研究中，对瑞舒伐他汀在男性和女性中的药代动力学进行了评估。安排了一项单剂量口服（40毫克瑞舒伐他汀）、开放标签且非对照的药代动力学研究。采用反相高效液相色谱法对血清样本中的瑞舒伐他汀进行定量分析。通过在95%置信区间应用学生t检验，比较了瑞舒伐他汀在男性和女性中的药代动力学参数。与男性相比，女性的瑞舒伐他汀Cmax、[公式：见原文]和[公式：见原文]显著更高（p < 0.05）。与女性相比，男性的瑞舒伐他汀Vd/F略高（p > 0.05），而在95%置信区间比较时，男性的CL/F显著更快（p < 0.05）。与男性相比，女性的瑞舒伐他汀血浆水平显著更高，这可能是女性心肌病和其他副作用发生率较高的一个可能原因。男性和女性药物药代动力学的差异可能需要调整剂量，以实现最大治疗效果和安全性。
