...
首页> 外文期刊>International journal of clinical pharmacology and therapeutics >Determination of pravastatin by high performance liquid chromatography.
【24h】

Determination of pravastatin by high performance liquid chromatography.

机译:高效液相色谱法测定普伐他汀的含量。

获取原文
获取原文并翻译 | 示例
           

摘要

BACKGROUND: Pravastatin is a hydrophilic liver-specific inhibitor of the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase. It effectively lowers plasma cholesterol and low-density lipoprotein concentrations in humans. Pharmacokinetic studies of pravastatin have been mostly performed by means of radioactively labelled drug or by measuring plasma concentrations with gas chromatography and mass spectrometry. AIMS OF THE STUDY: Aim of our study was to develop a simple, but reliable method which allows the determination of pravastatin plasma concentrations under clinical routine conditions. SUBJECTS, MATERIALS AND METHODS: Samples were prepared by solid-phase extraction on cyclohexyl bond elut cartridges. Chromatography was carried out on an octyl matrix. Triamcinolone acetonide was used as internal standard. The method was linear within the range of 5 to 200 microg/l pravastatin. The coefficient of variation depended on the pravastatin concentration, but was less than 10% throughout. The pharmacokinetics of pravastatin were determined in healthy individuals. Five healthy subjects received single oral doses of pravastatin (60 mg) and one of these subjects additionally received a dose of 80 mg at three different study days. In all subjects blood was sampled 0, 30, 60, 90, 120, 150, 180, 240 and 300 min after drug intake. RESULTS: Peak plasma concentrations of pravastatin were found between 60 min and 120 min after oral administration of 60 mg and reached values between 37 microg/l and 126 microg/l. The calculated AUCs were between 52 ng/ml x h and 311 ng/ml x h and the corresponding plasma elimination half-life times were between 95 min and 165 min. In all subjects plasma concentrations of pravastatin 5 hours after oral drug administration were near the detection limit of the method (5 microg/l). Intraindividually, there was only little variation in the kinetics of pravastatin. However, marked differences were encountered between the subjects studied. CONCLUSION: The data suggest that the determination of pravastatin plasma concentrations by means of a HPLC system can be used for routine analysis of pravastatin plasma concentrations. The obtained pharmacokinetic data in healthy individuals stand in ample agreement with the results of prior studies in which the concentrations of pravastatin were determined by other more sophisticated methods.
机译:背景:普伐他汀是3-羟基-3-甲基戊二酰辅酶A还原酶的亲水性肝特异性抑制剂。它可以有效降低人体内的血浆胆固醇和低密度脂蛋白浓度。普伐他汀的药代动力学研究主要通过放射性标记药物或通过气相色谱和质谱法测量血浆浓度来进行。研究目的:本研究的目的是开发一种简单但可靠的方法,该方法可在临床常规条件下测定普伐他汀的血浆浓度。受试者,材料和方法:通过在环己基键洗脱柱上进行固相萃取制备样品。在辛基基质上进行色谱。曲安奈德用作内标。该方法在5至200微克/升的普伐他汀范围内是线性的。变异系数取决于普伐他汀的浓度,但总体上小于10%。在健康个体中测定普伐他汀的药代动力学。五名健康​​受试者单次口服普伐他汀(60毫克),其中一名受试者在三个不同的研究日还接受了80毫克的剂量。在所有受试者中,在摄入药物后0、30、60、90、120、150、180、240和300分钟抽取血液。结果:普伐他汀的最高血浆浓度在口服60毫克后60分钟至120分钟之间,达到37微克/升至126微克/升之间的水平。计算的AUC在52 ng / ml x h至311 ng / ml x h之间,相应的血浆消除半衰期在95 min至165 min之间。在所有受试者中,口服药物5小时后的普伐他汀血浆浓度均接近该方法的检测极限(5 microg / l)。从个人而言,普伐他汀的动力学变化很小。但是,在研究的受试者之间遇到了明显的差异。结论:数据表明通过HPLC系统测定普伐他汀血浆浓度可用于普伐他汀血浆浓度的常规分析。在健康个体中获得的药代动力学数据与先前研究的结果充分一致,在先前研究中,普伐他汀的浓度是通过其他更复杂的方法确定的。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号