Ali Obaid, Obaid Roohi, Saify Zafar Saied, Ahmed Syed Waseemuddin
Government of Pakistan, Ministry of Health, Central Drugs Laboratory, Karachi, Pakistan.
Pak J Pharm Sci. 2005 Jan;18(1):25-32.
An open-label, randomized study was designed to determine the bioavailability (BA); pharmacokinetic (PK) and pharmacodynamic (PD) behaviour of Atenolol 50 mg (two pills) and 100 mg (one pill) tablet manufactured by a national pharmaceutical industry. Peak plasma concentration (Cmax): 1.33 +/- 0.31 microg/ml, time to peak plasma concentration (Tmax): 2.2 +/- 0.27 hours, AUC (area under the plasma concentration-time curve) 6.34 +/- 2.1 microg-hr/ml for 100 mg tab and Cmax: 1.07 +/- 0.23 microg/ml, Tmax: 2.5 +/- 0.35 hours, AUC 4.97 +/- 1.09 microg-hr/ml for 50 mg (two pills) tab were observed. The BA and PK parameters such as Cmax, Tmax, are comparable to previous studies, although significant decrease in diastolic and systolic blood pressure (mmHg) upto a certain limit for a considerable duration was observed. However, relation between PK and PD may not be established due to regulatory biochemical feedback mechanism.
一项开放标签的随机研究旨在确定由一家国家制药行业生产的50毫克（两片）和100毫克（一片）阿替洛尔片剂的生物利用度（BA）、药代动力学（PK）和药效学（PD）行为。观察到100毫克片剂的血浆峰浓度（Cmax）：1.33±0.31微克/毫升，达血浆峰浓度时间（Tmax）：2.2±0.27小时，血浆浓度-时间曲线下面积（AUC）6.34±2.1微克·小时/毫升；50毫克（两片）片剂的Cmax：1.07±0.23微克/毫升，Tmax：2.5±0.35小时，AUC 4.97±1.09微克·小时/毫升。尽管在相当长的一段时间内观察到舒张压和收缩压（毫米汞柱）显著下降至一定限度，但BA和PK参数如Cmax、Tmax与先前的研究相当。然而，由于调节性生化反馈机制，PK和PD之间的关系可能无法确立。
