Agarwal Sangita, Gowda Kadajji Veeran, Mandal Uttam, Ghosh Debotri, Bose Anirbandeep, Sarkar Amlan Kanti, Chattaraj Tapas Kumar, Pal Tapan Kumar
Department of Pharmaceutical Technology, Jadavpur University, Kolkata, 700 032 West Bengal, India.
Arzneimittelforschung. 2007;57(5):274-7. doi: 10.1055/s-0031-1296618.
The study was designed to determine the relative bioavailability of two sustained release fixed dose combination (FDC) products of two manufacturers containing esomeprazole (CAS 326602-80-6) 40 mg and domperidone (CAS 57808-66-9) 30 mg in 24 healthy male volunteers. The pharmacokinetics of esomeprazole and domperidone individually after oral administration of tablet formulation has been extensively evaluated in adult volunteers. However, no published data are available regarding the combined pharmacokinetics and bioavailability of this particular FDC.
The study was designed as a randomized, balanced, open-label, 2-period cross-over study. Each subject was randomized at the beginning of the study to receive either a single dose of the Test FDC or Reference FDC during Period I. Following a 7-day wash-out period, all subjects received the alternate formulation during Period II.
No statistically significant differences were obtained between the two products with respect to the mean concentration-time profiles or in the pharmacokinetic parameters, including area under the serum concentration-time curve from the present study. The relative extent of absorption as assessed by the AUC ratio (Test/Reference) and C(max), the average value was found to be 1.00 +/- .09 with 90% confidence limits (C.L.) of 0.82-1.18.
These findings clearly indicate that the two products are bioequivalent in terms of rate and extent of drug absorption. Both preparations were well tolerated with no adverse reactions throughout the study.
本研究旨在确定两种含有40毫克埃索美拉唑（CAS 326602-80-6）和30毫克多潘立酮（CAS 57808-66-9）的缓释固定剂量复方制剂（FDC）在24名健康男性志愿者中的相对生物利用度。在成年志愿者中，已对口服片剂后埃索美拉唑和多潘立酮各自的药代动力学进行了广泛评估。然而，关于这种特定FDC的联合药代动力学和生物利用度，尚无已发表的数据。
本研究设计为随机、平衡、开放标签的两期交叉研究。在研究开始时，每个受试者被随机分配在第一期接受单剂量的试验FDC或参比FDC。经过7天的洗脱期后，所有受试者在第二期接受另一种制剂。
两种产品在平均浓度-时间曲线或药代动力学参数方面，包括本研究中血清浓度-时间曲线下面积，均未获得统计学上的显著差异。通过AUC比值（试验/参比）和C(max)评估的吸收相对程度，平均值为1.00±0.09，90%置信区间（C.L.）为0.82-1.18。
这些发现清楚地表明，两种产品在药物吸收的速率和程度方面具有生物等效性。在整个研究过程中，两种制剂耐受性良好，均未出现不良反应。
