Kim Yunjeong, Jeon Ji-Young, Chung Young-Chul, Kim Min-Gul
Clinical Pharmacology Unit and Biomedical Research Institute, Chonbuk National University Hospital, Jeonju, Republic of Korea.
Department of Psychiatry, College of Medicine, Chonbuk National University Medical School, Jeonju, Republic of Korea.
Clin Ther. 2015 Dec 1;37(12):2772-9. doi: 10.1016/j.clinthera.2015.10.006. Epub 2015 Nov 3.
The main objective of this study was to compare the pharmacokinetic properties and relative bioavailability of two 15-mg aripiprazole formulations (an orally disintegrating tablet [ODT] as the test drug and a conventional tablet as the reference drug) in healthy middle-aged Korean subjects.
This study was conducted in a population of healthy middle-aged Korean subjects as a randomized, open-label, single-dose, 2-sequence, 2-period crossover trial. After administration of a single dose of a 15-mg aripiprazole standard tablet with 240 mL water or an aripiprazole 15-mg ODT without water, blood samples were collected at specific time intervals from 0 to 240 hours. Concentrations of aripiprazole in plasma were analyzed by using a LC-MS/MS method of detection. Data on the pharmacokinetic parameters were recorded, and the 90% CIs of the ratios of the geometric means of the parameters were determined from the logarithmically transformed data by using an ANOVA model.
Thirty-nine healthy middle-aged Korean subjects were enrolled (mean age, 52.7 years; mean height, 167 cm; mean weight, 67.6 kg); 33 participants completed the study (29 male subjects and 4 female subjects). The 90% CIs of the geometric means ratio (test drug/reference drug) of Cmax, AUC0-last, and AUC0-∞ values were 0.95 to 1.14, 0.98 to 1.09, and 0.97 to 1.08, respectively. All of the subjects who experienced adverse events recovered without sequelae, and no serious adverse events were observed.
The aripiprazole pharmacokinetics was similar for the ODT and standard tablet of 15-mg aripiprazole in these healthy middle-aged Korean subjects. The aripiprazole ODT formulation is therefore expected to offer a convenient alternative for patients who have difficulty swallowing tablets without water. The study was registered at http://cris.nih.go.kr (registration number: KCT0001677).
本研究的主要目的是比较两种15毫克阿立哌唑制剂（口服崩解片[ODT]作为受试药物，普通片剂作为参比药物）在健康中年韩国受试者中的药代动力学特性和相对生物利用度。
本研究在健康中年韩国受试者群体中进行，为随机、开放标签、单剂量、2序列、2周期交叉试验。在单次服用15毫克阿立哌唑标准片剂并饮用240毫升水或服用15毫克阿立哌唑ODT且不饮水后，在0至240小时的特定时间间隔采集血样。采用液相色谱-串联质谱检测法分析血浆中阿立哌唑的浓度。记录药代动力学参数数据，并使用方差分析模型从对数转换数据中确定参数几何均值比值的90%置信区间。
纳入39名健康中年韩国受试者（平均年龄52.7岁；平均身高167厘米；平均体重67.6千克）；33名受试者完成研究（29名男性受试者和4名女性受试者）。Cmax、AUC0-last和AUC0-∞值的几何均值比值（受试药物/参比药物）的90%置信区间分别为0.95至1.14、0.98至1.09和0.97至1.08。所有发生不良事件的受试者均康复且无后遗症，未观察到严重不良事件。
在这些健康中年韩国受试者中，15毫克阿立哌唑的ODT和标准片剂的阿立哌唑药代动力学相似。因此，阿立哌唑ODT制剂有望为无水吞服片剂困难的患者提供一种方便的替代选择。该研究已在http://cris.nih.go.kr注册（注册号：KCT0001677）。
