Pharmacokinetics and tolerability of paliperidone palmitate injection in Chinese subjects

Human Psychopharmacology: Clinical and ExperimentalVolume 29, Issue 2 p. 203-210 Short Communication Pharmacokinetics and tolerability of paliperidone palmitate injection in Chinese subjects Tianmei Si, Corresponding Author Tianmei Si Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, China Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, ChinaCorrespondence to: S. Tianmei, Peking University Institute of Mental Health, Haidian District, Huayuanbeilu 51#, Beijing, 100191, China. Tel: (86) 10 82801948; Fax: (86) 10 62027314 E-mail: si.tian-mei@163.comSearch for more papers by this authorYun'ai Su, Yun'ai Su Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, China Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, ChinaSearch for more papers by this authorYi Liu, Yi Liu Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, China Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, ChinaSearch for more papers by this authorHongyan Zhang, Hongyan Zhang Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, China Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, ChinaSearch for more papers by this authorHuafang Li, Huafang Li Shanghai Mental Health Center, Shanghai, ChinaSearch for more papers by this authorQing Rui, Qing Rui China R&D and Scientific Affairs, Xi'an Janssen Pharmaceutical Ltd, Beijing, ChinaSearch for more papers by this authorLiang Shu, Liang Shu Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, China Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, ChinaSearch for more papers by this author Tianmei Si, Corresponding Author Tianmei Si Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, China Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, ChinaCorrespondence to: S. Tianmei, Peking University Institute of Mental Health, Haidian District, Huayuanbeilu 51#, Beijing, 100191, China. Tel: (86) 10 82801948; Fax: (86) 10 62027314 E-mail: si.tian-mei@163.comSearch for more papers by this authorYun'ai Su, Yun'ai Su Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, China Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, ChinaSearch for more papers by this authorYi Liu, Yi Liu Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, China Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, ChinaSearch for more papers by this authorHongyan Zhang, Hongyan Zhang Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, China Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, ChinaSearch for more papers by this authorHuafang Li, Huafang Li Shanghai Mental Health Center, Shanghai, ChinaSearch for more papers by this authorQing Rui, Qing Rui China R&D and Scientific Affairs, Xi'an Janssen Pharmaceutical Ltd, Beijing, ChinaSearch for more papers by this authorLiang Shu, Liang Shu Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, China Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, ChinaSearch for more papers by this author First published: 03 March 2014 https://doi.org/10.1002/hup.2388Citations: 10Read the full textAboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinked InRedditWechat Abstract Objective The objective of this study was to characterize the pharmacokinetics of 25, 100, and 150 mg equivalents (eq.) of paliperidone long-acting injection in Chinese subjects with schizophrenia. Methods This was an open-label, randomized, parallel group, multicenter study. A total of 48 patients were randomized in a 1:1:1 ratio to one of three groups. Sequential blood samples were collected immediately before injection on day 1 and up to 210 days after the first injection. The plasma paliperidone concentrations were determined by a validated high-performance liquid chromatography/tandem mass spectrometry method. Results A total of 47 patients received at least one injection of the study medication, and 43 completed the study. The pharmacokinetic (PK) parameters, such as time to maximum concentration, t1/2, and CL/F, were comparable across the three treatment groups (p = 0.935, 0.349, and 0.794, respectively). The differences in maximum plasma concentration, AUC (035 days), AUC (0–210 days), and AUC (0–∞) were significant (p < 0.001) and dose proportional. The inter-individual variation of PK parameters was large. The most frequent treatment-emergent adverse events were prolactin level increasing, injection site pain, tremor, dry mouth, and constipation. Conclusions The pharmacokinetics of paliperidone palmitate are linear with respect to time in Chinese subjects with schizophrenia at injections from 25 to 150 mg eq. Copyright © 2014 John Wiley & Sons, Ltd. Citing Literature Volume29, Issue2March 2014Pages 203-210 RelatedInformation