HOME HELP FEEDBACK SUBSCRIPTIONS ARCHIVE SEARCH TABLE OF CONTENTS		QUICK SEARCH:   [advanced] Author: Keyword(s): Year:  Vol:  Page:

This Article Full Text Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Email this article to a friend Similar articles in this journal Similar articles in ISI Web of Science Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Request Permissions Request Reprints Citing Articles Citing Articles via HighWire Citing Articles via ISI Web of Science (4) Citing Articles via Google Scholar Google Scholar Articles by Ahmed, T. Articles by Batra, V. Search for Related Content PubMed PubMed Citation Articles by Ahmed, T. Articles by Batra, V. Social Bookmarking                   What's this?

Safety, Tolerability, and Single- and Multiple-Dose Pharmacokinetics of Piperaquine Phosphate in Healthy Subjects

From the Metabolism and Pharmacokinetic Department (Dr Ahmed, Dr Sharma, Mr Gautam, Mr Varshney, Dr Paliwal, Dr Batra) and Department of Medical Affairs and Clinical Research (Dr Kothari, Dr Ganguly, Dr Saha), Ranbaxy Research Laboratories, Haryana, India, and Medicines for Malaria Venture-MMV, International Center Cointrin, Geneva, Switzerland (Dr Moehrle).

Piperaquine phosphate is an orally active bisquinolone antimalarial drug that has been used for the past 3 decades. The authors report the safety, tolerability, and pharmacokinetics of piperaquine from a classical controlled phase I study. It was a double-blind, randomized, parallel-group, placebo-controlled, and single- and multiple-dose study. During the rising single-dose study, single ascending oral doses of 500, 750, 1000, 1250, and 1500 mg of piperaquine phosphate were administered, whereas in rising multiple-dose study, once-daily ascending oral doses of 500, 750, 1000, and 1500 mg were administered for 3 consecutive days. Pharmacokinetic analysis for both the rising single- and multiple-dose studies was done using the noncompartmental approach. The mean apparent terminal half-life ranged from 11 to 23 days. Increase in exposure was less than dose proportional and linear. Piperaquine concentrations were measurable up to 60 days postdose. Multiple peaks were observed in the plasma piperaquine concentration-time profiles and exhibited 3- to 7-fold accumulation following multiple dosing. Piperaquine was well tolerated following single and multiple doses.

Key Words: Piperaquine • pharmacokinetics • safety • healthy • subjects

Address for correspondence: Jyoti Paliwal, PhD, Metabolism and Pharmacokinetics Department, Ranbaxy Research Laboratories, Plot #20, Sector-18, Udhyog Vihar Industrial Area, Gurgaon-122015, Haryana, India; e-mail: jyoti.paliwal{at}ranbaxy.com.

CiteULike    Connotea    Del.icio.us    Digg    Reddit    Technorati    What's this?

This article has been cited by other articles:

				N. T. Chinh, N. N. Quang, N. X. Thanh, B. Dai, J. P. Geue, R. S. Addison, T. Travers, and M. D. Edstein Pharmacokinetics and Bioequivalence Evaluation of Two Fixed-Dose Tablet Formulations of Dihydroartemisinin and Piperaquine in Vietnamese Subjects Antimicrob. Agents Chemother., February 1, 2009; 53(2): 828 - 831. [Abstract] [Full Text] [PDF]

				N. T. Chinh, N. N. Quang, N. X. Thanh, B. Dai, T. Travers, and M. D. Edstein Pharmacokinetics of the Antimalarial Drug Piperaquine in Healthy Vietnamese Subjects Am J Trop Med Hyg, October 1, 2008; 79(4): 620 - 623. [Abstract] [Full Text] [PDF]