| Pharmacokinetics of orally administered single- and multiple-dose olopatadine in healthy Chinese subjects: an open-label study. | |
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MedLine Citation:
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PMID: 19499962 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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BACKGROUND AND OBJECTIVES: Olopatadine is a new selective histamine H(1) receptor antagonist with anti-inflammatory and anti-allergic effects. Its pharmacokinetics and safety have not previously been evaluated in Chinese subjects. The aims of this study were to assess the pharmacokinetics and safety of olopatadine after single- and multiple-dose oral administration in healthy Chinese subjects and to identify any differences in pharmacokinetics between males and females. METHODS: The pharmacokinetic parameters for olopatadine in 12 healthy Chinese subjects (six males and six females) were assessed by determining olopatadine concentrations with a validated liquid chromatography-tandem mass spectrometry method. Safety and tolerability were evaluated by monitoring adverse events, laboratory assay results, vital signs, physical examination findings and 12-lead ECG results. RESULTS: The pharmacokinetic parameters (mean +/- SD) for olopatadine following a single dose were: maximum plasma concentration (C(max)) 69.98 +/-20.87 ng/mL, time to reach C(max) (t(max)) 1.02 +/- 0.34 h, elimination half-life (t1/2) 5.87 +/- 4.24 h, area under the plasma-concentration curve (AUC) from time zero to the time of last quantifiable concentration (AUC(last)) 266.00 +/- 143.95 ng.h/mL, AUC from time zero extrapolated to infinity (AUC(infinity)) 283.46 +/- 152.96 ng.h/mL, apparent oral clearance (CL/F) 23.45 +/- 12.59 L/h and apparent volume of distribution after oral administration (V(d)/F) 133.83 +/- 43.07 L. The pharmacokinetic parameters of olopatadine after multiple doses were similar to those after a single dose. In both studies, significantly higher AUC(last), AUC(infinity) and C(max), longer t1/2 (single-dose only) and lower CL/F were observed in female subjects compared with male subjects after both single and multiple dosing. No serious adverse events occurred. CONCLUSION: Olopatadine was shown to be safe and well tolerated in healthy Chinese subjects. There were no changes in absorption and elimination of olopatadine following multiple doses and no accumulation was found. Possible sex-related differences in absorption and elimination of olopatadine were observed. |
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Authors:
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Nan-Nan Chu; Wei-Li Chen; Hong-Rong Xu; Xue-Ning Li |
Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Clinical drug investigation Volume: 29 ISSN: 1173-2563 ISO Abbreviation: Clin Drug Investig Publication Date: 2009 |
Date Detail:
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Created Date: 2009-06-08 Completed Date: 2009-08-14 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9504817 Medline TA: Clin Drug Investig Country: New Zealand |
Other Details:
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Languages: eng Pagination: 451-7 Citation Subset: IM |
Affiliation:
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Department of Clinical Pharmacology, ZhongShan Hospital, Fudan University, Shanghai, China. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*, pharmacology Area Under Curve Asian Continental Ancestry Group Chromatography, Liquid Dibenzoxepins / pharmacokinetics*, pharmacology Dose-Response Relationship, Drug Drug Administration Schedule Female Half-Life Humans Male Sex Factors Tandem Mass Spectrometry Young Adult |
| Chemical | |
Reg. No./Substance:
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0/Anti-Inflammatory Agents, Non-Steroidal; 0/Dibenzoxepins; 113806-05-6/olopatadine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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