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Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects
Alternative TitlePharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects
Zhang YF1; Chen XY1; Zhong DF1; Dong YM1
2003
Source PublicationACTA PHARMACOLOGICA SINICA
ISSN1671-4083
Volume24Issue:7Pages:715-718
AbstractAIM: To investigate the pharmacokinetics of loratadine (LOR) and its active metabolite descarboethoxyloratadine (DCL) in healthy Chinese subjects. METHODS: Twenty healthy Chinese male subjects received a single oral dose of LOR 20 mg. A sensitive liquid chromatography-tandem mass spectrometry method (LC/MS/MS) was used for the determination of LOR and DCL in plasma. RESULTS: Mean maximum concentration (C.) was found (17 14) mug/L for LOR at 1.2 h and (16+/-9) mug/L for DCL at 1.5 h. Mean area under the plasma concentration-time curve from zero to infinity (AUC(0-infinity)) was (47+/-49) gg-h-L(-1) for LOR and (181+/-22) mug.h.L(-1) for DCL, respectively. The apparent elimination half-life (T(1/2)) of LOR was (6+/-4) h, and that of DCL was (13.4+/-2.6) h. The ratios of AUC(DCL)/AUC(LOR) ranged from 0.36 to 54.5. CONCLUSION: LOR was rapidly absorbed and transformed to DCL. AUC of the parent drug was extremely variable, while AUC of the active metabolite DCL was moderately variable after an oral dose of LOR to Chinese subjects.
Other AbstractAIM: To investigate the pharmacokinetics of loratadine (LOR) and its active metabolite descarboethoxyloratadine (DCL) in healthy Chinese subjects. METHODS: Twenty healthy Chinese male subjects received a single oral dose of LOR 20 mg. A sensitive liquid chromatography-tandem mass spectrometry method (LC/MS/MS) was used for the determination of LOR and DCL in plasma. RESULTS: Mean maximum concentration (C_(max)) was found (17 ± 14) μg/L for LOR at 1.2 h and (16 ± 9) μg/L for DCL at 1.5 h. Mean area under the plasma concentration-time curve from zero to infinity (AUC_(0-∞)) was (47 ± 49) μg·h·L~(-1) for LOR and (181±122) μg·h·L~(-1) for DCL, respectively. The apparent elimination half-life (T_(1/2)) of LOR was (6 ± 4) h, and that of DCL was (13.4 ± 2.6) h. The ratios of AUC_(DCL)/AUC_(LOR) ranged from 0.36 to 54.5. CONCLUSION: LOR was rapidly absorbed and transformed to DCL. AUC of the parent drug was extremely variable, while AUC of the active metabolite DCL was moderately variable after an oral dose of LOR to Chinese subjects.
Keywordloratadine descarboethoxyloratadine pharmacokinetics mass spectrum analysis
Indexed ByCSCD
Language英语
CSCD IDCSCD:1273308
Citation statistics
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/145050
Collection中国科学院金属研究所
Affiliation1.中国科学院金属研究所
2.Peoples Hosp Liaoning Prov
Recommended Citation
GB/T 7714
Zhang YF,Chen XY,Zhong DF,et al. Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects[J]. ACTA PHARMACOLOGICA SINICA,2003,24(7):715-718.
APA Zhang YF,Chen XY,Zhong DF,&Dong YM.(2003).Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects.ACTA PHARMACOLOGICA SINICA,24(7),715-718.
MLA Zhang YF,et al."Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects".ACTA PHARMACOLOGICA SINICA 24.7(2003):715-718.
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