Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects

IMR OpenIR

	Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects
其他题名	Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects
	Zhang YF 1; Chen XY 1; Zhong DF 1; Dong YM 1
	2003
发表期刊	ACTA PHARMACOLOGICA SINICA
ISSN	1671-4083
卷号	24 期号:7 页码:715-718
摘要	AIM: 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.
其他摘要	AIM: 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.
关键词	loratadine descarboethoxyloratadine pharmacokinetics mass spectrum analysis
收录类别	CSCD
语种	英语
CSCD记录号	CSCD:1273308
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/145050
专题	中国科学院金属研究所
作者单位	1.中国科学院金属研究所 2.Peoples Hosp Liaoning Prov
推荐引用方式 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.