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In vitro and in vivo characterization of a newly developed clonidine transdermal patch for treatment of attention deficit hyperactivity disorder in children
Ke, GM; Wang, L; Xue, HY; Lu, WL; Zhang, X; Zhang, QA; Guo, HY
关键词clonidine KBD-transdermal therapeutic system (TTS) LC-MS transdermal penetration pharmacokinetics rabbit
刊名BIOLOGICAL & PHARMACEUTICAL BULLETIN
2005-02-01
28期:2页:305-310
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]HEALTHY-SUBJECTS ; MASS-SPECTROMETRY ; HUMAN-PLASMA ; PHARMACOKINETICS ; M-5041T ; PHARMACODYNAMICS ; CHROMATOGRAPHY
英文摘要

The aim of this study was to characterize a newly developed clonidine transdermal patch, KBD-transdermal therapeutic system (TTS), for the treatment of attention deficit hyperactivity disorder in children. fit vitro release, penetration, and in vivo pharmacokinetics in rabbits were investigated. The smaller size of KBD-TTS (2.5 mg/2.5 cm(2)) showed a similar in vitro penetration to those of Catapres-TTS (2.5 mg/3.5 cm(2), a clonidine transdermal patch used for the treatment of hypertension, Alza Corporation, U.S.A.). The transdermal penetration rate of clonidine was mainly controlled by the ethylene vinylacetate membrane used in the patch. The skin layer may be only a minor rate-limiting barrier after the topical skin layer at the dosing site is saturated with penetrating clonidine in the initial phase (0 to 12 h). A sensitive liquid chromatography-mass spectrometry method for the quantification of clonidine in rabbit plasma was developed using solid-phase extraction and gradient elution on LC combined with the selected-ion monitoring (SIM) mode. A single dose of clonidine transdermal patch (KBD-TTS) or Catapres-TTS was transdermally administered to rabbits (n = 6 each) and removed after 168 h. The average half-life, T-max, C-max, and C-ss values of clonidine in rabbits following administration of KBD-TTS were 19.27 +/- 4.68 h, 52.56 +/- 25.77 h, 27.39 +/- 9.03 ng/ml, and 25.82 +/- 9.34 ng/ml, similar to those of Catapres-TTS, respectively. The clonidine plasma concentration of KBD-TTS reached a steady state at 24 h through 168 h. The in vitro release rate of the clonidine from KBD-TTS significantly correlated with the in vivo absorption rate (p < 0.001).

语种英语
WOS记录号WOS:000226995300022
引用统计
被引频次:11[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/64485
专题北京大学药学院
作者单位1.Beijing Kangbeide Pharmaceut Ltd, Beijing 100089, Peoples R China
2.Beijing Univ Chem Technol, Coll Sci, Beijing 100029, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Ke, GM,Wang, L,Xue, HY,et al. In vitro and in vivo characterization of a newly developed clonidine transdermal patch for treatment of attention deficit hyperactivity disorder in children[J]. BIOLOGICAL &amp; PHARMACEUTICAL BULLETIN,2005,28(2):305-310.
APA Ke, GM.,Wang, L.,Xue, HY.,Lu, WL.,Zhang, X.,...&Guo, HY.(2005).In vitro and in vivo characterization of a newly developed clonidine transdermal patch for treatment of attention deficit hyperactivity disorder in children.BIOLOGICAL & PHARMACEUTICAL BULLETIN,28(2),305-310.
MLA Ke, GM,et al."In vitro and in vivo characterization of a newly developed clonidine transdermal patch for treatment of attention deficit hyperactivity disorder in children".BIOLOGICAL & PHARMACEUTICAL BULLETIN 28.2(2005):305-310.
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