• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

Prediction of plasma concentration of GTS-21 in hairless rats following monolithic transdermal delivery.

作者信息

Kawamata Hideki, Tojo Kakuji

机构信息

Department of Biochemical Science and Engineering, College of Computer Science and Systems Engineering, Kyusyu Institute of Technology, Kawazu, Iizuka, Japan.

出版信息

Biol Pharm Bull. 2002 Mar;25(3):342-5. doi: 10.1248/bpb.25.342.

DOI:10.1248/bpb.25.342
PMID:11913530
Abstract

The transdermal therapeutic systems (TTS) usually achieve constant plasma concentration for an extended period of time. This is because a sufficient drug stored in the device can keep the constant concentration on the surface of the stratum corneum during the system application. When the drug molecules are not enough to provide the constant surface concentration, the rate of drug penetration decreases with time because of decreased supply of the drug molecules from the delivery device. This paper has proposed an empirical simple approach to predict the plasma concentration for such a TTS. A novel compound, GTS-21, for Alzheimers' disease currently under development was used as a model drug. In vivo and in vitro experiments were carried out in hairless rats. The in vivo plasma concentration-time profile in hairless rats following the application of TTS well agreed with the predicted profile based on the skin pharmacokinetic model together with the model parameters determined from the in vitro experiment.

摘要

相似文献

1
Prediction of plasma concentration of GTS-21 in hairless rats following monolithic transdermal delivery.
Biol Pharm Bull. 2002 Mar;25(3):342-5. doi: 10.1248/bpb.25.342.
2
Simultaneous determination of GTS-21 and its metabolite in rat plasma by high-performance liquid chromatography using solid-phase extraction.
J Chromatogr B Biomed Appl. 1996 Nov 15;686(2):229-34. doi: 10.1016/s0378-4347(96)00233-2.
3
Pharmacokinetics and urinary excretion of DMXBA (GTS-21), a compound enhancing cognition.增强认知的化合物DMXBA(GTS-21)的药代动力学及尿排泄情况
Biopharm Drug Dispos. 1998 Apr;19(3):147-51. doi: 10.1002/(sici)1099-081x(199804)19:3<147::aid-bdd77>3.0.co;2-9.
4
First-pass of GTS-21 on canine gut wall and liver determined by portal-systemic concentration difference.
Eur J Pharm Sci. 2001 Sep;14(2):159-65. doi: 10.1016/s0928-0987(01)00166-x.
5
Pharmacokinetic Limitations on Effects of an Alpha7-Nicotinic Receptor Agonist in Schizophrenia: Randomized Trial with an Extended-Release Formulation.精神分裂症中 α7 烟碱型受体激动剂作用的药代动力学限制:用缓释制剂进行的随机试验。
Neuropsychopharmacology. 2018 Feb;43(3):583-589. doi: 10.1038/npp.2017.182. Epub 2017 Aug 21.
6
Evaluation of the predicted time-concentration profile of serum tulobuterol in human after transdermal application.透皮给药后人体血清妥洛特罗预测时间-浓度曲线的评估。
Chem Pharm Bull (Tokyo). 2012;60(3):300-5. doi: 10.1248/cpb.60.300.
7
Metabolism and disposition of GTS-21, a novel drug for Alzheimer's disease.GTS-21(一种用于治疗阿尔茨海默病的新型药物)的代谢与处置
Xenobiotica. 1999 Jul;29(7):747-62. doi: 10.1080/004982599238362.
8
Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo.新型神经元烟碱型乙酰胆碱受体配体GTS-21的体内外功能特性研究
Pharmacol Biochem Behav. 1997 May-Jun;57(1-2):231-41. doi: 10.1016/s0091-3057(96)00354-1.
9
Hydroxy metabolites of the Alzheimer's drug candidate 3-[(2,4-dimethoxy)benzylidene]-anabaseine dihydrochloride (GTS-21): their molecular properties, interactions with brain nicotinic receptors, and brain penetration.阿尔茨海默病候选药物3-[(2,4-二甲氧基)亚苄基]-阿那abaseine二盐酸盐(GTS-21)的羟基代谢物:它们的分子特性、与脑烟碱受体的相互作用以及脑渗透性。
Mol Pharmacol. 2004 Jan;65(1):56-67. doi: 10.1124/mol.65.1.56.
10
A method for predicting steady-state rate of skin penetration in vivo.一种预测体内皮肤渗透稳态速率的方法。
J Invest Dermatol. 1989 Jan;92(1):105-8. doi: 10.1111/1523-1747.ep13071314.