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学科主题: 药学
题名:
A novel transdermal patch incorporating isosorbide dinitrate with bisoprolol: In vitro and in vivo characterization
作者: Zhao, Ji-Hui; Fu, Ji-Hua; Wang, Shu-Ming; Su, Chang-Hai; Shan, Ying; Kong, Shu-Jia; Wang, Yuan; Lu, Wan-Liang; Zhang, Hua; Zhang, Shuang; Li, Lin; Zhang, En-Hong; Wang, Li; Pei, Qiu-Ling; Wang, Jian-Cheng; Zhang, Xuan; Zhang, Qiang
关键词: transdermal delivery ; hypertension ; isosorbide dinitrate ; bisoprolol ; pharmacodynamics ; pharmacokinetics
刊名: INTERNATIONAL JOURNAL OF PHARMACEUTICS
发表日期: 2007-06-07
DOI: 10.1016/j.ijpharm.2006.12.030
卷: 337, 期:1-2, 页:88-101
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]: SUSTAINED-RELEASE FORMULATIONS ; PENETRATION ENHANCERS ; PERCUTANEOUS PENETRATION ; BETA-BLOCKERS ; RAT SKIN ; HYPERTENSION ; ISOSORBIDE-5-MONONITRATE ; EFFICACY ; PLASMA ; PHARMACOKINETICS
英文摘要:

The combination therapy of nitrate and selective beta-adrenoceptor antagonist has shown benefits for treatment of hypertension and heart disease than either drug alone. The objectives of the present study were to define effects on the antihypertension activity and pharmacokinetics of a novel transdermal patch incorporating isosorbide dinitrate (ISDN) with bisoprolol (BP). The 3:2 ratio of ISDN to BP (mg/mg) in the transdermal patches exhibited better anti-hypertension effect synergistically with a similar inhibiting heart rates effect to that of BP alone in renovascular hypertensive rats, and was therefore selected as a final formulation. The in vitro transdermal penetration of both ISDN and BP from the patches displayed a zero-order process, and the penetration rate constants were 7.4 mu g/(cm(2) h) for ISDN, and 5.9 mu g/(cm(2) h) for BP, respectively. After transdermal administration at single dose or multiple doses, the synergistic anti-hypertension effect was confirmed in spontaneously hypertensive rats also. The effect of each patch lasts for 3 days, and increased with the total dose of two drugs (2mg/cm(2), ISDN:BP=3:2, mg/mg), showing a dose dependant manner. After transdermal administration to rabbits, the absolute bioavailabilities were 33.6% for ISDN, and 31.3% for BP, respectively. The maximal concentrations (C._) of both drugs were significantly reduced while the areas under the plasma concentration-time curve (AUC), and mean residence times (MRT) were evidently increased and extended, respectively. As a patient-friendly, convenient, and multi-day dosing therapeutic system, the transdermal patches incorporating ISDN and BP could be promising for prevention and treatment of hypertension. (c) 2007 Elsevier B.V. All rights reserved.

语种: 英语
WOS记录号: WOS:000247355800010
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59264
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
2.China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Peoples R China
3.Beijing Kangbeide Pharmaceut Co Ltd, Beijing 100029, Peoples R China
4.Shanxi Med Univ, Sch Publ Hlth, Taiyuan 030001, Peoples R China

Recommended Citation:
Zhao, Ji-Hui,Fu, Ji-Hua,Wang, Shu-Ming,et al. A novel transdermal patch incorporating isosorbide dinitrate with bisoprolol: In vitro and in vivo characterization[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2007,337(1-2):88-101.
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