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经皮途径给予β受体阻滞剂治疗高血压的全身给药方法。

Systemic delivery of β-blockers via transdermal route for hypertension.

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.

Department of Pharmaceutics, College of Pharmacy, Buraydah Private Colleges, P.O. Box 31, 717, Buraydah, Al-Qassim, Saudi Arabia ; Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), M. B. Road, New Delhi 110062, India.

出版信息

Saudi Pharm J. 2015 Nov;23(6):587-602. doi: 10.1016/j.jsps.2013.12.019. Epub 2014 Jan 3.

Abstract

Hypertension is the most common cardiovascular disease worldwide. Moreover, management of hypertension requires long-term treatment that may result in poor patient compliance with conventional dosage forms due to greater frequency of drug administration. Although there is availability of a plethora of therapeutically effective antihypertensive molecules, inadequate patient welfare is observed; this arguably presents an opportunity to deliver antihypertensive agents through a different route. Ever since the transdermal drug delivery came into existence, it has offered great advantages including non-invasiveness, prolonged therapeutic effect, reduced side effects, improved bioavailability, better patient compliance and easy termination of drug therapy. Attempts were made to develop the transdermal therapeutic system for various antihypertensive agents, including β-blockers, an important antihypertensive class. β-blockers are potent, highly effective in the management of hypertension and other heart ailments by blocking the effects of normal amounts of adrenaline in the heart and blood vessels. The shortcomings associated with β-blockers such as more frequent dose administration, extensive first pass metabolism and variable bioavailability, make them an ideal candidate for transdermal therapeutic systems. The present article gives a brief view of different β-blockers formulated as transdermal therapeutic system in detail to enhance the bioavailability as well as to improve patient compliance. Constant improvement in this field holds promise for the long-term success in technologically advanced transdermal dosage forms being commercialized sooner rather than later.

摘要

高血压是全球最常见的心血管疾病。此外,高血压的治疗需要长期进行,由于给药频率较高,患者可能难以长期依从传统剂型的治疗。尽管有大量具有治疗效果的降压分子,但患者的福利仍然不足;这可能为通过不同途径给药提供了机会。自从透皮给药系统问世以来,它提供了许多优势,包括非侵入性、延长治疗效果、减少副作用、提高生物利用度、更好的患者依从性和易于终止药物治疗。人们尝试开发各种降压药的透皮治疗系统,包括β受体阻滞剂,这是一种重要的降压药。β受体阻滞剂通过阻断心脏和血管中正常量肾上腺素的作用,对高血压和其他心脏疾病的治疗非常有效。β受体阻滞剂存在一些缺点,如给药频率较高、广泛的首过代谢和可变的生物利用度,这使它们成为透皮治疗系统的理想候选药物。本文详细介绍了不同的β受体阻滞剂作为透皮治疗系统的配方,以提高生物利用度并提高患者的依从性。这一领域的不断改进有望为技术先进的透皮给药系统的长期成功铺平道路,使其早日商业化。

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