Aqil Mohammed, Sultana Yasmin, Ali Asgar
Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India.
Expert Opin Drug Deliv. 2006 May;3(3):405-18. doi: 10.1517/17425247.3.3.405.
Beta-adrenoceptor blocking drugs (beta-blockers) are one of the most frequently used class of cardiovascular drugs that are mainly used in conventional dosage forms., which have their own limitations including hepatic first-pass metabolism, high incidence of adverse effects due to variable absorption profiles, higher frequency of administration and poor patient compliance. Essentially, attempts have been made to develop novel drug delivery systems for beta-blockers, including transdermal delivery systems, to circumvent the drawbacks of conventional drug delivery. However, so far none of the beta-blocker drugs have been marketed as transdermal delivery systems. Nevertheless, there have been noteworthy research endeavours worldwide at the laboratory level to investigate the skin permeation and to develop transdermal formulations of beta-blockers including: propranolol, metoprolol, atenolol, timolol, levobunolol, bupranolol, bopindolol, mepindolol, sotalol, labetolol, pindolol, acebutolol and oxprenolol. Innovative research exploiting penetration-enhancing strategies, such as iontophoresis, electroporation, microneedles and sonophoresis, holds promise for the successful use of these drugs as consumer-friendly transdermal dosage forms in clinical practice. This paper presents an overview of the transdermal research on this important class of drugs.
β-肾上腺素受体阻断药(β受体阻滞剂)是最常用的心血管药物之一,主要以传统剂型使用。这些传统剂型有其自身的局限性,包括肝脏首过代谢、由于吸收情况多变导致的不良反应发生率高、给药频率高以及患者依从性差。从本质上讲,人们一直在尝试开发用于β受体阻滞剂的新型药物递送系统,包括透皮给药系统,以规避传统药物递送的缺点。然而,到目前为止,尚无β受体阻滞剂药物以透皮给药系统上市。尽管如此,在全球范围内,实验室层面已有值得关注的研究工作,旨在研究β受体阻滞剂的皮肤渗透情况并开发其透皮制剂,这些β受体阻滞剂包括:普萘洛尔、美托洛尔、阿替洛尔、噻吗洛尔、左布诺洛尔、布普洛尔、波吲洛尔、甲吲洛尔、索他洛尔、拉贝洛尔、吲哚洛尔、醋丁洛尔和氧烯洛尔。利用渗透增强策略(如离子导入、电穿孔、微针和超声导入)的创新性研究,有望使这些药物在临床实践中成功用作方便消费者的透皮剂型。本文概述了对这类重要药物的透皮研究情况。