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口腔黏膜给药系统综述

Orotransmucosal drug delivery systems: a review.

作者信息

Madhav N V Satheesh, Shakya Ashok K, Shakya Pragati, Singh Kuldeep

机构信息

Faculty of Pharmacy, Dehradoon Institute of Technology, Mussorie Diversion Road, Bagawantpur, Makkawala, Uttarakhand 248009 Dehradoon, India.

出版信息

J Control Release. 2009 Nov 16;140(1):2-11. doi: 10.1016/j.jconrel.2009.07.016. Epub 2009 Aug 6.

Abstract

Oral mucosal drug delivery is an alternative method of systemic drug delivery that offers several advantages over both injectable and enteral methods and also enhances drug bioavailability because the mucosal surfaces are usually rich in blood supply, providing the means for rapid drug transport to the systemic circulation and avoiding, in most cases, degradation by first-pass hepatic metabolism. The systems contact with the absorption surface resulting in a better absorption, and also prolong residence time at the site of application to permit once or twice daily dosing. For some drugs, this results in rapid onset of action via a more comfortable and convenient delivery route than the intravenous route. Not all drugs, however, can be administered through the oral mucosa because of the characteristics of the oral mucosa and the physicochemical properties of the drug. Although many drugs have been evaluated for oral transmucosal delivery, few are commercially available. The clinical need for oral transmucosal delivery of a drug must be high enough to offset the high costs associated with developing this type of product. Transmucosal products are a relatively new drug delivery strategy. Transmucosal drug delivery promises four times the absorption rate of skin. Drugs considered for oral transmucosal delivery are limited to existing products, and until there is a change in the selection and development process for new drugs, candidates for oral transmucosal delivery will be limited. The present papers intend to overview a wide range of orotransmucosal routes being potentially useful for transmucosal drug delivery and remind us of the success achieved with these systems and the latest advancement in the field.

摘要

口腔黏膜给药是一种全身给药的替代方法,与注射给药和肠道给药方法相比具有多个优点,并且还能提高药物的生物利用度,因为黏膜表面通常血供丰富,为药物快速转运至体循环提供了途径,并且在大多数情况下可避免首过肝代谢导致的降解。这些给药系统与吸收表面接触可实现更好的吸收,还能延长在给药部位的停留时间,从而允许每日给药一次或两次。对于某些药物而言,与静脉给药途径相比,通过这种更舒适便捷的给药途径可实现快速起效。然而,由于口腔黏膜的特性和药物的理化性质,并非所有药物都能通过口腔黏膜给药。尽管许多药物已针对口腔黏膜给药进行了评估,但只有少数药物可用于商业用途。药物口腔黏膜给药的临床需求必须足够高,以抵消开发此类产品的高昂成本。黏膜给药产品是一种相对较新的给药策略。黏膜给药的吸收率有望达到经皮给药的四倍。考虑用于口腔黏膜给药的药物仅限于现有产品,并且在新药的选择和开发过程发生改变之前,口腔黏膜给药的候选药物将受到限制。本文旨在概述一系列对黏膜给药可能有用的口腔黏膜给药途径,并提醒我们这些给药系统已取得的成功以及该领域的最新进展。

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