de Vries M E, Boddé H E, Verhoef J C, Junginger H E
Division of Pharmaceutical Technology, Leiden State University, The Netherlands.
Crit Rev Ther Drug Carrier Syst. 1991;8(3):271-303.
The buccal mucosa offers excellent possibilities for the (long-term) delivery of suitable drugs, especially for metabolically unstable drugs, such as peptides. A review is given of the present knowledge about buccal drug absorption and drug delivery devices. The structure and physiology of the oral mucosae are described, as well as interspecies differences with respect to tissue permeability. Methods to determine mucosal drug absorption, either in vivo or in vitro, are discussed, as well as absorption pathways, mechanisms, and enhancement. Technological strategies to control transbuccal drug absorption comprise the design of mucoadhesive devices in order to shorten diffusion pathways and prolong administration, and structural and chemical modulation of the device with the aim of shifting the rate-limiting transport step from the tissue to the device. Finally, examples of buccally administered drugs are given and devices currently used in local therapy are described.
颊黏膜为(长期)递送合适的药物提供了绝佳的可能性,尤其是对于代谢不稳定的药物,如肽类药物。本文综述了目前关于颊部药物吸收和给药装置的知识。描述了口腔黏膜的结构和生理学,以及种间在组织通透性方面的差异。讨论了体内或体外测定黏膜药物吸收的方法,以及吸收途径、机制和增强作用。控制经颊药物吸收的技术策略包括设计黏膜黏附装置以缩短扩散途径并延长给药时间,以及对装置进行结构和化学调节,目的是将限速转运步骤从组织转移到装置。最后,给出了颊部给药药物的实例,并描述了目前用于局部治疗的装置。