Megwa S A, Benson H A, Roberts M S
Department of Medicine, University of Queensland, Australia.
J Pharm Pharmacol. 1995 Nov;47(11):891-6. doi: 10.1111/j.2042-7158.1995.tb03266.x.
Studies to determine the extent of local tissue penetration of topically applied, commercially available salicylate esters and salts were conducted in male Wistar rats. The salicylate concentration in plasma, tissues underlying the site of drug application, and similar tissues on the contralateral (control) side were measured. The plasma and tissue salicylate levels suggest that direct penetration of salicylate was predominant to the top muscle level on the treated site. Results also suggest that the drugs were first absorbed into the bloodstream and subsequently distributed to both the deeper tissues on the treated site and the contralateral tissues. The topical application of formulations of ester methyl salicylate and salts triethanolamine salicylate and diethylamine salicylate containing comparable salicylate concentrations yielded similar salicylate concentrations in the various tissues. The salicylate concentrations in the deeper tissues approached concentrations observed in the contralateral tissues suggesting that salicylate present in these tissues was due to the systemic blood supply.
在雄性Wistar大鼠中开展了研究，以确定局部应用市售水杨酸酯和盐后其在局部组织中的渗透程度。测量了血浆、药物应用部位下方组织以及对侧（对照）相同组织中的水杨酸盐浓度。血浆和组织中的水杨酸盐水平表明，水杨酸盐的直接渗透在治疗部位主要达到顶部肌肉水平。结果还表明，药物首先被吸收进入血液，随后分布到治疗部位的深层组织和对侧组织。局部应用含有相当水杨酸盐浓度的水杨酸甲酯制剂以及三乙醇胺水杨酸盐和二乙胺水杨酸盐，在各种组织中产生了相似的水杨酸盐浓度。深层组织中的水杨酸盐浓度接近对侧组织中观察到的浓度，这表明这些组织中存在的水杨酸盐是由于全身血液供应所致。
