Yamahara H, Suzuki T, Mizobe M, Noda K, Samejima M
Products Formulation Research Laboratory, Tanabe Seiyaku Company, Ltd., Osaka, Japan.
J Pharm Sci. 1990 Nov;79(11):963-7. doi: 10.1002/jps.2600791103.
To evaluate oral mucosal absorption of drugs in dogs, a newly designed in situ perfusion system with a circulating perfusion chamber was developed. The utility of the perfusion system was investigated by using three drugs: salicylic acid (SA), sulfadimethoxine (SM), and diltiazem (DIL). The oral mucosal absorption of the drugs could be adequately described by first-order rate processes. The absorption rate was independent of the amount of un-ionized drug, which varied with the pH of the solution. The absorption of SA was similar for various oral mucosal sites and for repeated experiments using the same site. Pharmacokinetic analysis for the plasma or medium concentration of SA after perfusion showed that SA was absorbed at the rate constant of 0.071 h-1, and that approximately 70% of SA absorbed from oral mucosa was transferred to the circulating blood.
为评估犬类口腔黏膜对药物的吸收情况,研发了一种新设计的带有循环灌注室的原位灌注系统。使用三种药物(水杨酸(SA)、磺胺二甲氧嘧啶(SM)和地尔硫䓬(DIL))对该灌注系统的实用性进行了研究。药物的口腔黏膜吸收可用一级速率过程充分描述。吸收速率与未离子化药物的量无关,而未离子化药物的量会随溶液pH值变化。SA在不同口腔黏膜部位以及在同一部位重复实验时的吸收情况相似。灌注后对SA血浆或介质浓度进行的药代动力学分析表明,SA以0.071 h-1的速率常数被吸收,且从口腔黏膜吸收的SA中约70%转移至循环血液中。