Kato Y, Yagi N, Yamada S, Sato M, Kimura R
Department of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka, Japan.
J Pharmacobiodyn. 1992 Jan;15(1):1-6. doi: 10.1248/bpb1978.15.1.
The nasal administration of digoxin was studied in rats and compared to intravenous, intraduodenal and rectal administration of the drug. The results indicated that the plasma level of digoxin after nasal administration was comparable to the level after intravenous injection. Administration by the intraduodenal and rectal routes resulted in considerably lower plasma levels. These data reveal that digoxin absorption across the nasal membranes is a reasonable approach. In the in situ nasal and intestinal perfusion experiments, digoxin disappeared from the perfusate following the apparent first-order kinetics. The nasal and intestinal absorption rate of digoxin was reduced by an increase in the perfusion volume. The plot of absorption rate constant against 1/volume resulted in a straight line, suggesting that digoxin is absorbed from nasal mucosa by a passive diffusion process.
在大鼠中研究了地高辛的鼻腔给药，并与该药物的静脉内、十二指肠内和直肠给药进行了比较。结果表明，鼻腔给药后地高辛的血浆水平与静脉注射后的水平相当。十二指肠内和直肠途径给药导致血浆水平显著降低。这些数据表明，地高辛跨鼻黏膜吸收是一种合理的给药途径。在原位鼻腔和肠道灌注实验中，地高辛按照明显的一级动力学从灌注液中消失。灌注体积增加会降低地高辛的鼻腔和肠道吸收速率。吸收速率常数与1/体积的关系图呈直线，表明地高辛通过被动扩散过程从鼻黏膜吸收。
