Seki J, Mukai H, Sugiyama M
J Pharmacobiodyn. 1985 May;8(5):337-43. doi: 10.1248/bpb1978.8.337.
To examine the absorption mechanism of sodium guaiazulene-3-sulfonate (GAS) through the nasal and the intestinal membrane, the apparent absorption rate under the various experimental conditions was measured with the in situ perfusion method in rats, and the apparent partition coefficient of GAS was also determined. The absorption rate of GAS changed biphasically depending on the initial GAS concentration in the perfusate. At the lower concentration range (less than 1 mg/ml), the absorption rate of GAS decreased with the increased in the concentration, and the absorption was inhibited by HgCl2 and ouabain. However, at the higher concentration range (greater than 1 mg/ml), the absorption rate from the nasal mucosa increased markedly with the increase in the concentration, and ouabain had no effect. The apparent partition coefficient of GAS increased with the increase in the concentration of GAS, and GAS was found to be readily transferred to the organic phase by forming ion-pair complexes with the cation such as NH4+ ion. These results suggested that GAS is absorbed through the nasal membrane by at least two kinds of mechanisms: one is a carrier mediated system and the other is a hydrophobic interaction with the nasal mucosa which is increased by forming an ion-pair complex of GAS with cation.
为研究愈创蓝油烃-3-磺酸钠（GAS）通过鼻黏膜和肠黏膜的吸收机制，采用大鼠原位灌注法测定了不同实验条件下的表观吸收率，并测定了GAS的表观分配系数。GAS的吸收率根据灌注液中GAS的初始浓度呈双相变化。在较低浓度范围（低于1mg/ml），GAS的吸收率随浓度增加而降低，且HgCl2和哇巴因可抑制其吸收。然而，在较高浓度范围（高于1mg/ml），鼻黏膜的吸收率随浓度增加而显著增加，且哇巴因无影响。GAS的表观分配系数随GAS浓度增加而增加，且发现GAS通过与阳离子（如NH4+离子）形成离子对复合物而易于转移至有机相。这些结果表明，GAS通过鼻黏膜至少通过两种机制吸收：一种是载体介导系统，另一种是与鼻黏膜的疏水相互作用，这种相互作用通过GAS与阳离子形成离子对复合物而增强。
