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药物的组织分布与代谢V:促胰液素和缩胆囊素对兔胰腺药物转运的影响

Tissue distribution and metabolism of drugs V: effect of secretin and pancreozymin on drug transport in rabbit pancreas.

作者信息

Arakawa M, Okumura K, Hori R

出版信息

J Pharm Sci. 1980 Jan;69(1):27-30. doi: 10.1002/jps.2600690108.

DOI:10.1002/jps.2600690108
PMID:7354435
Abstract

The effect of secretin and pancreozymin on the tissue distribution and penetration of drugs in the rabbit pancreas was studied to clarify hormonally regulated drug distribution. Drugs with high liquid solubility were distributed easily within the pancreas even during secretin or pancreozymin treatment, and these hormones had little effect on drug distribution from the blood to the pancreas. However, secretin increased the concentration ratio of dimethadione in the pancreatic juice (J) to plasma unbound dimethadione (Pf), probably because the pancreatic juice during secretin infusion is alkaline relative to the control. Secretin had no effect on the J/Pf of isonicotinamide and sulfanilamide. Secretin decreased the J/Pf of drugs with low lipophilicity or large molecular weight because the penetration rates of these drugs from cell water to pancreatic juice were not rapid enough to reach equilibrium. Pancreozymin was unable to change the J/Pf of any drug tested. These results suggest that the barrier between the blood and the pancreas or the barrier between the pancreas and the pancreatic juice is unchanged by secretin or pancreozymin.

摘要

为阐明激素调节的药物分布情况,研究了促胰液素和促胰酶素对家兔胰腺中药物组织分布及渗透的影响。即使在促胰液素或促胰酶素治疗期间,具有高水溶性的药物也能轻易地在胰腺内分布,并且这些激素对药物从血液到胰腺的分布影响很小。然而,促胰液素增加了胰液中二甲双酮(J)与血浆游离二甲双酮(Pf)的浓度比,这可能是因为输注促胰液素期间的胰液相对于对照组呈碱性。促胰液素对异烟酰胺和磺胺的J/Pf没有影响。促胰液素降低了低亲脂性或大分子药物的J/Pf,因为这些药物从细胞内液到胰液的渗透率不够快,无法达到平衡。促胰酶素无法改变所测试任何药物的J/Pf。这些结果表明,血液与胰腺之间的屏障或胰腺与胰液之间的屏障不会因促胰液素或促胰酶素而改变。

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