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口腔药物吸收研究:影响仓鼠颊囊吸收的物理化学因素。

Studies on drug absorption from oral cavity: physicochemical factors affecting absorption from hamster cheek pouch.

作者信息

Kurosaki Y, Aya N, Okada Y, Nakayama T, Kimura T

出版信息

J Pharmacobiodyn. 1986 Mar;9(3):287-96. doi: 10.1248/bpb1978.9.287.

DOI:10.1248/bpb1978.9.287
PMID:3723320
Abstract

A new experimental method using a hamster cheek pouch in vivo for studying absorption processes across the keratinized oral mucous membrane was developed and some characteristics of the oral-mucosal absorption were clarified. A positive correlation between the absorption rate and the lipophilicity was observed in 18 aromatic compounds examined. The absorption of ionizable compounds was poor in the ionized form. These results suggest that the absorption from the keratinized hamster cheek pouch is due to a passive diffusion mechanism and obeys pH-partition hypothesis. The systemic transfer of salicylic acid after intra-cheek-pouch administration could be approximated by the first-order absorption model including a lag time process and the plasma levels found were consistent with this model.

摘要

开发了一种新的实验方法,即利用金黄地鼠颊囊在体内研究角质化口腔黏膜的吸收过程,并阐明了口腔黏膜吸收的一些特性。在所检测的18种芳香族化合物中,观察到吸收速率与亲脂性之间呈正相关。可电离化合物以离子形式存在时吸收较差。这些结果表明,角质化金黄地鼠颊囊的吸收是由于被动扩散机制,并且符合pH分配假说。颊囊内给药后水杨酸的全身转运可以用包含滞后时间过程的一级吸收模型来近似,并且所测得的血浆水平与该模型一致。

相似文献

1
Studies on drug absorption from oral cavity: physicochemical factors affecting absorption from hamster cheek pouch.口腔药物吸收研究:影响仓鼠颊囊吸收的物理化学因素。
J Pharmacobiodyn. 1986 Mar;9(3):287-96. doi: 10.1248/bpb1978.9.287.
2
Carrier-mediated absorption of salicylic acid from hamster cheek pouch mucosa.载体介导的水杨酸从仓鼠颊囊黏膜的吸收。
J Pharm Sci. 1999 Jan;88(1):142-6. doi: 10.1021/js970412e.
3
Studies on drug absorption from oral cavity. II. Influence of the unstirred water layer on absorption from hamster cheek pouch in vitro and in vivo.口腔药物吸收的研究。II. 体外和体内未搅动水层对仓鼠颊囊吸收的影响。
J Pharmacobiodyn. 1987 Apr;10(4):180-7. doi: 10.1248/bpb1978.10.180.
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Absorption of salicylic acid through the oral mucous membrane of hamster cheek pouch.水杨酸通过仓鼠颊囊口腔黏膜的吸收。
Chem Pharm Bull (Tokyo). 1980;28(4):1056-61. doi: 10.1248/cpb.28.1056.
5
Fluoride absorption through the hamster cheek pouch: a pH-dependent event.通过仓鼠颊囊吸收氟化物:一个依赖于pH值的过程。
J Appl Toxicol. 1982 Dec;2(6):303-6. doi: 10.1002/jat.2550020608.
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Regional variation in oral mucosal drug absorption: permeability and degree of keratinization in hamster oral cavity.口腔黏膜药物吸收的区域差异:仓鼠口腔的通透性和角化程度
Pharm Res. 1991 Oct;8(10):1297-301. doi: 10.1023/a:1015812114843.
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Application of propranolol to the keratinized oral mucosa: avoidance of first-pass elimination and the use of 1-dodecylazacycloheptan-2-one (Azone) as an absorption enhancer of bioadhesive film-dosage form.普萘洛尔在角化口腔黏膜的应用:避免首过消除及使用1-十二烷基氮杂环庚烷-2-酮(氮酮)作为生物黏附膜剂型的吸收促进剂。
J Pharmacobiodyn. 1988 Dec;11(12):824-32. doi: 10.1248/bpb1978.11.824.
8
Rate constants of absorption versus physico-chemical parameters.吸收速率常数与物理化学参数的关系
Int J Clin Pharmacol Biopharm. 1978 Sep;16(9):413-6.
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A membrane model of the human oral mucosa as derived from buccal absorption performance and physicochemical properties of the beta-blocking drugs atenolol and propranolol.
J Pharm Pharmacol. 1978 Mar;30(3):137-47. doi: 10.1111/j.2042-7158.1978.tb13185.x.
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Buccal drug absorption. II: In vitro diffusion across the hamster cheek pouch.颊部药物吸收。II:体外透过仓鼠颊囊的扩散。
J Pharm Sci. 1989 Feb;78(2):160-4. doi: 10.1002/jps.2600780218.

引用本文的文献

1
Perfusion cells for studying regional variation in oral-mucosal permeability in humans. I: Kinetic aspects in oral-mucosal absorption of alkylparabens.
Pharm Res. 1997 Sep;14(9):1241-5. doi: 10.1023/a:1012171227272.
2
Carrier-mediated transport of monocarboxylic acids in primary cultured epithelial cells from rabbit oral mucosa.载体介导的一元羧酸在兔口腔黏膜原代培养上皮细胞中的转运。
Pharm Res. 1997 Mar;14(3):320-4. doi: 10.1023/a:1012046021028.
3
The use of cultured epithelial and endothelial cells for drug transport and metabolism studies.利用培养的上皮细胞和内皮细胞进行药物转运和代谢研究。
Pharm Res. 1990 May;7(5):435-51. doi: 10.1023/a:1015800312910.
4
Regional variation in oral mucosal drug absorption: permeability and degree of keratinization in hamster oral cavity.口腔黏膜药物吸收的区域差异:仓鼠口腔的通透性和角化程度
Pharm Res. 1991 Oct;8(10):1297-301. doi: 10.1023/a:1015812114843.