Differences in the promotion mechanism of the colonic absorption of antipyrine, phenol red and cefmetazole

Author:

SHIGA MASAHARU1,HAYASHI MASAHIRO1,HORIE TOSHIHARU1,AWAZU SHOJI1

Affiliation:

1. Department of Biopharmaceutics, Tokyo College of Pharmacy, 1432–1 Horinouchi, Hachioji, Tokyo 192–03, Japan

Abstract

Abstract The promotion of antipyrine, phenol red and cefmetazole absorption by sodium ethylenediaminetetraacetate (EDTA-Na) as a paracellular promoter, diethyl maleate (DEM) as a transcellular promoter, and sodium taurocholate (TC-Na), whose promotion mechanism is still unclear, has been investigated by the rat in-situ colonic loop technique. All these promoters increased AP absorption and water influx from the lumen to the blood. Ouabain treatment suppressed the increase in antipyrine absorption and water influx induced by TC-Na and EDTA-Na, but did not modify the enhancing effect of DEM. Thus, the promotion mechanism of TC-Na may be similar to that of EDTA-Na. Phenol red and cefmetazole absorption were increased by TC-Na and EDTA-Na but not by DEM. Accordingly, phenol red and cefmetazole absorption appears to be promoted via paracellular but not transcellular routes. The collection of blood for plasma samples reduced the influx of water which had been increased by TC-Na or EDTA-Na. Consequently, the enhancement in antipyrine plasma concentration by these promoters was reduced to the control level. The inhibitory mechanism for this is discussed on the basis of the blood-flow limitation of antipyrine and water absorption.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Cited by 16 articles. 订阅此论文施引文献 订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献

1. REVIEW ON ADVANCES IN COLON TARGETED DRUG DELIVERY SYSTEM;International journal of pharmaceutical sciences and research;2012-09-01

2. Synthesis and microbial degradation of azopolymers for possible applications for colon specific drug delivery I;Journal of Saudi Chemical Society;2011-10

3. Natural polysaccharides as targeting tools of drugs to the human colon;Drug Development Research;2000

4. Intranasal insulin delivery and therapy1Abbreviations: α-CD, α-cyclodextrin; β-CD, β-cyclodextrin; γ-CD, γ-cyclodextrin; AUC, area under the plasma/serum concentration versus time curve; Cmax, maximum or peak plasma/serum concentration; Cmin, minimum plasma/serum concentration; DDPC, didecanoyl-L-α-phosphatidylcholine; DM-β-CD, dimethyl-β-cyclodextrin; EDTA, ethylenediaminetetraacetic acid; FITC, fluorescein isothiocyanate; HLB, hydrophile–lipophile balance; hGH, human growth hormone; HP-β-CD, hydroxy-propyl-β-cyclodextrin; HPC, hydroxypropylcellulose; HSA, human serum albumin; Hyaff 11, hyaluronic acid ester; IDDM, insulin-dependent diabetes mellitus; Ig, immunoglobulin; Laureth-9, polyoxyethylene-9-lauryl ether; LPC, lysophosphatidylcholine; LPG, lysophosphatidylglycerol; MCC, microcrystalline cellulose; MTR, mucociliary transport rate; NIDDM, non-insulin-dependent diabetes mellitus; PC, phosphatidylcholine; RAMEB, randomly methylated β-cyclodextrin; SDC, sodium deoxycholate; SGC, sodium glycocholate; STDHF, sodium taurodihydrofusidate; 99mTc, 99mtechnetium; TER, transepithelial resistance.1;Advanced Drug Delivery Reviews;1999-02

5. Effects of Enzyme Inhibitors and Insulin Concentration on Transepithelial Transport of Insulin in Rats;Journal of Pharmacy and Pharmacology;1996-10

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