Source:http://linkedlifedata.com/resource/pubmed/id/17869034
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1-2
|
pubmed:dateCreated |
2007-12-31
|
pubmed:abstractText |
The absorption enhancing effects of various combinations of a mucolytic agent and a non-ionic surfactant on the intestinal absorption of poorly absorbed hydrophilic compounds were examined. Fluorescein isothiocyanate-labeled dextran with an average molecular weight of ca. 4.4 kDa (FD-4) was used as a model compound. Cysteine derivatives such as N-acetylcysteine (NAC), S-carboxymethylcysteine (SCMC), S-ethylcysteine (SEC), and S-methylcysteine (SMC) were selected as mucolytic agents. A homogeneous series of single chain polyoxyethylene alkyl ethers were employed as non-ionic surfactants. Various dosing solutions were administered into rat jejunum, and the bioavailability of FD-4 was determined. Unlike NAC, the agents such as SCMC, SEC, and SMC, which do not possess a free thiol group, did not show any apparent enhancement of intestinal FD-4 absorption, when they were co-administered with p-t-octyl phenol polyoxyethylene-9.5 (Triton X-100, TX-100). In addition, the absorption enhancement was dependent on the kinds of polyoxyethylene alkyl ethers used, when used in combination with NAC. For a constant alkyl chain of 12 with a varying polyoxyethylene (POE) chain length, the surfactant with a short to medium POE chain length such as lauryl poly (4.2) oxyethylene ether (BL-4.2) and lauryl poly (9) oxyethylene ether (BL-9) were effective. In addition, for a constant alkyl chain of 18 with a varying POE chain length, the surfactants with a longer POE chain length such as oleyl poly (15) oxyethylene ether (BO-15) and stearyl poly (20) oxyethylene ether (BS-20) showed the effective enhancement. All these results suggest that a mucolytic agent not possessing a free thiol group is not effective for enhancing the intestinal absorption of poorly absorbed hydrophilic compounds. Also, they indicate that the combination of a mucolytic agent possessing a free thiol group and a non-ionic surfactant either with a short to medium POE chain length and a medium alkyl chain length, or with a longer POE chain length and a longer alkyl chain length shows the effective enhancement. This fundamental information might be useful for finding the optimal combination.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Acetylcysteine,
http://linkedlifedata.com/resource/pubmed/chemical/Dextrans,
http://linkedlifedata.com/resource/pubmed/chemical/Expectorants,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorescein-5-isothiocyanate,
http://linkedlifedata.com/resource/pubmed/chemical/Pharmaceutical Preparations,
http://linkedlifedata.com/resource/pubmed/chemical/Surface-Active Agents,
http://linkedlifedata.com/resource/pubmed/chemical/fluorescein isothiocyanate dextran
|
pubmed:status |
MEDLINE
|
pubmed:month |
Feb
|
pubmed:issn |
0378-5173
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
12
|
pubmed:volume |
349
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
94-100
|
pubmed:dateRevised |
2008-11-21
|
pubmed:meshHeading |
pubmed-meshheading:17869034-Acetylcysteine,
pubmed-meshheading:17869034-Animals,
pubmed-meshheading:17869034-Area Under Curve,
pubmed-meshheading:17869034-Chemistry, Physical,
pubmed-meshheading:17869034-Dextrans,
pubmed-meshheading:17869034-Expectorants,
pubmed-meshheading:17869034-Fluorescein-5-isothiocyanate,
pubmed-meshheading:17869034-Intestinal Absorption,
pubmed-meshheading:17869034-Kinetics,
pubmed-meshheading:17869034-Male,
pubmed-meshheading:17869034-Pharmaceutical Preparations,
pubmed-meshheading:17869034-Physicochemical Phenomena,
pubmed-meshheading:17869034-Rats,
pubmed-meshheading:17869034-Rats, Wistar,
pubmed-meshheading:17869034-Structure-Activity Relationship,
pubmed-meshheading:17869034-Surface-Active Agents
|
pubmed:year |
2008
|
pubmed:articleTitle |
Influence of various combinations of mucolytic agent and non-ionic surfactant on intestinal absorption of poorly absorbed hydrophilic compounds.
|
pubmed:affiliation |
Pharmaceutical Technology Department, CMC Research Laboratories, Tanabe Seiyaku Co. Ltd., 3-16-89 Kashima, Yodogawa-ku, Osaka 532-8505, Japan. s-taka@tanabe.co.jp
|
pubmed:publicationType |
Journal Article
|