| Relationship between lipophilicity and absorption from the liver surface of paraben derivatives and antipyrine in rats. | |
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MedLine Citation:
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PMID: 21492176 Owner: NLM Status: In-Data-Review |
Abstract/OtherAbstract:
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Objectives The importance of drug lipophilicity on absorption from the liver surface was examined in rats using paraben derivatives, antipyrine, Sudan III, and Sudan blue. Methods The log partition coefficient (PC) of n-octanol/water ranged from -1.39 to 4.62. The compounds were applied to the rat liver surface using a cylindrical diffusion cell (i.d. 9 mm). Key findings The rate of absorption at 15 min was calculated to be 13.9% for paraben, much lower than that for its derivatives methylparaben, propylparaben and butylparaben (∼80%). The obtained first-order absorption rate constant (k(a) ) of paraben, methylparaben, propylparaben and antipyrine increased according to lipophilicity. Further lipophilicity resulted in a fall in k(a) , implying the importance of affinity for lipids and water in absorption from the liver surface. Thus, a compound with a log PC of around 2.5 is considered to have maximum absorbability from the rat liver surface. A good relationship (r(2) = 0.97) was recognized between the log k(a) and log reciprocal value with the square root of molecular weight of the compounds with a log PC below 2.5. Conclusions The rate of absorption of a drug from the liver surface could be estimated from physicochemical properties such as lipophilicity and molecular weight. |
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Authors:
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Koyo Nishida; Masanori Kobayashi; Hirotaka Miyamoto; Naoki Yoshikawa; Shintaro Fumoto; Hitoshi Sasaki; Junzo Nakamura |
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Publication Detail:
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Type: Journal Article Date: 2011-03-31 |
Journal Detail:
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Title: The Journal of pharmacy and pharmacology Volume: 63 ISSN: 0022-3573 ISO Abbreviation: J. Pharm. Pharmacol. Publication Date: 2011 May |
Date Detail:
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Created Date: 2011-04-15 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0376363 Medline TA: J Pharm Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 736-40 Citation Subset: IM |
Copyright Information:
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© 2011 The Authors. JPP © 2011 Royal Pharmaceutical Society. |
Affiliation:
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Department of Clinical Pharmacy, Graduate School of Biomedical Sciences, Nagasaki University Department of Hospital Pharmacy, Nagasaki University Hospital, Nagasaki, Japan. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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