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The connection Between Plasma Protein Binding and Acute Toxicity as Determined by the LD50 Value
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
2016 (English)In: Drug development research (Print), ISSN 0272-4391, E-ISSN 1098-2299, Vol. 77, no 1, 3-11 p.Article in journal (Refereed) Published
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Abstract [en]

A dataset of three drug classes (acids, bases, and neutrals) with LD50 values in mice was analysed to investigate a possible connection between high plasma protein binding and acute toxicity. Initially, it was found that high plasma protein binding was associated with toxicity for acids and neutrals, but after compensating for differences in lipophilicity, plasma protein binding was found not to be associated with toxicity. The therapeutic index established by the quotient between mouse LD50 and the defined daily dose was unaffected by both lipophilicity and plasma protein binding.

Place, publisher, year, edition, pages
2016. Vol. 77, no 1, 3-11 p.
Keyword [en]
acute toxicity, distribution, free fraction
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-281838DOI: 10.1002/ddr.21286ISI: 000370734000001PubMedID: 26686875OAI: oai:DiVA.org:uu-281838DiVA: diva2:917299
Available from: 2016-04-06 Created: 2016-03-30 Last updated: 2017-11-30Bibliographically approved

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