Cited by 28Pharmacogenetics and Drug MetabolismPharmaceutical studies and practicesAnimal testing and alternatives

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Correlation of Unbound Plasma Clearances of Fifteen Extensively Metabolized Drugs Between Humans and Rats

Chiou, Win L., Hsu, Fung-Hwa·1988·Pharmaceutical Research

DOI 10.1023/a:1015935206569

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Abstract

Unbound plasma clearances (CLu) in humans and rats of 15 extensively metabolized drugs (phenytoin, hexobarbital, pentobarbital, phenylbutazone, warfarin, tolbutamide, valproate, phenobarbital, amobarbital, quinidine, chlorpromazine, propranolol, pentazocin, antipyrine, and diazepam), studied earlier by Sawada et al. (J. Pharmacokin, Biopharm. 13:477-491, 1985), were calculated. It was found that the ratio of CLu per square meter of body surface area between human and rat ranged from 0.38 for pentobarbital to 2.34 for tolbutamide, with a mean ratio of 1.07. When body weight (BW) was used for correlation, the mean CLu was proportional to BW 0.657 +/- 0.0935. A rationale for the above empirical findings is postulated. The present study seems to indicate the existence of a general similarity or predictability in the CLu of drugs between rats and humans. Low correlations were generally obtained when total (bound and unbound) plasma clearances were used for comparison.

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Authors: Chiou, W. L., & Hsu, F.-H.
Affiliations: University of Illinois Chicago (US)
ORCID: Chiou, Win L.
Venue: Pharmaceutical Research
Publisher: Springer Science and Business Media LLC
Published: 1988-10
Volume: 5
Issue: 10
Pages: 668-672
ISSN: 0724-8741 (ISSN-L)
1573-904X
DOI: 10.1023/a:1015935206569
OpenAlex: W39205234
Cited by: 28
References: 35
Citations by year: 2024: 1 · 2023: 1 · 2022: 1 · 2019: 1 · 2018: 1 · 2017: 1
FWCI: 0.81
Type: journal article
Language: en
Open access: closed
Licence: www.springernature.com/gp/researchers/text-and-data-mining (tdm)
www.springernature.com/gp/researchers/text-and-data-mining (vor)
Locations: Pharmaceutical Research (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Health Sciences › Medicine › Pediatrics, Perinatology and Child Health › Pharmaceutical studies and practices
Health Sciences › Veterinary › Small Animals › Animal testing and alternatives
Keywords: human-rat comparison, body surface area, body weight, drug metabolism, phenytoin, barbiturates, antiepileptic drugs, antipsychotic drugs, antihypertensive drugs, antipyrine, diazepam, warfarin, quinidine, chlorpromazine, propranolol, tolbutamide, valproic acid
MeSH terms: Animals, Body Surface Area, Pharmaceutical Preparations, Humans, Liver, Male, Species Specificity, Rats

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Correlation of Unbound Plasma Clearances of Fifteen Extensively Metabolized Drugs Between Humans and Rats

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