Population Pharmacokinetics of <i>Cis</i>-, <i>Trans</i>-, and Total Cefprozil in Healthy Male Koreans

Cefprozil, one of cephalosporin antibiotics, has been used extensively in clinics. However, pharmacokinetic (PK) information on cefprozil is still very limited. There have been no reports of population pharmacokinetics (PPKs). A PPK model for cefprozil will be a great advantage for clinical use. Thu...

Full description

Bibliographic Details
Main Authors: Ji-Hun Jang, Seung-Hyun Jeong, Hea-Young Cho, Yong-Bok Lee
Format: Article
Language:English
Published: MDPI AG 2019-10-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/11/10/531
_version_ 1811183928210358272
author Ji-Hun Jang
Seung-Hyun Jeong
Hea-Young Cho
Yong-Bok Lee
author_facet Ji-Hun Jang
Seung-Hyun Jeong
Hea-Young Cho
Yong-Bok Lee
author_sort Ji-Hun Jang
collection DOAJ
description Cefprozil, one of cephalosporin antibiotics, has been used extensively in clinics. However, pharmacokinetic (PK) information on cefprozil is still very limited. There have been no reports of population pharmacokinetics (PPKs). A PPK model for cefprozil will be a great advantage for clinical use. Thus, the aim of this study was to develop a PPK model for cefprozil for healthy male Koreans. Clinical PK and demographic data of healthy Korean males receiving cefprozil at a dose of 1000 mg were analyzed using Phoenix<sup>&#174;</sup> NLME&#8482;. A one-compartment model with first-order absorption with lag-time was constructed as a base model. The model was extended to include covariates that influenced between-subject variability. Creatinine clearance significantly influenced systemic clearance of cefprozil. The final PPK model for <i>cis</i>-, <i>trans</i>-, and total cefprozil was established and validated. PPK parameter values of <i>cis</i>- and total cefprozil were similar to each other, but different from those of <i>trans</i>-isomer. Herein, we describe the establishment of accurate PPK models of <i>cis</i>-, <i>trans</i>-, and total cefprozil for healthy male Koreans for the first time. It may be useful as a dosing algorithm for the general population. These results might also contribute to the development of stereoisomeric cefprozil.
first_indexed 2024-04-11T13:05:03Z
format Article
id doaj.art-6b57e3685f1543619b7f82bea92a19ab
institution Directory Open Access Journal
issn 1999-4923
language English
last_indexed 2024-04-11T13:05:03Z
publishDate 2019-10-01
publisher MDPI AG
record_format Article
series Pharmaceutics
spelling doaj.art-6b57e3685f1543619b7f82bea92a19ab2022-12-22T04:22:48ZengMDPI AGPharmaceutics1999-49232019-10-01111053110.3390/pharmaceutics11100531pharmaceutics11100531Population Pharmacokinetics of <i>Cis</i>-, <i>Trans</i>-, and Total Cefprozil in Healthy Male KoreansJi-Hun Jang0Seung-Hyun Jeong1Hea-Young Cho2Yong-Bok Lee3College of Pharmacy, Chonnam National University, 77 Yongbong-ro, Buk-Gu, Gwangju 61186, KoreaCollege of Pharmacy, Chonnam National University, 77 Yongbong-ro, Buk-Gu, Gwangju 61186, KoreaCollege of Pharmacy, CHA University, 335 Pangyo-ro, Bundang-gu, Seongnam-si, Gyeonggi-Do 13488, KoreaCollege of Pharmacy, Chonnam National University, 77 Yongbong-ro, Buk-Gu, Gwangju 61186, KoreaCefprozil, one of cephalosporin antibiotics, has been used extensively in clinics. However, pharmacokinetic (PK) information on cefprozil is still very limited. There have been no reports of population pharmacokinetics (PPKs). A PPK model for cefprozil will be a great advantage for clinical use. Thus, the aim of this study was to develop a PPK model for cefprozil for healthy male Koreans. Clinical PK and demographic data of healthy Korean males receiving cefprozil at a dose of 1000 mg were analyzed using Phoenix<sup>&#174;</sup> NLME&#8482;. A one-compartment model with first-order absorption with lag-time was constructed as a base model. The model was extended to include covariates that influenced between-subject variability. Creatinine clearance significantly influenced systemic clearance of cefprozil. The final PPK model for <i>cis</i>-, <i>trans</i>-, and total cefprozil was established and validated. PPK parameter values of <i>cis</i>- and total cefprozil were similar to each other, but different from those of <i>trans</i>-isomer. Herein, we describe the establishment of accurate PPK models of <i>cis</i>-, <i>trans</i>-, and total cefprozil for healthy male Koreans for the first time. It may be useful as a dosing algorithm for the general population. These results might also contribute to the development of stereoisomeric cefprozil.https://www.mdpi.com/1999-4923/11/10/531cefprozilpopulation pharmacokineticsmodeling<i>cis</i>- and <i>trans</i>-isomers
spellingShingle Ji-Hun Jang
Seung-Hyun Jeong
Hea-Young Cho
Yong-Bok Lee
Population Pharmacokinetics of <i>Cis</i>-, <i>Trans</i>-, and Total Cefprozil in Healthy Male Koreans
Pharmaceutics
cefprozil
population pharmacokinetics
modeling
<i>cis</i>- and <i>trans</i>-isomers
title Population Pharmacokinetics of <i>Cis</i>-, <i>Trans</i>-, and Total Cefprozil in Healthy Male Koreans
title_full Population Pharmacokinetics of <i>Cis</i>-, <i>Trans</i>-, and Total Cefprozil in Healthy Male Koreans
title_fullStr Population Pharmacokinetics of <i>Cis</i>-, <i>Trans</i>-, and Total Cefprozil in Healthy Male Koreans
title_full_unstemmed Population Pharmacokinetics of <i>Cis</i>-, <i>Trans</i>-, and Total Cefprozil in Healthy Male Koreans
title_short Population Pharmacokinetics of <i>Cis</i>-, <i>Trans</i>-, and Total Cefprozil in Healthy Male Koreans
title_sort population pharmacokinetics of i cis i i trans i and total cefprozil in healthy male koreans
topic cefprozil
population pharmacokinetics
modeling
<i>cis</i>- and <i>trans</i>-isomers
url https://www.mdpi.com/1999-4923/11/10/531
work_keys_str_mv AT jihunjang populationpharmacokineticsoficisiitransiandtotalcefprozilinhealthymalekoreans
AT seunghyunjeong populationpharmacokineticsoficisiitransiandtotalcefprozilinhealthymalekoreans
AT heayoungcho populationpharmacokineticsoficisiitransiandtotalcefprozilinhealthymalekoreans
AT yongboklee populationpharmacokineticsoficisiitransiandtotalcefprozilinhealthymalekoreans