Abstract：
PURPOSE:Although flomoxef (FMOX) has attracted substantial attention as an antibiotic against extended-spectrum beta-lactamase-producing Escherichia coli (ESBL-producing E. coli), the pharmacokinetics/pharmacodynamics (PK/PD) characteristics of FMOX against ESBL-producing E. coli is unclear. The aim of this study was to determine the PK/PD index of FMOX against ESBL-producing E. coli. METHODS:In vitro time-kill curve studies and in vivo PK/PD experiments were carried out. RESULTS:Time-kill curves exhibited a unique bactericidal activity: time-dependent activity at low concentrations and concentration-dependent activity at high concentrations. In neutropenic murine thigh infection experiments, the antibacterial activity of FMOX correlated with the time that the free drug concentration remaining above the minimum inhibitory concentration (MIC) (fT>MIC) and the ratio of the area under the free drug concentration-time curve for a 24 h period to the MIC (fAUC24/MIC). However, the burden of ESBL producing E. coli significantly reduced when the time intervals for administration were shorter among three dosage regimens with same magnitude of fAUC24/MIC, indicating that fT>MIC is significant PK/PD index. The target value of fT>MIC for 1 log10 kill reduction was 35.1%. CONCLUSIONS:fT>MIC is the most significant PK/PD index of FMOX against ESBL-producing E. coli and its target value is ≥ 40%.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Tashiro S,Hayashi M,Takemura W,Igarashi Y,Liu X,Mizukami Y,Kojima N,Enoki Y,Taguchi K,Yokoyama Y,Nakamura T,Matsumoto Kdoi
10.1007/s11095-020-02977-8subject
Has Abstractpub_date
2021-01-06 00:00:00eissn
0724-8741issn
1573-904Xpii
10.1007/s11095-020-02977-8pub_type
杂志文章abstract：:The pharmacokinetics of and biologic response modification by recombinant human interferon-beta ser (rIFN-beta ser) were evaluated in 12 healthy male volunteers. Subjects received a single intravenous (iv) injection of 90 x 10(6) IU of rIFN-beta ser followed by a single or eight consecutive daily 90 x 10(6) IU subcuta...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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abstract：PURPOSE:The specific interactions between three lectin-latex conjugates and different structures of rat intestinal mucosa have been studied ex vivo. METHODS:These systems were prepared by covalent coupling of different ligands, i.e., tomato lectin (TL), asparagus pea lectin (AL), mycoplasma gallisepticum lectin (ML), ...
journal_title：Pharmaceutical research
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abstract：PURPOSE:This work describes the synthesis of block co-polymeric micelles, methoxy-poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA) to encapsulate Curcumin (CUR), thereby improving the dispersibility and chemical stability of curcumin, prolonging its cellular uptake and enhancing its bioavailability. METHODS:CUR-mPEG...
journal_title：Pharmaceutical research
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abstract：:One of the authors has his name incorrectly indexed in PubMed and SpringerLink as "Laird Forrest M" (last name "Laird Forrest"). His name should index as "Forrest M. Laird" with last name as "Forrest". ...
journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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更新日期：2003-01-01 00:00:00
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更新日期：2006-10-01 00:00:00
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更新日期：2008-06-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2015-06-01 00:00:00
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更新日期：2012-04-01 00:00:00
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更新日期：2018-02-05 00:00:00
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更新日期：2006-04-01 00:00:00
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更新日期：2017-11-01 00:00:00
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更新日期：2020-01-06 00:00:00
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更新日期：2008-07-01 00:00:00
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journal_title：Pharmaceutical research
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更新日期：2008-09-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2007-06-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1996-05-01 00:00:00
abstract：PURPOSE:To characterize the pharmacokinetics of simvastatin (SV) and simvastatin acid (SVA), a lactone-acid pair known to undergo reversible metabolism, and to better understand mechanisms underlying pharmacokinetic interactions observed between SV and gemfibrozil. METHODS:Pharmacokinetic studies were conducted after ...
journal_title：Pharmaceutical research
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更新日期：2005-07-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1994-02-01 00:00:00
abstract：:To evaluate the effects of a neutron activation radiolabeling technique on an enteric-coated multiparticulate formulation of erythromycin, test quantities were produced under industrial pilot scale conditions. The pellets contained the stable isotope erbium oxide (Er-170), which was later converted by neutron activati...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015826229323
更新日期：1990-03-01 00:00:00
abstract：:Published permeability coefficient (Kp) data for the transport of a large group of compounds through mammalian epidermis were analyzed by a simple model based upon permeant size [molecular volume (MV) or molecular weight (MW)] and octanol/water partition coefficient (Koct). The analysis presented is a facile means to ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015810312465
更新日期：1992-05-01 00:00:00
