1998
DOI: 10.1128/aac.42.10.2602
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Stability of Cephalosporin Prodrug Esters in Human Intestinal Juice: Implications for Oral Bioavailability

Abstract: The levels of degradation of cefetamet pivoxil (CAT), cefuroxime axetil (CAE), and cefpodoxime proxetil (CPD) in 0.6 M phosphate buffer (pH 7.4) and human intestinal juice (pH 7.4) at 37°C over 24 h were compared. Significant differences in the time courses of degradation and in the patterns of degradation products were observed. (i) The relative proportions of the Δ2- and Δ3-cephalosporins were roughly reversed in the two incubation media. In phosphate buffer, the major degradation product was the Δ2-cephalos… Show more

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Cited by 39 publications
(22 citation statements)
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“…Such a difference in solubility behavior explains separation of Rand S-isomers on an achiral column and the more soluble Sisomer is eluted first during analysis. This is in line with previous reports where in a reverse phase C18 and C8 achiral columns without the use of any chiral column or chiral selector or chi- ral derivitization process, have been utilized for analysis of CP [8][9][10][11].…”
Section: Resultssupporting
confidence: 81%
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“…Such a difference in solubility behavior explains separation of Rand S-isomers on an achiral column and the more soluble Sisomer is eluted first during analysis. This is in line with previous reports where in a reverse phase C18 and C8 achiral columns without the use of any chiral column or chiral selector or chi- ral derivitization process, have been utilized for analysis of CP [8][9][10][11].…”
Section: Resultssupporting
confidence: 81%
“…CP has an asymmetric carbon at position 4 and is supplied as a racemic mixture of two enantiomers R and S forms. Few methods are reported to quantify CA [4][5][6][7], but analytical methods describing detection of CP are scarce only as a small part in few publications [8][9][10][11]. In the present study, a sensitive reversed-phase high performance liquid chromatographic (RP-HPLC) method was developed and validated, which can analyze both R and S isomers of CP in the samples obtained from rat in situ absorption studies.…”
Section: Introductionmentioning
confidence: 98%
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“…Being ubiquitously present in the enterocytes, they pose an important limitation in the absorption of drugs carrying an ester bond [1]. In addition to intracellular hydrolysis, several studies report on the instability of ester prodrugs in human intestinal fluids [2][3][4][5]. In view of the labile nature of ester prodrugs, assessment of stability in intestinal fluids is crucial.…”
Section: Introductionmentioning
confidence: 99%
“…Nevertheless, despite the been shown to inhibit P-gp functionality (Ingels et al, 2004). In 1186 addition, for some ester prodrugs, poor stability has been reported 1187 in aspirated human intestinal fluids, which may compromise the 1188 usefulness of the prodrug approach (Borde et al, 2012;Brouwers 1189Brouwers et al, 2007Granero and Amidon, 2006;Stoeckel et al, 1998). 1190 Therefore, in order to address the complexity of the intra- In addition to using biorelevant fluids, it is often suitable to use 1207 perfusion media with varying pH values.…”
mentioning
confidence: 97%