A Review of the Pharmacokinetics of Cefpodoxime Proxetil

Borin, Marie T.

doi:10.2165/00003495-199100423-00005

Cited by 81 publications

(35 citation statements)

References 16 publications

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“…In the biological system, CFP undergoes ester hydrolysis and is converted into CFA to exhibit its antibiotic activity. [1][2] CFP has an asymmetric carbon at position 4 and is supplied as racemic mixture of R-and S-enantiomers. Few methods are reported to quantify CFA.…”

Section: Introductionmentioning

confidence: 99%

Spectrophotometric Investigation of Oxidation of Cefpodoxime Proxetil by Permanganate in Alkaline Medium: A Kinetic Study

Khan¹,

Mohd²,

Bano³

et al. 2009

Journal of the Korean Chemical Society

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ABSTRACT.A Kinetics pathway of oxidation of Cefpodoxime Proxetil by permanganate in alkaline medium at a constant ionic strength has been studied spectrophotometrically. The reaction showed first order kinetics in permanganate ion concentration and an order less than unity in cefpodoxime acid and alkali concentrations. Increasing ionic strength of the medium increase the rate. The oxidation reaction proceeds via an alkali-permanganate species which forms a complex with cefpodoxime acid. The latter decomposes slowly, followed by a fast reaction between a free radical of cefpodoxime acid and another molecule of permanganate to give the products. Investigations of the reaction at different temperatures allowed the determination of activation parameters with respect to the slow step of proposed mechanism and fallows first order kinetics. The proposed mechanism and the derived rate laws are consistent with the observed kinetics.

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Section: Introductionmentioning

confidence: 99%

Spectrophotometric Investigation of Oxidation of Cefpodoxime Proxetil by Permanganate in Alkaline Medium: A Kinetic Study

Khan¹,

Mohd²,

Bano³

et al. 2009

Journal of the Korean Chemical Society

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“…The percentage of human intestinal absorption (% HIA) for selected prodrugs and precursors was obtained from pharmacokinetic data previously reported (18)(19)(20)(21)(22)(23)(24)(25)(26)(27)(28) and well-known databanks (29-31). The classification based on % HIA, previously reported by Zhao et al (24), was used to score the absorption profile of prodrugs and precursors as high, moderate and low (see Table 1).…”

Section: Drugs and Prodrugs Selectionmentioning

confidence: 99%

To Be Drug or Prodrug: Structure-Property Exploratory Approach Regarding Oral Bioavailability

et al. 2014

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-Purpose. Prodrug design is a strategy that can be used to adjust physicochemical properties of drugs in order to overcome pharmacokinetic problems, such as poor oral bioavailability. However, Lipinski´s and Veber´s rules predict whether compounds will have absorption problems even before the design of prodrugs. In this context, our goal was to evaluate the molecular properties which most influenced the absorption process of prodrugs compared to its precursor through exploratory data analysis approach. Methods: A variety of prodrugs and respective precursors were randomly selected and classified by its' percentage of human intestinal absorption. Subsequently, different molecular properties were calculated and hierarchical cluster analysis (HCA) and principal components analysis (PCA) were carried out. Results: According to the findings, antiviral, anti-hypertensive, and antibiotic prodrugs exhibited higher absorption levels than their respective precursors. Also, some relevant descriptors (molecular weight, MW, routable bonds, rot_bonds, hydrogen bond acceptors, HBA_count and polar surface area, PSA), which are included in Lipinski´s and Veber´s rules, influenced the separation process between prodrugs and drugs. Furthermore, other molecular properties, such as polarizability (α) and molar refractivity (MR), were pointed out. Conclusion: Lipinski´s and Veber´s rules proved to be important to design an orally administered drug but other descriptors should be considered by medicinal chemists in the prodrug designing process.

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“…13) CPP is stable in intestinal juice and phosphate buffer under neutral pH conditions, but unstable under high pH conditions.…”

Section: Introductionmentioning

confidence: 98%

“…12) Cefpodoxime proxetil (CPP) is an orally administered prodrug that is de-esteri ed by the intestinal mucosa to release cefpodoxime (CP). [13][14][15] CPP is stable to most common plasmid-mediated beta-lactamases. This antibiotic has a broad antibacterial spectrum with a potent activity against both Gram-positive and Gram-negative bacteria.…”

Section: Introductionmentioning

confidence: 99%

Stability of Ester Prodrugs with Magnesium Oxide Using the Simple Suspension Method

Suryani

Sugiyama

Kurata

et al. 2013

Jpn. J. Pharm. Health Care Sci.

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The simple suspension method is a method of administering drugs via a feeding or gastrostomy tube, and it involves allowing tablets or capsules to be disintegrated and suspended in warm water at 55℃ without crushing. The present study evaluated the stability of two prodrugs suspended alone or in combination with an alkaline agent according to the simple suspension method. The study used two ester-prodrugs, acemetacin (AMT) and cefpodoxime proxetil (CPP), which are hydrolyzed at higher pH. Drug concentrations in the suspension were measured by high-performance liquid chromatography. AMT and CPP were not hydrolyzed when suspended alone, but decomposed under alkaline conditions with the addition of magnesium oxide (MgO). The AMT concentration decreased to 55.5％ and 38.9％ at 30 min and 60 min, respectively, whereas its active metabolite, indomethacin (IMT), increased from 0 to 90.7 µg/mL and 122.7 µg/mL at 30 and 60 min, respectively. The CPP concentrations with MgO were decreased to 47.9, 28.5, 20.8 and 12.7％ at 30, 60, 90, and 120 min, respectively. Therefore, AMT and CPP should not be administered in the simple suspension method in combination with an alkaline drug that increases the suspension pH.

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A Review of the Pharmacokinetics of Cefpodoxime Proxetil

Cited by 81 publications

References 16 publications

Spectrophotometric Investigation of Oxidation of Cefpodoxime Proxetil by Permanganate in Alkaline Medium: A Kinetic Study

Spectrophotometric Investigation of Oxidation of Cefpodoxime Proxetil by Permanganate in Alkaline Medium: A Kinetic Study

To Be Drug or Prodrug: Structure-Property Exploratory Approach Regarding Oral Bioavailability

Stability of Ester Prodrugs with Magnesium Oxide Using the Simple Suspension Method

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