The present study deals with the development of mucoadhesive controlled release tablets of Cefpodoxime Proxetil to increase the gastric residence time and thus prolong drug release, reduce dosing frequency and improve oral bioavailability. Tablets were prepared using sodium alginate and karaya gum, a natural polymer, with a synthetic polymer hydroxypropylmethylcellulose (K100LV) and Karaya gum with HPMC K100LV in various ratios to optimize the drug release profile using D-Optimal technique. Pre- and post-compression parameters of tablets prepared with various formulations (S1-S9, C1-C9) were evaluated. The FTIR and DSC studies revealed that no physiochemical interaction between excipients and drug. The formulation S7 showed prolonged drug release, and the mechanism of drug release from the optimized formulation was confirmed using the Korsmeyer-Peppas model to be non-Fickian release transport and n value was found 0.605 indicating both diffusion and erosion mechanism from these natural gums. The optimized formulation showed mucoadhesive strength >35 g. An in vivo study was performed on rabbits using an X-ray imaging technique. The radiological evidence suggests that the tablets adheres (more than 10 hours) to a rabbit's stomach. No significant changes were found in the physical appearance, drug content, mucoadhesive study and in vitro dissolution pattern after storage at 40 °C/75% relative humidity for 3 months.
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Cefpodoxime, the deesterified part of the orally available cefpodoxime proxetil, is active against most Enterobacteriaceae with MIC50 of 0.06 to 2 mg/l. Only Enterobacter cloacae and Citrobacter freundii strains show MIC50 of 4 mg/l. Coagulase negative staphylococci have a MIC50 of 2, while Staphylococcus aureus strains have a MIC of 4 mg/l. In comparison to other orally available cephalosporins cefpodoxime is slightly less active than cefixime and cefotiam against gram-negative bacteria but more active than cefuroxime, cefaclor, and cephalexin. Against staphylococci the activity of cefpodoxime is comparable to that of cefotiam and cefuroxime and superior to cefaclor and cephalexin, while cefixime does not have sufficient activity against these species. Like all cephalosporins cefpodoxime has no activity against enterococci.
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The comparative pharmacokinetics of the new oral cephalosporins (ester and nonester types), together with that of the first generation carbacephem, loracarbef, are considered in healthy volunteers. Also in this review, pharmacokinetic and microbiological data are combined in order to predict the possible clinical efficacy of this group of agents. Despite apparent similarities in the structure of these agents, single dose studies have revealed marked differences in the pharmacokinetics of the oral cephalosporins. Multiple dose studies showed no evidence of accumulation with these agents. In the elderly, only minor changes in the pharmacokinetics of the oral agents were observed, and were insufficient to warrant dosage adjustment. Unlike that of the nonester compounds, the bioavailability of the ester cephalosporins is increased when they are administered after food. Variable effects are observed when the ester agents are coadministered with antacids or H2-antagonists; while the absorption of cefetamet pivoxil was unaffected by coadministered antacids or H2-antagonists, the absorption of cefpodoxime proxetil was reduced.
To discuss the chemistry, pharmacokinetics, spectrum of activity, clinical trials, adverse effects, drug interactions, and dosage guidelines of cefpodoxime proxetil.
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Cefpodoxime proxetil (CP) is a prodrug with poor oral bioavailability because of its metabolism to Cefpodoxime acid (CA) in luminal contents and intestinal epithelial cells. In the present investigation, regional variability in different segments of the gastrointestinal tract vis-à-vis solubility and metabolism were investigated, and the results indicated potential for a gastro retentive (GR) dosage form. Suitability of a GR dosage from for CP and finally in vivo efficacy were investigated. Thereafter, an effervescent floating GR dosage form was developed for CP and evaluated in rats. The GR dosage form improved the oral bioavailability of CP significantly by about 75%, hence providing a proof-of-concept. The Tmax value increased to 1.43+/-0.24 h from 0.91+/-0.23 h of pure drug, while Cmax values of 4735+/-802 ng/ml and 3094+/-567 ng/ml were obtained for the GR dosage form and pure drug respectively.
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Cefpodoxime proxetil is a new third generation oral cephalosporin, which shows potent antibacterial activity against both Gram-positive and Gram-negative bacteria, and high stability in the presence of beta-lactamases. Low concentrations of cefpodoxime inhibit most respiratory pathogens, including Haemophilus influenzae, Streptococcus pneumoniae, and Moraxella (Branhamella) catarrhalis. Cefpodoxime reaches concentrations of 0.24 +/- 0.06 mg/kg in tonsils, 0.89 +/- 0.80 mg/kg in lung parenchyma, and 0.91 +/- 0.01 mg/kg in bronchial mucosa; these values exceed by far the minimum inhibitory concentrations (MICs) of cefpodoxime for respiratory pathogens. Preliminary clinical studies were carried out in 181 patients with upper respiratory tract infections: the results indicated an overall clinical response in 88.4% of patients; in 30% the clinical efficacy was excellent and in 58.5% it was good. Further studies showed clinical cure in 90.3% of patients with pharyngotonsillitis, and clinical efficacy (cure plus improvement) in 95% of those with acute sinusitis. Moreover, bacterial eradication was obtained in 78 to 96.7% of cases, most of which involved H. influenzae, streptococci, or M. catarrhalis. Cefpodoxime appears to be an effective new antibacterial that can be recommended as a drug of first choice in the treatment of most upper respiratory tract infections.
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Electrochemical reduction behavior of cephalosporins, Cefixime (CF) and Cefpodoxime Proxetil (CP) have been studied by using different voltammetric techniques in Britton-Robinson buffer system. Two well defined cathodic waves are observed for both the compounds in the entire pH range. Number of electrons transferred in the reduction process was calculated and the reduction mechanism is proposed. The results indicate that the process of both the compounds is irreversible and diffusion-controlled. The peak currents for CF and CP are found to be linear over the range of concentration 6.0 x 10(-8) to 1.2 x 10(-5) mol l(-1) and 8.8 x 10(-8) to 1.1 x 10(-5) mol l(-1), respectively. The lower detection limits are found to be 4.6 x 10(-8) and 8.52 x 10(-8) mol l(-1) for the two compounds. A differential pulse voltammetric method has been developed for the determination of these drugs in pharmaceutical formulations and urine samples.
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Although fluoroquinolones remain the most reliable urinary antimicrobial, resistance rates have increased and effective fluoroquinolone-sparing antimicrobials are needed.
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Pathogenic bacteria were isolated from 90% of patients with acute otitis media. This higher-than-expected rate of positive cultures was probably related to the meticulous bacteriologic techniques used.
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Penicillin (PC) resistance of Streptococcus pneumoniae was tested by oxacillin disk method (Bauer-Kirby method) of the strains collected at the primary pediatric office. The rate of oxacillin resistance of S. pneumoniae was 36.4% in 1990, 41.4% in 1991, and 51.9% in 1992, respectively. The efficacy of oral antibiotics in the treatment of PC-insensitive S. pneumoniae infections was also studied retrospectively in 234 cases. Treatment failure rate was 17.7% in the amoxicillin group, 8.7% in the cefpodoxime proxetil group, while it was 42.9% in the cefixime group. These differences were statistically significant. From these data prevalence of PC-insensitive S. pneumoniae is very high in Japanese children, and amoxicillin and cefpodoxime proxetil can be used for the treatment of outpatients with PC-insensitive S. pneumoniae infections.