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Objective@#To study the efficacy and safety of Cefpodoxime proxetil granules in the treatment of acute bronchitis in children.@*Methods@#One hundred and sixty children of the First People′s Hospital of Nanning from June to December 2018 with acute bronchitis were randomly divided into cefpodoxime group and cefaclor group, with 80 cases in each group.All patients received routine treatment.On this basis, 80 patients in the cefpodoxime group received oral Cefpodoxime proxetil granules 5 mg/kg (not more than 100 mg/time), twice a day; 80 patients in the cefaclor group received oral Cefaclor.The granules were 10 mg/kg (not more than 250 mg/time), 3 times a day, and the course of treatment was 5 days.The clinical efficacy and adverse reactions were observed.@*Results@#The cure rate and effective rate of Cefpodoxime group were 91.3% (73/80 cases) and 95.0% (76/80 cases), respectively, while the cure rate and effective rate of Cefaclor group were 66.3%(53/80 cases) and 81.3%(65/80 cases), respectively, and the differences between the 2 groups were statistically significant (χ2=14.94, 7.23, all P<0.05). Sixty-three strains of pathogenic bacteria and 66 strains of pathogenic bacteria were obtained in Cefpodoxine group and Cefaclor group, respectively, and the detection rates of bacteria in the 2 groups were 78.75% and 82.50%, respectively.There was no significant diffe-rence in the number of bacterial strains and strains detected in each group (χ2=0.36, P>0.05), but the total bacterial clearance rate in Cefpodoxine group was 88.9%(56/63 cases) while the bacterial Clearance rate in Cefaclor group was 74.2%(49/66 cases), and the difference between the 2 groups was statistically significant (χ2=4.57, P<0.05). In particular, the bacterial clearance rate in Cefpodoxine group to Streptococcus pneumoniae, Staphylococcus aureus and Klebsiella pneumoniae were significantly higher than those in Cefaclor group, while the bacterial Clearance rate of Proteus and Escherichia coli were lower than those in Cefaclor group.The incidence of adverse reactions in Cefpodoxine group and Cefaclor group were 5.0% and 3.8%, respectively, with no significant difference (P>0.05).@*Conclusions@#The clinical effect of Cefpodoxime pro-xetil granules in treating children with acute bronchitis is more significant than that of Cefaclor.It has high safety and no serious side effect.
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Cefpodoxime proxetil(CPDX-PR) is the third generation cephalosporin with high oral efficiency.It has strong anti-gram negative bacteria and-gram positive bacteria effects, with wide tissue distribution, long plasma half-time(T1/2), stable to lactamase, good tolerance, small therapeutic dose, few times of administration, definite cli-nical efficacy and other advantages.It is recommended for application in the treatment guidelines of foreign children with various infectious diseases.It is of great clinical significance to discuss the rational application of CPDX-PR oral preparation under the condition of severe bacterial drug resistance.This article reviews the pharmacological characteristics of CPDX-PR and the research progress in the treatment of common infectious diseases in pediatrics, so as to promote the research on the rational clinical application of CPDX-PR in China.
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Objective To study the efficacy and safety of Cefpodoxime proxetil granules in the treatment of acute bronchitis in children.Methods One hundred and sixty children of the First People's Hospital of Nanning from June to December 2018 with acute bronchitis were randomly divided into cefpodoxime group and cefaclor group,with 80 cases in each group.All patients received routine treatment.On this basis,80 patients in the cefpodoxime group received oral Cefpodoxime proxetil granules 5 mg/kg (not more than 100 mg/time),twice a day;80 patients in the cefaclor group received oral Cefaclor.The granules were 10 mg/kg (not more than 250 mg/time),3 times a day,and the course of treatment was 5 days.The clinical efficacy and adverse reactions were observed.Results The cure rate and effective rate of Cefpodoxime group were 91.3％ (73/80 cases) and 95.0％ (76/80 cases),respectively,while the cure rate and effective rate of Cefaclor group were 66.3 ％ (53/80 cases) and 81.3％ (65/80 cases),respectively,and the differences between the 2 groups were statistically significant (x2 =14.94,7.23,all P ＜ 0.05).Sixty-three strains of pathogenic bacteria and 66 strains of pathogenic bacteria were obtained in Cefpodoxine group and Cefaclor group,respectively,and the detection rates of bacteria in the 2 groups were 78.75％ and 82.50％,respectively.There was no significant difference in the number of bacterial strains and strains detected in each group (x2 =0.36,P ＞ 0.05),but the total bacterial clearance rate in Cefpodoxine group was 88.9％ (56/63 cases) while the bacterial Clearance rate in Cefaclor group was 74.2％ (49/66 cases),and the difference between the 2 groups was statistically significant (x2 =4.57,P ＜ 0.05).In particular,the bacterial clearance rate in Cefpodoxine group to Streptococcus pneumoniae,Staphylococcus aureus and Klebsiella pneumoniae were significantly higher than those in Cefaclor group,while the bacterial Clearance rate of Proteus and Escherichia coli were lower than those in Cefaclor group.The incidence of adverse reactions in Cefpodoxine group and Cefaclor group were 5.0％ and 3.8％,respectively,with no significant difference (P ＞ 0.05).Conclusions The clinical effect of Cefpodoxime pro-xetil granules in treating children with acute bronchitis is more significant than that of Cefaclor.It has high safety and no serious side effect.
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Background: Fixed dose combination of cefpodoximeclavulanic acid and cefpodoxime both are commonly used in the treatment acute bacterial sinusitis. However, comparative clinical studies between the fixed dose combination of cefpodoxime-clavulanic acid versus cefpodoxime alone are not available. Objective: A postmarketing study was conducted to evaluate the efficacy and safety of fixed dose combination of cefpodoxime proxetil plus potassium clavulonate versus cefpodoxime proxetil in treatment of acute bacterial sinusitis. Material and methods: A total of 202 patients were enrolled in an open label, randomized, parallel group, two arms multicentric study. Patients were treated either with fixed dose combination of cefpodoxime 200 mg plus clavulanic acid 125 mg or cefpodoxime 200 mg; both given as one tablet twice daily for ten days. The efficacy was evaluated at baseline, day three, day five and day ten while the safety was assessed at screening and day 10. Statistical analysis: Intention to treat population was used to analyse the safety results while efficacy was evaluated in per protocol population. Chi square test was used to evaluate the efficacy parameters on six point Likert scale, global evaluation of efficacy and safety by investigators and patients. Results: Cure rate was higher in study group (58.43%) compared to control group (46.81%), however, the difference was not significant. No significant difference was seen in
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A simple, rapid and precise reverse phase liquid chromatographic (RP-HPLC) method was developed and subsequently validated for simultaneous estimation of Cefpodoxime proxetil and Ofloxacin in combined fixed dose oral formulation. The analysis was carried out using X-terra C8 (4.6 x 250mm, 5μm, Make: ACE), prepacked column. The separation was carried out using a mobile phase containing a 0.25%v/v triethyl amine buffer of pH 3.5 and acetonitrile (30:70 v/v), was pumped at a flow rate of 1.2 ml/min with UV-detector and PDA detection at 227 nm. Both the drugs were well resolved on the stationary phase and the retention times were around 2.747 minute for Cefpodoxime proxetil and 2.076 minute for Ofloxacin. The method was validated and shown to be linear for Cefpodoxime proxetil and Ofloxacin. The correlation coefficients for Cefpodoxime proxetil and Ofloxacin are 0.998 and 0.999 respectively. The relative standard deviations for five replicate measurements in two sets of each drug in the tablets is always less than 2% and mean % error of active recovery not more than ±1.5%. The method was validated for precision and accuracy. The developed method could be applied for routine analysis of Cefpodoxime proxetil and Ofloxacin in tablet dosage form without any interference of excipients.
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Reversed-phase liquid chromatography coupled with electrospray ionization tandem mass spectrometry (ESI-MS/MS) was used to characterize impurities in cefpodoxime proxetil, an ester-modified prodrug. Based on the mechanisms by which cephalosporins are degraded, stress tests were designed and performed. The bulk material and capsule were eluted through a C18 column with formic acid-methanol-water as the mobile phase. In total, 15 impurities were characterized in commercial samples, including 7 known impurities and 8 new impurities. The structures of these unknown compounds were deduced via comparison with the fragmentation patterns of cefpodoxime proxetil. Data from this systematic study will help improve the safety and quality of cefpodoxime proxetil.
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Objectives: To evaluate the efficacy and safety of Fixed Dose Combination of Cefpodoxime Proxetil and Potassium Clavulanate (Cefchamp) in comparison with Cefuroxime Axetil in patients with Lower Respiratory Tract Infections.Methods:In this open, randomized, and controlled, parallel-group study of 7 days, 57 patients of both gender above 18 years of age with diagnosis of lower respiratory tract infection were randomized to receive Fixed Dose Combination (FDC) of Cefpodoxime Proxetil plus Potassium Clavulanate (Cefchamp), or Cefuroxime Axetil (CA) for a period of 7 days. Efficacy was assessed by symptoms of cough, dyspnoea, wheezing, Rhonchi, and chest pain based on 4-point scale as 0=none,1=mild, 2=moderate, 3=severe. Fever was recorded as the patient’s actual temperature. Safety assessment included adverse events and adverse drug reactions during the study period.Results: Three patients lost to follow up with CA.The improvement in all symptoms except cough was greater with CC as compared to CA group(p, >0.05). Fever improved from 37.18°C at baseline to 37.01 on day 3 with CC, whereas with CA the fever improved from 37.l5 at baseline to 37.05 on day 3 with CA. Fever subsided in all the patients in both treatments by day 5 of study therapy. Clinical cure was seen in 57.14% (16/28) patients on CC, whereas 42.3% patients (11/26) on CA had clinical cure.Conclusions:The fixed dose combination of Cefpodoxime Proxetil 200 mg and Potassium Clavulanate 125mg (Cefchamp) in comparison with Cefuroxime Axetil 500 mg showed improvement in the cure of respiratory tract infections in terms of decreasing the patient’s LRTI symptoms, improving the patient’s general health and with few adverse events and adverse drug reactions. However, further studies of greater sample size and blinded nature are needed to further substantiate this effect.
Subject(s)
Adult , Amoxicillin-Potassium Clavulanate Combination/administration & dosage , Amoxicillin-Potassium Clavulanate Combination/therapeutic use , Ceftizoxime/administration & dosage , Ceftizoxime/administration & dosage , Ceftizoxime/therapeutic use , Cefuroxime/administration & dosage , Cefuroxime/analogs & derivatives , Cefuroxime/therapeutic use , Drug Combinations , Female , Humans , Male , Middle Aged , Respiratory Tract Infections/drug effects , Respiratory Tract Infections/drug therapy , Treatment OutcomeABSTRACT
The present work aims at the development and evaluation of Floating matrix tablets of Cefpodoxime Proxetil were undertaken to prolong gastric residence time. A visible Spectrophotometric method has been employed for the estimation of Cefpodoxime Proxetil at 263 nm and Beer’s law is obeyed in the concentration range of 5-40 μg/ml. Total 7 formulations (B1-B7) were prepared using guargum with carbopol 934P was used in different concentrations. Fourier transform Infrared spectroscopy confirmed the absence of any drug/polymers/excipients interactions. The tablets were prepared by direct compression technique, using polymer such as hydroxy propyl methyl cellulose (HPMC K4M), guargum and carbopol 934P in different combinations with other standard excipients like sodium bicarbonate and lactose. Tablets were evaluated for physical characterization viz. hardness, friability, swelling index, floating capacity, thickness and weight variation. Further tablets were evaluated in-vitro drug release for 12 hr. The effect of polymer concentrations on buoyancy and drug release pattern was also studied. In-vitro drug release mechanism was evaluated by PCP V-3 software. Carbopol 934P had a negative effect on the floating properties also decreased the drug release. A lesser FLT and a prolonged floating duration could be achieved by varying the amount of effervescent and using different polymer concentrations. The entire matrix tablets showed significantly greater swelling index, exhibited controlled and prolonged drug release profiles and some floated over the dissolution medium for more than12 hr. The paddle speed affected the floating lag time and floating duration it had a negative effect on the floating properties. The optimized formulation followed the higuchi release model and showed non-fickian diffusion mechanism. It also showed no significant change in physical appearance, drug content, floatability or in-vitro dissolution pattern after storage at 45 oC at 75 % RH for three months.
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The present manuscript describe simple, sensitive, rapid, accurate, precise and economical Q-absorbance ratio method for the simultaneous determination of cefpodoxime proxetil and ofloxacin in combined tablet dosage form. Absorbance ratio method uses the ratio of absorbances at two selected wavelengths, one which is an isoabsorptive point and other being the λ-max of one of the two components. Cefpodoxime proxetil and ofloxacin show an isoabsorptive point at 273.2 nm in methanol. The second wavelength used is 297 nm, which is the λ-max of ofloxacin in methanol. The linearity was obtained in the concentration range of 2-14 μg/ml for both cefpodoxime proxetil and ofloxacin. The concentrations of the drugs were determined by using ratio of absorbances at isoabsorptive point and at the λ-max of ofloxacin. The method was successfully applied to pharmaceutical dosage form because no interference from the tablet excipients was found. The results of analysis have been validated statistically and by recovery studies.
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Background : Cefpodoxime is a semisynthetic third generation cephalosporin analogue with a relatively broader spectrum of antimicrobial activity against gram negative and gram positive organisms. This is attributed to their somewhat increased resistance to degradation by the betalactamase. Cefpodoxime shows good activity against Klebsiella pneumonia, many members of enterobactericeae and almost all strains of Escherichia coli. It is extensively used in human beings against infections caused by susceptible organisms for a prolonged period and even without its judicious indication. Though various researchers have worked on the pharmacokinetic aspects of the drug, its effects on biochemical parameters and spermatozoa activity are scarcely available in literature. Aim : To determine the oral kinetic ( blood and tissue) after single therapeutic dose of cefpodoxime proxetil (20mg/kg oral bid 7 days) in rats of either sex on tissue half life and certain biochemical parameters such as glucose, hemoglobin, protein, ALT, AST and other parameters like tissue residue, sperm count and spermatozoa motility in male rats. Materials and Methods : For kinetic studies,24 Wister rats of either sex, 3 months of age, (180-210 gm) were used.(Group I-IV; n=6) Blood samples collected from each animal of Group IV through heart puncture at 0 hour to serve as predrug control. All the group (I-IV) received cefpodoxime proxetil 20 mg/kg once orally as a single dose. At the end of 1,4,12 and 24 hour post oral administration, GroupI,II,III and IVwere utilized for kinetic studies. Blood samples were collected from each animal and vital organs viz brain, lung, liver, spleen, kidney and heart were dissected out for drug analysis and determination of weight. For biochemical parameters, tissue residue and spermatozoa motility, twelve male rats were randomly divided into Groups A and B (n=6) Group B received cefpodoxime (20mg/kg orally bid 7 days) while Group A served as control. Biochemical parameters [Blood glucose, protein, Aspartate transaminase(AST), Alanine transaminase(ALT)and hemoglobin] were measured at 0 and 7 th day while sperm count (total,live and dead)and mean organ weight (study and control group) and tissue residue of drug were evaluated at the end of treatment. Absorption of cefpodoxime was observed at 2 hour and reached a maximum at 4 hour and persisted in blood till 24 hour. Elimination half life in lung was highest followed by heart, liver, kidney and spleen while t½ k in plasma was very low suggesting more affinity of cefpodoxime for tissues than blood. Results and Conclusion : Blood glucose, protein, AST and ALT activities were not significantly altered but the hemoglobin level and total and live sperm count decreased significantly in the study group compared to the control group. Residual level of cefpodoxime was highest in liver followed by kidney and other study organs. Therefore, the drug should be used in human beings judiciously and further study on human subjects is warranted.
Subject(s)
Animal Experimentation , Animals , Animals, Newborn , Ceftizoxime/analogs & derivatives , Ceftizoxime/pharmacokinetics , Pharmacokinetics , Rats, Wistar , Sperm Motility/drug effects , Tissue Distribution/drug effectsABSTRACT
OBJECTIVE:To modify the HPLC method for determining the contents of cefpodoxime proxetil and cefpodoxime proxetil capsules or suspension,and to compare it with the method of UV determination.METHODS:Column:ODS-C18,mobile phase:methanol-water(50∶50),flow rate :1.5mL?min-1,column temperature:40℃,detection wavelength:235nm.RESULTS:The standard curve was rectilinear when cefpodoxime proxetil was within the range of 25～150?g?mL-1(r=0.999 9).The average recovery rate was 98.56%(RSD=1.79%)and the average content of the samples was 101.54%.CONCLUSIONS:The method is simple,rapid,accurate and sensitive for determination of cefpodoxime proxetil and cefpodoxime proxetil capsules or suspension.
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BACKGROUND: Escherichia coli and Klebsiella pneumoniae resistant to 3rd generation cephalosporin have been reported with increasing frequency in tertiary-care hospital in Korea. MicroScan Neg Combo Panel Type 21 (Type 21) contains a 1 microgram/mL cepfodoxime (POD) in addition to other screen wells containing ceftazidime, cefotaxime, ceftriaxone, and aztreonam, which are designed for detecting extended-spectrum beta-lactamase (ESBL)-producing E. coli and Klebsiella species. We evaluated the Type 21 panel for its ability to detect ESBL. METHODS: From November to December in 1998, 496 E. coli and 326 K. pneumoniae strains isolated from clinical specimens were tested with Type 21 panel The isolates flagged as ESBL producers by the panel were confirmed by the double disk synergy test (DDS). To evaluate the specificity of POD, n-lactamases of 54 E, coli and 20 K. pneumoniae strains that were flagged by, POD only from January to May 1999 were analyzed by isoelectric focusing(IEF). RESULTS: 75/496(15%) E. coli and 68/326(21%) K. pneumoniae were flagged as ESBL producers by Type 21 panel. Of those, 94 isolates including 38/75 (51%) of E. coli and 56/68 (82%) of K. pneumoniae were positive for DDS. Among the 94 ESBL producers, all were detected by POD, 84% by cefotaxime, 85% by ceftazidime, 84% by ceftriaxone, and 86% by aztreonam. The 74 strains that were flagged as ESBL producers by POD screen well only were mostly DDS-negative, cefoxitin- resistant and showed beta-lactamases with pls of 5.4 and 7.6 or no band, which could be interpreted as the presence of TEM-1 or SHV-1 type beta-lactamases and/or basal AmpC beta-lactamases, not ESBL. CONCLUSION: MicroScan Neg Combo Panel Type 21 was able to detect a greater number of ESBL producers by inclusion of POD in its screening well. However, the specificity of POD was compromised by flagging a significant number of DDS negative strains. We conclude that the isolates with reduced susceptibility to 3rd generation cephalosporins as well as POD can be reported as ESBL-producers and those resistant to POD only should be confirmed by DDS.
Subject(s)
Aztreonam , beta-Lactamases , Cefotaxime , Ceftazidime , Ceftriaxone , Cephalosporins , Escherichia coli , Klebsiella , Klebsiella pneumoniae , Korea , Mass Screening , Pneumonia , Sensitivity and SpecificityABSTRACT
BACKGROUND: The prevalence of extended-spectrum -lactamase (ESBL)-producing Klebsiella pneumoniae and Escherichia coli has been increased in Korea, but the testing and reporting ESBL-mediated resistance remains unclear. We undertook a study to evaluate the method to screen isolates of ESBL-producing K. pneumoniae and E. coli using cefpodoxime disk. METHODS: Fifty-eight strains of K. pneumoniae and 28 strains of E. coli were tested for production of ESBLs by the double disk synergy test. Susceptibility to cefpodoxime, ceftazidime, cefotaxime, and aztreonam was determined by disk diffusion method. RESULTS: All strains that produced ESBLs were resistant to cefpodoxime, whereas those that not produced ESBLs were susceptible (97%) to this agents. The disk diffusion test exhibited 100% sensitivity and 97% specificity when NCCLS conventional interpretive criteria were used. All other oxyimino- -lactam agents tested were inferior discriminators between the two groups of organisms. When NCCLS ESBL interpretive criteria were used, the disk diffusion test using cefpodoxime exhibited 100% sensitivity and 83% specificity. CONCLUSIONS: Routine disk diffusion susceptibility test with cefpodoxime disk (10g) can be used to detect strains of ESBL-producing K. pneumoniae and E. coli without include supplemental testing for ESBL production.
Subject(s)
Aztreonam , Cefotaxime , Ceftazidime , Diffusion , Escherichia coli , Escherichia , Klebsiella pneumoniae , Klebsiella , Korea , Pneumonia , Prevalence , Sensitivity and SpecificityABSTRACT
0.05). The total cost of two drugs were 163.85 yuan and 104.04 yuan respectively,showing significant difference (P