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AIM: To evaluate the bioequivalence and safety of two cefdinir capsules under a fasting/high-fat fed condition in healthy people. METHODS: Twenty-six healthy volunteers were randomized to cross-test single-dose oral cefdinir capsules or reference preparations for fasting. Thirty-six healthy volunteers were randomized to crossed single-dose oral cefdinir capsule test preparations or reference preparations after high-fat meals. The blood concentration of cefdinir was determined by liquid chromatography-mass spectrometry (LC-MS/MS). Pharmacokinetic parameters and equivalence were calculated and evaluated using WinNonlin 6.4 and SAS 9.4 software. RESULTS: The 90% confidence intervals of the geometric mean ratios of the Cmax, AUC0-t, and AUC0-∞ for the test and reference preparations of cefdinir capsules taken by twenty-five healthy volunteers for fasting were 93.01%-109.22%, 96.16%-110.06%, and 96.38%-110.16%, all at 80.00%-125.00% within the range of bioequivalence. The 90% confidence intervals of the geometric mean ratios of the Cmax, AUC0-t, and AUC0-∞ for the test and reference preparations of cefdinir capsules taken by thirty-six healthy volunteers for a high-fat fed were 93.91%-103.28%, 92.93%-100.72% and 92.97%-101.26%, all at 80.00%-125.00% within the range of bioequivalence. The incidences of adverse reactions in healthy volunteers taking cefdinir capsules for the fasting test and reference preparations were 12.0% and 11.5%, respectively. The incidence of adverse reactions in healthy volunteers taking cefdinir capsules after the meal was 25.0% and 27.8%, respectively. CONCLUSION: The test preparation of cefdinir capsules and the reference preparation are bioequivalent, and the volunteers show good safety and tolerability under the test dose.
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OBJECTIVE:To compare therapeutic efficacy and safety of 3 ornidazole regimens in the treatment of chronic pel-vic inflammatory disease(PID). METHODS:A total of 120 chronic PID patients were randomly divided into ornidazole group(40 cases),combined with levofloxacin group(40 cases)and combined with cefdinir group(40 cases). Based on routine treatment,or-nidazole group was given Ornidazole tablet 0.5 g orally,day and night. Combined with levofloxacin group was additionally given Levofloxacin hydrochloride tablet 0.1 g orally,tid,on the basis of ornidazole group. Combined with cefdinir group was additional-ly given Cefdinir dispersible tablet 0.1 g orally,tid,on the basis of ornidazole group. Treatment course of 3 groups lasted for 10 d. Clinical efficacies of 2 groups were observed,and plasma viscosity (PV),hematocrit,CRP,IL-1,leucocyte count,lympho-cyte count,lymphocyte percentage and the occurrence of ADR were observed before and after treatment. RESULTS:Total response rate was in descending order:combined with cefdinir group(95.00%)>combined with levofloxacin group(82.50%)>ornidazole group(62.50%),with statistical significance(P<0.05). Before treatment,there was no statistical significance in PV,hematocrit, CRP,IL-1,leucocyte count,lymphocyte count or lymphocyte percentage among 3 groups(P>0.05). After treatment,above inel-exes of 3 groups were significantly lower than before;combined with cefdinir group<combined with levofloxacin group<ornida-zole group,there was statistical significance (P<0.05). The incidence of ADR in combined with levofloxacin group was signifi-cantly higher than ornidazole group and combined with cefdinir group,with statistical significance(P<0.05). There was no statis-tical significance between ornidazole group and combined with cefdinir group(P>0.05). CONCLUSIONS:Therapeutic efficacy of ornidazole combined with cefdinir is better than that of ornidazole combined with levofloxacin in the treatment of chronic PID,and its safety is similar to that of ornidazole alone.
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OBJECTIVE:To determine the concentration of cefdinir in rat plasma,and investigate its pharmacokinetics. METH-ODS:High performance capillary electrophoresis (HPCE) was adopted by using fused-silica capillary (75 μm,total length of 30 cm,effective length of 21.5 cm),buffer solution of 20 mmol/L citric acid,injection voltage of 10 kV for 10 s,separation voltage of -20 kV,and detection wavelength of 214 nm. 6 rats were intragastrically received cefdinir solution(20 mg/kg). 0.2 mL blood sample was taken from the tail vein before and 0.25,0.5,1,1.5,2,3,4,6,12,24 h after administration. BAPP 2.0 software was used to calculate the pharmacokinetics parameters. RESULTS:The linear range of cedinir ranged 0.2-50 μg/mL(r=0.9997), lower limit of quantification was 0.2 μg/mL. The intra-day(n=6)and inter-day RSDs of(n=3)precision test were no more than 12.2%;RSD of stability test was no more than 9.10%(n=6);method recovery rate was 95.4%-114.3%(RSD=9.0%,n=6);matrix effect was 63.5%-70.2%(RSD=10.39%,n=6). The t1/2 of cefdinir in rats in vivo was(0.54±0.01)h,MRT was(1.90± 0.14)h,cmax was(32.92±0.81)μg/mL,tmax was(1.50±0.02)h,AUC0-24 h was(46.65±0.44)μg·h/mL and AUC0-∞was(46.83± 0.44)μg·h/mL. CONCLUSIONS:The method is rapid,accurate and simple,and can be used for the determination of cefdinir con-centration in rat plasma and its pharmacokinetics research.
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The present study evaluates the effect of integrated nano-bio hybrid system involving nanoscale zero-valent iron (nFe0) and yeast Candida sp. SMN04 on degradation of cefdinir in aqueous medium. The nanoparticle was chemically synthesised and characterized by atomic force microscopy (AFM), scanning electron microscopy (SEM), EDAX analysis and particle size analyser. Nano-bio hybrid system was prepared using optimal concentration (50 mg/mL) of chemically synthesized nFe0, which were coated on the surface of yeast cells without causing any lethal effects to the cell. The survival and viability of the yeast cells were monitored by AFM and SEM images. Cefdinir (250 mg/L) degradation was studied, in both, the individual and hybrid system. The nano-bio hybrid system showed more effective cefdinir degradation compared to native yeast cell and nano zero-valent iron solely. The adherence of nanoparticles on the surface of the yeast cells increased the permeability of the cell membrane, thereby enhancing the entry of cefdinir into the cell. The kinetic data showed the half-life of cefdinir as 1.34 days for nano-bio hybrid system, 3.99 days for nFe0 and 2.96 days for native yeast, Candida sp. SMN04 confirming that nano-bio hybrid system reduced the half-life to less than half of the time taken by the yeast alone. This study signifies the potential efficacy of the nano-bio hybrid system to serve as an effective remedial tool for the treatment of pharmaceutical wastewater.
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OBJECTIVE: To evaluate the bioequivalence of cefdinir suspension and reference cefdinir capsule in Chinese healthy male subjects. METHODS: A single oral dose of 100 mg cefdinir suspension or cefdinir capsule was given to 24 subjects according to a 2-way crossover design. The plasma concentrations of cefdinir were determined by UPLC-MS/MS. The pharmacokinetic parameters were calculated and bioequivalence was compared by WinNonlin 6.3 program. RESULTS: The main pharmacokinetic parameters of cefdinir suspension and cefdinir capsule were as follow; ρmax were (1034.78±358.17), (969.71±297.38) ng·mL-1; tmax were (2.98±0.60), (3.44±0.70) h; AUC0-12 were (4911.24±1675.30), (4522.35±1600.13) ng·h·mL-1; AUC0-∞ were (5026.24±1735.32), (4680.69±1699.93) ng·h·mL-1;t1/2were (1.71±0.23), (1.79±0.39) h. The 90% confidential interval of ρmax, AUC0-12, AUC0-∞ of tested formulation were 95.6%-115.3%, 99.9%-117.2%, 99.0%-116.0%. CONCLUSION: The two formulations are bioequivalent.
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OBJECTIVE:To establish physiological pharmacokinetic (PBPK) model of cefdinir in healthy volunteers,and to predict pharmacokinetic process of cefdinir in volunteers after oral administration. METHODS:Using“toubao dini”“cefdinir”“logP”“pKa”as keywords,related literatures about physico-chemical constants of cefdinir were retrieved from CNKI,ScienceDi-rect,PubMed and other databases;according to related guidelines and preliminary clinical trial plan of FDA,GastroPlusTM 8.6 soft-ware was used to establish PBPK model of oral administration of cefdinir;the effectiveness of the model was evaluated by multiple error. The model was used to simulate the absorption of cefdinir in the gastrointestinal tracts. The bioequivalence of test preparation and reference preparation were evaluated through single and population(n=500)simulation tests using cmax and AUC0-∞ of cefdinir reference preparation (capsule and granular formulation) as factors when release rate t85%=15 min (i.e. accumulatively released 85% within 15 min). RESULTS:The blood concentration-time curves of cefdinir predicted by PBPK model fitted well with mea-sured value(R2≥0.95);the pharmacokinetic parameters(cmax,tmax,AUC0-∞)were close to measured results,and the multiple er-rors were less than 2. After oral administration,cefdinir was mainly absorbed by the intestinal tract (45.6%),especially by seg-ment 1 of jejunum(14.8%);the absorption amount was significantly lower than the release amount of absorption site,and reached the maximal value(about 40%)within 4 h. The results of single simulation test showed that there was no statistical significance in cmax and AUC0-∞ between cefdinir test and reference preparations (P>0.05). The results of population simulation test showed that the relative bioavailability of cefdinir test particle and test capsule respectively were 99.01%-102.99% and 97.60%-105.90%;90%CI of cmax and AUC0-∞ values were within 80%-125% of reference preparation. CONCLUSIONS:The PBPK model is accurate and reliable in this study,can provide reference for pharmacokinetic study and bioequivalence evaluation of cefdinir preparations. Test preparation and reference preparation are equivalent.
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Cefdinir being a semi-synthetic third generation cephalosporin antibiotic is considered as an emerging pollutant which demands removal from environment. Degradation of cefdinir by yeast Candida sp. SMN04 immobilized on various single and hybrid matrices was investigated using entrapment method. The biofilm forming ability of Candida sp. was evaluated by crystal violet staining assay and the formed biofilm was monitored by SEM and AFM analysis. The amount of exopolysaccharides (EPS) produced by Candida sp. was quantified and characterized by FTIR, HPLC and TGA analysis respectively. Cefdinir degradation from pharmaceutical wastewater was found to be 96.6% and 92.2% by PVA-alginate immobilized yeas tand yeast biofilm formed on gravels over a period of 48 h in batch mode. Effectiveness of the process was also tested involving continuous-flow column studies. This is the first successful attempt on cefdinir degradation using immobilized yeast cells and yeast biofilm on solid substrate.
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Objective To explore clinical effect of Cefdinir combined with Omidazole in treatment of pelvic inflammatory disease .Methods 60 cases of pelvic inflammatory disease from April 2014 to August 2015,were randomly divided into two groups and 30 cases in each group.Control group were given Ornidazole basic treatment, observation group were given Omidazole treatment given Cefdinir treatment on the basis of control group, after treated for 14d, patients were followed up and recorded C-reactive protein, blood rheology, compared clinical efficacy by statistical methods. Results After 2 weeks of treatment, observation group C-reactive protein value of (4.11 ±1.45)mg/L, lower than control group(7.63 ±1.57)mg/L (P<0.05).After 2 weeks of treatment, observation group plasma viscosity, hematocrit values were (1.12 ±0.26)mpass· s,(0.39 ±0.07)%, than control group (1.59 ±0.28)mpass· s,(0.48 ±0.09)% (P<0.05).After 2 weeks of treatment of patients in observation group total effective rate was 90.00%, significantly higher than 66.67%( P<0.05 ) .Conclusion It is good for Cefdinir combined with Omidazole in treatment of pelvic inflammatory disease better than Ornidazole medication use alone is worthy of further research and application .
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Objective To evaluate postprandial pharmacokinetics and bioequivalence of two preparations of cefdinir capsules in Chinese healthy volunteers. Methods In a two-way cross-over study, 24 healthy male volunteers were divided into two groups randomly and a single dose of cefdinir capsules of test and reference preparation were administered orally, respectively.The concentration in plasma was determined by LC-MS/MS. Pharmacokinetic parameters and bioequivalence were calculated and evaluated by DAS. Results The main pharmacokinetic parameters of test and reference were as follows: AUCt (4.35±1.09) μg??h??mL-1 and (4.12±1.22) μg??h??mL-1, AUC0-∞(4.53±1.12) and (4.53±1.73) μg??h??mL-1, t1/2 (1.74±0.29) h and (2.13±1.65) h, tmax(4.44±0.86) h and (4.54 ±1.16) h, Cmax(900±250) ng??mL-1 and (876±269) ng??mL-1 . Conclusion The test and reference preparation of cefdinir capsules are bioequivalent.
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The present work describes development and validation of four different stability indicating methods for quantitative analysis of cefdinir (CFD) in bulk powder and pharmaceuticals, and in the presence of its acid and alkaline induced hydrolytic degradation products. The first method is based on derivative spectrophotometry. First derivative spectrophotometry was applied where CFD was determined at 313.4 nm in the presence of its alkaline degradation product and also second derivative spectrophotometry where CFD was determined at 298.2 nm in the presence of its acid degradation product. The second method is based on the first derivative of ratio spectrophotometry of CFD at 312 nm in the presence of its acid degradation product and at 310.2 nm in the presence of its alkaline degradation product. The third method is based on the mean centering of ratio spectrophotometry where the drug was determined at 288.4 and 284.8nm in laboratory prepared mixtures with its acid and alkaline degradation products, respectively. The fourth method is HPTLC-densitometry using diethylether-methanol-water-glacial acetic acid (6: 3: 1: 0.05, v/v) as a developing system. Due to simplicity, rapidity and accuracy of the proposed stability indicating methods, they are effective for quality control analysis.
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OBJECTIVE:To study the pharmacokinetics and the bioequivalence of cefdinir dispersible tablets in healthy volunteers.METHODS:Microbiological assay method was used to determine the plasma concentration at different time in 20 healthy volunteers after oral administration of single dose of 400mg of cefdinir dispersible tablets(test preparation) and cefdinir capsule(reference preparation) by cross-over way.RESUTLS:The concentration-time curves of test preparation and reference preparation of cefdinir fitted one compartment open model.The pharmacokinetic parameters of the test preparation vs.the reference preparation were as follows:tmax(3.48?0.53)h vs.(3.60?0.48)h,Cmax(2.10?0.32)mg?L-1 vs.(2.15?0.26)mg?L-1.t1/2ke(2.41?0.39)h vs.(2.33?0.41)h,AUC0～12(9.51?1.65)mg?h?L-1 vs.(10.05?1.72)mg?h?L-1,AUC0～∞(10.43?1.62)mg?h?L-1 vs.(11.01?1.81)mg?h?L-1,respectively.The relative bioavailability of cefdinir dispersible tablet as against its reference preparation was(96.03?14.89)%.CONCLUSION:The two preparations of cefdinir were proved to be bioequivalent.
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Objective To evaluate the antibacterial activity of Cefdinir compared with other four antimicrobial agents against common isolates in vitro.Methods Minimal lnhibitory Concentrations (MIC) were determined by agar dilution method Results Staphylococcus aureus (MSSA) showed highest susceptibility to Cefdinir with 100% susceptible rate, Streptococcus pneumoniae (including PSSP and PISP) showed higher susceptibility to Cefdinir with 63 6% 100 0% susceptible rate Hemophilus influenza and Moraxelle catarrhalis both showed good susceptibility to three kinds of cephalosporins and Azithromycin Klebsiella pneumoniae (including ESBLs positive strains) were resistant to three kinds of cephalosporins, while ESBLs negative Klebsiella pneumoniae were sensitive to three kinds of cephalosporins, with 73 10%~88 50% susceptible rate Conclusion Compared with other four antimicrobial agents, Cefdinir has a powerful antibacterial activity to pathogen from respiratory tract infections