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OBJECTIVE:To investigate the compatible stability of Voriconazole for injection after mixed with Fructose injec-tion or Invert sugar injection. METHODS:Referring to package inserts,Voriconazole for injection 200 mg was dissolved with Wa-ter for injection to 20 mL,and then combined with Fructose injection 250 mL and Invert sugar injection 250 mL,respectively. At room temperature,the appearance of mixtures were observed 0,1,2,3,4,5 h after mixing,and pH value and the number of in-soluble particles were determined;the content of voriconazole was determined by HPLC. RESULTS:Under above condition,the appearance and pH value of mixtures had no significant change within 5 h;the number of particles ≥10 μm and ≥25 μm were all in line with the standard of Chinese Pharmacopoeia (2015 edition);the relative content of voriconazole was decreasing (95.28%-100%),but it changed within ±5%(RSD<2%,n=6). CONCLUSIONS:Voriconazole for injection could keep stable within 5 h after mixed with Fructose injection or Invert sugar injection.
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OBJECTIVE:To determine the concentration of dehydroisoandrosterone sulfate (DHEAS) in human plasma by LC-MS.METHODS:With estrogen sulfate (ES) served as an internal standard,the plasma samples were deproteinized with acetonitrile,extracted by solid phase,hydrolyzed and derivatized.Then the concentration of DHEAS was determined by HPLC-MSD on Agilent SB C18 with column temperature kept at 40℃.The mobile phase consisted of acetonitrile-water (in gradient elution).Atmosphere pressure chemical ion source in negative ion detection model was employed.The ions selected for SIM (selected ion monitoring) quantitative analysis included m/z 490.0 (DHEAS ) and m/z 472.1(ES)[M-H]-.RESULTS:The linear range of DHEAS was 250.0～320.0 ng?mL-1(r=0.999 4).The extraction recovery of the simulated human albumin samples ranged from 71.1%～78.9% and its relative recovery ranged from 98.3%～101.4%.Both the intra-day RSD and inter-day RSD were less than 10%.The mean concentration of DHEAS in 15 health aged male volunteers was (981.6?353.4) ng?mL-1.CONCLUSION:The method is simple,practical,accurate and sensitive,and it is applicable for the determination of plasma concentration of DHEAS.
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OBJECTIVE:To study the pharmacokinetics and relative bioavailability of clindamycin phosphate capsules in healthy volunteers METHODS:A single oral dose of 300mg domestic clindamycin phosphate capsules or imported Dalacin C was given to 18 healthy male volunteers in an open randomized crossover study Clindamycin concentrations in plasma were determined by microbiologic assay The pharmacokinetic parmameters as well as relative bioavailability were calculated with 3p97 software and bioequivalence was analysed with NDST software RESULTS:The concentration-time curves of domestic clindamycin phosphate capsules or imported Dalacin C were well fitted for one-compartment open model The pharmacokinetic parameters of domestic and imported products were:Tmax(0 94?0 51) and(0 75?0 35)h;Cmax(3 86?0 62)?g/ml and (4 08?0 60)?g/ml;AUC0～12(14 88?3 64)?g/(ml?h)and(16 07?3 68)?g/(ml?h)respectively There were no significant differences in AUC0～12 and Cmax between two products CONCLUSION:The relative bioavailability of clindamycin phosphate capsules was(93 4?14 9)% compared with imported Dalacin C The results showed that the two formulations were bioequivalent
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OBJECTIVE:To evaluate the bioavailability of two nimesulide preparations.METHODS:A total of 20 healthy male volunteers were enrolled in a randomized crossover study in which the subjects were randomly assigned to receive single dose of 200 mg nimesulide orally disintegrating tablets(test)or nimesulide tablets(reference).The plasma concentrations of nimesulide were determined by RP-HPLC,and the pharmacokinetic parameters and bioavailability were calculated with DAS program.RESULTS:The main pharmacokinetic parameters of nimesulide test and reference preparations were as follow:AUC0～24:(54.67?18.25)vs.(56.15?15.54)?g?h?mL-1;AUC0～∞:(56.38?18.03)vs.(57.63?15.26)?g?h?mL-1;Cmax:(7.61?2.72)vs.(7.50?2.19)?g?mL-1;tmax:(3.83?1.39)and(3.80?1.28)h.The relative bioavailability of nimesulide or-ally disintegrating tablets as against nimesulide tablet was(98.7?22.9)%.CONCLUSION:Nimesulide test and reference preparations were bioequivalent.
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OBJECTIVE:Using in vitro studies,we evaluated the antibacterial activity of amoxicillin/tazobactam against 128 strains of pathogens isolated from patients and compared with amoxicillin/clavulanic acid and amoxicillin/sulbactam.METHODS:To detect the minimum inhibitory concentrations (MIC)of four ?-lactams against 128 clinically isolated strains with agar dilution method.RESULTS:The results indicated that the in vitro antibacterial activity of amoxicillin/tazobactam(2∶1) was the best.The MIC50 of amoxicillin/tazobactam(2∶1) is 1/4～1/8 times than those of amoxicillin/sulbutam and amoxicillin/clavulanic acid.The MIC90 of amoxicillin/tazobactam(2∶1) was 1/2～1/4 of those of amoxicillin/sulbutam and amoxicillin/clavulanic acid.The combination ratio 2∶1(amoxicillin/tazobactam)of the two compounds was more suitable than other combination ratios(4∶1 and 8∶1)for inactivating ?-lactamase.CONCLUSION:The in vitro antibacterial activities of amoxicillin/tazobactam(2∶1) against MRSA,MRSE,MSSA and E.coli are high.It showed that amoxicillin/tazobactam(2∶1)is stable to ?-lactamase and is an effective bactericidal agent.