ABSTRACT
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 establish a method for the concentration determination of gabapentin (GBP) in human plasma.METHODS:After precipitated by methanol,using sulfamethoxazole as intemal standard,LC-MS/MS method was adopted.The determination was performed on Diamonsil C18 column with mobile phase consisted of water (containing 0.05％ formic acid)-methanol using a gradient elution program at the flow rate of 1 mL/min.The column temperature was 30 ℃,and sample size was 20 μL.The ESI was equipped and quantitative analysis was operated in positive ion and MRM mode.The mass transition ion-pairs were followed as m/z 172.0→154.1(GBP) and m/z 279.0→124.0 (internal standard).RESULTS:The linear range of GBP was 13.4-10 720.4 ng/mL (r=0.992 3,n=5).The limit of quantitation was 13.4 ng/mL,and the minimum detection limit was 4.0 ng/mL.RSDs of inter-day and intra-day were all lower than 10％.Relative errors ranged-4.93％-5.10％.The recoveries ranged 86.2％-90.3％ (RSD＜5％,n=6),and matrix effects ranged 87.6％-92.1％.The plasma concentration of GBP in 10 epileptic patients ranged 2 075.19-4 078.87 ng/mL (n=20).CONCLUSIONS:The method is proved to be sensitive,specific,practical and suitable for plasma concentration monitoring and pharmacokinetic study of GBP in epileptic patients.
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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.