ABSTRACT
OBJECTIVE:To develop a method for rapid,accurate and simultaneous determination of dexzopiclone,zolpidam and zaleplon in human plasma. METHODS:After the plasma sample was processed by liquid-liquid extraction,UPLC-MS/MS was established to detect plasma sample with carbamazepine as internal standard. The separation was performed on a Waters ACQUITY UPLC HSS T3 column with mobile phase composed of 0.1% ammonium solution-acetonitrile (gradient elution) at flow rate of 0.2 ml/min. The column temperature was set at 40 ℃,and sample size was 5 μl. The detection was performed by multiple reaction monitoring (MRM) via electrospray ionization (ESI) source in positive mode. The mass transition ion-pairs were as follows:m/z 308.2→263.1(zolpidem),m/z 389.3→245.0(dexzopiclone),m/z 306.2→236.1(zaleplon),m/z 237.3→151.2(internal standard). RE-SULTS:The linear range of zolpidem,dexzopiclone and zaleplon were 0.02-20.00,0.50-20.00,0.02-20.00 ng/ml,respectively (r=0.990 1,0.996 8,0.991 7). LLOQ of them were 0.02,0.50,0.02 ng/ml,and detection limit were 0.01,0.20,0.01 ng/ml. RS-Ds of intra-day and inter-day were all lower than 15% ;extraction recovery were 88.9% -106.5% ;matrix effect were 94.8%-106.3%. CONCLUSIONS:The method is simple,rapid,sensitive and specific,and it can be used for simultaneous deter-mination of zaleplon,zolpidem and dexzopiclone in human plasma.
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OBJECTIVE:To evaluate the efficacy and safety of new agent zaleplon in treatment of insomnia.METHODS:A randomized,double-blind,controlled and dosage-adjusted clinical trial was conducted.The subjects had been treated with zaleplon5～10mg/d and zopicolone7.5～15mg/d for14days,respectively.RESULTS:The scores of sleep dysfunction rating scale at endpoint were significantly reduced as compared with the baseline in both groups(P
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OBJECTIVE:To build up a method for determining the concentration of zaleplon in human plasma by HPLC. METHODS:The Kromasil-C 8 column was used and mobile phase consisted of methanol-water(65∶35);the flow rate was1.0ml/min,fluorescence excitation wave-length was233nm;fluorescence emission wave-length was460nm.RESULTS:The calibration curve revealed linearity in the concentration range of0.42～73.92ng/ml(r=0.9999)with a regressive equation of Y=1.870?147.The average recovery was99.47%.The with-day and between-day RSDs were4.9%and4.73%respec?tively.CONCLUSION:The method is accurate,reliable and highly sensitive so it can be used in study of pharmacokinetics of zaleplon.
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OBJECTIVE:To study the pharmacokinetics of domestic zaleplon tablets in Chinese healthy volun?teers.METHODS:20male healthy subjects received a single oral dose of15mg zaleplon tablets.The plasma concentrations of zaleplon were determined by an improved HPLC method.RESULTS&CONCLUSION:The main pharmacokinetic parameters of zaleplon were as follow:C max was55.90?16.20ng/ml,T max was1.05?0.32h,Ke was0.74?0.18h -1 ,T 1/2Ke was1.00?0.29h,AUC 0～8 was123.70?25.64ng?h/ml,AUC 0～∞ was125.20?25.80ng?h/ml.The results are compara?ble to those reported in foreign literature.