In order to evaluate the pharmacokinetic profile of paliperidone extended-release tablets in vivo,a simple and rapid ultra-high performance liquid chromatographyetandem mass spectrometry(UHPLCeMS/MS)method was develop...In order to evaluate the pharmacokinetic profile of paliperidone extended-release tablets in vivo,a simple and rapid ultra-high performance liquid chromatographyetandem mass spectrometry(UHPLCeMS/MS)method was developed and validated for the determination of paliperidone in beagle dog plasma.Paliperidone and diazepam(internal standard)were extracted from plasma samples with diethyl ether,and then separated on a C_(18) column(2.1×50 mm,2.6 mm)under gradient elution with methanol-0.1%formic acid at a flow rate of 0.3 ml/min.The compounds were detected using a triple-quadrupole mass spectrometer equipped with an electrospray ionization(ESI)source.The validated method was linear over the concentration range of 1.00-1000.00 ng/ml and the lower limit of quantitation was 1.00 ng/ml.The intra-day and inter-day precision values were not more than 15%(relative standard deviation<20%at low levels),while the accuracy was within±10%of nominal values.The validated UHPLC-MS/MS method was successfully applied to an oral pharmacokinetic study of paliperidone extended-release tablets in a beagle dog.展开更多
Introduction Erdosteine [ N-（ carboxymethylthioacetyl ）-homocysteine thiolactone ] （ Fig. 1 ） is a synthetic derivative of natural amino acid methionine. It has been commonly used in clinical practice as a mucoly...Introduction Erdosteine [ N-（ carboxymethylthioacetyl ）-homocysteine thiolactone ] （ Fig. 1 ） is a synthetic derivative of natural amino acid methionine. It has been commonly used in clinical practice as a mucolytic drug and as an enhancer of respiratory ventilation in the treatment of patients with chronic obstructive respiratory disease. Erdosteine contains 2 blocked sulfhydryl groups, which are released after metabolic transformation in the liver. The liberated sulfhydryl groups break the disulphide bonds, which hold the glycoprotein fibres of mucus together; this makes the bronchial secretions more fluid and allows more rapid elimination. The reducing potential of these sulfhydryl groups accounts for the free radical scavenging and antioxidant properties of erdosteine.展开更多
文摘In order to evaluate the pharmacokinetic profile of paliperidone extended-release tablets in vivo,a simple and rapid ultra-high performance liquid chromatographyetandem mass spectrometry(UHPLCeMS/MS)method was developed and validated for the determination of paliperidone in beagle dog plasma.Paliperidone and diazepam(internal standard)were extracted from plasma samples with diethyl ether,and then separated on a C_(18) column(2.1×50 mm,2.6 mm)under gradient elution with methanol-0.1%formic acid at a flow rate of 0.3 ml/min.The compounds were detected using a triple-quadrupole mass spectrometer equipped with an electrospray ionization(ESI)source.The validated method was linear over the concentration range of 1.00-1000.00 ng/ml and the lower limit of quantitation was 1.00 ng/ml.The intra-day and inter-day precision values were not more than 15%(relative standard deviation<20%at low levels),while the accuracy was within±10%of nominal values.The validated UHPLC-MS/MS method was successfully applied to an oral pharmacokinetic study of paliperidone extended-release tablets in a beagle dog.
基金Supported by the National Nature Science Foundation of China(No.39930180).
文摘Introduction Erdosteine [ N-（ carboxymethylthioacetyl ）-homocysteine thiolactone ] （ Fig. 1 ） is a synthetic derivative of natural amino acid methionine. It has been commonly used in clinical practice as a mucolytic drug and as an enhancer of respiratory ventilation in the treatment of patients with chronic obstructive respiratory disease. Erdosteine contains 2 blocked sulfhydryl groups, which are released after metabolic transformation in the liver. The liberated sulfhydryl groups break the disulphide bonds, which hold the glycoprotein fibres of mucus together; this makes the bronchial secretions more fluid and allows more rapid elimination. The reducing potential of these sulfhydryl groups accounts for the free radical scavenging and antioxidant properties of erdosteine.
