Naloxone is a well-known opioid antagonist indicated for the treatment of CNS （central nervous system） and respiratory depression induced by natural or synthetic opioid in adults and neonates whose mothers have rece...Naloxone is a well-known opioid antagonist indicated for the treatment of CNS （central nervous system） and respiratory depression induced by natural or synthetic opioid in adults and neonates whose mothers have received opioids. While it has been reported that an injection of 0.2 mg/mL of naloxone hydrochloride is physically and chemically stable, data on photostability on continuous i.v. infusion of 0.2 mg/mL of naloxone hydrochloride has not been reported. Therefore, a method was required for assessment of naloxone hydrochloride photostability. A high performance LC-MS （liquid chromatography/mass spectrometry） method was established to evaluate the photostability of naloxone hydrochloride. Injections of naloxone hydrochloride in 0.9% sodium chloride were exposed to artificial light and stored at room temperature （22 ~C） and 37 ~C. Naloxone losses up to 9.79% of its initial concentration when exposed to light at room temperature for 192 h, but the degradation increased up to 14.91% as the storage temperature increase. The disappearance of naloxone hydrochloride was correlated with the appearance of nor-oxymorphonedegradant. Naloxone hydrochloride is photosensitive and degradation increased at highly temperature and light intensity. Therefore, naloxone i.v. infusion solutions should either be protected from light and/or be frequently replaced when being administered to patients.展开更多
Correction:Natural Products and Bioprospecting(2024)14:33 https://doi.org/10.1007/s13659-024-00455-x Following publication of the original article[1],the authors reported that the original version of this article unfo...Correction:Natural Products and Bioprospecting(2024)14:33 https://doi.org/10.1007/s13659-024-00455-x Following publication of the original article[1],the authors reported that the original version of this article unfortunately contained mistakes.Page 1,section“Abstract”,the originally published texts were:Despite low bioavailability(0.024%),N-hydap exhibited a higher distribution in the lungs(26.26%),accounting for its efficacy against SCLC.展开更多
A simple and rapid liquid chromatography-tandem mass spectrometry（LC-MS/MS）method was developed and validated for the quantitative determination of glycyrrhetic acid（GA）,metabolite of glycyrrhizin and glycyrrhetat...A simple and rapid liquid chromatography-tandem mass spectrometry（LC-MS/MS）method was developed and validated for the quantitative determination of glycyrrhetic acid（GA）,metabolite of glycyrrhizin and glycyrrhetate,in human plasma.GA and internal standard（IS,thiamphenicol）were separated on a C_（18）column by elution with acetonitrile-ammonium acetate solution（5 mmol/L）（70：30,v/v）after a simple liquid-liquid extraction with ethyl acetate.The flow rate was 0.8 mL/min. They were detected by tandem mass spectrometry in the negative ion multiple reaction monitoring（MRM）mode with ion transitions of m/z 469.3→355.3 for GA and m/z 354.1→185.0 for IS.The calibration curve was linear over GA concentration range of 0.5-500 ng/mL（r^20.99）,with intra-and inter-day precisions（RSD）of less than 7.1%,and mean extraction recovery of 74.3%. The method was used for the pharmacokinetic study of ammonium glycyrrhetate after its oral administration of a single dose of 75 mg ammonium glycyrrhetate tablet in humans.The main pharmacokinetic parameters of GA were as follows：AUC_（0-t） （3457.26±1999.01）ng·h/mL;AUC_（0-∞）（3708.85±2428.36）ng·h/mL;MRT_（0-t）（19.69±4.03）h;MRT_（0-∞）（22.83±8.45）h;t_（1/2）Z （11.71±7.77）h;T_（max）（13.40±4.84）h;CLz/F（29.17±19.82）L/h;Vz/F（487.38±518.07）L;C_（max）（215.85±99.88）ng/mL.展开更多
A liquid chromatography with tandem mass spectrometry（LC-MS/MS） method has been developed and validated for the measurement of sunitinib in rabbit plasma. After protein precipitation with acetonitrile, samples were ...A liquid chromatography with tandem mass spectrometry（LC-MS/MS） method has been developed and validated for the measurement of sunitinib in rabbit plasma. After protein precipitation with acetonitrile, samples were analyzed on a Zorbax Extend-C18 column（150 mm×4.6 mm, 5μm）. The mobile phase consisted of a mixture of acetonitrile and deionized water（containing 0.05% formic acid） at a ratio of 27：73（v/v）, and the flow rate was set at 0.8 mL /min. The column temperature was maintained at 30 oC. The LC eluate was detected by an electrospray ionization（ESI） source operated in the positive ion mode, and quantification was conducted using MRM of the transitions m/z 399.24→283.01 and m/z 415.19→178.00 for sunitinib and internal standard（IS, diltiazem hydrochloride）, respectively. The calibration curve was linear in the range of 2–600 ng/m L. The lower limit of quantification was 2 ng/mL. The method also exhibited satisfactory results in terms of sensitivity, specificity, accuracy（with relative error ranging from –4.0% to 1.1%）, precision（with intra- and inter-day relative standard deviations ranging from 2.8% to 9.5%）, matrix effect, recovery as well as stability. Taken together, our newly developed method was reliable to monitor sunitinib concentrations in rabbit plasma.展开更多
A simple, rapid and sensitive LC-MS/MS method was developed to quantify erlotinib and its active metabolite, OSI-420, simultaneously in BALB/c nude mice plasma. Erlotinib, OSI-420 and propranolol （internal standard）...A simple, rapid and sensitive LC-MS/MS method was developed to quantify erlotinib and its active metabolite, OSI-420, simultaneously in BALB/c nude mice plasma. Erlotinib, OSI-420 and propranolol （internal standard） were extracted from nude mice plasma samples by liquid-liquid extraction. Separation was achieved on a reversed phase ClS column with a mobile phase of acetonitrile-water （35：65, v/v） containing 5 mM ammonium formate （pH = 3.0）. All compounds were monitored by mass spectrometry with electrospray positive ionization. The lower limit of quantification was 0.5 ng/mL for both erlotinib and OSI-420; accuracy was estimated by relative error, which was in the range from 0.07% to 8.00% for erlotinib and -2.83% to 6.67% for OSI-420; precision was validated by relative standard deviation, which was from 2.28% to 15.12% for erlotinib and from 1.96% to 11.50% for OSI-420. This method was applied to a pharmacokinetic study of BALB/c nude mice following oral administration of erlotinib at 12.5 mg/kg. A 2-compartment model was used to fit the pharmacokinetics of erlotinib and 1-compartment model for the pharmacokinetics of OSI-420. The ratio of the active metabolite to parent drug in mice was greater than previously reported in humans and probably reflects interspecies difference in the rate of conversion of erlotinib to OSI-420.展开更多
In the current study, we established and validated a simple and sensitive liquid chromatography-tandem mass spectrometric method for the determination of 21-hydroxy deflazacort in nude mice plasma, and such a method w...In the current study, we established and validated a simple and sensitive liquid chromatography-tandem mass spectrometric method for the determination of 21-hydroxy deflazacort in nude mice plasma, and such a method was applied to a pharmacokinetic study. Using betamethasone as the internal standard, the plasma samples were pre-treated by precipitation with acetonitrile and then analyzed on a reversed-phase C18 column （50 mm×2 mm, 5 μm） with a mobile phase consisting of acetonitrile and 4.0 mM ammonium formate （pH was adjusted to 3.5 with formic acid （40：60, v/v））. The analyte was detected by a triple quadrupole tandem mass spectrometer using electrospray, and multiple reaction monitoring was employed to select 21-hydroxy deflazacort at m/z 400.2/124.0 and betamethasone at m/z 393.3/147.0 in the positive ion mode. The calibration curves were linear （r〉0.99） over the range of 0.5~,00 ng/mL. The intra- and inter-day precisions and accuracies were 4.5%-10.1% and -1.7%-10.7% respectively. This method was successfully applied to a preclinical administered with a single oral dose of 4 mg/kg deflazacort, and its pharmacokinetic study of deflazacort on female nude mice pharmacokinetics was characterized by a two-compartment model with first-order absorption.展开更多
文摘Naloxone is a well-known opioid antagonist indicated for the treatment of CNS （central nervous system） and respiratory depression induced by natural or synthetic opioid in adults and neonates whose mothers have received opioids. While it has been reported that an injection of 0.2 mg/mL of naloxone hydrochloride is physically and chemically stable, data on photostability on continuous i.v. infusion of 0.2 mg/mL of naloxone hydrochloride has not been reported. Therefore, a method was required for assessment of naloxone hydrochloride photostability. A high performance LC-MS （liquid chromatography/mass spectrometry） method was established to evaluate the photostability of naloxone hydrochloride. Injections of naloxone hydrochloride in 0.9% sodium chloride were exposed to artificial light and stored at room temperature （22 ~C） and 37 ~C. Naloxone losses up to 9.79% of its initial concentration when exposed to light at room temperature for 192 h, but the degradation increased up to 14.91% as the storage temperature increase. The disappearance of naloxone hydrochloride was correlated with the appearance of nor-oxymorphonedegradant. Naloxone hydrochloride is photosensitive and degradation increased at highly temperature and light intensity. Therefore, naloxone i.v. infusion solutions should either be protected from light and/or be frequently replaced when being administered to patients.
文摘Correction:Natural Products and Bioprospecting(2024)14:33 https://doi.org/10.1007/s13659-024-00455-x Following publication of the original article[1],the authors reported that the original version of this article unfortunately contained mistakes.Page 1,section“Abstract”,the originally published texts were:Despite low bioavailability(0.024%),N-hydap exhibited a higher distribution in the lungs(26.26%),accounting for its efficacy against SCLC.
文摘A simple and rapid liquid chromatography-tandem mass spectrometry（LC-MS/MS）method was developed and validated for the quantitative determination of glycyrrhetic acid（GA）,metabolite of glycyrrhizin and glycyrrhetate,in human plasma.GA and internal standard（IS,thiamphenicol）were separated on a C_（18）column by elution with acetonitrile-ammonium acetate solution（5 mmol/L）（70：30,v/v）after a simple liquid-liquid extraction with ethyl acetate.The flow rate was 0.8 mL/min. They were detected by tandem mass spectrometry in the negative ion multiple reaction monitoring（MRM）mode with ion transitions of m/z 469.3→355.3 for GA and m/z 354.1→185.0 for IS.The calibration curve was linear over GA concentration range of 0.5-500 ng/mL（r^20.99）,with intra-and inter-day precisions（RSD）of less than 7.1%,and mean extraction recovery of 74.3%. The method was used for the pharmacokinetic study of ammonium glycyrrhetate after its oral administration of a single dose of 75 mg ammonium glycyrrhetate tablet in humans.The main pharmacokinetic parameters of GA were as follows：AUC_（0-t） （3457.26±1999.01）ng·h/mL;AUC_（0-∞）（3708.85±2428.36）ng·h/mL;MRT_（0-t）（19.69±4.03）h;MRT_（0-∞）（22.83±8.45）h;t_（1/2）Z （11.71±7.77）h;T_（max）（13.40±4.84）h;CLz/F（29.17±19.82）L/h;Vz/F（487.38±518.07）L;C_（max）（215.85±99.88）ng/mL.
文摘A liquid chromatography with tandem mass spectrometry（LC-MS/MS） method has been developed and validated for the measurement of sunitinib in rabbit plasma. After protein precipitation with acetonitrile, samples were analyzed on a Zorbax Extend-C18 column（150 mm×4.6 mm, 5μm）. The mobile phase consisted of a mixture of acetonitrile and deionized water（containing 0.05% formic acid） at a ratio of 27：73（v/v）, and the flow rate was set at 0.8 mL /min. The column temperature was maintained at 30 oC. The LC eluate was detected by an electrospray ionization（ESI） source operated in the positive ion mode, and quantification was conducted using MRM of the transitions m/z 399.24→283.01 and m/z 415.19→178.00 for sunitinib and internal standard（IS, diltiazem hydrochloride）, respectively. The calibration curve was linear in the range of 2–600 ng/m L. The lower limit of quantification was 2 ng/mL. The method also exhibited satisfactory results in terms of sensitivity, specificity, accuracy（with relative error ranging from –4.0% to 1.1%）, precision（with intra- and inter-day relative standard deviations ranging from 2.8% to 9.5%）, matrix effect, recovery as well as stability. Taken together, our newly developed method was reliable to monitor sunitinib concentrations in rabbit plasma.
基金National Integrity Innovational Technology Platform of New Drug and Development (Grant No. 2009ZX09301-010)Innovation Team of Ministry of Education (Grant No. BMU20110263)
文摘A simple, rapid and sensitive LC-MS/MS method was developed to quantify erlotinib and its active metabolite, OSI-420, simultaneously in BALB/c nude mice plasma. Erlotinib, OSI-420 and propranolol （internal standard） were extracted from nude mice plasma samples by liquid-liquid extraction. Separation was achieved on a reversed phase ClS column with a mobile phase of acetonitrile-water （35：65, v/v） containing 5 mM ammonium formate （pH = 3.0）. All compounds were monitored by mass spectrometry with electrospray positive ionization. The lower limit of quantification was 0.5 ng/mL for both erlotinib and OSI-420; accuracy was estimated by relative error, which was in the range from 0.07% to 8.00% for erlotinib and -2.83% to 6.67% for OSI-420; precision was validated by relative standard deviation, which was from 2.28% to 15.12% for erlotinib and from 1.96% to 11.50% for OSI-420. This method was applied to a pharmacokinetic study of BALB/c nude mice following oral administration of erlotinib at 12.5 mg/kg. A 2-compartment model was used to fit the pharmacokinetics of erlotinib and 1-compartment model for the pharmacokinetics of OSI-420. The ratio of the active metabolite to parent drug in mice was greater than previously reported in humans and probably reflects interspecies difference in the rate of conversion of erlotinib to OSI-420.
基金National Natural Science Foundation of China(NSFC,Grant No.81673500)
文摘In the current study, we established and validated a simple and sensitive liquid chromatography-tandem mass spectrometric method for the determination of 21-hydroxy deflazacort in nude mice plasma, and such a method was applied to a pharmacokinetic study. Using betamethasone as the internal standard, the plasma samples were pre-treated by precipitation with acetonitrile and then analyzed on a reversed-phase C18 column （50 mm×2 mm, 5 μm） with a mobile phase consisting of acetonitrile and 4.0 mM ammonium formate （pH was adjusted to 3.5 with formic acid （40：60, v/v））. The analyte was detected by a triple quadrupole tandem mass spectrometer using electrospray, and multiple reaction monitoring was employed to select 21-hydroxy deflazacort at m/z 400.2/124.0 and betamethasone at m/z 393.3/147.0 in the positive ion mode. The calibration curves were linear （r〉0.99） over the range of 0.5~,00 ng/mL. The intra- and inter-day precisions and accuracies were 4.5%-10.1% and -1.7%-10.7% respectively. This method was successfully applied to a preclinical administered with a single oral dose of 4 mg/kg deflazacort, and its pharmacokinetic study of deflazacort on female nude mice pharmacokinetics was characterized by a two-compartment model with first-order absorption.
