BACKGROUND Prior studies have noted great variability in the plasma levels of risperidone(RIS).Plasma concentrations of RIS and its active moiety are highly variable and depend on absorption,metabolism,and other predi...BACKGROUND Prior studies have noted great variability in the plasma levels of risperidone(RIS).Plasma concentrations of RIS and its active moiety are highly variable and depend on absorption,metabolism,and other predictors of metabolic dysregulation;however,these factors are poorly understood and the association between metabolic change and change in psychopathology is uncertain.AIM To ascertain the characteristics of chronic schizophrenic patients treated with RIS,and to assess their relationship with plasma RIS levels.METHODS This was a descriptive cross-sectional study of 50 patients with a diagnosis of schizophrenic psychosis treated with RIS in a psychiatric service.The plasma concentrations of RIS and its metabolite 9-hydroxyrisperidone were determined by high performance liquid chromatography.The patients’demographic and clinical characteristics,and psychopathologies were assessed,and the associations between clinical variables and plasma levels of RIS were explored.RESULTS Male patients received higher doses of RIS than female ones,but plasma concentrations of RIS and risperidone+9-hydroxyrisperidone(active moiety)were higher in female patients.Age and the mean scores of the general psychopathology subscale of the Positive and Negative Syndrome Scale(PANSS)were significantly positively correlated with plasma concentrations of risperidone+9-hydroxyrisperidone adjusted for weight and dose in all 50 subjects.In male subjects,we found a statistically significant positive correlation between the concentrations of risperidone+9-hydroxyrisperidone in plasma/(dose×kg)and age,mean PANSS negative subscale scores,mean PANSS general psychopathology subscale scores,and mean PANSS total scores.CONCLUSION Long-term use of RIS should be closely monitored in older patients and females to minimize the risk of high concentrations which could induce side effects.展开更多
Guan-fu base A(GFA),a new antiarrhythmic alkaloid with a structure of C_(20)-diterpenoid could react rapidly and quantitatively with trifluoroacetic anhydride(TFAA) to produce GFA—TFAA of which the structure was iden...Guan-fu base A(GFA),a new antiarrhythmic alkaloid with a structure of C_(20)-diterpenoid could react rapidly and quantitatively with trifluoroacetic anhydride(TFAA) to produce GFA—TFAA of which the structure was identified by GC—MSD.There was a wide linear range of the GC-ECD method from 10 to 20000ng/ml(r=0.9984).The average recovery of GFA from the spiked plasma was 97.52%.The coefficients of variation of within-day and between-day were less than 7% and 9%,respectively.The method was used in the preclinical experiment of pharmacology of GFA and the results showed that GFA con- centrations in rabbits' plasma within 6 hours after the administration ranged from 0.338± 0.014 to 13.459±5.393μg/ml for dosage 10mg/kg,from 0.133±0.038 to 2.546±0.480 μg/ml for dosage 2mg/kg and from 45.25±10.34 to 535.86±24.36ng/ml for dosage 0.4 mg/kg.展开更多
A fast, simple and sensitive high performance liquid chromatographic (HPLC) method has been developed for determination of 10a-methoxy-6-methyl ergoline-8b-methanol (MDL, a main metabolite of nicergoline) in human pla...A fast, simple and sensitive high performance liquid chromatographic (HPLC) method has been developed for determination of 10a-methoxy-6-methyl ergoline-8b-methanol (MDL, a main metabolite of nicergoline) in human plasma. One-step liquid–liquid extraction (LLE) with diethyl ether was employed as the sample preparation method. Tizanidine hydrochloride was selected as the internal standard (IS). Analysis was carried out on a Diamonsil ODS column (150 mm 4.6 mm, 5 mm) using acetonitrile–ammonium acetate (0.1 mol/L) (15/85, v/v) as mobile phase at detection wavelength of 224 nm. The calibration curves were linear over the range of 2.288–73.2 ng/mL with a lower limit of quantitation (LLOQ) of 2.288 ng/mL. The intra-and inter-day precision values were below 13% and the recoveries were from 74.47% to 83.20% at three quality control levels. The method herein described was successfully applied in a randomized crossover bioequivalence study of two different nicergoline preparations after administration of 30 mg in 20 healthy volunteers.展开更多
目的：建立测定人血浆中白消安浓度的高效液相色谱法。方法：血浆样品经衍生化处理后，以甲醇-水（74：26）为流动相，流速0．9mL·min^-1，选用Nova Pak C18色谱柱（3．9mm×150mm，4μm），在280nm波长下进行检测。结果：白...目的：建立测定人血浆中白消安浓度的高效液相色谱法。方法：血浆样品经衍生化处理后，以甲醇-水（74：26）为流动相，流速0．9mL·min^-1，选用Nova Pak C18色谱柱（3．9mm×150mm，4μm），在280nm波长下进行检测。结果：白消安血浆质量浓度的线性范围为0．050～3．20mg·L^-1，以加权最小二乘法运算得到回归方程为Y=4．575X-37．04（r=0．9993，n=9），方法回收率（100．6±1．6）%（99．66％～102．4％），血浆萃取回收率（83．6±2．4）％（81．70％～86．35％），日内和日间RSD均小于15％。检测限为0．6ng，最低血浆检测质量浓度为0．030mg·L^-1。结论：该方法准确、灵敏，适用于白消安血浆浓度测定及其药动学研究。展开更多
基金Supported by Shanghai Civil Administration Bureau,No.8-2-50.
文摘BACKGROUND Prior studies have noted great variability in the plasma levels of risperidone(RIS).Plasma concentrations of RIS and its active moiety are highly variable and depend on absorption,metabolism,and other predictors of metabolic dysregulation;however,these factors are poorly understood and the association between metabolic change and change in psychopathology is uncertain.AIM To ascertain the characteristics of chronic schizophrenic patients treated with RIS,and to assess their relationship with plasma RIS levels.METHODS This was a descriptive cross-sectional study of 50 patients with a diagnosis of schizophrenic psychosis treated with RIS in a psychiatric service.The plasma concentrations of RIS and its metabolite 9-hydroxyrisperidone were determined by high performance liquid chromatography.The patients’demographic and clinical characteristics,and psychopathologies were assessed,and the associations between clinical variables and plasma levels of RIS were explored.RESULTS Male patients received higher doses of RIS than female ones,but plasma concentrations of RIS and risperidone+9-hydroxyrisperidone(active moiety)were higher in female patients.Age and the mean scores of the general psychopathology subscale of the Positive and Negative Syndrome Scale(PANSS)were significantly positively correlated with plasma concentrations of risperidone+9-hydroxyrisperidone adjusted for weight and dose in all 50 subjects.In male subjects,we found a statistically significant positive correlation between the concentrations of risperidone+9-hydroxyrisperidone in plasma/(dose×kg)and age,mean PANSS negative subscale scores,mean PANSS general psychopathology subscale scores,and mean PANSS total scores.CONCLUSION Long-term use of RIS should be closely monitored in older patients and females to minimize the risk of high concentrations which could induce side effects.
文摘Guan-fu base A(GFA),a new antiarrhythmic alkaloid with a structure of C_(20)-diterpenoid could react rapidly and quantitatively with trifluoroacetic anhydride(TFAA) to produce GFA—TFAA of which the structure was identified by GC—MSD.There was a wide linear range of the GC-ECD method from 10 to 20000ng/ml(r=0.9984).The average recovery of GFA from the spiked plasma was 97.52%.The coefficients of variation of within-day and between-day were less than 7% and 9%,respectively.The method was used in the preclinical experiment of pharmacology of GFA and the results showed that GFA con- centrations in rabbits' plasma within 6 hours after the administration ranged from 0.338± 0.014 to 13.459±5.393μg/ml for dosage 10mg/kg,from 0.133±0.038 to 2.546±0.480 μg/ml for dosage 2mg/kg and from 45.25±10.34 to 535.86±24.36ng/ml for dosage 0.4 mg/kg.
文摘A fast, simple and sensitive high performance liquid chromatographic (HPLC) method has been developed for determination of 10a-methoxy-6-methyl ergoline-8b-methanol (MDL, a main metabolite of nicergoline) in human plasma. One-step liquid–liquid extraction (LLE) with diethyl ether was employed as the sample preparation method. Tizanidine hydrochloride was selected as the internal standard (IS). Analysis was carried out on a Diamonsil ODS column (150 mm 4.6 mm, 5 mm) using acetonitrile–ammonium acetate (0.1 mol/L) (15/85, v/v) as mobile phase at detection wavelength of 224 nm. The calibration curves were linear over the range of 2.288–73.2 ng/mL with a lower limit of quantitation (LLOQ) of 2.288 ng/mL. The intra-and inter-day precision values were below 13% and the recoveries were from 74.47% to 83.20% at three quality control levels. The method herein described was successfully applied in a randomized crossover bioequivalence study of two different nicergoline preparations after administration of 30 mg in 20 healthy volunteers.
文摘目的：建立测定人血浆中白消安浓度的高效液相色谱法。方法：血浆样品经衍生化处理后，以甲醇-水（74：26）为流动相，流速0．9mL·min^-1，选用Nova Pak C18色谱柱（3．9mm×150mm，4μm），在280nm波长下进行检测。结果：白消安血浆质量浓度的线性范围为0．050～3．20mg·L^-1，以加权最小二乘法运算得到回归方程为Y=4．575X-37．04（r=0．9993，n=9），方法回收率（100．6±1．6）%（99．66％～102．4％），血浆萃取回收率（83．6±2．4）％（81．70％～86．35％），日内和日间RSD均小于15％。检测限为0．6ng，最低血浆检测质量浓度为0．030mg·L^-1。结论：该方法准确、灵敏，适用于白消安血浆浓度测定及其药动学研究。
