抗心律失常新药关附甲素(Guan—fu base A)与三氟醋酐反应,迅速定量地生成双-三氟乙酸酯衍生物,其结构经GC-MSD的分析得到证实。关附甲素衍生物经气相色谱分离后,在电子捕获检测器上有较高的响应,线性范围宽(10～2.0×10~4ng/ml,r=0...抗心律失常新药关附甲素(Guan—fu base A)与三氟醋酐反应,迅速定量地生成双-三氟乙酸酯衍生物,其结构经GC-MSD的分析得到证实。关附甲素衍生物经气相色谱分离后,在电子捕获检测器上有较高的响应,线性范围宽(10～2.0×10~4ng/ml,r=0.9984)。血中平均回收率为97.52％。本法以烯丙洛尔(alprenolol)为内标,定量准确,日内及日间差的变异系数分别小于7％和9％,并已成功地用于关附甲素临床前的药代动力学研究。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
文摘抗心律失常新药关附甲素(Guan—fu base A)与三氟醋酐反应,迅速定量地生成双-三氟乙酸酯衍生物,其结构经GC-MSD的分析得到证实。关附甲素衍生物经气相色谱分离后,在电子捕获检测器上有较高的响应,线性范围宽(10～2.0×10~4ng/ml,r=0.9984)。血中平均回收率为97.52％。本法以烯丙洛尔(alprenolol)为内标,定量准确,日内及日间差的变异系数分别小于7％和9％,并已成功地用于关附甲素临床前的药代动力学研究。
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.
