CAJ | 학술논문

[目的]分析加替沙星在家兔体内的药代动力学过程.[方法]家兔口服5、10和20 mg/kg加替沙星后于0.25、0.50、1.00、2.00、4.00、8.00、12.00和24.00 h分别取静脉血,应用毛细管区带电泳-二极管阵列检测法测定血药浓度并计算代谢动力学参数.家兔口服10 mg/kg加替沙星后于0.25、0.50、1.00、2.00和4.00 h分别测定心、肺、肌肉等组织中的药物浓度.[结果]加替沙星在0.05～5.00 μg/ml范围内具有良好线性关系,最低检测限为0.05 μg/ml,在家兔血液代谢动力学过程符合一室模型.5、10和20 mg/kg剂量组主要动力学参数如下:峰浓度(Cmax)分别为2.28、3.35和7.93 μg/ml;达峰时间(Tmax)分别为1.36、1.83和1.69 h;吸收半衰期(t1/2Ka)分别为0.39、0.51和0.42 h;消除半衰期(t1/2Ke)分别为5.63、6.07和6.81 h;药时曲线下面积(AUC)分别为21.67、33.59和97.07 (μg·h)/ml.加替沙星被家兔摄入后,迅速分布于各组织中.[结论]加替沙星在家兔体内吸收迅速,消除半衰期长,组织分布广泛,是一种值得推广的新型氟喹诺酮类抗生素.
[목적]분석가체사성재가토체내적약대동역학과정.[방법]가토구복5、10화20 mg/kg가체사성후우0.25、0.50、1.00、2.00、4.00、8.00、12.00화24.00 h분별취정맥혈,응용모세관구대전영-이겁관진렬검측법측정혈약농도병계산대사동역학삼수.가토구복10 mg/kg가체사성후우0.25、0.50、1.00、2.00화4.00 h분별측정심、폐、기육등조직중적약물농도.[결과]가체사성재0.05～5.00 μg/ml범위내구유량호선성관계,최저검측한위0.05 μg/ml,재가토혈액대사동역학과정부합일실모형.5、10화20 mg/kg제량조주요동역학삼수여하:봉농도(Cmax)분별위2.28、3.35화7.93 μg/ml;체봉시간(Tmax)분별위1.36、1.83화1.69 h;흡수반쇠기(t1/2Ka)분별위0.39、0.51화0.42 h;소제반쇠기(t1/2Ke)분별위5.63、6.07화6.81 h;약시곡선하면적(AUC)분별위21.67、33.59화97.07 (μg·h)/ml.가체사성피가토섭입후,신속분포우각조직중.[결론]가체사성재가토체내흡수신속,소제반쇠기장,조직분포엄범,시일충치득추엄적신형불규낙동류항생소.
[Objective] The study aimed to analyze the pharmacodynamics process of gatifloxacin in rabbits. [Method] Following the oral administration of a single dose of 5,10 and 20 mg/kg gatifloxacin to rabbits,their vein blood was selected resp. at 0.25,0.50,1.00,2.00,4.00,8.00,12.00 and 24.00 h after administration,and the gatifloxacin concn. in the plasma were determined by coupling capillary Zone Electrophoresis with Diode Array Detection (CZE-DAD),resp. and then the pharmacodynamics parameters were calculated. After the oral administration of a single dose of 10 mg/kg gatifloxacin to the rabbits,the gatifloxacin concn. in different tissues such as heart,lung,muscle were determined resp. at 0.25,0.50,1.00,2.00,4.00 h after administration. [Result] The gatifloxacin had good linear relation over the range from 0.05 to 5.00 μg/ml,with a detection limit of 0.05 μg/ml. The pharmacodynamics process of rabbits fitted to one compartment model. The main kinetic parameters for the dose groups at 5,10,and 20 mg/kg were follows:Cmax were 2.28,3.35 and 7.93 μg/ml resp.; Tmax were 1.36,1.83 and 1.69 h respe.; t1/2Ka were 0.39,0.51 and 0.42 h resp.; t1/2Ke were 5.63,6.07 and 6.81 h resp.; AUC were 21.67,33.59 and 97.07 distributed to all tissues. [Conclusion] The gatifloxacin was rapidly absorbed in rabbits,with a longer t1/2Ke and extensive distribution,which is a new and effective fluoro-guinolone antibiotic that was worth to be extended.