摘要
目的 :进行琥珀酸罗哌卡因和盐酸罗哌卡因的药物生物等效性比较。方法 :静脉给予家兔琥珀酸罗哌卡因和盐酸罗哌卡因 (按罗哌卡因游离碱计均为 6 .3mg/kg)后 ,用 HPL C法测定血清中的罗哌卡因游离碱含量 ,进行药物的生物等效性比较。以 C1 8柱为固定相 ,流动相为乙腈 - 0 .2 mol/L 硫酸胺 [30∶ 70 ( V/V) ],流速为 1ml/min,检测波长 2 15 nm。结果 :盐酸罗哌卡因组给药后主要的药代动力学参数 :峰浓度为 ( 2 .37± 0 .35 )μg/ml,[t1 / 2 ]α 和 [t1 / 2 ]β分别为 ( 13.96±5 .0 7)和 ( 6 8.6 8± 13.0 2 ) min;AUC0～∞ 为 78.5 3μg· min/ml( 95 %可信限 :6 0 .0 4～ 93.12 )。琥珀酸罗哌卡因组的主要药代动力学参数 :峰浓度为 ( 2 .72± 0 .38)μg/ml,[t1 / 2 ]α和 [t1 / 2 ]β分别为 ( 13.6 7± 9.32 )和 ( 6 2 .4 8± 19.2 3) min;AUC0～∞ 为73.15 μg· min/ml( 95 %可信限 :6 5 .18～ 78.4 9)。用方差分析和双向单侧 t-检验法考察结果并进行统计学分析 ,琥珀酸罗哌卡因相对于盐酸罗哌卡因的生物利用度 ( F)为 97.2 %。结论 :静脉给予琥珀酸罗哌卡因与盐酸罗哌卡因后 。
Object To study the bioequivalence of ropivacaine chelidoninic acid and ropivacaine hydrochloride in rabbits. Methods A single intravenous dose of 6 3 mg/kg (free base of ropivacaine), ropivacaine chelidoninic acid or ropivacaine hydrochloride was given to rabbits. The plasma concentrations were determined by HPLC. The extract was analyzed subsequently on C 18 column with 0.2 mol/L ammoniasulfate acetonitrile (70∶30) as mobile phase, the flow rate 1 0 ml/min, and detected at 215 nm. Results The concentration time curves of ropivacaine chelidoninic acid or ropivacaine hydrochloride were fitted to two compartment open models. The main pharmacokinetic parameters were : Cmax(2.37±0 35)and (2.72±0.38)μg/ml; AUC 73.15 and 78.53 μg·min/ml, respectively. The pharmacokinetic parameters obtained showed no significant difference between the two products (P>0.05). The relative bioequivalence of ropivacaine chelidoninic acid versus ropivacaine hydrochloride was 97.2%. Conclusion The results suggested that the pharmacokinetic characteristics of the two preparations were similar.
出处
《天津药学》
2004年第2期7-9,共3页
Tianjin Pharmacy
