溴新斯的明多囊脂质体在大鼠体内的药动学研究
发布时间：2019-06-06 01:13
【摘要】：目的研究溴新斯的明多囊脂质体(neostigmine bromide multivesicular liposomes,NB-MVLs)与溴新斯的明(neostigmine bromide,NB)注射剂在大鼠体内的药物代谢动力学。方法12只健康大鼠,雌雄各半,随机分为2组,分别单次皮下注射给予SD大鼠NB-MVLs或NB注射剂(0.15 mg/kg)。采用反相高效液相色谱法测定不同时间点大鼠血浆中NB的浓度,计算药动学参数并进行生物等效性分析。结果 NB-MVLs与NB注射剂给药后,测得药时曲线下面积分别为(35.56±4.62)mg·h·L-1和(15.97±5.22)mg·h·L-1,峰浓度(Cmax)分别为(2.49±0.31)mg/L和(4.61±0.91)mg/L,达峰时间(Tmax)分别为(2.40±0.89)h和(0.45±0.11)h,半衰期分别为(15.14±6.81)h和(1.79±0.27)h,AUC0-t、AUC0-∞及Cmax采用DAS 2.1.1软件进行双单侧t检验和[1-2α]90%可信区间考察,Tmax采用Wilcoxon非参数检验,生物等效性分析结果表明NB-MVLs与NB具有生物不等效性。结论将NB制成多囊脂质体后,生物利用度明显提高,释放药物平稳缓慢,NB-MVLs与NB具有生物不等效性。
[Abstract]:Objective to study the pharmacokinetics of (neostigmine bromide multivesicular liposomes,NB-MVLs and neostigmine bromide,NB injection in rats. Methods Twelve healthy rats, half male and half female, were randomly divided into two groups. SD rats were given NB-MVLs or NB injection (0.15 mg/kg). The concentration of NB in plasma of rats at different time points was determined by reversed-phase high performance liquid chromatography (RP-HPLC). The pharmacokinetics parameters were calculated and the bioequivalence was analyzed. Results after administration of NB-MVLs and NB injection, the area under the curve was (35.56 卤4.62) mg 路h 路L-1 and (15.97 卤5.22) mg 路h 路L-1, respectively. The peak concentration (Cmax) was (2.49 卤0.31) mg/L and (4.61 卤0.91) mg/L, respectively. The (Tmax) was (2.40 卤0.89) h and (0.45 卤0.11) h, respectively. The half-lives were (15.14 卤6.81) h and (1.79 卤0.27) h, respectively. AUC _ 0 and Cmax were tested by DAS 2.1.1 software for double unilateral t test and [1 鈮，
本文编号：2493956
[Abstract]:Objective to study the pharmacokinetics of (neostigmine bromide multivesicular liposomes,NB-MVLs and neostigmine bromide,NB injection in rats. Methods Twelve healthy rats, half male and half female, were randomly divided into two groups. SD rats were given NB-MVLs or NB injection (0.15 mg/kg). The concentration of NB in plasma of rats at different time points was determined by reversed-phase high performance liquid chromatography (RP-HPLC). The pharmacokinetics parameters were calculated and the bioequivalence was analyzed. Results after administration of NB-MVLs and NB injection, the area under the curve was (35.56 卤4.62) mg 路h 路L-1 and (15.97 卤5.22) mg 路h 路L-1, respectively. The peak concentration (Cmax) was (2.49 卤0.31) mg/L and (4.61 卤0.91) mg/L, respectively. The (Tmax) was (2.40 卤0.89) h and (0.45 卤0.11) h, respectively. The half-lives were (15.14 卤6.81) h and (1.79 卤0.27) h, respectively. AUC _ 0 and Cmax were tested by DAS 2.1.1 software for double unilateral t test and [1 鈮，
本文编号：2493956
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