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目的:研究盐酸哌甲酯(methylphenidate hydrochloride,MPH)速溶膜(oral fast dissolving films,OFDF)在大鼠体内的药动学。方法:12只大鼠随机分为MPH灌胃组(40 mg·kg-1)、MPH-OFDF舌下给药组(40 mg·kg~(-1))2组,每组6只。麻醉后分别给药并在不同时间点取血。采用高效液相色谱法测定大鼠血浆中MPH浓度,用DAS 2.1软件计算药动学参数,并用SPSS 20.0统计软件进行独立性t检验分析。结果:MPH灌胃组t1/2为(1.81±0.81)h,AUC0~4h为(3.49±0.42)mg·L~(-1)·h,tmax和Cmax分别为(0.58±0.13)h和(2.44±0.36)mg·L~(-1)。MPH-OFDF舌下给药组t1/2为(1.35±0.53)h,AUC0~4h为(15.36±0.53)mg·L~(-1)·h,tmax和Cmax分别为(0.33±0.13)h和(9.49±0.70)mg·L~(-1)。MPH-OFDF舌下组与MPH灌胃组相比,t1/2缩短,但无显著性差异,而tmax显著缩短(P<0.01),AUC0~4h和Cmax显著增大(P<0.01)。结论:与MPH口服给药相比,MPH-OFDF舌下给药吸收快,生物利用度有所提高。
OBJECTIVE: To study the pharmacokinetics of oral inulin dissolving films (OFDF) in rats by methylphenidate hydrochloride (MPH). Methods: Twelve rats were randomly divided into MPH group (40 mg · kg -1), MPH-OFDF group (40 mg · kg -1), two rats in each group. After anesthesia were administered and blood at different time points. MPH concentrations in rat plasma were determined by high performance liquid chromatography (HPLC). Pharmacokinetic parameters were calculated by DAS 2.1 software and SPSS 20.0 statistical software was used for independent t test. Results: The t 1/2 and t max of C group were (1.81 ± 0.81) h and (3.49 ± 0.42) mg · L -1 · h after AUC0 ~ 4h and (0.58 ± 0.13) h and 2.44 ± 0.36) mg · L -1. T1 / 2 was (1.35 ± 0.53) h in MPH-OFDF group, and (15.36 ± 0.53) mg · L -1 · h in AUC0-4h, and the values of tmax and Cmax were (0.33 ± 0.13) h And (9.49 ± 0.70) mg · L -1, respectively. In MPH-OFDF group, t1 / 2 shortened compared with MPH group, but there was no significant difference between the two groups (P <0.01). CONCLUSIONS: MPH-OFDF is absorbed sublingual and has improved bioavailability compared to oral administration of MPH.