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目的考察不同给药途径苦参碱注射液在大鼠体内的药动学。方法 20只健康SD大鼠,随机分为两组,分别单剂量腹腔和尾静脉注射15 mg·kg~(-1)的苦参碱注射液。分别于给药前及给药后0.033、0.083、0.167、0.333、0.5、0.75、1、2、3、4、6、8、12 h分别采集静脉血0.3~0.4 m L。采用LC-MS/MS测定血浆样品中苦参碱的血药浓度,并计算主要的药动学参数。结果单剂量腹腔和尾静脉注射15 mg·kg~(-1)的苦参碱注射液后AUC0~(-1)2分别为(10 166±2 426)和(12 217±2 968)ng·m L~(-1)·h;AUC0-∞分别为(10 230±2 432)和(12 300±3 031)ng·m L~(-1)·h;MRT0~(-1)2分别为(1.91±0.41)和(2.14±0.54)h,MRT0-∞分别为(2.01±0.41)和(2.26±0.64)h;t1/2分别为(2.26±0.89)和(2.60±1.25)h,Vd分别为(4 998±2 010)和(6 175±2 540)m L;CL分别为(1 531±315.0)和(1 727±475.6)m L·h~(-1)·kg~(-1);ρmax分别为(5 246±1 187)和(8 503±1 101)ng·m L~(-1)。腹腔注射的生物利用度为83.21%。结论比较腹腔和尾静脉注射2种给药途径时苦参碱的药动学参数,AUC、MRT、t1/2和CL均无统计学差异,ρmax和Vd比较具有统计学差异。
Objective To investigate the pharmacokinetics of matrine injection in rats by different route of administration. Methods Twenty healthy SD rats were randomly divided into two groups. A single dose of 15 mg · kg -1 matrine was injected intraperitoneally into the tail vein. Venous blood 0.3 ~ 0.4 m L were collected before administration and after administration respectively at 0.033,0.083,0.167,0.333,0.5,0.75,1,2,3,4,6,8,12 h. Plasma concentrations of matrine in plasma samples were determined by LC-MS / MS and the main pharmacokinetic parameters were calculated. Results AUC0 ~ (-1) 2 was (10 166 ± 2 426) and (12 217 ± 2 968) ng · (-1) after intraperitoneal and tail vein injection of 15 mg · kg -1 matrine injection m L -1 h -1 and AUC 0 -∞ were (10 230 ± 2 432) and (12 300 ± 3 031) ng · m L -1 h respectively; MRT 0 -1 (2.01 ± 0.41) and (2.26 ± 0.64) h for (1.91 ± 0.41) and (2.14 ± 0.54) h respectively, and (2.26 ± 0.89) and (2.60 ± 1.25) Vd were (4 998 ± 2 010) and (6 175 ± 2 540) m L, respectively; CL was (1 531 ± 315.0) and (1 727 ± 475.6) m L · h -1 · kg ~ -1); ρmax were (5 246 ± 1 187) and (8 503 ± 1 101) ng · m L -1, respectively. The bioavailability of intraperitoneal injection was 83.21%. Conclusions The pharmacokinetic parameters of matrine, AUC, MRT, t1 / 2 and CL are not statistically different between the two routes of intraperitoneal and tail vein injection. The difference between ρmax and Vd is statistically significant.