五酯软胶囊对西罗莫司在大鼠体内药动学的影响
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篇名: | 五酯软胶囊对西罗莫司在大鼠体内药动学的影响 |
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摘要: | 目的:考察五酯软胶囊对西罗莫司在大鼠体内药动学的影响。方法:取Wistar大鼠随机分为5组,每组6只,分别按极低、低、中、高剂量(67、134、268、536 mg/kg) ig五酯软胶囊内容物或空白溶剂,0.5 h后再ig西罗莫司0.4 mg/kg。分别于西罗莫司给药前(0 h)和给药后0.5、0.75、1、1.5、2、2.5、3、4、6、8、12、24、36 h毛细管眼眶取全血100 μl于乙二胺四乙酸抗凝试管中,采用液相色谱-质谱联用法测定全血中西罗莫司的浓度,采用DAS 2.0药动学软件以非隔室模型计算药动学参数。结果:极低、低、中、高剂量组和溶剂对照组大鼠体内西罗莫司的药动学参数cmax为(6.79±1.15)、(17.40±3.13)、(21.24±3.14)、(22.06±4.82)、(2.80±0.72) ng/ml;t1/2为(11.01±0.82)、(12.20±2.02)、(12.28±2.38)、(12.36±0.73)、(10.59±0.69) h;AUC0-∞为(85.79±15.26)、(162.18±41.75)、(273.12±73.69)、(268.79±28.46)、(36.72±3.01) ng·h/ml。与溶剂对照组比较,极低、低、中、高剂量组大鼠体内西罗莫司的cmax 和AUC0-∞均升高,但t1/2变化不明显。结论:五酯软胶囊可明显促进西罗莫司在大鼠体内的吸收。 |
ABSTRACT: | OBJECTIVE: To investigate the effect of Wuzhi soft capsule on the pharmacokinetics of sirolimus in rats. METHODS: Wistar rats were randomly divided into 5 groups, with 6 rats in each group. They were given very low-dose, low-dose, medium-dose and high-dose of Wuzhi soft capsule (67, 134, 268 and 536 mg/kg) ig or blank solvent, respectively; and then given sirolimus 0.4 mg/kg. The blood 100 μl was sampled by capillary eyes before giving sirolimus (0 h) and 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 and 36 h after giving sirolimus and put into edetic acid anticoagulation tube. Blood concentration of sirolimus was assayed by LC-MS/MS. The pharmacokinetic parameter was calculated by DAS 2.0 software using non-compartment model. RESULTS: The pharmacokinetic parameters of sirolimus in very low-dose, low-dose, medium-dose and high-dose groups and blank solvent group were cmax of (6.79±1.15),(17.40±3.13),(21.24±3.14),(22.06±4.82),(2.80±0.72) ng/ml; t1/2 of (11.01±0.82),(12.20±2.02),(12.28±2.38),(12.36±0.73),(10.59±0.69) h; AUC0-∞ of (85.79±15.26),(162.18±41.75),(273.12±73.69),(268.79±28.46),(36.72±3.01) ng·h/ml, respectively. Compared with blank solvent group, cmax and AUC0-∞ of sirolimus were all increased in very low-dose, low-dose, medium-dose and high-dose groups, but t1/2 changed slightly. CONCLUSIONS: Wuzhi soft capsule can substantially enhance the absorption of sirolimus in rats. |
期刊: | 2016年第27卷第10期 |
作者: | 徐文,刘涛,付晓悦,曹志红,马敏,隋忠国 |
AUTHORS: | XU Wen,LIU Tao,FU Xiaoyue,CAO Zhihong,MA Min,SUI Zhongguo |
关键字: | 五酯软胶囊;西罗莫司;药动学;大鼠 |
KEYWORDS: | Wuzhi soft capsule; Sirolimus; Pharmacokinetics; Rats |
阅读数: | 474 次 |
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