阿苯达唑纳米微粉在大鼠体内的药动学研究
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篇名: 阿苯达唑纳米微粉在大鼠体内的药动学研究
TITLE:
摘要: 目的:研究阿苯达唑(ABZ)纳米化后在大鼠体内的药动学变化,为ABZ纳米制剂的进一步研发奠定基础。方法:将16只大鼠随机分为ABZ原料药组(ABZ原料药混悬液)与ABZ纳米微粉组(ABZ纳米微粉混悬液),每组8只,ig给药,剂量为63 mg/kg。各组大鼠于给药0.5、1、2、4、8、12、24、36、48、72 h后眼眶采血0.2~0.3 ml,以甲苯咪唑为内标,采用反相高效液相色谱法(RP- HPLC)测定各时间点药物血药浓度,并采用3p97药动学软件拟合药动学参数。结果: ABZ原料及纳米微粉在大鼠体内的药动学符合二室模型,ABZ原料药组、ABZ纳米微粉组大鼠的cmax分别为(3.20±1.41)、(6.11±0.74) μg/ml,tmax分别为(3.42±0.91)、(3.15±0.27) h, t1/2分别为(7.53±1.20)、(6.26±0.85) h,AUC0-72 h分别为(49.90±15.50) 、(78.36±8.78) μg·h/ml,AUC0-∞分别为(52.30±10.10)、(80.27±8.26) μg·h/ml。与ABZ原料药组比较,ABZ纳米微粉组大鼠的cmax、AUC0-72 h、AUC0-∞均显著升高(P<0.05)。结论:ABZ纳米化后在一定程度上提高了药物的吸收速率,增加了药物的吸收,提高了ABZ的口服生物利用度。
ABSTRACT: OBJECTIVE: To study the pharmacokinetic change of albendazole (ABZ) in rats after nanocrystallization, and to lay a foundation for further study of ABZ nano-preparation. METHODS: 16 rats were randomly divided into ABZ raw material (ABZ suspension) group and ABZ nano-powder (ABZ nano-powder suspension) group, with 8 rats in each group. They were given relevant medicine 63 mg/kg intragastrically. 0.2-0.3 ml blood samples were collected from orbital cavity 0.5, 1, 2, 4, 8, 12, 24, 36, 48, 72 h after medication, respectively. Using mebendazole as internal standard, blood concentration of ABZ were determined by RP-HPLC, and pharmacokinetics parameters were calculated by using 3p97 software. RESULTS: The pharmacokinetics of ABZ raw material and ABZ nano-powder in rats were in line with two-compartment model. The main pharmacokinetic parameters of ABZ raw material group vs. ABZ nano-powder group were as follows as cmax (3.20±1.41) μg/ml vs. (6.11±0.74) μg/ml; tmax (3.42±0.91) h vs. (3.15±0.27) h; AUC0-72 h (49.90±15.50) μg·h/ml vs. (78.36±8.78) μg·h/ml; AUC0-∞ (52.30±10.10 ) μg·h/ml vs. (80.27±8.26) μg·h/ml. Compared with ABZ raw material group, cmax, AUC0-72 h and AUC0-∞ of ABZ nano-powder group were increased significantly (P<0.05). CONCLUSIONS: The nanocrystallization of ABZ can enhance the absorbability rate and improve the absorption of drugs to some extent, and it also improves oral bioavailability of ABZ.
期刊: 2016年第27卷第34期
作者: 马运芳,王建华,陈迹,任洁如
AUTHORS: MA Yunfang,WANG Jianhua,CHEN Ji,REN Jieru
关键字: 阿苯达唑;纳米微粉;药动学;大鼠
KEYWORDS: Albendazole; Nano-powder; Pharmacokinetics; Rats
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