摘要
为了解决阿苯达唑的溶解性和口服吸收难题,借助高分子活性剂的稳定作用,利用反溶剂法-高压匀质法制备阿苯达唑纳米混悬剂,并考察该制剂的药学特征及稳定性,研究该制剂在大鼠体内的药代动力学特征。研究创制的纳米混悬液在电镜下药物形状大小均一,中位粒径为358.1 nm。其药学特征符合中国《兽药质量标准》(2017版)中对混悬液的质量要求。稳定性试验表明,6个月加速考察该制剂外观、色泽、含量、pH值、沉降体积比、重分散性均未发生明显变化。大鼠单剂量(45 mg/kg bw)口服阿苯达唑纳米混悬液的C_(max)为5.895μg/mL,显著高于参比制剂阿苯达唑伊维菌素粉、佛山正典阿苯达唑混悬液的2.804和2.053μg/mL。与阿苯达唑伊维菌素粉、佛山正典阿苯达唑混悬液相比,该制剂的相对生物利用度分别为214%和299.74%,表明该阿苯达唑纳米混悬液能显著提高阿苯达唑的吸收,将有助于提高临床治疗效果。
In order to solve the problem of the solubility and oral absorption of albendazole,with the help of the stabilizing effect of polymer active agent,this paper adopts the anti-solvent and high pressure homogenization technology,preparation of albendazole nanosuspension.Then,to investigate the pharmaceutical characteristics and stability of the preparation,and evaluate the pharmacokinetics of the preparation in rats.The albendazole nanosuspension was uniform in shape and size under the scanning electron microscope,and the median particle size was 358.1 nm.The test results of albendazole nanosuspension characteristics meet with the quality requirement of the suspension agent in China Quality Standards for Veterinary Drugs(2017 Edition).The stability test showed that the appearance,color,content,pH value,sedimentation volume ratio,and redispersibility of the preparation did not change significantly after 6-month accelerated inspection.The Cmax of a single-dose oral albendazole nanosuspension(45 mg/kg bw)in rats was 5.895μg/mL,which was significantly higher than the reference preparation albendazole-ivermectin powder and Foshan zhengdian albendazole suspension,those Cmax were 2.804μg/mL and 2.053μg/mL.Compared with albendazole-ivermectin powder and Foshan zhengdian albendazole suspension,the relative bioavailability of the albendazole nanosuspension was 214%and 299.74%,respectively;therefore the albendazole nanosuspension can significantly improved the absorption of albendazole in vivo,which will result in a significant promote of albendazole in the clinical treatment effect.
作者
田凯
许丹
卢迪
谢书宇
赵宝凯
TIAN Kai;XU Dan;LU Di;XIE Shu-yu;ZHAO Bao-kai(Shenyang Vica Animal Biotechnology Technology Co.,Ltd,Shenyang 110020,China;Huangzhong Agricultural University,Wuhan 430070,China)
出处
《中国兽药杂志》
2022年第7期60-67,共8页
Chinese Journal of Veterinary Drug
关键词
阿苯达唑
纳米晶体
混悬液
药动学
生物利用度
albendazole
nanocrystals
suspension
pharmacokinetics
bioavailability
