豆腐果苷缓释片的研制及在Beagle犬体内的药动学  

Preparation and Pharmacokinetics in Beagle Dogs of Helicid Sustained-release Tablets

作　　者：李红莲 舒婷 刘源[1] 刘涛[1] 孙文霞[1] LI Honglian;SHU Ting;LIU Yuan;LIU Tao;SUN Wenxia(Engineering Research Center for Pharmaceuticals and Equipments of Sichuan Province,Sichuan Industrial Institute of Antibiotics,School of Pharmacy,Chengdu University,Chengdu 610052)

机构地区：[1]成都大学药学院,四川抗菌素工业研究所,四川省药物制剂及装备工程技术研究中心,四川成都610052

出　　处：《中国医药工业杂志》2022年第8期1162-1166,共5页Chinese Journal of Pharmaceuticals

基　　金：四川省科技厅应用基础项目(2018JY0592)、省级大学生创新创业大赛资助项目(S202111079134S)。

摘　　要：为延长豆腐果苷在体内的作用时间、减少给药次数,以羟丙甲纤维素和卡波姆为骨架材料,采用湿法制粒制备豆腐果苷缓释片,并考察了该缓释片的体外释放及在Beagle犬体内的药动学过程。体外释放结果表明,豆腐果苷缓释片在去离子水中10 h累积释放率为98.3%,释放行为符合Higuchi方程(r=0.9982)。Beagle犬体内药动学结果显示,缓释片与普通片的AUC_(0→∞)、c_(max)、t_(1/2)分别为(1.665±0.264)和(1.552±0.076)μg·ml^(–1)·h、(0.46±0.05)和(1.24±0.12)μg/ml、(5.29±2.30)和(0.57±0.12)h。上述试验结果表明,豆腐果苷缓释片具有明显的缓释特征,减小了血药浓度波动。To prolong action time and reduce administration frequency,helicid sustained-release tablets were prepared by wet granulation with hypromellose and carbomer as the matrix materials.And the in vitro release and pharmacokinetics in Beagle dogs were investigated.The results of in vitro release test showed that the cumulative release at 10 h in deionized water reached 98.3%,and Higuchi equation fit the release data of helicid well(r=0.9982).The pharmacokinetics was carried out in Beagle dogs.The parameters AUC_(0→∞),c_(max),t_(1/2)for the sustained-release tablets and the common tablets were as follows:(1.665±0.264)and(1.552±0.076)μg·ml^(–1)·h,(0.46±0.05)and(1.24±0.12)μg/ml,(5.29±2.30)and(0.57±0.12)h,respectively.The above results showed that helicid sustained-release tablets had an obvious sustained-release characteristics and reduced the fluctuation of blood drug concentration.

关 键 词：豆腐果苷 缓释片 羟丙甲纤维素 体外释放 药动学 

分 类 号：R944.4[医药卫生—药剂学]