期刊
AAPS PHARMSCITECH
卷 24, 期 1, 页码 -出版社
SPRINGER
DOI: 10.1208/s12249-022-02402-w
关键词
bioavailability; chitosan; enteric capsule; metformin hydrochloride; mucosal nanoparticles
资金
- National Natural Science Foundation of China
- Key Project of Natural Science Foundation for the Higher Education Institutions of Anhui Province [81973488, 22003002]
- Key Project of Key Laboratory of Xin'an Medicine (Anhui University of Chinese Medicine) [GXXT-2020-025(10-4), KJ2019A0451, KJ2020A0382]
- Ministry of Education
- [2020xayx02]
A metformin hydrochloride mucosal nanoparticles enteric-coated capsule (MH-MNPs-EC) was developed to improve the bioavailability and hypoglycemic effect duration of metformin hydrochloride for the treatment of type 2 diabetes. The capsule showed improved efficacy and prolonged residence time in the intestine compared to commercial metformin hydrochloride capsules.
Metformin hydrochloride enteric-coated capsule (MH-EC) is a commonly used clinical drug for the treatment of type 2 diabetes. In this study, we described a metformin hydrochloride mucosal nanoparticles enteric-coated capsule (MH-MNPs-EC) based on metformin hydrochloride chitosan mucosal nanoparticles (MH-CS MNPs) and its preparation method to improve the bioavailability and hypoglycemic effect duration of MH-EC. In intestinal adhesion study, the residue rates of free drugs and mucosal nanoparticles were 10.52% and 67.27%, respectively after cleaned with PBS buffer. MH-CS MNPs could significantly improve the efficacy of MH and promote the rehabilitation of diabetes rats. In vitro release test of MH-MNPs-EC showed continuous release over 12 h, while commercial MH-EC released completely within about 1 h in intestinal environment (pH 6.8). Pharmacokinetic study was performed in beagle dogs compared to the commercial MH-EC. The durations of blood MH concentration above 2 mu g/mL were 9 h for MH-MNPs-EC versus 2 h for commercial MH-EC. The relative bioavailability of MH-MNPs-EC was determined as 185.28%, compared with commercial MH-EC. In conclusion, MH-CS MNPs have good intestinal adhesion and can significantly prolong the residence time of MH in the intestine. MH-MNPs-EC has better treatment effect compared with MH-EC, and it is expected to be a potential drug product for the treatment of diabetes because of its desired characteristics.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据