title: A simple and effective method to improve bioavailability of glimepiride by utilizing hydrotropy technique.
abstract: The purpose of this study was to improve the solubility and bioavailability of glimepiride (GLMP) by utilizing hydrotropy technique. Meglumine (MU) as a hydrotrope could form the stable complex with glimepiride. The optimal glimepiride and meglumine (GLMP-MU) complex powder was obtained by using lyophilization. GLMP-MU powder was characterized by Fourier transform infrared spectroscopy (FT IR), X-ray powder diffraction (XRD) and differential scanning calorimetry (DSC). The formation of hydrogen bond between glimepiride and meglumine was confirmed by FT IR. The XRD studies indicated the amorphous state of glimepiride was appeared in the GLMP-MU. The DSC results were further confirmed GLMP-MU complex was prepared successfully. Moreover, the in vitro drug release rate of GLMP-MU powder was dramatically faster than that of glimepiride. Meanwhile, the AUC of GLMP-MU solution at an i.g./or i.v. dose of 5mg/kg in rat was significantly higher than that of the glimepiride suspensions. Together our results showed that hydrotropy technique was a simple and effective method to increase the solubility of glimepiride.
authors.affiliation: College of Pharmacy & Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China.
authors.forename: Haiying
authors.initials: H
authors.lastname: Li
authors.affiliation: College of Pharmacy & Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China.
authors.forename: Lilan
authors.initials: L
authors.lastname: Ma
authors.affiliation: College of Pharmacy & Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China.
authors.forename: Xiaxia
authors.initials: X
authors.lastname: Li
authors.affiliation: College of Pharmacy & Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Cui
authors.affiliation: College of Pharmacy & Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China. Electronic address: wenzhi_yang@sina.com.
authors.forename: Wenzhi
authors.initials: W
authors.lastname: Yang
authors.affiliation: College of Pharmacy & Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China.
authors.forename: Shigang
authors.initials: S
authors.lastname: Shen
authors.affiliation: Institute of Biomedical and Pharmaceutical Technology, Fuzhou University, Fuzhou 350108, China. Electronic address: ibptcmm@fzu.edu.cn.
authors.forename: Mingmao
authors.initials: M
authors.lastname: Chen
mesh_terms: D000818:Animals; D001682:Biological Availability; D005260:Female; D007004:Hypoglycemic Agents / Q000493:pharmacokinetics*; D033362:Powder Diffraction; D051381:Rats; D017208:Rats, Wistar; D017550:Spectroscopy, Fourier Transform Infrared; D013453:Sulfonylurea Compounds / Q000493:pharmacokinetics*
chemical_list: D007004:Hypoglycemic Agents; D013453:Sulfonylurea Compounds; C057619:glimepiride
keywords: Bioavailability; Complex; Glimepiride; Hydrotropy technique; Meglumine