title: Enhancement of solubility and antidiabetic effects of Repaglinide using spray drying technique in STZ-induced diabetic rats.
abstract: The purpose of the study was to enhance the solubility of the poorly water-soluble drug, Repaglinide using spray drying based solid dispersion technique by different carriers including Eudragit E100, hydroxyl propyl cellulose Mw 80 000 and poly vinyl pyrollidone K30. Optimization of the best formulation was carried out according to drug solubility, release profile, particle size and angle of repose of the solid dispersions. The optimized sample was characterized using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). The morphology of the dispersions was studied by SEM. The blood glucose lowering effect of spray dried solid dispersions was studied in normal and streptozocin-induced diabetic rats. The results showed that Eudragit E100 in 1:3 ratio could enhance drug solubility by 100-fold. DSC studies indicated a marked change in melting point of the drug possibly due to strong hydrogen bonds between the drug and Eudragit, while FT-IR study did not show obvious interactions between them. According to XRPD results Repaglinide converted to an amorphous state in the spray dried dispersions. Spray dried Repaglinide reduced the blood glucose level significantly during the 8 h of obtaining blood samples in comparison with untreated drug (p < 0.05).
authors.affiliation: a Novel Drug Delivery Systems Research Center, Department of Pharmaceutics , School of Pharmacy, Isfahan University of Medical Sciences , Isfahan , Islamic Republic of Iran and.
authors.forename: Jaleh
authors.initials: J
authors.lastname: Varshosaz
authors.affiliation: b Department of Pharmacology , School of Pharmacy, Isfahan University of Medical Sciences , Isfahan , Islamic Republic of Iran.
authors.forename: Mohsen
authors.initials: M
authors.lastname: Minayian
authors.affiliation: a Novel Drug Delivery Systems Research Center, Department of Pharmaceutics , School of Pharmacy, Isfahan University of Medical Sciences , Isfahan , Islamic Republic of Iran and.
authors.forename: Mahdieh
authors.initials: M
authors.lastname: Ahmadi
authors.affiliation: a Novel Drug Delivery Systems Research Center, Department of Pharmaceutics , School of Pharmacy, Isfahan University of Medical Sciences , Isfahan , Islamic Republic of Iran and.
authors.forename: Erfaneh
authors.initials: E
authors.lastname: Ghassami
mesh_terms: D000818:Animals; D002152:Calorimetry, Differential Scanning; D002219:Carbamates / Q000008:administration & dosage / Q000737:chemistry; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000737:chemistry; D010880:Piperidines / Q000008:administration & dosage / Q000737:chemistry; D051381:Rats; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D002219:Carbamates; D007004:Hypoglycemic Agents; D010880:Piperidines; C072379:repaglinide
keywords: Diabetic rats; Eudragit E100; Repaglinide; solid dispersion; spray drying