Gliclazide Microcrystals Prepared by Two Methods of In Situ Micronization: Pharmacokinetic Studies in Diabetic and Normal Rats
- 5 May 2010
- journal article
- research article
- Published by Springer Science and Business Media LLC in AAPS PharmSciTech
- Vol. 11 (2), 786-792
- https://doi.org/10.1208/s12249-010-9441-9
Abstract
The low water-solubility of gliclazide (GL) leads to a low dissolution rate and variable bioavailability. The aim of this study was to investigate the effect of micronization on the absorption and pharmacokinetics of GL after oral administration in rats. GL microcrystals were prepared using solvent-change and pH-shift methods. Scanning electron microscopy showed considerable changes in the shape and size of crystals using both methods. In the optimized formulation of each method, the particle size of treated GL was reduced about 30 (from 290 to 9.9 μm) and 61 times (to 4.76 μm) by solvent-change and pH-shift methods, respectively. Recrystallized samples showed faster dissolution rate than untreated GL particles. Glucose-lowering effect, C max, and area under the drug concentration-time profile (area under the curve (AUC)) were compared in diabetic and normal rats. AUC and C max were increased by microcrystals in both groups of animals. Administration of 40 mg/kg of GL in the form of untreated drug and microcrystals obtained by solvent-change and pH-shift methods caused 12.49% and 21.04% enhancement in glucose-lowering effect of GL in diabetic rats, respectively.Keywords
This publication has 33 references indexed in Scilit:
- Micronization of atorvastatin calcium by antisolvent precipitation processInternational Journal of Pharmaceutics, 2009
- Applying the Taguchi Design for Optimized Formulation of Sustained Release Gliclazide Chitosan Beads: An In Vitro/In Vivo StudyAAPS PharmSciTech, 2009
- Dissolution enhancement of gliclazide using in situ micronization by solvent change methodPowder Technology, 2008
- Hypoglicemic effect of Leandra lacunosa in normal and alloxan-induced diabetic ratsFitoterapia, 2008
- Microcrystallization of indomethacin using a pH-shift methodInternational Journal of Pharmaceutics, 2003
- THEIN VIVOINTERACTION BETWEEN GLICLAZIDE AND GLIBENCLAMIDE AND INSULIN ON GLUCOSE DISPOSAL IN THE RATPharmacological Research, 1999
- Study of the inclusion of gliclazide in α-cyclodextrinJournal of Pharmaceutical and Biomedical Analysis, 1998
- Nuclear Magnetic Resonance Investigations of the Inclusion Complexation of Gliclazide with β-CyclodextrinJournal of Pharmaceutical Sciences, 1997
- Enhancement of dissolution of glyburide by solid dispersion and lyophilization techniquesInternational Journal of Pharmaceutics, 1995
- GliclazideDrugs, 1993