IN-VIVO EVALUATION OF GLICLAZIDE SOLID DISPERSIONS INCORPORATED TABLETS FOR CONTROLLED DRUG RELEASEAbstract
Gliclazide is an anti-diabetic medication used to treat diabetes mellitus type 2.It suffers from deprived solubility, reduced drug dissolution, and bioavailability. The current paper is aimed to formulate and evaluate gliclazide solid dispersion with HP β Cyclodextrin for enhanced solubility and incorporate into controlled-release tablet formulation. Gliclazide solid dispersion (SD) was prepared using varying ratios of HP β Cyclodextrin and evaluated. The optimized SD formulation was incorporated into the tablet by using hydroxypropyl cellulose and HPMC K 100M. The formulation SD 3 was chosen based on solubility and evaluation parameters, hence formulated into a controlled release matrix tablet formulation. Around 15 formulations of controlled release tablet blends evaluated for micrometric properties demonstrate that all the formulations posses good flow properties. The controlled release tablet formulation F15 with maximum drug content of 99.99% and drug dissolution of 99.96 % over 16h was chosen optimal and characterized. In-vivo bioavailability studies of optimized formulation (F15) and marketed products are performed on rabbits. The Cmax of the optimized formulation (132.56 ± 0.08ng/ml) was higher than the marketed product (98.73±0.063ng/ml), Tmax of F15 and marketed product were found to be 6 and 4 h, respectively. AUC0-∞ infinity for F15 formulation was higher (464.21 ± 1.47ng.h/ml) than the gliclazide marketed formulation (353.8±0.82ng.h/ml). Statistically, AUC0-t of the controlled release solid dispersion formulation was significantly higher (p<0.05) as compared to the Gliclazide marketed product formulation. The combination of SD and controlled release formulations of Gliclazide can facilitate prolonged action with better solubility, bioavailability, and greater patient acceptance.
Ramisetty Sunitha *, K. Venugopal and S. V. Satyanarayana
Department of Pharmaceutical Sciences, R & D, Jawaharlal Nehru Technological University, Anantapuramu, Andhra Pradesh, India.
11 September 2020
15 November 2021
27 January 2022
01 May 2022