Formulation Development and Invitro Evaluation of Gliclazide Pellets using Superdisintegrants by Extrusion Spheronization Technique

Abstract

Introduction: Gliclazide is a sulfonylurea derivative used for the treatment of type 2 Diabetes, it is an anti-diabetic drug it is marketed under the brand name Diamicron. It is taken orally and used when dietary changes, lack of exercise, and weight loss are not sufficient.  Aim: The principal objective of this work was to develop, formulate and evaluate the pellet formulations prepared with the incorporation of different super disintegrants in different ratios and in different combinations. In this research work, the drug gliclazide was chosen as a model drug and it was formulated into fast-dissolving pellets, which can be compressed into pelltabs and can also be filled into capsules.  Methods: Pellets were prepared by extrusion and Spheronization containing microcrystalline cellulose (MCC) and using gliclazide as a model drug with different super disintegrants namely croscarmellose sodium, crospovidone and sodium starch glycolate in different ratios, and in different combinations. Thus, in the present study, gliclazide pellets were developed using Extrusion-Spheronization for immediate drug delivery. The pellets were evaluated for percentage drug content, flow properties, friability, size analysis, shape analysis, disintegration test, and dissolution studies. Preformulation studies were then performed using solubility studies, partition co-efficient studies, infrared spectroscopy, and drug-excipients compatibility studies between the drug and selected excipients (croscarmellose sodium, crospovidone, and sodium starch glycolate) investigated. Results: Formulations containing MCC, super disintegrants, and drugs in different ratios of 60/0/40, 55/5/40, and 50/10/40 w/w of croscarmellose sodium, crospovidone, and sodium starch glycolate were found to show faster release of            the drug for 9 hours. Croscarmellose sodium releases the drug as it disintegrates the  pellets. Sodium starch glycolate releases the drug by inducing swelling in the pellet  matrix. Unlike the other two super disintegrants, there was no apparent change in the swelling capability of the pellets of polymer crospovidone (Polyplasdone XL10) in water. The percentage increase in diameter for Ac-Di-Sol (croscarmellose sodium), Primojel (sodium starch glycolate), and Polyplasdone XL10 were 104%, 251%, and 29% in water. Conclusions: Various types of super disintegrants can be investigated for their suitability in formulating pellets. In vivo drug release rate, and bioavailability studies on animals and humans may be carried out to assess the superiority of the pellets over the tablet dosage form.