The Study Of Gliclazide Oral Controlled (Sustained) Release Formulations

Gliclazide (GL) was an oral antihyperglycaemic agent widely used in the management of non-insulin-dependent diabetes mellitus (NIDDM or type-2 diabetes). Based on the investigations of the character of the drug and the excipients, gliclazide sustained release tablets, bi-layer osmotic pump tablets and sustained release pellets were prepared by different pharmaceutical technologies.According to the dissolution profile of the market sale products, by chosing lactose, two kinds of HPMC as the experiment factors, the formulation of gliclazide sustained release tablets was optimized through orthogonal experiment design. The dissolution profiles of the market sale tablet and self-made tablet were evaluated through similar factor f₂. The f₂ value was 84 and indicated they had the similar dissolution behavior. The dissolution profiles were almost the same in different media and at different rotation speed. Gliclazide sustained release tablets conformed to the first-order release model.In this paper, the formulation of tablet core, coating membrane, preparation technology and in vitro drug release environment were all fully investigated to get the best drug release formulation for Gliclazide bi-layer osmotic pump tablets. Used the similar factor F₂ to evaluate the formulation dissolution bahaviour. The effects of many factors including formulation of drug layer, push layer and membrane, hardness of tablet and the condition of drug release on the release behavior of controlled release tablets were investigated.The results indicated the following conclusion: For the drug containing layer, the molecular weight of PEO, the amount of lactose, the quantity of the HPMC and the drug containing amount had effect on the drug release behavior, and the amount of PVP had no effect on the drug release behavior. For the push layer, the molecular weight and quantity of...