Formulations Of Sustained Releaase Tablets Of Poorly Soluble Drug Carbamazepine By Melt Granulation Technique

In order to provides some reference data of formulations of sustained releaasetablets of poorly soluble drug using glyceryl behenate by melt granulation technique,the aim of this study was to investigate the influence of prescription variable andprocess parameters on druge release rate.Forthermore,it can also provides sometechnical supports and guidances for the application of the materials used for futureindustrial hot melt granulation. According to the principle of hot melt granulation,wedesigned and assembled laboratory equipment of melt granulation.Carbamazepine(CBZ) was chosen as the poorly soluble drug to make sustained releaase tablets eitherwith glyceryl behenate(Compritol888ATO) alone or with combinations of glycerylbehenate and hydroxypropyl methylcellulose(HPMC), and evalute how the levels andgrades of these excipients affect the drug release; The release rates of tables madeby three types of formulation techniques–melt granulation、wet granulation anddirect compression–were compared;The carbamazepine sustained-release tabletsbeing prepared the day and stored30days were evaluated by f2.When glycerylbehenate alone, adjusting the ratio of lactose and glyceryl behenate, does not exceed40%; When combining glyceryl behenate with HPMC, carbamazepine release rateshowed an increasing trend with the proportion of glyceryl behenate and HPMCviscosity decreasing; The cumulative release of carbamazepine prepared by the meltgranulation was about70%after12h and more than95%after24h;While, Thecumulative release of carbamazepine prepared by wet granulation and directcompression were more than90%after12h；Compared with the sustained-releasetablets prepared the day, f2values of tablets which stored for3days,7days and30days were82.72,72.87,76.00. The release rate of carbamazepine was negativelyassociated with the ratio of glyceryl behenate prescriptions accounted for acorrelation; Compared with the single application of glyceryl behenate, the releaserate was when adding the HPMC; the retarding effect of tablets made by meltgranulation was stronger than wet granulation and direct compression,which can beused to achieve the best result with the least Excipients,and can helps to reduce the cost of the formulation; As can be seen from the f2value, compared with thesustained-release tablets prepared the day, f2values of tablets which stored for30days is still bigger than50, indicating a little impact on the release rate of tabletstored30days.