CONTRIBUTION OF WAXES ON GRANULATION AND COMPRESSION OF NONCOMPRESSABLE DRUG:TABLETTING, DRUG RELEASE AND PHYSICO-CHEMICAL STRUCTURE

Abstract

Tablets were pressed under constant condition from different paracetamol granules prepared using either SA or GMS (part one). The Pharmacopeal and non-Pharamcopeal tests were carried out and the results showed that it depends on the type and concentration of granulating agent used. I.R. scan showed no chemical interaction between the drug and either SA or GMS. Powder x-ray diffraction showed there is change in the crystallinety of the drug which is depending on the the type and the concentration of the granultaing agent used. The drug release indicated there is no burst effect. There was nearly complete drug release on using SA as granulating agent while the use of GMS led incomplet drug release. In every case the drug release rate is depending on the concentration of the antiaggregating agent used. The release kientics from all tablets did not follow zero oder except that from tablet prepared on using 5% GMS. The application of first order kinetics showed one phase release peroid from tablet prepared on using SA as granulating agent and two Phases peroids from tablet prepared on using GMS. The same results obtained on applying Hixsion-Crowell model. All release data from different tablets which prepared from different products followed the krosmeyer-peppes model with n value indicating that the drug release is non-Fickian mechanism. All of obtained result could be explained as a result of the mechanism of the granulating agent used. From the results and because of using much lower concentrations of either SA or GMS, it is clear the efficiencies of the preparation technique over mixing melting waxes with the drug especially the highest amount of initial drug released is only 10% from the total amount of drug in the tablet which can not considered as burst effect. It can also concluded that both granulating agents used are effective in the conversion of noncomprisable drug to comprisable one without any change in the chemical properties of the drug.