OPTIMIZATION OF EUDRAGIT OR CELLULOSIC POLYMERS-IBUPROFEN SUSTAINED RELEASE SYSTEMS USING PRINCIPAL COMPONENT ANALYSIS

Document Type : Original Article

Authors

1 Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt

2 Faculty of Pharmacy, Louis Pasteur University, France

Abstract

In order to retard the release of ibuprofen from its prepared tablets Eudragit polymers including Eudragit L100, Eudragit RS, Eudragit RLPM and Eudragit RSPM as well as cellulosic polymers including ethyl cellulose 20, hydroxyl propyl-methyl cellulose 606 (Pharmacoat 606) and hydroxyl propyl-methyl cellulose phthalate 55 (HP 55 f) have been used as granulating agents and excipients. The principal component analysis helped to investigate 13 variables on 23 formulae (ibuprofen granulated with Eudragit polymers) and 10 variables on 31 formulae (ibuprofen granulated with cellulosic polymers). It was possible by this method to represent all the relations existing between the 13 and 10 variables on simple circles of correlations. These variables include: concentration of the drug, concentration of the polymer, dissolution of the drug at pH 1.5 and pH 7.5, the tablet breaking strength, the tablet friability, the tablet hardness/friability ratio, the time of 50 and 80% drug release, the drug release rate constant of first order kinetic at pH 1.5 and pH 7.5, the drug release rate constant of Higuchi equation and dissolution efficiency.
Principal component analysis allowed to separate the formulae according to their compression characteristics, the dissolution efficiency, the kinetic parameters, the quality and the best choosing polymer for the retardation of ibuprofen and choosing the preferable excipient for the sustained release formulations. Dissolution was identified as the predominant parameter of the system next by compression characteristics.
From the principal component analysis investigations, it could be concluded that the formula of ibuprofen granulated with 15% Eudragit RSPM and containing 23% Avicel pH 102 and the formula granulated with 3% ethyl cellulose 20 and containing 23% Avicel pH 102 were found to be the optimum formulae.