FORMULATION DESIGN AND EVALUATION OF METRONIDAZOLE ENTERIC COATED TABLETS FOR COLON TARGETING DRUG DELIVERY SYSTEM
Ibrahim M.E., Fatehalrahman F. Magbool*, Mahjoub. N.M. Ahmed, Dhia Eldin Elhag, Asim Halfawi, Zuheir Osman, Abdrhman Mahmoud Gamil and Mohamed E. Adam
Colon-targeted drug delivery has been the focus of numerous studies in recent years due to its potential to improve treatment of local diseases affecting the colon, while minimizing systemic side effects. Methods. Metronidazole core tablets were formulated using different polymers in different ratios and the core tablets were coated with an enteric polymer. The formulated enteric coated tablets were evaluated for their compatibility between the active ingredient and the excipients. The prepared tablets were evaluated for weight variation, hardness, friability, content uniformity and in vitro drug release. Results. The pre-compression aspect including determination of various flow property, compatibility testing for the active ingredient and the excipients was conducted using Fourier transform infrared spectrophotometer (FT-IR), all the formulations were passed the tests. The tablets were coated by using polymers, in post-compression aspect the coated tablets were subjected to pharmaceutical evaluation using official and non-official experiments. The overall pharmaceutical acceptability were satisfactory for the developed tablets regarding chemical and physical investigations. also drug content was in the range of 98.44 to 99.89 % indicating good content uniformity in the formulations. The tablets were passed all the tests. Among all the formulations F5 formula was found to be optimized and show better targeted site controlled drug delivery as it was retarded the drug release up to 6 hours and showed maximum of 98.32% drug release. The optimum formulation F5 was stable when it was stored at 45 ± 2°C /75% RH for 3 months. The formulation F5 was considered the most suitable formula for targeted the colon. The pharmaceutical evaluations and in vitro results showed that the Metronidazole tablets formulations can be a potential candidate for colon-targeted drug delivery, with better in vitro characteristics and physicochemical properties. As a result, colon-targeted drug delivery of Metronidazole appeared to be a promising alternative to traditional drug administration routes.
Keywords: Metronidazole, Enteric coated tablets, Pre-compression aspect, In vitro drug release, Colon-targeted drug.
[Full Text Article]