Sustained Release Hydrophilic Matrix Tablet of Ibuprofen: Influence of Polymers on In-Vitro Release and Bioavailability

Author(s)

Kumar, V., Soni, G. C., Prajapati, S. K.

Author's Affiliation

Abstract

In the present study, an attempt has been made to evaluate the effect of hydrophilic polymers on the release profile of drug from matrix system. Ibuprofen, a non-steroidal anti-inflammatory drugs (NSAIDs) was used as a model drug to evaluate its release characteristics from different matrices. Matrix tablets of Ibuprofen were prepared by direct compression process using different hydrophilic excipients (Methocel K4M, Methocel K100M, PolyoxWSR 1105 & Metolose 90 SH 100 SR).Before compression the formulations were evaluated for angle of repose, % compressibility and Hausner’s ratio. Tablets were evaluated for hardness, friability, weight variation, uniformity of thickness & diameter, and drug content and results were found in acceptable limits. In-vitro drug release studies were carried out using USP XXII dissolution apparatus type II at 50 rpm with 900 ml 0.1N HCl & phosphate buffer solutions (PBS) of pH 7.4, maintained at 37±0.50C. The release kinetics was analyzed using the zero-order, first-order model equation, Higuchi’s square-root equation, and the Korsmeyer-peppas model. In vitro release studies revealed that the release rate decreased with increases in polymer proportion. The matrix tablet containing 20% Methocel K100M & Polyox WSR 1105 (in ratio 1:1) (Formulation F6) were found to show good initial release (34.52% in initial hour) and allowed sustained release up to 12 hours. Bioavailability parameters including Cmax, Tmax, AUC(0-t), for both tablet were compared. The sustained release tablet produce optimized Cmax and extended Tmax. Relative bioavailability of the test tablet was calculated as 124.14% for 12 hr. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets was dependent on polymer concentration and it was found to be diffusion coupled with erosion. Bioavailability parameters including Cmax, Tmax, AUC(0-t), for both tablet were compared. The sustained release tablet produce optimized Cmax and extended Tmax. Relative bioavailability of the test tablet was calculated as 124.14% for 12 hr. The developed controlled release matrix tablets of Ibuprofen, with sustained release characteristics might be able to minimise the demerits of conventional therapy having Ibuprofen.

Keywords

Ibuprofen, sustained release, in-vitro, Bioavailability

Cite This Article

Kumar, V., Soni, G. C., & Prajapati, S. K. (2012). Sustained Release Hydrophilic Matrix Tablet of Ibuprofen: Influence of Polymers on In-Vitro Release and Bioavailability. International Journal for Pharmaceutical Research Scholars (IJPRS), 1(4), 68-83.