The aim of this research work was to develop the controlled release of two model drugs i.e. water insoluble drug - resveratrol and water soluble drug - lignan by matrix tableting with an eccentric tablet machine. For this purpose different kinds of polymers i.e. Metolose 90 SH-4000® (HMPC), Fetocel RT-N-100® (EC) and Eudragit RLPO® (polymethacrylate) were used. The matrix tablets containing 2 %wt of a model drug which were mixed with 5, 10, 20, 30 and 50 %wt of the polymers mentioned above. In addition, a glidant composed of 1 %wt talc and 1 %wt magnesium stearate as well as a filler Ludipress® were processed. Different physical properties of the powder mixtures (e.g. flowability) and of the tablets (e.g. hardness, uniformity of mass or drug content, drug release, etc.) were determined. Most of the tablets met the physical requirements. If the polymer content got higher the release was slower, which can be confirmed by the lower values of k. The release kinetics were described by three typical mathematic models i.e. biphasic, Noyes-Whitney and KorsmeyerPeppas. The best fitting results were ordered as follows: biphasic > Noyes-Witney > KorsmeyerPeppas.
For the development of colon delivery systems (CDS) formulations have to be gastric resistant. The advantage of the CDS is the ability for a local treatment for colon diseases but also its systemic action. CDS can also increase the bioavailability of poorly water soluble drugs e.g. resveratrol, which can be degraded in the upper gastrointestinal tract or by the First-Pass-Effect. In this project the coating technique with different polymer mixtures containing Kollicoat MAE-30DP, Eudragit-NM, Eudragit-L, and Eudragit-NE was investigated. Resveratrol was used as a model drug and all formulations were coated with a polymer mixture in a small scale fluidized bed apparatus. Morphology, roughness and film thickness of the coated tablets were determined by a scanning electron microscope and a 3D light microscope. Drug amount was determined by UV-spectrometry. Release studies were performed in a dissolution apparatus type II. Kinetic profiles of drug release were demonstrated. Results exhibit the advantages of polymer mixtures for CDS in comparison with results of pure Kollicoat MAE-30DP which were published in one of our latest publications.
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