Characterization of Natural Substances in the Line of Design and Evaluation of Clopidogrel Bisulphate Mucoadhesive Tablet

Abstract

Mucoadhesive agents were successfully isolated from natural sources using simple isolation and purification methods. Isolated mucoadhesive agents were characterized using phytochemical studies, physicochemical studies, in vitro and in vivo mucoadhesion studies, FTIR spectroscopic studies and DSC studies. Mucoadhesive properties of natural mucoadhesive agents were studied against Carbopol 934P. Preformulation studies were performed. Five isolated natural mucoadhesive agents were selected for formulation studies by considering their better mucoadhesive properties. 16 tablet formulations were prepared by wet granulation and compression. Tablets were evaluated for granule properties, tablet properties, tablet swelling studies, mucoadhesion studies, drug release studies, in vivo bioavailability studies, drug excipient compatibility and stability study. These results were compared against marketed product. Acetone was used as precipitating solvent for the isolation of mucoadhesive agents. Isolated mucoadhesive agents were composed of carbohydrate, mucilage and reducing sugars. FTIR studies indicated that natural mucoadhesive agents bear hydroxyl, carbonyl and amino functional groups which influences formation of mucoadhesive bonds. Isolated mucoadhesive agents were found poor flowing. Natural mucoadhesive agents were shown better swelling in distilled water than in 0.1 N HCl. Mucoadhesive properties of isolated natural mucoadhesive agents were studied using various in vitro and in vivo methods. Natural mucoadhesive agents were shown concentration and time dependent mucoadhesion. FTIR spectrum and DSC curves indicated that natural mucoadhesive agents were compatible with Clopidogrel bisulphate. Mucoadhesive agent isolated from Prosopis juliflora seed and Abelmoschus esculentus root were shown better results for mucoadhesion in its pure form and in tablet formuation. Mucoadhesive agent isolated from Prosopis juliflora seed was shown better mucoadhesion strength and retention time than the Carbopol 934P.