Novel gastroretentive formulation of an Ayurvedic churna for peptic ulcers: Optimization and evaluation

Abstract

Avipattikar churna is well known Ayurvedic formulation in India for Amalpitta. Voluminous dose leading to poor patient compliance, less residence time in stomach and less stability are the major limitations of the Churna. Thus, the objective of research work was to develop a novel gastroretentive floating drug delivery system of Avipattikar churna. The churna was prepared and evaluated for phytochemical analysis. The main constituents, Jalap, and Clove, contained scopoletin and eugenol as active markers. A floating tablet of Avipattikar churna was optimized using a factorial design, with HPMC K4M and HPMC K100M concentrations as independent factors and floating lag time (FLT) and % release of scopoletin and eugenol at 1 h, at 4 h and at 8h as dependent variables. The optimized formulations were evaluated by physical parameters. The optimized formulation was selected based on factorial design and numerical desirability Index values. In-vitro dissolution study was performed for optimized formulation and compared with marketed Avipattikar churna. Release mechanisms of markers were determined using various kinetic models and DD solver. The stability studies followed ICH guidelines. The preliminary trial batches were formulated by using direct compression method. 15% of the mixture of HPMC K100M and HPMC K4M was finalised based on the factorial design results and desirability index. Optimized formulation showed FLT of 88 ± 0.3 sec, with cumulative eugenol release at 1h (18.78%), 4h (60.23%), and 8h (95.36%). Scopoletin cumulative release was 21.43%, 68.51%, and 89.34% at 1h, 4h, and 8h, respectively. In a release kinetics, formulation showed diffusion mechanism followed by anomalous diffusion. The formulation was stable as revealed by 3 months accelerated stability studies as per ICH guidelines. From the experiments, 15% of HPMC K100M and HPMC K4M gave shorter floating lag time, good consistency and extended the duration of drug release over time frame of 8h. The formulation was found to be stable.