Abstract

DESIGN AND PROCESS OPTIMIZATION OF ORAL FLOATING DRUG DELIVERY SYSTEM OF AMOXICILLIN TRIHYDRATE

Manojkumar S. Patil* and Prof. Dr. G. Vidyasagar

ABSTRACT

The main purpose of this research was to design and process optimization of oral floating drug delivery system of amoxicillin trihydrate floating tablet by using the hydrophilic polymer hydroxypropyl methyl cellulose and gas generating agent sodium bicarbonate and citric acid. Amoxicillin trihydrate is a broad-spectrum semisynthetic antibiotic. Amoxicillin trihydrate is used as antibacterial. It is also used for the treatment of infections of the ear, nose, and throat, the genitourinary tract, the skin and skin structure, and the lower respiratory tract. A 3 2 randomized full factorial design was constructed to study. In this design 2 factors were evaluated, each at 3 levels and experimental trials were performed at all 9 possible combinations. The amount of citric acid (X1) and HPMC K100 M (X2) were selected as independent variables. The dependent variables chosen were percentage drug release at 8hours (Q8), percentage drug release at 12 hours (Q12), and Floating lag time (FLT). The results of factorial design indicated that high level HPMC K 100M and citric acid favors preparation of floating tablet. The Result of multiple regression analysis indicated that both factors X1 and X2 significantly affect on the dependent parameters. The granules were prepared by wet granulation method and evaluated for their granules properties. Granules were compressed into tablets by using 10 station Rotary Tablet compression Machine (Karnavati Mini press I) using 13 mm punch and evaluated with different parameters like diameter, thickness, average weight, hardness, friability, in-vitro buoyancy study, swelling characteristics and stability study. According to stability study it was found that there was no significant change in dissolution profile of optimized formulation. In-vivo radiographic study of the final formulation (F1) was performed using New Zeal Albino rabbits by X-ray imaging technique. The in-vivo X-ray imaging study clearly indicated that the prepared optimized floating tablet was retained in the rabbit stomach over a prolonged period of time. In-vivo radiographic studies showed that the optimized tablet formulation was retained in stomach for more than six hours.

Keywords: Amoxicillin trihydrate, Gastroretentive, floating drug delivery system, Invivo radiographic study, factorial design.