Development and evaluation of cefadroxil sustained release pellets by extrusion spheronization technique

Prajwal Y; K Manjunath; Pavithra Evangeline

Development and evaluation of cefadroxil sustained release pellets by extrusion spheronization technique

Authors
Prajwal Y, K Manjunath, Pavithra Evangeline

Abstract
Objective: The aim of the present study is to design and develop sustained release pellets of cefadroxil. cefadroxil is widely used in the management of anti-biotics and in the treatment of urinary tract infection. Cefadroxil is freely soluble in water and possesses pKa 1.5. Cefadroxil (C₁₆H₁₄N₃O₅S) a first-generation antibiotic. To carry out compatibility studies by FTIR. Pellets are evaluated for their bulk density, tapped density, angle of repose, carr’s index, flow rate, friability, drug-content and in-vitro drug release. Methods and results: Cefadroxil pellets were prepared by using HPMC K100 M or ETHYL CELLULOSE by extrusion and spheronization technique. The in-vitro release studies of pellets were carried out in 6.8 phosphate buffer for 12 hours. The studies indicated that the drug release can be modulated by varying the concentration of the PEG 4000 as release modulator with polymers. The release data was fitted to various mathematical models such as, Higuchi, Korsmeyer-Peppas, First-order, and Zero-order to evaluate the kinetics and mechanism of the drug release. Kinetic modelling of in-vitro dissolution profiles revealed the release mechanism ranges from Quasi-Fickian transport to Anomalous (non-Fickian transport), which was only dependent on the type and amount of release modulator used. The drug release of the optimized formulation (F4) is 98.86% in 12 hours, follows then first order release kinetics (R²: 0.864 to 0.988), Zero order kinetics shows (R²: 0.903 to 0.998), and the ‘n’value lies between (0.026 to 0.8421). The mechanism was found to be diffusion controlled. The compatibility studies were performed by using FTIR which reveals that there is no interaction between the drug and the polymer/excipients mixture.

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