Abstract
Objective: Calcium pectinate is an insoluble hydrophilic material used for sustained release delivery. The objective of the study was formulation and evaluation pectin-calcium chloride beads of azathioprine.Methods: Calibration curves of azathioprine were prepared in 0.1N HCl solution (pH-1.2) and phosphate buffer (pH-6.8 and pH-7.4). Fourier transform infrared spectroscopy and differential scanning calorimetry was used to determine compatibility between azathioprine and excipients. Formulation and optimization of calcium-pectinate beads were performed. The coating of the optimized batch was performed with eudragit S100. Micrometric properties, scanning electron microscopy, in vitro azathioprine release, and stability study was performed. Dissolution kinetic study was assessed for various kinetics models of the optimized batch. The Wilcoxon test followed by the Dunnett’s multiple comparison tests were performed between uncoated and coated beads in vitro dissolution profile of optimized batch in 0.1N HCl after 2 h.Results: Fourier transform infrared spectroscopy and differential scanning calorimetry had identical peaks with that of pure azathioprine in compatibility study. Scanning electron microscopy of an uncoated optimized batch of beads indicated the smooth and uniform surface of prepared beads. Eudragit S100 coating was decreased release of azathioprine release in 0.1N HCl after 2 h (p = 0.049, q = 3.533). Korsmeyer/Peppa's model was applied with release exponent higher than 1. In vitro percentage cumulative azathioprine release was identical before and after stability study.Conclusion: Calcium pectinate beads of azathioprine, a multi-particulate dosage form using pH-dependent approaches were prepared.
Highlights
Inflammatory bowel disease (IBD) is a collective term encompassing related but distinct chronic inflammatory disorders of the gastrointestinal tract such as Crohn's disease, ulcerative colitis, indeterminate colitis, microscopic colitis, and collagenous colitis [1]
Since pectin can react with calcium ions forms calcium pectinate as an insoluble hydrophilic material used for sustained release delivery [4]
In differential scanning calorimetry study of a physical mixture of azathioprine and excipients, the pick was observed at 245 °C, which is the peak of azathioprine
Summary
Inflammatory bowel disease (IBD) is a collective term encompassing related but distinct chronic inflammatory disorders of the gastrointestinal tract such as Crohn's disease, ulcerative colitis, indeterminate colitis, microscopic colitis, and collagenous colitis [1]. In IBD, colon-specific drug delivery system is preferred dosage form because of having advantages of oral administration and site-specific action [2]. Colon targeted drugs are more effective in fewer dose [3]. Pectin is a purified polysaccharide obtained from the diluted acid extract of the inner portion of the rind of citrus fruits or from apple pomace. It consists of partially methoxylated polygalacturonic acids. Low methoxy pectin (with a degree of esterification
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