Abstract
Objective: The objective is to design and optimize a floating tablet of furosemide using a novel floating agent Saccharomyces boulardii. Methods: In this study floating tablet based on principle of combination of floating and swelling prepared by direct compression technique. Saccharomyces boulardii probiotics preparation is used as a floating agent due to its bloating property i.e. production of CO2 gas and hydrophilic polymer HPMC E LV 15 used as swellable polymer. Furosemide is a BCS class IV drug selected as model drug which shows pH dependent solubility and permeability and it is better absorbed from the gastric region, hence to improve dissolution and residence at absorption site of such drug, floating drug delivery system is needed. Calcium hydroxide used as pH modifier which increase rate of dissolution of furosemide and also maintain integrity of tablet matrix. Formulation designed and developed using central composite design response surface methodology technique, so as to explore the effect of formulation variables such as amount of Saccharomyces boulardii preparation and calcium hydroxide on floating lag time and % drug release after 12h. Results: The numerical and graphical optimization technique were used to choose the optimal formulation. Floating lag time was found to be 12.6 min and 88.18% drug release for the optimized formulation. In vivo buoyancy studies depicted that formulation stay more then 6h in stomach. Conclusion: Study indicate that Saccharomyces boulardii is a promising floating agent, and the formulation containing this novel floating agent is suitable for gastro retention and it increases bioavailability of furosemide.
Highlights
Yeasts are a significant source for procurement products with probiotic activity and a good alternative to probiotic bacteria [1]
The percentage swelling index, which is expressed in terms of weight gain of all batches shown in fig
Buoyancy is achieved due to hydration of swelling material like polymer Hydroxypropyl methylcellulose and carbon dioxide gas [26] generation from Saccharomyces boulardii formulation when it come in contact with water from acidic media
Summary
Yeasts are a significant source for procurement products with probiotic activity and a good alternative to probiotic bacteria [1]. Saccharomyces boulardii retains many properties that make it an impending probiotic agent, i.e. it survives during GI transit, it grow well at temperature 37 °C, both in vitro and in vivo [2], its high tolerance to gastric acidity, proteolysis and are able to attain higher populations in the GI tract. They can forever colonize in the colon and do not move out from the intestinal tract [3]. Bloating is a feeling of increased gas in the stomach that subsides over a few days [7]
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