Abstract
The objective of the present investigation was to prepare and evaluate a floating granular delivery system for the treatment of mucosal ulcer consisting of (i) calcium silicate (CS) as a porous carrier; (ii) ranitidine hydrochloride (RH), an anti-ulcer agent; and (iii) hydroxypropyl methylcellulose K4M (HPMC) and ethylcellulose (EC) as matrix-forming polymers. The effect of various formulation and process variables on the particle morphology, particle size, micromeritic properties, percent drug content, in vitro floating behavior, and in vitro drug release from the floating granules was studied. Scanning electron microscopy (SEM) of the granules revealed that that more pores of CS in secondary coated granules (SCG) were covered by the polymer solution than those in primary coated granules (PCG). The formulation demonstrated favorable in vitro floating and sustained drug release characteristics. The in vivo evaluation for the determination of pharmacokinetic parameters was performed in albino rats. Higher plasma concentration was maintained throughout the study period from the floating granules of RH. The enhanced bioavailability and elimination half-life observed in the present study may be due to the floating nature of the dosage form and the reduction of the absolute alcohol-induced ulcerogenic index from 3.0 to 0.6. The results suggested that CS is a useful carrier for the development of floating and sustained release preparations.
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Acknowledgements
One of the authors, Ashish Jain, expresses his sincere thanks to the All India Council of Technical Education, New Delhi, India for awarding a Junior Research Fellowship during his M.Pharm. programme. The authors gratefully acknowledge M/s Cadila Pharmaceuticals, Ltd., Ahmedabad, India for the supply of ranitidine hydrochloride as a gift sample. The authors also wish to thank Dr. Rajesh Pathania of the All India Institute of Medical Sciences, New Delhi, India for providing facilities for the SEM study.
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Jain, A., Jain, P., Jain, S.K. et al. Calcium-silicate-based floating granular delivery system of ranitidine hydrochloride for effective management of peptic ulcer. Med Chem Res 17, 305–317 (2008). https://doi.org/10.1007/s00044-007-9066-z
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DOI: https://doi.org/10.1007/s00044-007-9066-z