Design and development of gastric floating microsponge of ranitidine hydrochloride

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Publication Details
Author list: Alkhateeb F, MOHSIN A, KHALID M, Alshahrani A, Alqarni A, Jafar M
Publication year: 2019
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Some drugs show region-specific absorption that can be related to different solubility and stability in different regions of the intestine as a result of changes in environmental pH, degradation by enzymes present in the lumen of the intestine or interaction with endogenous compounds such as bile have been well described. Ranitidine HCl (RT) is the safest antiulcer drug and acts as a reversible histamine inhibitor of the histamine H2 receptors on gastric cells, while having a limited impact on H1 receptors. RT is used for treating active duodenal and gastric ulcers, oesophageal reflux, oesophagitis, and Zollinger-Ellison syndrome. The accepted oral dosage of ranitidine is 150 mg twice daily or 300 mg once daily. RT has a short biological half-life of 2–3 h and poor bioavailability of approximately 50% and is absorbed only in the upper part of the small intestine. One reason for the low bioavailability of RT is its susceptibility to colonic metabolism. Therefore, various slow drug releasing multiparticulate systems for ranitidine HCl have been developed to deliver them in gastric cavity. Nevertheless, the problem with these microparticulate systems is that they possess low drug loading capacity. Gastric floating microsponge, offer an efficient drug delivery system in stomach and unlike above microparticulate systems it has high drug loading capacity. The characteristic features mainly better absorption from upper GI tract and short biological half-life of ranitidine HCl makes it good candidate for the development of a novel sustained release gastro retentive microsponge. Moreover, due to the lack of availability of literature on ranitidine HCl gastric floating microsponge systems, we aimed to develop this novel system for Ranitidine HCl that would improves its oral bioavailability thus clinical response and reduces the frequent dosing, which in turns increases patient compliance .

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Last updated on 2019-28-04 at 09:34