Development and in Vitro/In Vivo Evaluation of Itopride Hydrochloride Expanding Tablets

PurposeGastroretentive drug delivery systems (GRDDS) have attracted interest for enhancement of absorption and bioavailability of some drugs. Itopride hydrochloride (ITOP) is a drug used for treatment of gastroesophageal reflux and other gastric motility disorders, but is characterized by narrow absorption window and short in vivo half-life. Therefore, it is expected that its formulation in expanding gastroretentive tablets would increase its gastric residence, thus leading to decreased frequency of administration and increased patient compliance.MethodsThe direct compression method was used for formulation of tablets. Four different hydrophilic polymers (xanthan gum, sodium alginate, gellan gum, pectin) were screened separately with Avicel 102 and PVP k30 as excipients. The effect of different factors (polymer type and amount, and excipient amount) on the tablet properties such as hardness, friability, thickness, diameter, weight variation, swelling, and in vitro drug dissolution was studied. In addition, swelling test, accelerated stability test, and in vivo study were performed on the optimized formulation.ResultsTablets prepared using xanthan gum exhibited favorable properties compared to tablets prepared using the other gums, however increasing the polymer amount led to increased tablet friability. The selected formulation exhibited obvious expansion reaching 17.45 mm and lasting for 24 h, coupled with a sustained release behavior. X-ray scans in human volunteers suggested the residence of the tablet in the stomach for a period of 6 h in fed state.ConclusionSuccessful preparation of directly compressible ITOP expanding tablets was achieved in this study, which is expected to result in better therapeutic outcome in gastroesophageal reflux.