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Abstract

An Innovative Mucoadhesive Thermosensitive In situ Gelling Liquid Suppository of Metoclopramide Hydrocloride for Treatment of Nausea and Vomiting Associated with Diseases

Author(s): Z. D. SALMAN, A.T. ALHAMDANY* AND N. Z. YOUSIF
Department of Pharmaceutics, College of Pharmacy, Mustansiriyah University, Baghdad, Iraq

Correspondence Address:
Department of Pharmaceutics, College of Pharmacy, Mustansiriyah University, Baghdad, Iraq,E-mail: [email protected]

The main purpose of presently study was to formulate and evaluate a controlled release thermogelling mucoadhesive system of Metoclopramide Hydrocloride given for emetic patients as an alternative for conventional oral dosage forms. Twelve formulations were prepared by the addition of mucoadhesive polymers (Hydroxypropyl methylcellulose K15M and Hydroxypropyl methylcellulose K100M, carbopol 934p, and sodium alginate) to the formulations of the thermosensitive gelling solutions containing poloxamer 407 and poloxamer P188. Each of the eleven formulations containing metoclopramide Hydrocloride as an active drug was evaluated for pH, clarity, drug content, gelation temperature, gel strength, mucoadhesive force and viscosity. While the succeeded in situ gelling liquid suppository, formulations were evaluated for spreadability, syringeability, the in vitro release profile of the drug and kinetic studies. Also, the optimum formulation was evaluated and identified for drug-excipients compatibility study using Fourier transform infrared spectroscopy. From the characterization of Metoclopramide Hydrocloride in situ gelling liquid suppositories, it was revealed that the optimized formulation (F4) displayed the best syringeability time (7.5±0.77 s) that is confirmed by viscosity measurement (335±0.15 cp at 25Ë? and 27 470±0.09 cp at 37Ë?) with a suitable pH determination (7.01±0.90). While gelation temperature at (37±0.04°) was established with a spreadability measurement (17.5±0.02 g cm/s). Moreover, adhesiveness at the administration site was assured by both mucoadhesive and gel strength studies that were realized to be (20.90±0.83 dyne/cm2 .100) and (17.5±0.34 N/m2 ), respectively. Whereas the drug release method was affirmed through in vitro drug release profile that shows good control of the release, reaching 97.5 % after 3 h with an appropriate content uniformity at (98.19±0.0011). The kinetic test of the release data was founded to obey both diffusion and erosion mechanisms, as the correlation coefficient (R2 ) was best fitted with the Korsmeyer-Peppas model and release exponent (n) shown to be between 0.5-1 that was (0.5190). Put together, our results concluded that thermosensitive liquid in-situ gelling suppositories of Metoclopramide Hydrocloride were effective, potential, and more convenient alternative for a conventional oral dosage form that was given for emetic patients; thereby improving patient compliance and medication adherencet.

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