Jornal de Bioequivalência e Biodisponibilidade

Abstrato

Formulation, Development and Evaluation of Meclozine Hydrochloride Microspheres

Rasha M Kharshoum and Heba A Aboutaleb

Microspheres of meclozine hydrochloride (MCZ HCl) were formulated in order to prolong the residence time at the absorption site by intimate contact with the mucous membrane. The microspheres were prepared by orifaceionotropic gelation method using bioadhesive polymers such as xanthan, sodium, carboxy methyl cellulose (Na- CMC) and hydroxy propyl methylcellulose (HPMC k15) in combination with different ratio of sodium alginate. Totally nine different formulations of MCZ HCl were prepared by using the above polymers. The microspheres were evaluated for percentage yield, entrapment efficiency, particle size analysis, surface morphology (scanning electron microscopy), differential scanning calorimetry (DSC), swelling index, drug content and in-vitro dissolution study. The relative bioavailability of the optimized microspheres was compared with commercially available product after oral administration on healthy human volunteers using a randomized, cross-over design. The results revealed that mean particle sizes of the microspheres ranged from 565 to 649 μm and the efficiency of entrapment ranged from 53.46% to 81.58%. SEM photomicrograph showed microspheres with rough surface and spherical in shape. The DSC analysis revealed that the drug was uniformly distributed in the microspheres. The optimized microspheres exhibited a slow release over 8 hours. The pharmacokinetic data of the optimized microspheres formula showed prolonged tmax, and improved the relative bioavailability by 146.47% compared with commercially available tablets.