Formulation and évaluation of itopride microcapsules in human volunteers

• Published in: Journal of drug delivery science and technology 2013-01, Vol.23 (3), p.239-245
• Main Authors: Yehia, S.A., Elshafeey, A.H., ElMeshad, A.N., Al-Bialey, H.
• Format: Article
• Language: English
• Subjects: Eudragit; Hydroxypropylmethyl cellulose; Itopride hydrochloride; Microencapsulation; Solvent evaporation; Sustained release
• ISSN: 1773-2247
• DOI: 10.1016/S1773-2247(13)50036-0

In this study an attempt to sustain the oral release of itopride hydrochloride (ITO), a highly water-soluble drug, by microencapsulation using différent polymers was carried out. The prepared microcapsules were characterized according to: particle size, encapsulation efficiency, and in vitro drug release and in vivo study in healthy human volunteers. Results showed that the particle size of microcapsules ranged from 591 ± 2 to 886 ± 4 μm and the encapsulation efficiency of ITO inside microcapsules ranged from 63 ± 1 to 90 ± 1 %. The optimum formulation had a particle size of 860 ± 11 μm and was able to entrap 90 ± 1 % ITO. The in vitro release study showed that 88 ± 1 % of ITO was released from the optimum formulation after 12 h using Eudragit RS-100. The pharmacokinetic parameters of the optimum formulation in human volunteers showed that the maximum plasma concentration was 1624 ± 168 ng/mL, AUC0-∝ was 85835 ± 6116 ng.h/mL, AUC0-48 was 29728 ± 761 ng.h/mL, and the mean residence time was 108 ± 9 h. The relative bioavailability of ITO from the optimum formulation compared to commercial oral tablets Ganaton as a reference standard was 317.9 %.