Design and Formulation of Mebeverine HCl Semisolid Formulations for Intraorally Administration


BALOĞLU E. , KARAVANA S. Y. , Hyusein I. Y. , Koese T.

AAPS PHARMSCITECH, vol.11, no.1, pp.181-188, 2010 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 11 Issue: 1
  • Publication Date: 2010
  • Doi Number: 10.1208/s12249-009-9374-3
  • Title of Journal : AAPS PHARMSCITECH
  • Page Numbers: pp.181-188
  • Keywords: hydroxypropylmethylcellulose, mebeverine hydrochloride, mucoadhesion, poloxamer 407, sol-gel transition, VITRO RELEASE KINETICS, MUCOADHESIVE PROPERTIES, DRUG-DELIVERY, MECHANICAL CHARACTERIZATION, TOPICAL ANESTHETICS, BIOADHESIVE, GELS, SYSTEMS, SYRINGEABILITY, TETRACYCLINE

Abstract

Gel formulations of mebeverine hydrochloride (MbHCl) containing hydroxypropylmethylcellulose (HPMC), metolose (MTL), and poloxamer 407 (PLX) were prepared to be used in the treatment of different oral painful conditions. HPMC was used as a mucoadhesive gel base while MTL and PLX were used to prepare sol-gel thermosensitive gels. MTL and PLX formulations showed proper sol-gel transition temperature for intraoral application. Formulations were evaluated in terms of their viscosity, mechanical properties, mucoadhesivity, stability, and in vitro drug release. The formulation prepared with 2% of HPMC K100M provided the highest viscosity at room temperature. However, the viscosity of HPMC-PLX mixture showed a significant increase at body temperature. The greatest mucoadhesion was also noted in HPMC PLX combinations. Texture pro. le analysis exhibited the differences of the adhesion, hardness, elasticity, cohesiveness, and compressibility of the formulations. The release profiles of MbHCl were obtained, and non-Fickian release was observed from all the formulations. The formulations were stored at different temperature and relative humidity. No significant changes were observed at the end of the 3 months. HPMC-PLX formulation of MbHCl was chosen for in vivo studies, and it remained longer than dye solution on the rabbit's intraoral mucosal tissue. It was found worthy of further clinical evaluation.