Preparation and evaluation of mebeverine hydrochloride as mucoadhesive buccal tablet for local anesthesia

Seham S Abdulhady,Khaled M Hosny Ibrahim

doi:10.4314/tjpr.v16i8.8

Seham S Abdulhady, Khaled M Hosny Ibrahim

Open Access

https://doi.org/10.4314/tjpr.v16i8.8

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Abstract

Purpose: To formulate and evaluate an antispasmodic drug, mebeverine hydrochloride (Mbv-HCl), as a local anesthetic mucoadhesive buccal tablet.Methods: Mbv-HCl loaded tablets were formulated, using a direct compression technique, with varying polymer concentrations including carbopol 934P alone, carbopol 934P/hydroxypropyl methylcellulose (HPMC) mixture, or carbopol 934P/chitosan mixture. The tablets were evaluated for physicochemical characteristics, in-vitro drug release, bioadhesive strength, swelling, ex-vivo residence time, ex-vivo permeation, drug permeation through the buccal membrane of sheep, and stability.Results: The results indicate that formulation F4, which contains HPMC/carbopol 934P (3:1), showed the best in-vitro drug release profile. The release kinetics for all the formulations fitted well with Hixson- Crowell kinetic model. Bioadhesive strength, surface pH, and swelling index of F4 were 41.52, 6.36, and 231.2 %, respectively. Maximum residence time ex-vivo was exhibited by formulation F4, showing a maximum residence time of about 330 min with 80 % of Mbv-HCl permeated in 6 h ex-vivo. F4 was stable after storage for 60 days at 25 oC/60 % RH and 40 oC/75 % RH, with non-significant change (p < 0.05) in drug content, bioadhesive strength and in vitro release.Conclusion: The optimized mucoadhesive buccal formulation is promising for delivery of Mbv-HCl, and displays high bioadhesion and adequate permeability through sheep buccal membrane to achieve a local anesthetic action.Keywords: Mebeverine hydrochloride, Buccal, Mucoadhesive tablet, Swelling index, Bioadhesive strength, Local anesthetic

Highlights

Mebeverine hydrochloride (Mbv-HCl) is an antispasmodic agent reported to have a strong local anesthetic activity with insignificant side effects when compared to other local anesthetics [1]
Previous literature revealed that the activity of Mbv-HCl as a spasmolytic is not due to one particular system
The objective of this research was to formulate and evaluate mucoadhesive oral formulations of Mbv-HCl, which is an antispasmodic agent for use as a buccal anesthetic tablet

Summary

Introduction

Mebeverine hydrochloride (Mbv-HCl) is an antispasmodic agent reported to have a strong local anesthetic activity with insignificant side effects when compared to other local anesthetics [1]. It is a crystalline powder, white in color, with good solubility in ethanol and water [2]. A non-specific relaxant effect on vascular, cardiac and other smooth muscle is shown by Mbv-HCl [3]. Previous literature revealed that the activity of Mbv-HCl as a spasmolytic is not due to one particular system. Mbv-HCl has a polyvalent spasmolytic action where about three different mechanisms are involved. Detailed study and explanation of these mechanisms have been previously described by Hameed et al [4]

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