Colon specific drug delivery for mebeverine hydrochloride
H, .Omar, S., Aldosari, B., Al-Gohary, O.M.N., and Refai . 2007
Mebeverine Hydrochloride (MB-HCl), an effective spasmolytic drug, was formulated as CODESTM. Colon-specific drug delivery technology CODESTM was designed to avoid the inherent problems associated with pH- or time-dependent systems. Moreover, to achieve more protection and to control the drug release, MB-HCl was prepared as microspheres and compressed as the core tablet of CODESTM (modified CODESTM). The core tablet contained the drug in free form [formula 1 (F1)], or as microspheres with 2 different polymer : drug : lactulose ratios (1:1:0.5 [formula 2 (F2)] and 2:1:0.5 [formula 3 (F3)]. The release profiles of the coated CODESTM systems were compared with uncoated compressed tablets. The uncoated tablet showed a drug release of 94% after 1 hour in simulated gastric condition (pH = 1.2). The release characteristics of the coated systems revealed that the enteric coating (EudragitÒ L100) prevented any drug release in simulated gastric or duodenal conditions in the first 3 hours (pH 1.2 - 6.1), drug was slightly liberated in simulated intestinal fluid (pH 7.4) {phase 1 (P1)}. After 4 hours pH was adjusted at 7 and β-glucose-oxidase was added, which is an enzyme produced by enterobacteriapresent in the colon. The acid soluble coat (EudragitÒ E100) was dissolved and the drug release suddenly increased to reach 95%, 72% and 60.4% for F1, F2 and F3, respectively. IR spectrum study showed a covalent bond between the drug and the polymer in the formulae F2 and F3 resulting in the sustained drug release from the microspheres with a significant difference (p > 0.05) to F1. The formulated (MB-HCl) CODESTM was confirmed by the in vivo investigation using X-ray images for guinea pigs, where the tablet began to disintegrate after 10 hrs of tablet intake. The results of our study showed that Mebeverine Hydrochloride CODESTM colon-specific drug delivery can act as a successful trigger for drug targeting in the colon. Furthermore, a sustained release of the drug can be achieved from CODESTM containing the drug in form of microspheres.
Author Keywords: Colon-specific drug delivery; Colon targeting; Polysaccharides; Mebeverine Hydrochloride CODESTM; CODESTM containing microspheres.
Mebeverine hydrochloride suppositories were prepared using Witepsol H15 suppository base. The effect of different concentrations of various enhancers (surfactants, amino acids and osmotic…
Mebeverine Hydrochloride (MB-HCl), an effective spasmolytic drug, was formulated as CODESTM.