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Colon specific drug delivery for Mebeverine Hydrochloride

Samia Omar1 *, Basmah Aldosari1, Hanan Refai2, Omaimah Al Gohary1

1 Department of Pharmaceutics, Faculty of Pharmacy, King Saud University, Riyadh KSA

2 Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Cairo Egypt

Journal of drug targeting, 15(10): 691-700, 2007

* Correspondence: Dr. Samia Omar (omarsamia@hotmail.com)

   Abstract

    

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 CODES TM). 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 enterobacteria present 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. 

 
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