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KMID : 0370019960100000097
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Chung-Ang Journal of Pharmacal Sciences
1996 Volume.10 No. 0 p.97 ~ p.108
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Glibenclamide Release Characteristics and Effects of Hydrophilic Additives on Ethyl Cellulose Microcapsules Prepared by coacervation-Phase Separation Method
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Abstract
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Glibenclamide (GBC) is a well-known antidiabetic agent, which stimulates the secretion of endogenous insulin by pancreatic βcells. However, administration of GBC at a high dose can occasionally induced the fatal hypoglycemia, especially in the patients with impaired liver function. Therefore, in order to develop an oral sustained-release preparation which reduces the side effect, microcapsulation of GBC has been carried out in this experiment. Microcapsules of GBC were prepared by coacervation-phase separation method with ethylcellulose as a wall-forming material in cyclohexane, using polyisobutylene as a coacervation-inducing agent. Different amounts of hydrophilic additives. L-arginine(ARG) and polyethylene glycol 4000 (PEG), were added to the microcapsule wall, in order to alter the porosity of the wall and hence to enhance the release of the core material. The microcapsules prepared were examined for physical properties by scanning electron microscopy (SEM) and particle size analysis. The release of the poorly water-soluble GBC was found to be very slow from the microcapsules and strongly dependent on the core to wall ratio of the microcapsules, but it was accelerated considerably with increasing amount of PEG or ARG. In general, on the basis of dissolution kinetics, GBC releases from microcapsules were followed apparent first-order kinetics, while the dissolution data of GBC powder conformed to Hixon-Crowell´s cube root law. Therefore, in conclusion, it might be possible to design the sustained-release formulation by the combination of both GBC powder and microcapsules of different core wall ratio with or without hydrophilic additives.
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