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KMID : 0370019960100000121
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Chung-Ang Journal of Pharmacal Sciences
1996 Volume.10 No. 0 p.121 ~ p.131
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Sustained-Released Product Design of Glipizide Using Chitosan and Chitosan Latctate
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Abstract
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Glipizide(GPZ) is a second generation non-halogenated sulphonylurea hypoglycemic agent in maturity onset diabetes mellitus which stimulates the secretion of endogenous insulin from pancreatic β-cells. GPZ is almost completely absorbed with peak serum concentration being attained 1 to 3 hours after an oral administration. However, administration of GPZ at a high dose can occasionally induce the severe hypoglycemia, especially in the patients with renal impairment as well as impaired liver function due to some of the administered dose being excreted in the urine as unchanged drug and first-pass hepatic metabolism. Therefore, in order to develop an oral sustained-release preparation which reduces the side effect, chitosan and chtosan lactate were employed as a matrix for sustained-release tablet of GPZ in this experiment. Chitosan is a natural, biocompatible and biodegradable polymer, showing extrmemly low toxicity and it has been used as a vehicle for sustained felease preparations of drugs. Chitosan and chitosan lactate tablets of GPZ were prepared by directed compression using Hydraulic Lab. Press. at 340kg/cm^2 for 30sec. The tablet formulation of GPZ with chitosan alone ded not show sustained release properties at any concentrations(30-80%) of chitosan, but the release of GPZ from chitosan tablet containing citric acid shiowed prolonged characteristics. Chitosan readily forms a gel at lower pH, but shows poor gel-forming ability at higher pH.
The effect of contents of chitosan lactate(10, 30 and 50%) or GPZ (5,10, 30 and 40%) on GPZ release profiles was studied. As the contents of chitosan lactate or GPZ increased, the release of GPZ decreased. And chitosan lactate showed sustained release properties even at lower concentration. In general, on the basis of dissolution kinetics, the release of GPZ from chitosan and chitosan lactate matrix tablet were followed Higuchi´s square root of time equation and Bambe´s equation. Therefore in conclusion, it might be possible to design the sustained release formulation of GPZ using chitosan and chitosan lactate.
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