KMID : 0369819920220020105
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Jorunal of Korean Pharmaceutical Sciences 1992 Volume.22 No. 2 p.105 ~ p.113
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Dissolution and Stability Enhancements of Trimethoprim by ¥â - Cyclodextrin Polymer Inclusion Complexation
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±èÇüÅÂ/Kim HT
¹Ú°æ¿Á/¼¼ºÈÆ/Park KO/Seo SH
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Abstract
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To improve the solubility and dissolution rate of trimethoprim (TMP), which is slightly soluble drug, its inclusion complexes were prepared and studied in this experiment. Inclusion complexes of TMP with ${\beta}-cyclodextrin$ ¼ö½Ä À̹ÌÁö and ${\beta}-cyclodextrin$ ¼ö½Ä À̹ÌÁö polymer (CDPS) were prepared according to Fenyvesi method. These were compared with TMP and its physical mixture with CDPS. Water, diluted hydrochloric acid and phosphate buffer solution were used as dissolution media. And accelerated stability test was studied at $50,\;70\;and \;80^{\circ}C$ ¼ö½Ä À̹ÌÁö. It was found that solubility and dissolution rate of inclusion complexes were increased in water. Especially, the solubility and dissolution rate of TMP was found to be markedly increased by inclusion complexation with CDPS. In stability test, ${\beta}-cyclodextrin$ ¼ö½Ä À̹ÌÁö inclusion complexes were more or less stable than TMP alone. This tendency was not led in CDPS. Consequently, CDPS was useful in increasing dissolution rate and stability of TMP.
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KEYWORD
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Inclusion complex, accelerated stability analysis, dissolution rate, degradation, solubility, cyclodextrin polymers, Fenyvesi method
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