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KMID : 0369819960260030169
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Jorunal of Korean Pharmaceutical Sciences
1996 Volume.26 No. 3 p.169 ~ p.174
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Solubility and In vivo Absorption Enhancement of Diclofenac Sodium by β-Cyclodextrin Complexation
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이경태/Lee KT
김종환/김주일/김승조/서희경/서성훈/Kim JH/Kim JI/Kim SJ/Seo HK/Seo SH
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Abstract
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Inclusion complexes of diclofenac sodium with β?cyclodextrin were prepared in aqueous solution, alkaline solution and solid phase. The interaction of diclofenac sodium with β?cyclodextrin in pH 9.0 alkaline solution was evaluated by the solubility method and the instrumental analysis such as thermal analysis, infrared spectroscopy, X-ray diffractometry. The solubility of diclofenac sodium was increased linearly with the increase in the concentration of β?cyclodextrinup to 0.15 mol and showed that the aqueous solubility rate of diclofenac sodium was significantly increased by complex with β?cyclodextrin. The optimum composition of this complex was one molecule of β?cyclodextrin included 1.59 molecular weight of diclofenac sodium as a guest molecule. The pharmacokinetic parameters of the diclofenac sodium and the complex with β?cyclodextrin were studied in rats by oral route. Tmax between drug alone and inclusion complex showed significant difference to be 120 minute and 20 minute respectively. Both of Cmax and AUC of inclusion complex was about 40% higher than drug alone. It is estimated from the data in this study that complexation of diclofenac sodium with β?cyclodextrin increased the absorption rate and improved the bioavalability of the diclofenac sodium by the formation of a water-soluble complexes.
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KEYWORD
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Solubility, Absorption, Diclofenac sodium, β?cyclodextrin, Complexation
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