KMID : 0369820000300040267
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Jorunal of Korean Pharmaceutical Sciences 2000 Volume.30 No. 4 p.267 ~ p.271
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Effect of Cyclodextrins on the Solubility and Stability of Aspalatone in Aqueous Solutions
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°ûÇý¼±/Gwak HS
ÀüÀα¸/Chun IK
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Abstract
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The effect of cyclodextrins on the solubility and stability of aspalatone (acetylsalicylic acid maltol ester, AM, CAS 147249-33-0), which has been recently found to have an antithrombotic effect, was investigated. The addition of ¥â?cyclodextrin(¥â?CD),dimethyl?¥â?cyclodextrin(DMCD)or2?hydroxypropyl?¥â?cyclodextrin(HPCD) to the aqueous solution increased the solubility of AM concentration-dependently. From the phase solubility diagram, stability constants for AM?¥â?CD, -DMCD or -HPCD complexes were calculated to be 43.1, 78.3 and 53.0M?1. The addition of ¥â?CD, DMCD or HPCD to AM solution retarded the degradation rate of AM in the acidic region. However, ¥â?CD and HPCD rather acted as an accelerator of degradation in the neutral and alkaline regions. DMCD had a stabilizing effect at all pHs studied.
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KEYWORD
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Aspalatone, Solubility, Stability, Cyclodextrins
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