Analysis of the Phase Solubility Diagram of a Phenacetin/Competitor/β-Cyclodextrin Ternary System, Involving Competitive Inclusion Complexation
スポンサーリンク
概要
- 論文の詳細を見る
The competitive inclusion complexations in the ternary phenacetin/competitors/β-cyclodextrin(β-CyD)systems were investigated by the solubility method, where m-bromobenzoic acid(m-BBA)and o-toluic acid(o-TA)were used as competitors. The solubility changes of the drug and competitors as a function of β-CyD concentration in the ternary systems were formulated using their stability constants and intrinsic solubilities. The decrease in solubility of phenacetin by the addition of competitors could be quantitatively simulated by the formulation, when both drug and competitor give A_L type solubility diagrams. On the other hand, when one of the guests gives a B_S type solubility diagram, its solubility change was clearly reflected in that of the another guest, i.e., phenacetin gave an A_L type solubility diagram in the binary phenacetin/β-CyD system and o-TA gave a B_S type diagram in the binary o-TA/β-CyD system, but in the ternary phenacetin/o-TA/β-CyD system, a new plateau region appeared in the original A_L type diagram of phenacetin. This was explained by the solubilization theory of Higuchi and Connors. The solubility analysis of the ternary drug/competitor/CyD systems may be particularly useful for determination of the stability constant of a drug whose physicochemical and spectroscopic analyses are difficult, because they can be calculated by monitoring the solubility change of a competitor, without monitoring that of a drug. Furthermore, the present results suggest that attention should be paid to the type of the phase solubility diagram, as well as the magnitude of the stability constant and the solubility of the complex, for a rational formulation design of CyD complexes.
- 社団法人日本薬学会の論文
- 2001-01-01
著者
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HIRAYAMA Fumitoshi
Faculty of Pharmaceutical Sciences, Sojo University
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UEKAMA Kaneto
Faculty of Pharmaceutical Sciences, Sojo University
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ARIMA Hidetoshi
Faculty of Pharmaceutical Sciences, Kumamoto University
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ONO Naomi
Faculty of Pharmaceutical Sciences, Kumamoto University
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有馬 英俊
熊本大学薬学部
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上釜 兼人
崇城大・薬
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上釜 兼人
熊本大・薬
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上釜 兼人
熊本大学 歯
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平山 文俊
Faculty Of Pharmaceutical Sciences Sojo University
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上釜 兼人
Faculty Of Pharmaceutical Sciences Kumamoto University
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Ono Naomi
Faculty Of Pharmaceutical Sciences Kumamoto University
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Ono N
Kobe Pharmaceutical University
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有馬 英俊
Graduate School Of Pharmaceutical Sciences Kumamoto University
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Arima Hidetoshi
Faculty Of Maritime Sciences - Division Of Maritime System Management Science - Kobe University
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Arima Hidetoshi
School Of Pharmacy Tokyo University Of Pharmacy And Life Science
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Hirayama Fumitoshi
Faculty Of Pharmaceutical Sciences Kumamoto University
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Hirayama Fumitoshi
Faculty Of Pharmaceutical Sciences Sojo University
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上釜 兼人
崇城大 薬
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Uekama Kaneto
Faculty Of Pharmaceutical Sciences Kumamoto University
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上釜 兼人
熊本大学薬学部製剤学研究室
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