Measurement of Diffusion Coefficients of Parabens and Steroids in Water and 1-Octanol

Diffusion coefficients (D) of parabens and steroids in water and 1-octanol were determined by using the chromatographic broadening method at 37 °C, and the relationships between the D values and the physicochemical properties of the drugs were discussed. The D values in 1-octanol were lower than tho...

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Veröffentlicht in:Chemical & Pharmaceutical Bulletin 2003, Vol.51(6), pp.734-736
Hauptverfasser: Seki, Toshinobu, Mochida, Junko, Okamoto, Maiko, Hosoya, Osamu, Juni, Kazuhiko, Morimoto, Kazuhiro
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Sprache:eng
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Zusammenfassung:Diffusion coefficients (D) of parabens and steroids in water and 1-octanol were determined by using the chromatographic broadening method at 37 °C, and the relationships between the D values and the physicochemical properties of the drugs were discussed. The D values in 1-octanol were lower than those in water because of the higher viscosity of 1-octanol. The D values depend on not only the molecular weight (MW), but also the lipophilicity of the drugs in water and on the ability for hydrogen-bonding in 1-octanol. When the lipophilic index (LI), calculated from the retention time using in a reverse-phase column, was used as a parameter of drug lipophilicity, the following equation was obtained for D in water (Dw); log Dw=−0.215·log MW−0.077·log LI−4.367. When the hydrogen bond index (HI), the logarithm of the ratio of the partition coefficient of the drugs in 1-octanol and cyclohexane, was used as an index of hydrogen-bonding, the following equation was obtained for D in 1-octanol (Do); log Do=−0.690·log MW−0.074·log HI−4.085.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.51.734