Simultaneous Transport and Metabolism of Nicotinic Acid Derivatives in Hairless Mouse Skin

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概要

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• In vitro simultaneous transport and metabolism of three ester prodrugs of nicotinic acid (NA), methyl nicotinate (MN), ethyl nicotinate (EN) and butyl nicotinate (BN) were studied using excised skin from hairless mouse. Hydrolysis studies of these esters with and without skin homogenate were also done at 37℃. Both the ester and NA were detected in all receiver solutions in permeation studies, and no chemical hydrolysis of the esters was found, indicating that the esters were hydrolyzed during the skin permeation process. The total (ester+NA) flux from a saturated solution of ester prodrugs was higher than that of NA and was highest for MN, followed by EN and BN, whereas the total permeability coefficient of ester prodrugs increased from MN to BN. A difference in the NA/total flux ratio was found among these prodrugs; thus, esterase activity was also dependent on the alkyl chain length of the esters. The total flux from each ester solution increased linearly with the donor concentration. NA flux from MN and EN solutions increased with an increase in the donor concentration and reached a plateau at the high concentration range, suggesting that metabolic saturation occurred. NA fluxes at the plateau were similar among ester prodrugs and corresponded to the V_<max> estimated from the hydrolysis experiment. The order of donor concentration at which NA reched a plateau also corresponded to the order of K_m. It was confirmed that a difference in alkyl chain length of the ester prodrugs affected not only permeability but also metabolism in the skin permeation process.

• 社団法人日本薬学会の論文
• 1999-03-15

著者

• KATAYAMA Kazunori

  Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University

• KOIZUMI Tamotsu

  Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University

• Koizumi T

  Toyama Medical & Pharmaceutical Univ. Toyama Jpn

• Katayama K

  Toyama Medical And Pharmaceutical Univ. Toyama Jpn

• Katayama K

  Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University

• HATANAKA Tomomi

  Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University

• RITTIROD Theera

  Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University

• KAGAMI Naoki

  Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University

• Hatanaka Tomomi

  Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University

• Hatanaka Tomomi

  Faculty Of Pharmaceutical Sciences Josai University

• Koizumi T

  Toyama Medical And Pharmaceutical Univ. Toyama Jpn

• Katayama Kazunori

  Faculty Of Pharmaceutical Science Toyama Medical And Pharmaceutical University

• Koizumi Tamotsu

  Faculty Of Pharmaceutical Science Toyama Medical And Pharmaceutical University

• Kagami Naoki

  Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University

• Rittirod Theera

  Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University

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