On the modulating effects of temperature, albumin, pH and calcium on the free fractions of phenobarbitone and phenytoin

The effects of temperature, albumin, pH and Ca2+ on the binding of phenobarbitone and phenytoin to human serum albumin in buffer have been investigated using equilibrium dialysis. The free fractions of both anticonvulsants were much increased by raising the temperature. Lower free fractions were obs...

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Bibliographic Details
Published inJournal of pharmacy and pharmacology Vol. 38; no. 9; p. 643
Main Authors Melten, J W, Wittebrood, A J, Wemer, J, Faber, D B
Format Journal Article
LanguageEnglish
Published England 01.09.1986
Subjects
Calcium - blood
Dialysis
Humans
Hydrogen-Ion Concentration
Phenobarbital - blood
Phenytoin - blood
Serum Albumin - metabolism
Temperature
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Summary:The effects of temperature, albumin, pH and Ca2+ on the binding of phenobarbitone and phenytoin to human serum albumin in buffer have been investigated using equilibrium dialysis. The free fractions of both anticonvulsants were much increased by raising the temperature. Lower free fractions were observed by increasing the albumin concentration from 5-8 g litre-1 and by raising pH from 6 to 9. No significant effect on the free fractions was observed by changing (at pH 7.4) the Ca2+ concentration from 0 to 5 mM. The observed differences in free fractions at 37 degrees C, as determined in phosphate, borate and Krebs-Ringer buffer at pH 7.4, indicate that great care is needed in the choice of dialysis fluid for dialysis of clinical samples.
ISSN:0022-3573
DOI:10.1111/j.2042-7158.1986.tb03102.x