Partition coefficients of some purine derivatives and its application to pharmacokinetics.
Metazathioprine (MAZA), a methylated derivative of azathioprine (AZA), demonstrated the greatest values of apparent and specific partition coefficients in n-octanol/phosphate buffer at pH 5.7 and pH 7.4 among purine derivatives such as 6-mercaptopurine (6-MP), 6-thioguanine (6-TG) and AZA. Introduction of a methyl group into the imidazole ring of AZA increases lipophilic properties of MAZA compared to AZA. Mass balance of purine derivatives in n-octanol and in phosphate buffer indicated their chemical stability in those media.
Chrzanowska
M
M
Department of Physical Pharmacy and Pharmacokinetics, Poznań University of Medical Sciences, Poznań, Poland. mchrzan@ump.edu.pl
Sobiak
J
J
Kuehn
M
M
Dorawa
E
E
Hermann
T
T
D020003:1-Octanol; D000465:Algorithms; D002021:Buffers; D007202:Indicators and Reagents; D010710:Phosphates / Q000737:chemistry; D011687:Purines / Q000737:chemistry* / Q000493:pharmacokinetics*; D012995:Solubility; D012997:Solvents; D013056:Spectrophotometry, Ultraviolet
D002021:Buffers; D007202:Indicators and Reagents; D010710:Phosphates; D011687:Purines; D012997:Solvents; D020003:1-Octanol