Phenformin HCL/ CAS No.834-28-6 CAS NO.834-28-6

Phenformin hydrochloride is a white crystalline powder, Mp 175° to 178°, soluble 1 in 8 parts of water and 1 in 15 of ethanol; practically insoluble in chloroform and ether, dissociation Constant pKa 2.7, 11.8 (32°), Partition Coefficient Log P(octanol/water) = –0.8. Phenformin is well absorbed after oral administration. The major metabolic reaction is aromatic hydroxylation to form 4–hydroxyphenformin which is then conjugated with glucuronic acid. Up to about 50% of a dose is excreted in the urine in 24 h, about two–thirds in the form of unchanged drug and one–third as the hydroxy metabolite. Following a single oral dose of 50 mg to 8 subjects, peak plasma concentrations of 0.08 to 0.18 mg/L (mean 0.13) were attained in about 3 h; plasma concentrations were higher in 4 subjects who were poor metabolisers of debrisoquine in comparison with the 4 extensive metabolisers. Following daily oral doses of 50 mg three times a day to 8 subjects, plasma concentrations of 0.10 to 0.24 mg/L (mean 0.18) were reported 2 h after a dose. Plasma half–life of phenformin is 10 to 15 h. Phenformin protein binding in plasma, is about 12 to 20%.

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