Protein binding of nifedipine

Abstract
The protein binding of nifedipine in concentrations up to 1200 ng ml−1 has been measured in serum, pure human albumin solution and pure human α1-acid glycoprotein (AAG) solutions by ultrafiltration. The drug was extensively bound in serum from four healthy volunteers with a mean (±s.d.) fraction bound of 0.992 ± 0.008. In albumin solution (40 g litre−1) the mean (±s.d.) fraction bound 0.970 ± 0.012, was not significantly different (P > 0.05) from that in serum, suggesting that albumin is the major, but not necessarily the only, binding protein for nifedipine in serum. The binding of nifedipine in solutions of A AG was proportional to the AAG concentration and ranged from 0.514 ± 0.059 to 0.755 ± 0.035 in solutions containing 50 and 150 mg% AAG, respectively. Binding of nifedipine in all protein solutions was linear.

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