A Study on the Protein Binding of Nifedipine in the Sera of Liver Disease Patients.

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The purpose of the present study was to assess the influence of liver diseases on in vitro protein binding. The protein binding of nifedipine and concentrations of albumin, α<SUB>1</SUB>-acid glycoprotein (AAG), HDL-cholesterol (HDL-cho), bilirubin and non-esterified fatty acids (NEFA) were analyzed in sera collected from 6 healthy volunteers, 10 patients with hepatitis and 10 patients with liver cirrhosis. Separation of the unbound fraction was performed by ultracentrifugation at 220, 000g for 18h at 4°C.<BR>The bound fraction (mean ± S. D.) of nifedipine was 98.10 ± 0.91% in normal subjecs, 96.08 ± 1.44% in hepatitis patients (p<0.05) and 94.84 ± 1.60% in cirrhotic patients (p<0.05). The bound fraction was significantly correlated with serum concentrations of AAG (r=0.737, p<0.0001), HDL-cho (r=0.733, p<0.0001), albumin (r=0.5903, p<0.005) and total protein (r=0.459, p<0.05). Multiple regression analysis showed that these varia tions were related to changes in HDL-cho, AAG and NEFA concentrations.
一般社団法人日本臨床薬理学会の論文