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We evaluated the pharmacokinetics of silymarin solid dispersion in pigs to determine whether silybin bioavailability would be increased over that of a silymarin premix.  In vitro  dissolution testing was conducted using dissolution apparatus 1 (baskets) at 100 rpm at 37 ± 0.5°C in pH 1.2 HCl, pH 6.8 phosphate, and pH 4.3 acetate buffers containing 0.5% Tween-80.  In vivo  pharmacokinetics were studied using 16 healthy pigs (Yorkshire × Landrace) that were randomly assigned to two groups. Silymarin as solid dispersion and premix dosage forms were administered directly by stomach tubes at 50 mg kg −1  silybin.  In vitro  dissolution of silybin for the premix was 35.02, 35.90, and 38.70% in these buffers, respectively. In contrast, silybin dissolution in solid dispersions was increased to 82.92, 87.48, and 99.70%, respectively. Silymarin solid dispersion administered at a single dose resulted in a peak concentration (C max ) of 1,190.02 ± 246.97 ng ml −1  with the area under the curve (AUC 0−∞ ) at 1,299.19 ± 67.61 ng ml −1  h. These parameters for the premix groups were 411.35 ± 84.92 ng ml −1  and 586.82 ± 180.99 ng ml −1  h, respectively. The C max  and AUC 0−∞  values for the solid dispersion were about twice that of the premix and were consistent with the  in vitro  dissolution data.

In vitro Dissolution Testing and Pharmacokinetic Studies of Silymarin Solid Dispersion After Oral Administration to Healthy Pigs