Table 1.
Site-specific association equilibrium constants (Ka) measured for repaglinide at Sudlow sites I and II of normal or modified HSAa
| Type of HAS | Sudlow site I Ka (M−1) | Change vs. Normal HSA | Sudlow site II Ka (M−1)c | Change vs. Normal HSA |
|---|---|---|---|---|
| Normal HSA | 4.2 (± 0.3) × 104 | ------ | 6.1 (± 0.2) × 104 | ------ |
| GoHSA1 | 5.4 (± 0.5) × 104 | ↑ 1.29-fold | 1.4 (± 0.1) × 105 | ↑ 2.30-fold |
| GoHSA2 | 7.2 (± 0.3) × 104 | ↑ 1.71-fold | 2.1 (± 0.4) × 105 | ↑ 3.44-fold |
| MGoHSA1 | 3.8 (± 0.4) × 104 | ↓ 9.5% (N.S.)b | 1.8 (± 0.2) × 105 | ↑ 2.95-fold |
| MGoHSA2 | 3.4 (± 0.4) × 104 | ↓ 19% | 2.2 (± 0.2) × 105 | ↑ 3.61-fold |
These results were measured at 37 °C in pH 7.4, 0.067 M potassium phosphate buffer. The values in parentheses represent a range of ± 1 S. D. Except were indicated otherwise, all changes shown for modified HSA vs. normal HSA were significant at the 95% confidence level based on the Student’s t-test.
The result for MGoHSA1 at Sudlow site I was not significantly different (N.S.) from normal HSA at the 95% confidence level but was significantly different at the 90% confidence level.
The listed result for normal HSA is consistent with values obtained for several columns and batches of silica that contained this immobilized binding agent.