Siebler D, Kinawi A
Institut für Pharmazie, Freie Universität Berlin.
Arzneimittelforschung. 1989 Jun;39(6):659-60.
Binding of Racemic Indoprofen and its Enantiomers to Human Serum Albumin. The binding to 2% and 4% human serum albumin (HSA) of (+/-)-indoprofen, (-)-indoprofen, and (+)-indoprofen was examined applying a modified ultrafiltration process. The binding properties to HSA were characterized by determining the unbound portions of the drug (a), the overall binding constants (K1), the free reaction energy (delta F degrees), the apparent binding constants (k*), and slope (m). The following results were obtained: 1. Racemic indoprofen and its enantiomers show a high affinity to human serum albumin (a = 1-2%). 2. At higher HSA concentrations the free portion (a) diminishes. 3. The affinity to HSA is reduced in the order of levo-indoprofen racemic indoprofen, and dex-indoprofen.
消旋布洛芬及其对映体与人血清白蛋白的结合。采用改良超滤法研究了（±）-布洛芬、（-）-布洛芬和（+）-布洛芬与2%和4%人血清白蛋白（HSA）的结合情况。通过测定药物的未结合部分（a）、总结合常数（K1）、自由反应能（ΔF°）、表观结合常数（k*）和斜率（m）来表征其与HSA的结合特性。得到以下结果：1. 消旋布洛芬及其对映体与人血清白蛋白具有高亲和力（a = 1 - 2%）。2. 在较高的HSA浓度下，游离部分（a）减少。3. 对HSA的亲和力按左旋布洛芬>消旋布洛芬>右旋布洛芬的顺序降低。
