Kinawi A, Siebler D
Institut für Pharmazie der Freien Universität Berlin.
Arzneimittelforschung. 1988 Aug;38(8):1089-92.
The binding characteristics of several oxicam derivatives (tenoxicam, 4-hydroxy-2-methyl-N-phenyl-2H-1,2-benzothiazixine-3- carboxamide-1,1-dioxide (CP 14,304), 4-hydroxy-2-methyl-N-2-(3-methyl)-pyridyl-2H-1,2-benzothiazixine-3 -carboxamide- 1,1-dioxide (CP 16,460), piroxicam, meloxicam [corrected], isoxicam, 5-hydroxy-piroxicam) to 2% and 4% human serum albumin (HSA) were determined using a modified ultrafiltration process. The binding properties to HSA were characterized by determining the overall binding constant, the apparent binding constant, the slope, the free reaction energy, and the unbound portion of the drug. The following results were obtained: 1. These oxicam derivatives show a high affinity to HSA. The unbound fraction amounts to 1-3%. 2. The affinity of the compounds to HSA decreases in the order mentioned above. 3. Doubling of the HSA concentration reduces the unbound fraction, to the half, with piroxicam being the only exception.
采用改良超滤法测定了几种昔康衍生物（替诺昔康、4-羟基-2-甲基-N-苯基-2H-1,2-苯并噻嗪-3-羧酰胺-1,1-二氧化物（CP 14,304）、4-羟基-2-甲基-N-2-(3-甲基)-吡啶基-2H-1,2-苯并噻嗪-3-羧酰胺-1,1-二氧化物（CP 16,460）、吡罗昔康、美洛昔康[校正后]、异昔康、5-羟基-吡罗昔康）与2%和4%人血清白蛋白（HSA）的结合特性。通过测定总结合常数、表观结合常数、斜率、自由反应能和药物的未结合部分来表征与HSA的结合特性。得到以下结果：1. 这些昔康衍生物对HSA表现出高亲和力。未结合部分占1-3%。2. 化合物对HSA的亲和力按上述顺序降低。3. 将HSA浓度加倍会使未结合部分减半，但吡罗昔康是唯一的例外。
