Nash J F, Bechtol L D, Bunde C A, Bopp R J, Farid K Z, Spradlin C T
J Pharm Sci. 1979 Sep;68(9):1087-90. doi: 10.1002/jps.2600680907.
The bioavailability of fenoprofen from three different fenoprofen calcium capsule formulations containing the equivalent of 60, 165, and 300 mg of fenoprofen was determined in two studies. In the first study, 12 subjects received one capsule of each formulation according to a three-period crossover design. The second study required each of 13 subjects to receive 300 mg of fenoprofen equivalent of the 60- and 300-mg capsules and 330 mg of the 165-mg capsule. The initial study provided information on the linearity of fenoprofen pharmacokinetics, and the second study established that the three capsule formulations were bioequivalent. The bioavailability parameters Cmax, tmax, and AUC0--12 hr for the drug in plasma were consistent with a linear pharmacokinetic model, as were the amounts of fenoprofen and hydroxyfenoprofen excreted in the urine. These data show linearity of kinetics for fenoprofen in plasma throughout the 60--300-mg dosage range after a single dose. Physical measurements of each capsule formulation drug content, weight variation, and dissolution showed the products to be uniform and readily soluble.
在两项研究中测定了三种不同的含60毫克、165毫克和300毫克非诺洛芬等效量的非诺洛芬钙胶囊制剂中非诺洛芬的生物利用度。在第一项研究中，12名受试者按照三周期交叉设计服用每种制剂的一粒胶囊。第二项研究要求13名受试者每人服用相当于60毫克和300毫克胶囊的300毫克非诺洛芬以及165毫克胶囊的330毫克非诺洛芬。第一项研究提供了非诺洛芬药代动力学线性方面的信息，第二项研究确定这三种胶囊制剂具有生物等效性。血浆中该药物的生物利用度参数Cmax、tmax和AUC0-12小时与线性药代动力学模型一致，尿液中排泄的非诺洛芬和羟基非诺洛芬量也是如此。这些数据表明，单次给药后，在60-300毫克剂量范围内，非诺洛芬在血浆中的动力学呈线性。对每种胶囊制剂的药物含量、重量差异和溶出度进行的物理测量表明，这些产品均匀且易溶。
