Kamada A K, Wiener M B, LaVallee N M, Scott M B, Selner J C, Szefler S J
Department of Pediatrics, National Jewish Center for Immunology and Respiratory Medicine, Denver, CO 80206, USA.
Pharmacotherapy. 1997 Mar-Apr;17(2):353-6.
To compare pharmacokinetics of liquid prednisolone and prednisone solutions and to assess relative bioavailability, six healthy adult men were administered 15 mg of each formulation. Blood samples were obtained and assayed for plasma prednisolone concentrations by high-performance liquid chromatography. Peak concentration was significantly higher with liquid prednisolone (mean +/- SD 430.3 +/- 62.5 vs 333.0 +/- 27.8 ng/ml, p = 0.013), with similar times to peak concentration. Prednisolone liquid gave higher concentrations at every time point (statistically significant for all except 0.25 hrs after the dose), resulting in a significantly greater total area under the curve (2029.8 +/- 246.9 vs 1633.3 +/- 221.1 ng/ml.hour, respectively, p = 0.002). Clearance was slower for prednisolone (128.3 +/- 15.1 vs 149.1 +/- 17.6 ml/min/1.73 m2, p = 0.01), and the relative bioavailability of the prednisolone liquid using prednisone liquid as the reference standard was 116 +/- 14%. Thus, prednisolone liquid has similar pharmacokinetic characteristics as prednisone liquid, with improved bioavailability.
为比较液体泼尼松龙和泼尼松溶液的药代动力学并评估相对生物利用度，对6名健康成年男性分别给予每种制剂15毫克。采集血样，采用高效液相色谱法测定血浆泼尼松龙浓度。液体泼尼松龙的峰值浓度显著更高（平均值±标准差为430.3±62.5 vs 333.0±27.8纳克/毫升，p = 0.013），达到峰值浓度的时间相似。泼尼松龙液体在每个时间点的浓度都更高（给药后0.25小时除外，其他时间点均具有统计学显著性），导致曲线下总面积显著更大（分别为2029.8±246.9 vs 1633.3±221.1纳克/毫升·小时，p = 0.002）。泼尼松龙的清除率较慢（128.3±15.1 vs 149.1±17.6毫升/分钟/1.73平方米，p = 0.01），以泼尼松液体为参比标准，泼尼松龙液体的相对生物利用度为116±14%。因此，泼尼松龙液体与泼尼松液体具有相似的药代动力学特征，但生物利用度有所提高。
