Georgitis J W, Flesher K A, Szefler S J
J Allergy Clin Immunol. 1982 Oct;70(4):243-7. doi: 10.1016/0091-6749(82)90060-4.
To assess the relative bioavailability of a recently developed liquid prednisone preparation, prednisolone pharmacokinetics were evaluated after the administration of three separate steroid preparations. On 3 study days, each 2 wk apart, 12 healthy subjects received in random order: prednisone liquid, prednisone tablet, and prednisolone sodium phosphate. Plasma samples were collected over a 12 hr study period and analyzed for prednisolone concentration by high-pressure liquid chromatography. Tablet data demonstrated a time-to-peak concentration of 1.23 +/- 0.68 hr (SD), mean residence time of 5.1 +/- 0.49 hr, and absolute bioavailability (tablet/i.v.) of 97.5% +/-- 17.5%. Liquid data demonstrated a significantly (p less than 0.01) shorter time-to-peak concentration, 0.54 +/- 0.20 hr, and mean residence time 4.6 +/- 0.34 hr, with no significant difference in absolute bioavailability (liquid/i.v.), 88.2% +/- 15.8%. This resulted in significantly (p less than 0.05) higher plasma prednisolone concentrations for the liquid preparation in the first 0.75 hr and significantly lower concentrations after 1.5 hr as compared with the tablet. Prednisolone area under the plasma concentration vs time curve for the liquid prednisone formulation was 90.0% +/- 13.2% of the tablet preparation. Thus prednisone liquid has comparable bioavailability to the tablet, with an earlier peak plasma prednisolone concentration and significantly higher plasma prednisolone concentrations within the first hour of administration.
为评估一种新开发的液体泼尼松制剂的相对生物利用度，在给予三种不同的类固醇制剂后对泼尼松龙的药代动力学进行了评估。在3个研究日，每隔2周，12名健康受试者按随机顺序接受：液体泼尼松、泼尼松片和泼尼松龙磷酸钠。在12小时的研究期间采集血浆样本，并通过高压液相色谱法分析泼尼松龙浓度。片剂数据显示达峰时间为1.23±0.68小时（标准差），平均驻留时间为5.1±0.49小时，绝对生物利用度（片剂/静脉注射）为97.5%±17.5%。液体数据显示达峰时间显著缩短（p<0.01），为0.54±0.20小时，平均驻留时间为4.6±0.34小时，绝对生物利用度（液体/静脉注射）为88.2%±15.8%，无显著差异。这导致与片剂相比，液体制剂在最初0.75小时内血浆泼尼松龙浓度显著更高（p<0.05），而在1.5小时后显著更低。液体泼尼松制剂的血浆浓度-时间曲线下泼尼松龙面积为片剂制剂的90.0%±13.2%。因此，液体泼尼松与片剂具有相当的生物利用度，其血浆泼尼松龙浓度峰值出现更早，且在给药后第一小时内血浆泼尼松龙浓度显著更高。
