Goshima E, Yasuda K, Fuwa Y, Adachi K, Minamori Y, Murase H, Murayama M, Yamakita N, Miura K
Nihon Naibunpi Gakkai Zasshi. 1986 Jun 20;62(6):697-712. doi: 10.1507/endocrine1927.62.6_697.
We studied the pharmacokinetics of prednisolone (PSL) in eight patients (two each with subacute thyroiditis, systemic lupus erythematosus, and nephrotic syndrome: and one each of Crohn's disease and aortitis syndrome) before and during the daily treatment with PSL(duration of 0.5-4.0 months with the mean of 1.9 months; total amount of 0.3-8.0 g with the mean of 2.8 g). PSL was measured by radioimmunoassay. Cmax, Tmax and AUCp.o. were calculated on the single oral administration of 40 mg PSL, and T1/2 beta, Vd and MCR were calculated when 25.6 mg of PSL sodium succinate (equivalent to 20 mg of PSL) was injected intravenously. Bioavailability was calculated by the ratio of AUCp.o. X PSL i.v. dose to AUCi.v. X PSL p.o. dose. With the oral administration, there was no difference in Cmax, Tmax and AUCp.o. between before and during the treatment, respectively. With the intravenous PSL administration, significant increase of AUCi.v. (p less than 0.01), significant decrease of MCR (p less than 0.01), significant elongation of T1/2 beta (p less than 0.05), and significant decrease of the bioavailability (p less than 0.001) were found in the PSL treatment period compared with before the treatment, but no significance was found in Vd between, before, and during the treatment. There was no difference in these changes in parameters among the diseases. Nor were any correlations found between the changes in these parameters of T1/2 beta, MCR or bioavailability and the duration or the total amount of PSL administered, respectively. These results indicate that the decreased MCR, elongated T1/2 beta and the decreased bioavailability of PSL were brought about by daily administration of PSL, regardless of the kind of diseases, or the total amount or the duration of PSL administration.
我们研究了8例患者（亚急性甲状腺炎、系统性红斑狼疮和肾病综合征各2例，克罗恩病和大动脉炎综合征各1例）在每日服用泼尼松龙（PSL）治疗前及治疗期间（疗程0.5 - 4.0个月，平均1.9个月；总量0.3 - 8.0 g，平均2.8 g）的药代动力学情况。PSL采用放射免疫分析法测定。单次口服40 mg PSL后计算Cmax、Tmax和AUCp.o.，静脉注射25.6 mg PSL琥珀酸钠（相当于20 mg PSL）时计算T1/2 beta、Vd和MCR。生物利用度通过AUCp.o.×PSL静脉剂量与AUCi.v.×PSL口服剂量之比计算得出。口服给药时，治疗前与治疗期间的Cmax、Tmax和AUCp.o.分别无差异。静脉注射PSL时，与治疗前相比，PSL治疗期间AUCi.v.显著升高（p＜0.01），MCR显著降低（p＜0.01），T1/2 beta显著延长（p＜0.05），生物利用度显著降低（p＜0.001），但治疗前、治疗期间的Vd无显著差异。这些参数变化在各疾病之间无差异。T1/2 beta、MCR或生物利用度这些参数的变化与PSL给药的疗程或总量之间也未发现相关性。这些结果表明，无论疾病种类、PSL给药总量或疗程如何，每日服用PSL均会导致PSL的MCR降低、T1/2 beta延长和生物利用度降低。
