van den Borne B E, Landewé R B, Goei The H S, Mattie H, Breedveld F C, Dijkmans B A
Department of Rheumatology, University Hospital, Leiden, The Netherlands.
Br J Clin Pharmacol. 1995 Feb;39(2):172-5. doi: 10.1111/j.1365-2125.1995.tb04425.x.
The relative bioavailability of cyclosporin A (CsA) from a new microemulsion oral formulation (NEO) and the currently used soft gelatine capsule (SGC) was determined at steady state in 12 patients with rheumatoid arthritis. The AUC(0,12 h) values of cyclosporin A were significantly greater after NEO than SGC (2873 +/- 848 ng ml-1 h (mean +/- s.d.) vs 2355 +/- 1128 ng ml-1 h; P = 0.02, 95% CI (confidence interval of the difference: 81 to 955 ng ml-1 h). Cmax values were significantly higher after NEO than after SGC (811 +/- 244 ng ml-1 vs 495 +/- 291 ng ml-1, P < 0.0001, 95% CI of the difference: 209 to 422 ng ml-1).
在12例类风湿性关节炎患者中,以稳态测定了新的微乳口服制剂(NEO)和目前使用的软胶囊(SGC)中环孢素A(CsA)的相对生物利用度。环孢素A的AUC(0,12 h)值在服用NEO后显著高于SGC(2873±848 ng ml-1 h(平均值±标准差)对2355±1128 ng ml-1 h;P = 0.02,95%置信区间(差异的置信区间:81至955 ng ml-1 h)。NEO后的Cmax值显著高于SGC后(811±244 ng ml-1对495±291 ng ml-1,P < 0.0001,差异的95%置信区间:209至422 ng ml-1)。