Bökenkamp A, Offner G, Hoyer P F, Vester U, Wonigeit K, Brodehl J
Children's Hospital, Hanover Medical School, Germany.
Pediatr Nephrol. 1995 Apr;9(2):196-8. doi: 10.1007/BF00860745.
Recently, a new oral microemulsion formulation of cyclosporin A (CsA)--Neoral (Sandoz, Basle, Switzerland)--with a higher bioavailability has become available. Ten stable paediatric renal transplant recipients with excessive variations in CsA trough levels with the original Sandimmun (Sandoz, Basle, Switzerland) preparation were switched to Neoral on a 1:1 basis. Pharmacokinetic studies revealed impaired absorption of Sandimmun in six patients. Compared with equal doses of Sandimmun, the 8-h area under the concentration-time curve increased from 1,422 to 2,657 ng x h/ml and the peak concentration rose from 319 to 824 ng/ml (P < 0.01). In six patients with Sandimmun malabsorption, conversion on a 1:1 basis led to a reduction in creatinine clearance which was reversible after dose reduction by 9%-25%. With trough levels at the lower end of the present target range, creatinine clearance stabilised around pre-conversion values.
最近，一种具有更高生物利用度的新型环孢素A（CsA）口服微乳制剂——新山地明（Neoral，山德士公司，瑞士巴塞尔）已上市。10名稳定的儿科肾移植受者，其使用原山地明（Sandimmun，山德士公司，瑞士巴塞尔）制剂时环孢素A谷浓度波动过大，被一对一转换为新山地明。药代动力学研究显示，6名患者存在山地明吸收受损情况。与等量的山地明相比，浓度-时间曲线下8小时面积从1422增加至2657 ng·h/ml，峰值浓度从319升至824 ng/ml（P<0.01）。在6名山地明吸收不良的患者中，一对一转换导致肌酐清除率降低，在剂量降低9%-25%后可逆转。当谷浓度处于当前目标范围下限水平时，肌酐清除率稳定在转换前的值附近。
