尸肾移植术后免疫抑制剂Sandimmun和Neoral药物动力学参数比较及临床应用研究

The comparative pharmacokinetics ofSandimmun and Neoral and the clinical ap-plication in cadaveric renal transplantation

Ｎｅｏｒａｌ胶囊是继Ｓａｎｄｉｍｍｕｎ口服液后的另一种剂型。本文研究二者药物动力学参数及临床应用结果。第一部分选择５例肾移植术后超过３个月的稳定患者作自身对照。改用剂型按照１：１的转换剂量，改用前和口服Ｎｅｏｒａｌ８天后，每小时分别测二种剂型血ＣｓＡ浓度，连续测１２ｈ．第二部分对１２例尸肾移植术后分两组，分别口服二种剂型ＣｓＡ，长达１２周，同法测血ＣｓＡ浓度，求出药物动力学参数，加上临床观察。结论：①Ｎｅｏ－ｒａｌ胶囊比Ｓａｎｄｉｍｍｕｎ口服液吸收好，而且稳定。相对生物利用度比Ｓａｎｄｉｍｍｕｎ口服液高２７．５％；②Ｎｅｏｒａｌ胶囊达峰时间比Ｓａｎｄｉｍｍｕｎ口服液短和达峰浓度高，ＡＵＣ也比Ｓａｎｄｉｍｍｕｎ口服液大；③Ｎｅｏｒａｌ胶囊的谷浓度和其ＡＵＣ相关性好，用谷浓度估计ＡＵＣ和调整临床用药量，可靠性大。

eoral gelatin capsule is a new formu-lation of CsA,different from the traditionaloral solution Sandimmun. In this clinical tri-al, pharmacokinetic studies were made tocompare these two formulation of CsA. Partone: The steadystate pharmacokinetics ofSandimmum oral solution and Neoralgelatin capsule were observed in 5 stable re-nal transplant patients with self-controlstudy. Whole blood CsA concentrations ofSandimmum oral solution were monitered12h before taking Neoral gelatin capsule.The dosage conversion from Sandimumm o-ral solution to Neoral gelatin capsule wasmade in a 1 : 1 ratio. One week later,wholeblood CsA concentrations of Neoral gelatinwere monitered in the same manner asSandimmum. Part two :Sandimmum oral solution and Neoral gelatin capsule were givenrespectively to two groups of transplanta-tion patients (6 cases in each group) for 12weeks. It was concluded :1. Absorpton of Neoral gelatin capsulewas better and more steady than that ofSandimmum oral solution. The relativebioavailability of Neoral gelatin capsule is27. 5% higher than that of Sandimmun oralsolu tion .2. Tmax of Neoral gelatin capsule wasshorter than that of Sandimmum oral solu-tion;Cmax of Neoral gelatin capsule washigher than that of Sandimmun oral solu-tion; AUC of Neoral gelatin capsule is largerthan that of Sandimmum oral solution.3. The correlation of trough concentra-tion and AUC of CsA was better shown inNeoral gelatin capsule group than theSandimmun oral solution group. For assess-ing their AUC and adjusting clinicaldosages ,the trough concentration of Neoralgelatin capsule was more reliable than thatof Sadimmun oral solution.