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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。
Neoral Capsule is another form of Sandimmun oral solution. This article studies both the pharmacokinetic parameters and clinical application results. In the first part, 5 stable patients who were more than 3 months after renal transplantation were selected as self-control. Switching to the dosage form in accordance with the conversion dose of 1: 1, switch to before and after oral administration of Neoral for 8 days, each hour were measured two types of blood CsA concentration, continuous measurement of 12h. The second part of 12 cadaveric renal transplantation divided into two groups, respectively, two oral administration of CsA, up to 12 weeks, the same method of measuring blood CsA concentration, pharmacokinetic parameters, combined with clinical observation. Conclusion: Neo-ral capsule absorbed better than Sandimmun oral solution, and stable. Relative bioavailability was 27.5% higher than that of Sandimmun oral solution; ② Peak time of Neoral capsule was shorter and higher than that of Sandimmun oral solution; AUC was also higher than Sandimmun oral solution; Estimating the AUC with trough concentration and adjusting the amount of clinical medication, reliability.