Jiang W, Wang X, Xu X, Kong L
Department of Neonatal Surgery, Nanjing Children's Hospital Affiliated to Nanjing Medical University, China.
Int J Clin Pharmacol Ther. 2010 Mar;48(3):224-9. doi: 10.5414/cpp48224.
Tacrolimus (Tac) is widely used to prevent allograft rejection after liver transplantation. We found that the concentration of Tac in blood was significantly increased in liver transplant patients who were receiving Schisandra sphenanthera extract (SchE). The objective of this study was to determine the effect of SchE on the concentration of Tac in the blood of liver transplant patients.
Patients were initially administered Tac (first phase) and then SchE was provided (second phase). During the first phase of treatment, 46 patients received the same oral dose of Tac. In the second phase of treatment, 21 patients (Group A) received the same dose of Tac and 25 patients (Group B) received a lower dose of Tac. The concentration of Tac in the blood and the biochemical indices of liver function, as well as symptoms of Tac-related toxicity, were determined, and 14 patients were selected for a pharmacokinetic study.
After co-administration of Tac and SchE, the average increase in the mean concentration of Tac in the blood was 339% and 262% in Groups A and B, respectively. The liver function indices were decreased significantly (p < 0.01); whereas the average increase of Cmax, AUC0-12 and AUMC0-12 of Tac was 183%, 212% and 227%, respectively. Tac-associated side-effects, such as diarrhoea and agitation, decreased significantly in all patients, but the incidence of other side-effects did not change significantly.
SchE markedly increased the concentration of Tac in the blood of liver transplant patients, improved liver function and reduced the incidence of Tac-associated side-effects.
他克莫司（Tac）被广泛用于预防肝移植后的同种异体移植排斥反应。我们发现，接受五味子提取物（SchE）的肝移植患者血液中他克莫司的浓度显著升高。本研究的目的是确定SchE对肝移植患者血液中他克莫司浓度的影响。
患者最初接受他克莫司治疗（第一阶段），然后给予SchE（第二阶段）。在治疗的第一阶段，46名患者接受相同口服剂量的他克莫司。在治疗的第二阶段，21名患者（A组）接受相同剂量的他克莫司，25名患者（B组）接受较低剂量的他克莫司。测定血液中他克莫司的浓度、肝功能生化指标以及与他克莫司相关的毒性症状，并选择14名患者进行药代动力学研究。
他克莫司与SchE联合使用后，A组和B组血液中他克莫司平均浓度的平均升高分别为339%和262%。肝功能指标显著下降（p<0.01）；而他克莫司的Cmax、AUC0-12和AUMC0-12的平均升高分别为183%、212%和227%。所有患者中与他克莫司相关的副作用，如腹泻和躁动，显著减少，但其他副作用的发生率没有显著变化。
SchE显著提高了肝移植患者血液中他克莫司的浓度，改善了肝功能，并降低了与他克莫司相关的副作用的发生率。
