Zhu Wei, Wang Xue-Mei, Zhang Li, Li Xiao-Ye, Wang Bao-Xiu
Peking University First Hospital, Beijing 100034, China.
Am J Chin Med. 2005;33(6):839-50. doi: 10.1142/S0192415X05003508.
Rhubarb is a common herb used in traditional Chinese medicine. However, few publications exist about its pharmacokinetic profiles in animals or healthy volunteers. Whether retention enema administration of rhubarb extract affects its pharmacokinetics as well as its tolerability is unknown. Therefore, we set out to compare the pharmacokinetic parameters of rhein administered by retention enemas with those of conventional oral dosing of rhubarb extract. Eight healthy male volunteers were enrolled in a prospective crossover study. All subjects received a single dose of rhubarb extract (50 mg.kg(-1)) on two separate occasions, once orally, once by a retention enema. Rhein plasma concentration was measured by HPLC. The C(max), AUC(0-infinity), AUMC were significantly higher in oral administration than those in retention enema administration (p < 0.05), while V(d) of rhein after oral administration of rhubarb extract was significantly lower (p < 0.05) than that after retention enema administration. However, no statistically significant differences between the two treatments were observed for any of the other pharmacokinetic parameters (T(max), t(1/2), MRT(0-infinity), CL). Dosage adjustment is advisable for retention enema administration of rhubarb extract in patients.
大黄是一种常用于传统中药的草药。然而，关于其在动物或健康志愿者体内的药代动力学特征的出版物很少。大黄提取物保留灌肠给药是否会影响其药代动力学以及耐受性尚不清楚。因此，我们着手比较大黄提取物保留灌肠给药与传统口服给药的大黄酸药代动力学参数。八名健康男性志愿者参加了一项前瞻性交叉研究。所有受试者在两个不同的时间接受单剂量的大黄提取物（50mg·kg⁻¹），一次口服，一次通过保留灌肠给药。通过高效液相色谱法测定大黄酸血浆浓度。口服给药的Cmax、AUC(0-∞)、AUMC显著高于保留灌肠给药（p<0.05），而口服大黄提取物后大黄酸的V(d)显著低于保留灌肠给药后（p<0.05）。然而，两种治疗方法在任何其他药代动力学参数（Tmax、t1/2、MRT(0-∞)、CL）方面均未观察到统计学上的显著差异。对于患者，大黄提取物保留灌肠给药建议调整剂量。
