Department of Integrative Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China.
Department of Clinical Pharmacology, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China.
Evid Based Complement Alternat Med. 2014;2014:389576. doi: 10.1155/2014/389576. Epub 2014 Feb 16.
Aim. To compare the pharmacokinetics and pharmacodynamics of herbal ointment Liu-He-Dan (LHD) and micron LHD (MLHD) in rats with acute pancreatitis (AP). Methods. Twenty rats were allocated into normal, AP, LHD, and MLHD groups. LHD or MLHD was applied on rats' abdomens. Plasma levels of emodin, rhein, aloe emodin, physcion, and chrysophanol were determined by high performance liquid chromatography-mass spectrometry-mass spectrometry (HPLC-MS-MS) at different time points, and the pharmacokinetic parameters were calculated. Serum amylase, TNF- α , IL-6, and IL-10 levels, and the pancreatic pathological scores were determined at 48 h after LHD or MLHD treatment. Results. T 1/2 α and area under the curve (AUC) of emodin in the MLHD group were lower than those in the LHD group, while T 1/2 α and AUC of aloe emodin in the MLHD group were higher than those in the LHD group (P < 0.05). T 1/2 α and T max of physcion in the MLHD group were significantly shorter than those in the LHD group (P < 0.05). Compared with the AP group, the amylase, malondialdehyde (MDA), TNF- α , and IL-6 levels decreased significantly after three days of treatment in LHD and MLHD groups, while the levels of superoxide dismutase (SOD), TNF- α , and the pancreatic pathological score, were similar. The pharmacodynamic parameters between the LHD and MLHD groups were similar. Conclusion. MLHD had better pharmacokinetics than, and similar pharmacodynamics to, LHD in the management of rats with AP, which indicated that MLHD might be substituted for LHD in the treatment of AP and thus reduce the amount of medicinal herbs used.
比较 Liu-He-Dan(LHD)草药软膏和微粉化 LHD(MLHD)在急性胰腺炎(AP)大鼠中的药代动力学和药效学。
将 20 只大鼠随机分为正常组、AP 组、LHD 组和 MLHD 组。LHD 或 MLHD 应用于大鼠腹部。在不同时间点采用高效液相色谱-串联质谱法(HPLC-MS-MS)测定血浆大黄素、大黄酸、芦荟大黄素、大黄素、大黄酚的浓度,并计算药代动力学参数。在 LHD 或 MLHD 治疗后 48 小时测定血清淀粉酶、TNF-α、IL-6、IL-10 水平和胰腺病理评分。
与 LHD 组相比,MLHD 组大黄素的 T 1/2α和 AUC 较低,而芦荟大黄素的 T 1/2α和 AUC 较高(P<0.05)。MLHD 组大黄酚的 T 1/2α和 T max 明显短于 LHD 组(P<0.05)。与 AP 组相比,LHD 和 MLHD 组治疗 3 天后淀粉酶、丙二醛(MDA)、TNF-α和 IL-6 水平显著降低,而超氧化物歧化酶(SOD)、TNF-α和胰腺病理评分水平相似。LHD 和 MLHD 组之间的药效学参数相似。
与 LHD 相比,MLHD 在治疗 AP 大鼠方面具有更好的药代动力学特性,且药效学相似,这表明 MLHD 可能替代 LHD 治疗 AP,从而减少草药用量。