HPLC测定结肠黏膜中氢化可的松的浓度及其局部作用机理初探

Determination of the hydrocortisone in colonic mucosa and exploring its mechanisms of the local effect of hydrocortisone by HPLC

目的 建立检测结肠黏膜中氢化可的松 (HD)浓度的方法 ,并初步探讨HD灌肠治疗溃疡性结肠炎 (UC)的局部作用机理。方法 采用HPLC测定HD灌肠后不同时间血及肠黏膜活检组织中的药物浓度 ,并由药动学软件算出相应药动学参数。结果 检测了两例患者在使用HD灌肠剂后的 6个不同时点 ,血及肠黏膜组织中HD的浓度 ,并算出相应药动学参数。HD在黏膜中Tmax=1.16h ,T1 2 =0 .84h ;在血中Tmax0 .2 5h ,T1 2 =11.2 3。

OBJECTIVE To establish a method to determine the hydrocortisone levels in colonic biopsied mucosa and explore its mechanisms of the topical effect of the drug.METHODS The hydrocortisone concentrations in plasma and endoscopic mucosal were measured by HPLC. Pharmacokinetic parameters were calculated using a pharmacokinetic software. RESULTS Hydrocortisone concentrations of plasma and colonic mucosa in two patients with active distal ulcerative colitis were investigated after hydrocortisone enema. Pharmacokinetic parameters were calculated. T max in mucosa was 1.16 h and 0.25 h in plasma; T 1/2 in mucosa was 0.84 h and 11.23 h in plasma.CONCLUSION It was conjectured that hydrocortisone enema had both topical and systematic effects.