氯化钾缓释片的人体生物等效性研究

Study on Bioequivalence of Potassium Chloride Sustained-Release Tablets in Healthy Volunteers

目的采用原子吸收/火焰发射分光光度法测定尿钾含量对氯化钾缓释片进行人体生物等效性研究。方法将20名健康受试者随机分2组进行单剂量双交叉试验,冲洗期为7 d。每一周期的给药前3 d为饮食平衡期和基线期,用以排除非药物性钾的影响。第4天为给药期,分别po试验制剂或参比制剂3 g（相当于40.27 mEq）,收集0～2,2～4,4～6,6～8,8～10,10～12,12～24,24～48 h尿样,测定尿钾排泄总量。结果口服氯化钾缓释片参比制剂和试验制剂的0～48 h尿钾累积净排泄量（Ae0-48 h）分别为（26.63±5.71）和（26.46±6.72）mEq,最大净排泄速率（Rmax）分别为（2.85±1.10）和（2.64±1.12）mEq·h^-1,最大净排泄时间（tmax）分别为（5.50±2.42）和（5.60±1.96）h。以Ae0-48 h计算,氯化钾缓释片试验制剂的相对生物利用度平均为99.2%。试验制剂与参比制剂相比,Ae0-48 h（经自然对数转换）、Rmax和tmax均无显著性差异。结论2种制剂在人体内生物等效。

OBJECTIVE To determine the contents of potassium in human urine. Using to atom absorption/flame emission spectrophotometric method. In order to evaluate the bioequivalence of potassium chloride sustained-release tablets in healthy volunteers. METHODS Twenty healthy volunteers were classified into two groups in a two-crossing design. A single dose of 3 g （40. 27 mEq） was administrated to subjects. The wash time was 7 d tests. The urine were reserved at 0 -2,2 -4,4 -6,6 -8,8 - 10,10 - 12,12 - 24 and 24 -48 hours. The contents of potassium were determined. RESULTS The amount of excretory potassium of two formulations in 0 -48 h（Ae0-48 h ） was （26. 63±5.71 ） and （26.46±6. 72）mEq, Rmax was （2.85±1.10） and （2. 64±1.12） mEq·h^-1, tmax was （5. 50±2.42） and （5.60±1.96）h, and the relative bioavailability was 99. 2%. The pharmacokinetic parameters obtained from our studies showed no significant difference between two formulations. CONCLUSION The two formulations are bioequivalence.