氯化钾泡腾片人体相对生物利用度研究  

RELATIVE BIOAVAILABILITY OF EFFERVESCENT TABLET OF POTASSIUM CHLORIDE IN HEALTHY VOLUNTEERS

作　　者：马越鸣[1] 裘福荣[2] 冒国光[2] 曾照宏[2] 陈波[2] 孙华[2] 

机构地区：[1]皖南医学院药理学教研室,安徽芜湖241001 [2]皖南医学院附属弋矶山医院临床医学研究所,安徽芜湖241001

出　　处：《药学学报》2001年第9期699-702,共4页Acta Pharmaceutica Sinica

摘　　要：目的　探讨内源性药物人体药代动力学及相对生物利用度研究方法。方法　 18名健康志愿者按随机三交叉设计进行试验。在研究的 3周期中 ,两周期分别po氯化钾泡腾片或氯化钾普通片剂 2g,另一周期不服药作对照 ,用以排除非药物性钾的影响。每一周期在给药后收集 0 - 2 ,2 - 4,4- 6 ,6 - 8,8- 10 ,10 - 12 ,12 - 2 4,2 4- 48h尿样 ,测定尿钾量。用带一级吸收的一室模型拟合尿钾累积排泄量 时间数据。以给药后 0 - 48h尿钾累积排泄量计算生物利用度 ,用方差分析和双单侧t检验进行制剂的等效性分析。结果　氯化钾泡腾片的药代动力学参数为T1 2ke=(6± 5 )h ,T1 2ka=(0 0 8± 0 0 8)h ,ku=(0 0 9± 0 0 4)h- 1 ,Xmax f=(18± 8)mmol;氯化钾普通片的药代动力学参数为T1 2ke=(8± 5 )h ,T1 2ka=(0 11± 0 11)h ,ku=(0 0 7± 0 0 4)h- 1 ,Xmax f=(18± 8)mmol。氯化钾泡腾片相对生物利用度F =97 5 %± 15 2 %。结论　氯化钾泡腾片和氯化钾普通片剂有生物等效性。AIM To probe the approach by which the pharmacokinetics and relative bioavailability of endogenous medicinal substances can be studied. METHODS A randomized three-crossover study was performed in 18 healthy male volunteers. In two of the three study periods, a single 2 g dose of either effervescent tablet or common tablet of potassium chloride was administered; whereas in one of three periods no drug treatment was given to allow the nondrug-related (endogenous) potassium in urine to be determined. In each period the urine samples were collected at the following intervals: 0-2, 2-4, 4-6, 6-8, 8-10, 10-12, 12-24, 24-48 h after dose. Urine potassium was determined and the cumulative urine potassium-time data were fitted to a one-compartment model with first-order absorption. Bioavailability was represented by cumulative amount of potassium excreted in urine during 48 hours after drug administration and the bioequivalence of the two formulations was evaluated by analysis of variance and two one-sided t -test. RESULTS The pharmacokinetic parameters were as follows: effervescent tablet T 1/2 ke =(6±5) h, T 1/2 ka =(0 08±0 08) h, k u=(0 09±0 04) h -1 , X max / f =(18±8) mmol; common tablet T 1/2 ke =(8±5) h, T 1/2 ka =(0 11±0 11) h, k u=(0 07±0 04) h -1 , X max / f =(18±8) mmol. Relative bioavailability of effervescent tablet was 97 5%±15 2% compared with common tablet. CONCLUSION The two formulations were of bioequivalence. The methods used in this study might be applicable to other similar studies involving endogenous medicinal substances.

关 键 词：药代动力学 生物利用度 内源性药物 氯化钾泡腾片 

分 类 号：R977.7[医药卫生—药品] R969.1[医药卫生—药学]