地高辛口服液在健康人体的药代动力学和相对生物利用度  

Pharmacokinetics and relative bioavailability of digoxin solutionin healthy volunteers

作　　者：杨宏[1] 田蕾[1] 黄一玲[1] 李一石[1] 

机构地区：[1]中国医学科学院,中国协和医科大学阜外心血管病医院临床药理中心,北京100037

出　　处：《中国临床药理学杂志》2006年第1期44-46,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究地高辛口服溶液与片剂在健康人体的药代动力学和相对生物利用度。方法20名健康受试者随机交叉、单剂量口服地高辛口服溶液和片剂;用偏振荧光免疫法测定血清中地高辛浓度,计算2种制剂的药代动力学参数,并进行生物等效性评价。结果地高辛口服液和片剂的药代动力学参数AUC0→∞分别为(65.19±12.09)和(67.59±9.77)μg·h·L-1,AUC0→72分别为(42.04±6.25)和(44.91±6.03)μg·h·L-1,tmax分别为(0.64±0.17)和(1.36±0.79)h,Cmax分别为(3.99±1.23)和(3.53±1.02)μg.L-1,t1/2分别为(44.66±8.12)和(44.67±5.02)h。2种制剂(tmax外)均无显著性差异(P>0.05);地高辛口服液的相对生物利用度为(94.8±16.4)%。结论2种制剂具有生物等效性。Objective To study the pharmacokinetics and relative bioavailability of digoxin solution and tablet in 20 healthy male volunteers. Methods A single oral dose of 0.75 mg digoxin solution （ 15 mL） or tablet were given to each volunteer according to an open randomized crossover design. The concentration of digoxin in serum was determined by fluorescent polarization immunoassay. The pharmacokinetic parameters were calculated and the bioequivalence were compared. Results The main pharmacokinetic parameters of digoxin solution and tablet were as follows： AUC0→∞ were （65.19 ± 12.09） and （67.59±9.77）μg·h·L^-1 ; AUC0→72 were （42.04 ±6.25 ） and （44.91±6.03 ）μg·h · L^-1 ; tmax were （0.64±0.17） and （1.36±0.79） h; Cmax were （3.99±1.23） and （3.53±1.02）μg· L^-t; t1/2 were （44.66±8.12） and （ 44.67±5.02 ） h. The relative bioavailability of the drug was （ 94.8±16.4 ） %. Conclusion The two digoxin formulations are bioequivalent.

关 键 词：地高辛口服液及片剂 药代动力学 相对生物利用度 

分 类 号：R969.1[医药卫生—药理学] R972.1[医药卫生—药学]