Mahmood I
Division of Pharmaceutical Evaluation I, Food and Drug Administration, Rockville, MD 20852, USA.
Biopharm Drug Dispos. 1997 Aug;18(6):465-73. doi: 10.1002/(sici)1099-081x(199708)18:6<465::aid-bdd41>3.0.co;2-c.
In order to determine the absolute bioavailability, both oral and intravenous administrations of a drug are often used. Recently a new method has been proposed to determine absolute bioavailability in the absence of intravenous dose. Following a single oral dose, this method requires oral and renal clearance data from normal subjects and renal failure patients. The bioavailability is calculated from a plot of oral against renal clearance following an oral dose, where the inverse of the slope is equal to absolute bioavailability. This study examines the prediction of absolute bioavailability from the proposed method for eight drugs which have a wide range of oral and renal clearance. From this study, it appears that the proposed method may not be reliable for the prediction of absolute bioavailability and further investigation is needed to test the validity of this method.
为了确定绝对生物利用度，通常会采用药物的口服和静脉给药方式。最近，有人提出了一种在无静脉给药剂量的情况下测定绝对生物利用度的新方法。单次口服给药后，该方法需要正常受试者和肾衰竭患者的口服清除率及肾脏清除率数据。生物利用度通过口服给药后口服清除率与肾脏清除率的关系图来计算，其中斜率的倒数等于绝对生物利用度。本研究考察了所提出的方法对八种口服清除率和肾脏清除率范围广泛的药物的绝对生物利用度预测情况。从这项研究来看，所提出的方法在预测绝对生物利用度方面可能不可靠，需要进一步研究以检验该方法的有效性。
