Interspecies scaling: Predicting clearance of drugs in humans. Three different approaches

被引:205
作者
Mahmood, I
Balian, JD
机构
[1] Div. of Pharmaceutical Evaluation I, Off. Clin. Pharmacol. Biopharmaceut., Woodmont Office Center II, Rockville, MD 20852
[2] Neuropharmacological Drug Products, Food and Drug Administration, Woodmont Office Center II, Rockville, MD 20852
关键词
D O I
10.3109/00498259609052491
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. The interspecies scaling approach to predict clearance in humans from animal data was tested for a wide variety of drugs. 2. Three different methods were utilized to generate plots to scale-up the clearance values: (i) method I, clearance versus body weight (simple allometric equation); (ii) method II, product of clearance and maximum life-span potential; (iii) method III, product of clearance and brain weight versus body weight. 3. The circumstances under which the three methods can be applied to predict clearance in humans were evaluated. 4. If the exponent lies between 0.55 to 0.7 then method I predicts clearance reasonably well. 5. If the exponent lies between 0.71 to 1.0 clearance can be predicted reasonably well by method II. 6. If the exponent is > 1.0 clearance can be predicted using method III.
引用
收藏
页码:887 / 895
页数:9
相关论文
共 41 条
[2]   COMPARATIVE PHARMACOKINETICS OF THE NEWER ANTIEPILEPTIC DRUGS [J].
BIALER, M .
CLINICAL PHARMACOKINETICS, 1993, 24 (06) :441-452
[3]   INTERSPECIES COMPARISON OF INVIVO CAFFEINE PHARMACOKINETICS IN MAN, MONKEY, RABBIT, RAT, AND MOUSE [J].
BONATI, M ;
LATINI, R ;
TOGNONI, G ;
YOUNG, JF ;
GARATTINI, S .
DRUG METABOLISM REVIEWS, 1985, 15 (07) :1355-1383
[4]   SCALING OF ANTIPYRINE INTRINSIC CLEARANCE OF UNBOUND DRUG IN 15 MAMMALIAN-SPECIES [J].
BOXENBAUM, H ;
FERTIG, JB .
EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS, 1984, 9 (02) :177-183
[5]   FIRST-TIME-IN-HUMAN DOSE SELECTION - ALLOMETRIC THOUGHTS AND PERSPECTIVES [J].
BOXENBAUM, H ;
DILEA, C .
JOURNAL OF CLINICAL PHARMACOLOGY, 1995, 35 (10) :957-966
[6]   INTERSPECIES VARIATION IN LIVER WEIGHT, HEPATIC BLOOD-FLOW, AND ANTIPYRINE INTRINSIC CLEARANCE - EXTRAPOLATION OF DATA TO BENZODIAZEPINES AND PHENYTOIN [J].
BOXENBAUM, H .
JOURNAL OF PHARMACOKINETICS AND BIOPHARMACEUTICS, 1980, 8 (02) :165-176
[7]  
BOXENBAUM H, 1985, PHARMACOKINETICS PHA, P93
[8]  
BRAZZELL RK, 1990, DRUG METAB DISPOS, V18, P435
[9]   PHARMACOKINETICS OF A NOVEL ANTIARRHYTHMIC DRUG, ACTISOMIDE [J].
COOK, CS ;
ROZEK, LF ;
STOLZENBACH, J ;
ANDERSON, S ;
SCHOENHARD, GL ;
KARIM, A .
PHARMACEUTICAL RESEARCH, 1993, 10 (03) :427-433
[10]   INTERSPECIES SCALING OF TEBUFELONE PHARMACOKINETIC DATA AND APPLICATION TO PRECLINICAL TOXICOLOGY [J].
CRUZE, CA ;
KELM, GR ;
MEREDITH, MP .
PHARMACEUTICAL RESEARCH, 1995, 12 (06) :895-901