Bioequivalence model for evaluation of losartan in human plasma with special reference to drugmetabolite ratio drug-active metabolite ratio dipanjan Goswami et al.

Clinical Research and Regulatory Affairs

Volumn 26, Issue 4, 2009, Pages 101-112

  Goswami, Dipanjan ^a   Gurule, Sanjay ^a   Khuroo, Arshad H ^a   Monif, Tausif ^a  

^a RANBAXY LABORATORIES LTD   (India)

Author keywords

Drug metabolism; Losartan bioequivalence; Losartan:Losartan carboxylic acid metabolic ratio (MR) comparative analysis; Pharmacokinetics (DMPK)

Indexed keywords

CARBOXYLIC ACID DERIVATIVE; HYDROCHLOROTHIAZIDE PLUS LOSARTAN; LOSARTAN; LOSARTAN CARBOXYLIC ACID; LOSARTAN POTASSIUM; UNCLASSIFIED DRUG;

ADULT; AGED; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG ELIMINATION; DRUG FORMULATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG SCREENING; HUMAN; HUMAN EXPERIMENT; IN VIVO STUDY; INDIAN; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; NUCLEAR MAGNETIC RESONANCE; PHARMACOLOGICAL PARAMETERS; PLASMA; RACE DIFFERENCE; REFERENCE VALUE; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION;

EID: 70449372680     PISSN: 10601333     EISSN: 15322521     Source Type: Journal    
DOI: 10.3109/10601330903271263     Document Type: Article

References (22)

1. Timmermans PBMWM, Wong PC, Chiu AT, Herblin WF, Benfield P, Carini DJ, Lee RJ, Wexler RR, Saye JAM, Smith RD. Angiotensin II receptors and angiotensin II receptor antagonists. Pharmacol Rev 1993;45:205-251.
2. Munafo A, Christen Y, Nussberger J, Shum LY, Borland RM, Lee RJ, Waeber B, Biollaz J, Brunner HR. Drug concentration response relationship in normal volunteers after oral administration of losartan, an angiotensin II receptor antagonist. Clin Pharmacol Ther 1992;51:513-521.
3. Lo MW, Goldberg MR, McCrea JB, Lu H, Furtek CI, Bjornsson TD. Pharmacokinetics of losartan, an angiotensin II receptor antagonist, and its active metabolite EXP3174 in humans. Clin Pharmacol Ther 1995;58:641-649.
4. Sica DA, Gehr TW, Ghosh S. Clinical pharmacokinetics of losartan. Clin Pharmacokinet 2005;44:797-814.
5. Munafo A, Christen Y, Nussberger J, Shum LY, Borland RM, Lee RJ, Waeber B, Biollaz J, Brunner HR Drug concentration response relationship in normal volunteers after oral administration of losartan, an angiotensin II receptor antagonist. Clin Pharmacol Ther 1992;51:513-521.
6. Ohtawa1 M, Takayama F, Saitoh K, Yoshinaga T, Nakashima M. Pharmacokinetics and biochemical efficacy after single and multiple oral administration of losartan, an orally active nonpeptide angiotensin II receptor antagonist, in humans. Br J Clin Pharm 1993;35:290-297.
7. Kolocouri F, Dotsikas Y, Apostolou C, Kousoulos C, Loukas YL. Simultaneous determination of losartan, EXP- 3174 and hydrochlorothiazide in plasma via fully automated 96-well-format-based solid-phase extraction and liquid chromatography-negative electrospray tandem mass spectrometry. Anal Bioanal Chem 2007;387:593-601.
8. Tamimi JJI, Salema II, Alamb SM, Zamanb Q, Dhamb R. Comparative pharmacokinetics of two tablet formulations of Losartan: bioequivalence assessment. Biopharm Drug Dispos 2005;26: 205-210.
9. Prasaja B, Sasongko L, Harahap Y, Hardiyanti, Lusthom W, Grigg M. Simultaneous quantification of losartan and active metabolite in human plasma by liquid chromatography-tandem mass spectrometry using irbesartan as internal standard. J Pharm Biomed Anal 2009;49:862-867.
10. Dickson TZ, Zagrobelny JA, Lin CC, Ritter MA, Snavely D, Ramjit D, Shahinfar S, Lo MWJ. Pharmacokinetics, safety, and antihypertensive efficacy of losartan in combination with hydrochlorothiazide in hypertensive patients with renal impairment. Clin Pharmacol 2003;43:591.
11. Sandwall P, Lo MW, Jonzon B, Furtek PDC, Ritter MA, Alvan G, McCrea J, Sjoqvist F. Lack of polymorphism of the conversion of losartan to its active metabolite E-3174 in extensive and poor metabolizers of debrisoquine (cytochrome P450 2D6) and mephenytoin (cytochrome P450 2C19). Eur J Clin Pharmacol 1999;55:279-283.
12. Agnieszka B, Rafal B, Edyta S, Vitali D, Edmund G, Stanislaw D, Leon D, Anna W, Magdalena OR. Bioequivalence study of two losartan formulations administered orally in healthy male volunteers. Arzneimittel-Forschung (Arzneimittelforschung) 2006;56:723-728.
13. Neves R, Almeida S, Filipe A, Spinola AC, Abolfathi Z, Yritia M, Ortuno J. Bioequivalence study of two different film-coated tablet formulations of losartan-hydrochlorothiazide in healthy volunteers. Arzneimittelforschung 2008;58:369-375.
14. Goswami D, Kumar A, Khuroo AH, Monif T, Thudi NR, Shrivastav VK, Dubey SK, Shingla AK, Prakash M, Mehra S. Pharmacokinetic estimation of losartan, losartan carboxylic acid and hydrochlorothiazide in human plasma by LC/MS/MS validated method. Clin Res Regul Affairs 2008;25:235-258.
15. Schuirmann DJ. A comparison of two one-sided test procedure and the power approach for assessing the equivalence of the average bioavailability. J Pharmacokinet Biopharm 1987;15:657-680.
16. Chow CS, Liu JP. Design and analysis of bioavailability and bioequivalence studies. New York: Marcel Dekker; 1992.
17. Food and Drug Administration. Guidance for industry: Bioavailability and bioequivalence studies for orally administered drug products-General considerations. March, 2003. Available online at: www.fda.gov/cder/guidance/ 5356fnl.pdf, accessed February 22, 2009.
18. Validation of analytical procedures: Methodology, ICH-Q2B, International Conference on Harmonization of Technical Requirements for the Registration of Pharmaceuticals for Human Use, Geneva, Switzerland; 1996. Guidance for Industry: Q2B Validation of Analytical Procedures: Methodology; 1996. http://www.fda.gov/downloads/Drugs/ GuidanceComplianceRegulatoryInformation/ Guidances/ ucm073384.pdf
19. Raghavan K, Dwivedi A, Campbell Jr GC, Johnston E, Levorse D, McCauley J, Hussian MA. Spectroscopic investigation of losartan polymorphs. Pharm Res 1993;6:900-904.
20. Patoèka J, Dvoøak A. Biomedical aspects of chiral molecules. J Appl Biomed 2004;2:95-100.
21. Caldwell J. Do single enantiomers have something special to offer? Hum Psycopharmacol Clin Exp 2001;16:S67-S71.
22. Lin Y, Lu P, Tang C, Mei Q, Sandig G, Rodrigues AD, Rushmore TH, Shou M. Substrate inhibition kinetics for cytochrome P-450-catalyzed reactions. Drug Metab Dispos 2001;29:368-374. (Pubitemid 32275548)