Comparative bioavailability of rifampicin and isoniazid in fixeddose combinations and single-drug formulations

International Journal of Tuberculosis and Lung Disease

Volumn 18, Issue 12, 2014, Pages 1505-1512

  Hao, L H ^a   Guo, S C ^a   Liu, C C ^a   Zhu, H ^a   Wang, B ^a   Fu, L ^a   Chen, M T ^b   Zhou, L ^b   Chi, J Y ^b   Yang, W ^a   Nie, W J ^a   Lu, Y ^a  

^a CAPITAL MEDICAL UNIVERSITY   (China)

^b National Center for Tuberculosis Control and Prevention   (China)

Author keywords

Bioavailability; Fixed dose combination; Pharmacokinetics; Tuberculosis

Indexed keywords

ISONIAZID; RIFAMPICIN; DRUG COMBINATION; TABLET; TUBERCULOSTATIC AGENT;

ACCURACY; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; CHINA; COMPARATIVE STUDY; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG FORMULATION; DRUG HALF LIFE; DRUG TOLERABILITY; HUMAN; HUMAN EXPERIMENT; INTER ASSAY PRECISION; INTER DAY PRECISION; INTRA ASSAY PRECISION; INTRA DAY PRECISION; LIMIT OF DETECTION; LIMIT OF QUANTITATION; LIQUID CHROMATOGRAPHY; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; RECEIVER OPERATING CHARACTERISTIC; SINGLE DRUG DOSE; TABLET; TANDEM MASS SPECTROMETRY; TIME TO MAXIMUM PLASMA CONCENTRATION; VALIDATION PROCESS; ADOLESCENT; ADULT; BIOAVAILABILITY; BLOOD; DRUG COMBINATION; DRUG INTERACTION; HALF LIFE TIME; MEDICINAL CHEMISTRY; METABOLIC CLEARANCE RATE; MIDDLE AGED; ORAL DRUG ADMINISTRATION; RANDOMIZED CONTROLLED TRIAL; THERAPEUTIC EQUIVALENCE; YOUNG ADULT;

ADMINISTRATION, ORAL; ADOLESCENT; ADULT; ANTITUBERCULAR AGENTS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; CHINA; CROSS-OVER STUDIES; DRUG COMBINATIONS; DRUG INTERACTIONS; HALF-LIFE; HEALTHY VOLUNTEERS; HUMANS; ISONIAZID; MALE; METABOLIC CLEARANCE RATE; MIDDLE AGED; RIFAMPIN; TABLETS; THERAPEUTIC EQUIVALENCY; YOUNG ADULT;

EID: 84911436619     PISSN: 10273719     EISSN: 18157920     Source Type: Journal    
DOI: 10.5588/ijtld.13.0647     Document Type: Article

References (29)

1. Jindani A, Nunn A J, Enarson D A. Two 8-month regimens of chemotherapy for treatment of newly diagnosed pulmonary tuberculosis: International multicentre randomised trial. Lancet 2004; 364: 1244-1251.
2. Mitchison D A. How drug resistance emerges as a result of poor compliance during short course chemotherapy of tuberculosis. Int J Tuberc Lung Dis 1998; 2: 10-15.
3. Prasad B, Bhutani H, Singh S. Study of the interaction between rifapentine and isoniazid under acid conditions. J Pharm Biomed Anal 2006; 41: 1438-1441.
4. Laserson K F, Kenyon A S, Kenyon T A, et al. Substandard tuberculosis drugs on the global market and their simple detection. Int J Tuberc Lung Dis 2001; 5: 448-454.
5. Food and Drug Administration. Guidance for industry: Bioanalytical method validation (updated 2001). Silver Spring, MD, USA: FDA, 2001. http: //www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm070107.pdf. Accessed September 2014.
6. Agrawal S, Kaur K J, Singh I, et al. Determination of rifampicin bioequivalence in a three-drug FDC by WHO and Indian protocols: Effect of sampling schedule and size. Int J Tuberc Lung Dis 2005; 9: 75-80.
7. Agrawal S, Kaur K J, Singh I, et al. Minimum sample size and sampling time requirements for assessment of rifampicin bioequivalence from FDC formulations. Int J Tuberc Lung Dis 2005; 9: 1273-1280.
8. Zhu H, Li P, Lu Y, et al. LC-MS/MS determination of isoniazid, ethambutol and pyrazinamide in human plasma. Chin J Pharm Anal 2012; 32: 11-15. [Chinese]
9. The promise and reality of fixed-dose combinations with rifampicin. A joint statement of the International Union Against Tuberculosis and Lung Disease and the Tuberculosis Programme of the World Health Organization. Tubercle Lung Dis 1994; 75: 180-181.
10. Blomberg B, Fourie B. Fixed-dose combination drugs for tuberculosis: Application in standardised treatment regimens. Drugs 2003; 63: 535-553.
11. Mitchison D A. Pharmacokinetic/pharmacodynamic parameters and the choice of high-dosage rifamycins. Int J Tuberc Lung Dis 2012; 16: 1186-1189.
12. Peloquin C. Therapeutic drug monitoring in the treatment of tuberculosis. Drugs 2002; 62: 2169-2183.
13. Singh S, Mariappan T T, Sanka R, et al. A critical review of the probable reasons for the poor/variable bioavailability of rifampicin from anti-tubercular fixed-dose combination (FCD) products, and the likely solutions to the problem. Int J Pharm 2001; 228: 5-17.
14. Panchagnula R, Agrawal S. Biopharmaceutic and pharmacokinetic aspects of variable bioavailability of rifampicin. Int J Pharm 2004; 271: 1-4.
15. Panchagnula R, Parmar J, Kaur K, et al. Statistical evaluation of physiological variability of rifampicin in fixed dose combinations. Int J Pharm 2006; 313: 5-13.
16. Agrawal S, Panchagnula R. Implication of biopharmaceutics and pharmacokinetics of rifampicin in variable bioavailability from solid oral dosage forms. Biopharm Drug Dispos 2005; 26: 321-334.
17. Becker C, Dressman J B, Junginger H E, et al. Biowaiver monographs for immediate release solid oral dosage forms: Rifampicin. J Pharm Sci 2009; 98: 2252-2267.
18. Singh S, Mariappan T T, Sharda N, et al. The reason for an increase in decomposition of rifampicin in the presence of isoniazid under acid conditions. Pharm Pharmacol Commun 2000; 6: 405-410.
19. Singh S, Mohan B. A pilot stability study on anti-tuberculosis four drug fixed dose combination products. Int J Tuberc Lung Dis 2003; 7: 298-303.
20. Bhutani H, Mariappan T T, Singh S. The physical and chemical stability of anti-tuberculosis fixed-dose combination (FDC) products under accelerated climatic conditions. Int J Tuberc Lung Dis 2004; 8: 1073-1080.
21. Vamshi T, Girish K, Naveen D, et al. Formulation and evaluation of fixed dose combination products of rifampicin and isonizid with improved rifampicin stability. Int J Pharm Pharm Sci 2013; 5 (Suppl 3): S431-S433.
22. Bhagwat P, Hemant B, Saranjit S. Study of the interaction between rifapentine and isoniazid under acid conditions. J Pharm Biomed Anal 2006; 41: 1438-1441.
23. Singh H, Bhandari R, Indu P K. Encapsulation of rifampicin in a solid lipid nanoparticulate system to limit its degradation and interaction with isoniazid at acidic pH. Int J Pharm 2013; 446: 106-111.
24. Padgaonkar K A, Revankar S N, Bhatt A D, et al. Comparative bioequivalence study of rifampicin and isoniazid combinations in healthy volunteers. Int J Tuberc Lung Dis 1999; 3: 627-631.
25. Milán-Segovia R C, Domínguez-Ramírez A M, Jung-Cook H, et al. Relative bioavailability of rifampicin in a three-drug fixed-dose combination formulation. Int J Tuberc Lung Dis 2010; 14: 1454-1460.
26. Agrawal S, Singh I, Kaur K J, et al. Comparative bioavailability of rifampicin, isoniazid and pyrazinamide from a four drug fixed dose combination with separate formulations at the same dose levels. Int J Pharm 2004; 276: 41-49.
27. Agrawal S, Kaur K J, Singh I, et al. Assessment of bioequivalence of rifampicin, isoniazid and pyrazinamide in a four drug fixed dose combination with separate formulations at the same dose levels. Int J Pharm 2002; 233: 169-177.
28. Jian X, Haixia J, Hui Z, et al. Oral bioavailability of rifampicin, isoniazid, ethambutol, and pyrazinamide in a 4-drug fixed-dose combination compared with the separate formulations in healthy Chinese male volunteers. Clin Ther 2013; 35: 161-168.
29. Singh S, Mariappan T T, Bhutani H. Novel anti-tuberculosis FDC formulations without reduced bioavailability of rifampicin: From concept to market. Int J Tuberc Lung Dis 2005; 9: 701-702.