View More View Less
  • 1 Laboratório de Desenvolvimento de Medicamentos, Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal Do Rio Grande Do Norte—UFRN, R. Brigadeiro Cordeiro de Farias, s/n Petrópolis, CEP 59010-180, Natal, RN, Brazil
  • | 2 Laboratório de Desenvolvimento de Medicamentos, Programa de Pós-Graduação em Desenvolvimento e Inovação Tecnológica em Medicamentos, Universidade Federal do Rio Grande Do Norte—UFRN, R. Brigadeiro Cordeiro de Farias, s/n, Petrópolis, Natal, RN, CEP 59010-180, Brazil
  • | 3 Laboratório de Desenvolvimento de Medicamentos, Departamento de Farmácia, Universidade Federal Do Rio Grande Do Norte—UFRN, R. Brigadeiro Cordeiro de Farias, s/n, Petrópolis, Natal, RN, CEP 59010-180, Brazil
Restricted access

Abstract

Worldwide Brazil is among one of the 22 countries with high rates of tuberculosis placing this disease as a priority for the Government Health Policies in this country. Studies with the main tuberculostatic drugs rifampicin, isoniazid, pyrazinamide, and ethambutol, aiming the development of fixed-dose combination formulations (FDCs) have been performed. The aim of this study was to evaluate the thermal behavior of these drugs by DSC, TG/DTG, and DTA in order to predict possible physical and chemical interactions between tuberculostatics. DSC and DTA curves suggested incompatibility and/or interactions among drug preparations resulting from new thermal events, as well as the disappearance and shift of the melting point of the drugs. TG/DTG curves of drug mixtures presented different profiles from those observed for the individually tested drugs, supporting the evidence of drug incompatibility and indicating that mixtures are less stable when compared to the drugs alone.

  • 1. World Health Organization. WHO report 2007, Global tuberculosis control: surveillance, planning, financing, Geneva. World Health Organization; 2007. http://www.who.int/tb/publications/global_report/2008/pdf/fullreport.pdf. Accessed 11 Jan 2010.

    • Search Google Scholar
    • Export Citation
  • 2. World Health Organization. Ministério da Saúde. Secretaria de Vigilância em Saúde. Programa Nacional de Controle da Tuberculose—PNCT, 2008. http://www.cve.saude.sp.gov.br. Accessed 2 Feb 2010.

    • Search Google Scholar
    • Export Citation
  • 3. Singh, S, Bhutani, H, Mariappan, TT. Quality problems of anti-tuberculosis fixed-dose combinations (FDCs): a way forward. Ind J Tuberc. 2006;5:201205.

    • Search Google Scholar
    • Export Citation
  • 4. Bottom, R. The role of modulated temperature differential scanning calorimetry in the characterisation of a drug molecule exhibiting polymorphic and glass forming tendencies. Int J Pharm. 1999;192:4753. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 5. McDaid, FM, Barker, SA, Fitzpatrick, S, Petts, CR, Craig, DQM. Further investigations into the use of high sensitivity differential scanning calorimetry as a means of predicting drug-excipient interactions. Int J Pharm. 2003;252:235240. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 6. Singh, S, Bhutani, H, Mariappan, TT, Kaur, H, Bajaj, M, Pakhale, SP. Behavior of uptake of moisture by drugs and excipients under accelerated conditions of temperature and humidity in the absence and the presence of light. Part 1: pure anti-tuberculosis drugs and their combinations. Int J Pharm. 2002;245:3744. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 7. Cheng, SZD, Li, CY, Calhoun, BH, Zhu, L, Zhou, WW. Thermal analysis: the next two decades. Thermochim Acta. 2000;355:5968. .

  • 8. Procópio JVV , Souza VG de, Costa RA da, Correia LP, Souza FS de, Macêdo RO. Application of thermal analysis and pyrolysis coupled to GC/MS in the qualification of simvastatin pharmaceutical raw material. J Therm Anal Calorim. 2010. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 9. Vemuri, NM, Chrzan, Z, Cavatur, R. Use of isothermal microcalorimetry in pharmaceutical preformulation studies. Part I. Monitoring crystalline phase transitions. J Therm Anal Calorim. 2004;78:4754. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 10. Cavatur, R, Vemuri, NM, Chrzan, Z. Use of isothermal microcalorimetry in pharmaceutical preformulation studies. Part III. Evaluation of excipient compatibility of a new chemical entity. J Therm Anal Calorim. 2004;78:6372. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 11. Pinto, MF, de Moura, EA, De Souza, FS, Macêdo, RO. Thermal compatibility studies of nitroimidazoles and excipients. J Therm Anal Calorim. 2010;102:323329. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 12. Nunes, RS, Semaan, FS, Riga, AT, Cavalheiro, ETG. Thermal behavior of verapamil hydrochloride and its association with excipients. J Therm Anal Calorim. 2009;97:349353. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 13. Freitas, MN, Alves, R, Matos, JR, Marchetti, JM. Thermal analysis applied in the osmotic tablets pre-formulation studies. J Therm Anal Calorim. 2007;87:905911. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 14. Freire, FD, Aragão, CFS, de Le Moura, TA, Raffin, FN. Compatibility study between chlorpropamide and excipients in their physical mixtures. J Therm Anal Calorim. 2009;97:355357. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 15. Freire, FD, Aragão, CFS, de Le Moura, TA, Raffin, FN. Thermal studies of isoniazid and mixtures with rifampicin. J Therm Anal Calorim. 2009;97:333336. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 16. Avula, SG, Alexander, K, Riga, AT. Predicting eutectic behavior of drugs and excipients by unique calculations. J Therm Anal Calorim. 2010;99:655658. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 17. Aigner Z , Heinrich R, Sipos E, Farkas G, Ciurba A, Berkesi O, Szabó-Révész P. Compatibility studies of aceclofenac with retard tablet excipients by means of thermal and FT–IR spectroscopic methods. J Therm Anal Calorim. 2010. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 18. Tita B , Fulias A, Szabadai Z, Rusu G, Bandur G, Tita D. Compatibility study between ibuprofen and excipients in their physical mixtures. J Therm Anal Calorim. 2010. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 19. Tita D , Fulias A, Tita B. Thermal stability of ketoprofen-active substance and tablets. J Therm Anal Calorim. 2010. .

  • 20. Castro, RAE, Maria, TMR, Évora, AOL, Feiteira, JC, Silva, MR, Beja, AM, Canotilho, J, Eusébio, MES. A new insight into pyrazinamide polymorphic forms and their thermodynamic relationships. Cryst Growth Des. 2010;10:274282. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 21. Bertol, CD, Cruz, AP, Stulzer, HK, Murakami, FS, Silva, MAS. Thermal decomposition kinetics and compatibility studies of primaquine under isothermal and non-isothermal conditions. J Therm Anal Calorim. 2010;102:187192. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 22. Agrawal, S, Ashokraj, Y, Bharatam, PV, Pillai, O, Panchagnula, R. Solid-state characterization of rifampicin samples and its biopharmaceutic relevance. Eur J Pharm Sci. 2004;22:127144. .

    • Crossref
    • Search Google Scholar
    • Export Citation
  • 23. Alves R . Estudo termoanalítico e de compatibilidade fármaco-excipiente de rifampicina e alguns medicamentos utilizados na terapêutica da tuberculose. Dissertation, Postgraduate in in drugs and medicines, USP, 2007.

    • Search Google Scholar
    • Export Citation
  • 24. Prasad, B, Bhutani, H, Kumar, V, Singh, S. A new validated differential scanning calorimetric procedure for monitoring the less active r, s isomer of ethambutol dihydrochloride in bulk drug samples and anti-tuberculosis formulations. Pharm Forum. 2007;33:326333.

    • Search Google Scholar
    • Export Citation
  • 25. Wesolowski, M, Konarski, T. Characteristics of the thermal decomposition of antituberculosis drugs. J Therm Anal Calorim. 1995;45:11991204. .

  • 26. Takaki, Y, Sasada, Y, Watanabe, T. The crystal structure of 2-pyrazinamide. Acta Crystallogr. 1960;13:693702. .

  • 27. Bhutani, H, Singh, S, Jindal, KC. Drug-drug interaction studies on first-line anti-tuberculosis drugs. Pharm Dev and Techn. 2005;10:517524. .

    • Crossref
    • Search Google Scholar
    • Export Citation

Manuscript Submission: HERE

  • Impact Factor (2019): 2.731
  • Scimago Journal Rank (2019): 0.415
  • SJR Hirsch-Index (2019): 87
  • SJR Quartile Score (2019): Q3 Condensed Matter Physics
  • SJR Quartile Score (2019): Q3 Physical and Theoretical Chemistry
  • Impact Factor (2018): 2.471
  • Scimago Journal Rank (2018): 0.634
  • SJR Hirsch-Index (2018): 78
  • SJR Quartile Score (2018): Q2 Condensed Matter Physics
  • SJR Quartile Score (2018): Q2 Physical and Theoretical Chemistry

For subscription options, please visit the website of Springer.

Journal of Thermal Analysis and Calorimetry
Language English
Size A4
Year of
Foundation
1969
Volumes
per Year
4
Issues
per Year
24
Founder Akadémiai Kiadó
Founder's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher Akadémiai Kiadó
Springer Nature Switzerland AG
Publisher's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible
Publisher
Chief Executive Officer, Akadémiai Kiadó
ISSN 1388-6150 (Print)
ISSN 1588-2926 (Online)

Monthly Content Usage

Abstract Views Full Text Views PDF Downloads
May 2021 4 0 0
Jun 2021 3 0 0
Jul 2021 1 0 0
Aug 2021 3 0 0
Sep 2021 3 0 0
Oct 2021 0 0 0
Nov 2021 0 0 0