Gastric-resistant isoniazid pellets reduced degradation of rifampicin in acidic medium

Authors

  • Fátima Duarte Freire Federal University of Rio Grande do Norte
  • Manuela Bernardo Câmara Federal University of Rio Grande do Norte
  • Monique Gomes Dantas Federal University of Rio Grande do Norte
  • Cícero Flávio Soares Aragão Federal University of Rio Grande do Norte
  • Túlio Flávio Accioly de Lima e Moura Federal University of Rio Grande do Norte
  • Fernanda Nervo Raffin Federal University of Rio Grande do Norte

DOI:

https://doi.org/10.1590/S1984-82502014000400010

Abstract

Isoniazid and rifampicin are considered the first-line medication for preventing and treating tuberculosis. Rifampicin is degraded in the stomach acidic environment, especially when combined with isoniazid, factor contributing to treatment failure. In this study, gastric-resistant isoniazid pellets were obtained to physical contact of this drug with rifampicin and to bypass the stomach´s acidic environment. The pellets were fabricated using the extrusion-spheronization technique. The coating process was conducted in a fluid spray coater using Acrycoat L 100(r) solution as the coating agent. The pellets obtained were submitted to a dissolution test in HCl 0.1 N and phosphate buffer media. The results indicated that optimum gastric-resistance was only attained with the highest amount of coating material, with isoniazid almost fully released in phosphate buffer. The amount of rifampicin released from its mixture with non-coated isoniazid pellets in HCl 0.1 N was less than that released from its mixture with the enteric-coated pellets. Acrycoat L 100(r) was shown to be an effective enteric/gastric-resistant coating since the stability of rifampicin appeared to be enhanced when physical contact of this drug with isoniazid was prevented at low pH.

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Published

2014-12-01

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Articles

How to Cite

Gastric-resistant isoniazid pellets reduced degradation of rifampicin in acidic medium . (2014). Brazilian Journal of Pharmaceutical Sciences, 50(4), 749-755. https://doi.org/10.1590/S1984-82502014000400010