Stability of rifampicin in dissolution medium in presence of isoniazid

Shishoo, C. J.; Shah, Shailesh; Rathod, Ishwarsinh S.; Savale, S. S; Kotecha, Jignesh; Shah, Pankaj B.

doi:10.1016/s0378-5173(99)00286-0

Cited by 76 publications

(60 citation statements)

References 11 publications

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“…Under gastric conditions, RIF is gradually hydrolysed to the non-active form 3-formyl RIF SV. This degradation pathway is hastened by INH [18,19]; the co-administration of RIF/ INH in fixed dose combinations is employed to prevent mono-therapy [20]. The WHO has raised awareness of the reduced oral bioavailability of RIF in these formulations [21].…”

Section: Introductionmentioning

confidence: 99%

Cryoprotection–lyophilization and physical stabilization of rifampicin-loaded flower-like polymeric micelles

Morettón

Chiappetta

Sosnik

2011

J. R. Soc. Interface.

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Rifampicin-loadedpoly(e-caprolactone)-b-poly(ethylene glycol) -poly(e-caprolactone) flower-like polymeric micelles display low aqueous physical stability over time and undergo substantial secondary aggregation. To improve their physical stability, the lyoprotectionlyophilization process was thoroughly characterized. The preliminary cryoprotectant performance of mono-and disaccharides (e.g. maltose, glucose), hydroxypropyl-bcyclodextrin (HPbCD) and poly(ethylene glycol) (PEG) of different molecular weights was assessed in freeze -thawing assays at 2208C, 2808C and 21968C. The size and size distribution of the micelles at the different stages were measured by dynamic light scattering (DLS). A cryoprotectant factor ( f c ) was determined by taking the ratio between the size immediately after the addition of the cryoprotectant and the size after the preliminary freeze -thawing assay. The benefit of a synergistic cryoprotection by means of saccharide/ PEG mixtures was also assessed. Glucose (1 : 20), maltose (1 : 20), HPbCD (1 : 5) and glucose or maltose mixtures with PEG3350 (1 : 20) (copolymer:cryoprotectant weight ratio) were the most effective systems to protect 1 per cent micellar systems. Conversely, only HPbCD (1 : 5) cryoprotected more concentrated drug-loaded micelles (4% and 6%). Then, those micelle/ cryoprotectant systems that displayed f c values smaller than 2 were freeze-dried. The morphology of freeze-dried powders was characterized by scanning electron microscopy and atomic force microscopy and the residual water content analysed by the Karl Fisher method. The HPbCD-added lyophilisates were brittle porous cakes (residual water was between 0.8% and 3%), easily redispersable in water to form transparent systems with a minimal increase in the micellar size, as determined by DLS.

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Section: Introductionmentioning

confidence: 99%

Cryoprotection–lyophilization and physical stabilization of rifampicin-loaded flower-like polymeric micelles

Morettón

Chiappetta

Sosnik

2011

J. R. Soc. Interface.

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“…On the other hand, the absorption of isoniazid at this pH is extremely poor, while most of its content is absorbed in the intestine (Shishoo, 1999). Therefore, an alternative to reduce the degradation of rifampicin in the presence of isoniazid is the prevention of physical contact between these drugs, which can be achieved by enteric-coating of isoniazid.…”

Section: Resultsmentioning

confidence: 99%

“…The degradation rate of RMP was shown to be higher in the presence of INH in HCl 0.1 N and simulated gastric fluid. Consequently, the dose available for absorption is significantly decreased (Shishoo et al, 1999;Singh et al, 2000Singh et al, , 2001.…”

Section: Introductionmentioning

confidence: 99%

“…It has been reported that rifampicin is well absorbed from the stomach due to its maximum solubility in the pH range of 1-2, whereas isoniazid is less permeable through the stomach, but well absorbed from all three segments of the intestine (Shishoo et al, 1999). Therefore, the distinct physicochemical properties of these drugs, especially in terms of solubility and stability at different pH values, suggests that delivering each compound at different sites in the GI tract would be advantageous.…”

Section: Introductionmentioning

confidence: 99%

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

Freire

Câmara

Dantas

et al. 2014

Braz. J. Pharm. Sci.

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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 ® 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 entericcoated pellets. Acrycoat L 100 ® 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. Uniterms:Rifampicin. Gastric-resistant isoniazids/pellets. Pellets/enteric coating. Acrycoat L 100®/ use/enteric coating.Isoniazida e rifampicina são fármacos de primeira escolha para a prevenção e tratamento da tuberculose. A rifampicina degrada-se em condições ácidas do estômago, principalmente na presença da isoniazida, o que contribui para a falha do tratamento. O presente trabalho teve como objetivo a obtenção de péletes de isoniazida gastrorresistentes, visando a evitar contato da rifampicina com isoniazida e consequente degradação no meio ácido estomacal. Os péletes foram produzidos pela técnica de extrusão-esferonização. O processo de revestimento foi conduzido em leito fluidizado com solução orgânica de Acrycoat L 100 ® . Os péletes obtidos foram submetidos ao teste de dissolução em HCl 0,1 N e tampão fosfato. Os resultados indicam que a gastrorresistência foi obtida somente com a maior quantidade de revestimento, sendo a isoniazida liberada completamente no meio tampão fosfato. A quantidade de rifampicina dissolvida em meio ácido, quando associada a péletes de isoniazida não revestidos, foi menor do que a observada na presença de péletes de liberação entérica. O polímero Acrycoat L 100® mostrou-se eficiente para o recobrimento com a função de gastrorresistência, indicando que a instabilidade da rifampicina pode ser reduzida nas associações com a isoniazida através do revestimento entérico da isoniazida.Unitermos: Rifampicina. Isoniazidas gastrorresistentes/péletes. Péletes/revestimento entérico. Acrycoat L 100®/uso/revestimento entérico.

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“…Several studies have dealt upon degradation of anti-tuberculosis drugs. [5][6][7] Several anti-tuberculosis drugs except ka- namycin and capreomycin was found to deteriorate even as early as 1 week and ethionamide after 2 weeks of incubation at 37°C. 8 Degradation of drugs during combined therapy was reported especially in rifampicin when used with isoniazid.…”

Section: Introductionmentioning

confidence: 99%

Effect of temperature on storage of ethionamide during susceptibility testing

Lakshmi¹

2013

Jmid

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Objective: Ethionamide being thermolabile in nature, effect of temperature on the drug and its stability in liquid and solid media during susceptibility testing procedures was assessed to understand the inconsistency in DST formats.Methods: Working solution of ethionamide and Lowenstein-Jensen (LJ) media incorporated with ethionamide were preincubated at 4°C and 37°C prior to DST methods was incubated till 4 weeks at different temperatures and utilized for DST in MGIT 960.Results: Degradation of ethionamide working solution was observed at 37°C after 3 weeks of incubation. Ethionamide incorporated LJ media can be stored without compromise on susceptibility up to 5 weeks. But, a week of prior incubation at 37°C has deleterious effect on the DST profile. Ethionamide was found to degrade at 37°C after different time points when stored as solution or as LJ media. Bulgular: Ethionamide çalışma solusyonunda 37°C'de 3 haftalık inkübasyonun ardından bozunma olduğu gözlenmiştir. Ethionamide LJ ortamında beş haftaya kadar etkinliğinde bozulma olmadan saklanabilir. Fakat 37°C de bir hafta daha bekletilmesi ilaç duyarlılık profiline zararlı etkili olabilir. Ethionamide 37°C bekletilmesiyle farklı zaman aralıklarında sıvı ya da LJ ortamında bekletilmesiyle etkinliğinde değişmeler olduğu saptandı. ConclusionSonuç: DST ortamında ethionamide için iki haftaya kadar olan testlerin değerlendirilmesi önerilir.

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Stability of rifampicin in dissolution medium in presence of isoniazid

Cited by 76 publications

References 11 publications

Cryoprotection–lyophilization and physical stabilization of rifampicin-loaded flower-like polymeric micelles

Cryoprotection–lyophilization and physical stabilization of rifampicin-loaded flower-like polymeric micelles

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

Effect of temperature on storage of ethionamide during susceptibility testing

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