Impaired bioavailability of rifampicin in presence of isoniazid from fixed dose combination (FDC) formulation

Shishoo, C. J.; Shah, Shailesh; Rathod, Ishwarsinh S.; Savale, S. S; Vora, M.J

doi:10.1016/s0378-5173(01)00831-6

Cited by 111 publications

(82 citation statements)

References 17 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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“…Rifampicin is one of the first-line drugs recommended by the World Health Organization in the treatment of tuberculosis despite of the drawbacks of poor bioavailability and short biological half-life (5,6). In order to overcome the problems of poor absorption, fast degradation, and adverse side effects of rifampicin, many researchers have concentrated their attention in the development of controlled-release rifampicin formulations (7)(8)(9)(10)(11).…”

Section: Introductionmentioning

confidence: 99%

Rehydrated Lyophilized Rifampicin-Loaded mPEG–DSPE Formulations for Nebulization

2010

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Abstract. Rifampicin-loaded nanoparticles were prepared using two different molecular weights of poly-(ethylene oxide)-block-distearoyl phosphatidyl-ethanolamine (mPEG2000-DSPE and mPEG5000-DSPE) polymers. Particle sizes of all formulations studied were in the range of 162-395 nm. The entrapment efficiency (EE) was not affected by the copolymer's molecular weight, and the highest EE (100%) was obtained with drug to copolymer ratio of 1:5. The differential scanning calorimetry (DSC) thermograms showed Tg of rifampicin-loaded PEG-DSPE nanoparticles that shifted to a lower value, indicating entrapment of rifampicin in polymer matrix. The Fourier transformed infrared spectra revealed no chemical interactions between the drug and both copolymers. The in vitro drug release from the formulations occurred over 3 days and followed first-order release kinetic and Higuchi diffusion model. The nebulization of rehydrated lyophilized rifampicin mPEG-DSPE formulations had mass median aerodynamic diameter of 2.6 µm and fine particle fraction of 42%. The aerodynamic characteristic of the preparations was not influenced by the molecular weight of the copolymers. Therefore, it is suggested that both mPEG-DSPE are promising candidates as rifampicin carrier for pulmonary delivery.

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“…Tuberculosis kills more people worldwide than any other single infectious disease (8). Isoniazid is one of the most important "first-line" anti-tubercular drugs used in the treatment of tuberculosis (9).…”

Section: Introductionmentioning

confidence: 99%

Controlled Release Hydrophilic Matrix Tablet Formulations of Isoniazid: Design and In Vitro Studies

Hiremath

Saha

2008

AAPS PharmSciTech

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Abstract. The aim of the present investigation was to develop oral controlled release matrix tablet formulations of isoniazid using hydroxypropyl methylcellulose (HPMC) as a hydrophilic release retardant polymer and to study the influence of various formulation factors like proportion of the polymer, polymer viscosity grade, compression force, and release media on the in vitro release characteristics of the drug. The formulations were developed using wet granulation technology. The in vitro release studies were performed using US Pharmacopoeia type 1 apparatus (basket method) in 900 ml of pH 7.4 phosphate buffer at 100 rpm. The release kinetics was analyzed using KorsmeyerPeppas model. The release profiles were also analyzed using statistical method (one-way analysis of variance) and f 2 metric values. The release profiles found to follow Higuchi's square root kinetics model irrespective of the polymer ratio and the viscosity grade used. The results in the present investigation confirm that the release rate of the drug from the HPMC matrices is highly influenced by the drug/ HPMC ratio and viscosity grade of the HPMC. Also, the effect of compression force and release media was found to be significant on the release profiles of isoniazid from HPMC matrix tablets. The release mechanism was found to be anomalous non-Fickian diffusion in all the cases. In the present investigation, a series of controlled release formulations of isoniazid were developed with different release rates and duration so that these formulations could further be assessed from the in vivo bioavailability studies. The formulations were found to be stable and reproducible.

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Impaired bioavailability of rifampicin in presence of isoniazid from fixed dose combination (FDC) formulation

Cited by 111 publications

References 17 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

Rehydrated Lyophilized Rifampicin-Loaded mPEG–DSPE Formulations for Nebulization

Controlled Release Hydrophilic Matrix Tablet Formulations of Isoniazid: Design and In Vitro Studies

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