Biowaiver monographs for immediate release solid oral dosage forms: Rifampicin

Becker, Corina; Dressman, Jennifer B.; Junginger, Hans E.; Kopp, Sabine; Midha, K. K.; Shah, Vinod P.; Stavchansky, Salomon A; Barends, D. M.

doi:10.1002/jps.21624

Cited by 73 publications

(74 citation statements)

References 80 publications

(110 reference statements)

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“…The most important aspect from these results presented here is that ethambutol did not show any significant in vitro protein binding in serum using this method, which clearly contradicts earlier results [17,20]. This may partly be caused by the difference in temperature, as this factor is known to influence protein binding [26].…”

Section: Discussioncontrasting

confidence: 96%

“…In the adsorption test, ethambutol showed a significant loss of approximately 35% in peak area when injected from the standard glass vial. Earlier reported protein binding results [17,20] vary and may be obscured by adsorption of ethambutol to non deactivated glass STURKENBOOM MGG [33]. As protein binding of isoniazid, pyrazinamide and ethambutol proved low, ultrafiltration as a means of sample preparation could be applied resulting in a fast and simple method of analysis.…”

Section: Discussionmentioning

confidence: 99%

“…Reported protein binding levels vary considerably for the three compounds: ranging from 0 to 74% for isoniazid [17,18] from 5 to 50% for pyrazinamide [17,19] and from 10 to 30% for ethambutol [17,20]. However, one expects protein binding to be limited as isoniazid, pyrazinamide and ethambutol are very polar compounds.…”

Section: Protein Binding and Ultrafiltrationmentioning

confidence: 99%

“…We successfully applied ultrafiltration as a means of sample preparation for the polar compound ribavirin [13] and we were interested whether this might also be applied for the first-line anti-TB drugs. However, rifampin shows high protein binding of around 80-90% [14], which makes it a less suitable candidate for ultrafiltration compared to isoniazid, pyrazinamide and ethambutol. Therefore, it was decided to split the patient sample, followed by a subsequent separate analysis of rifampin and a separate one for isoniazid, pyrazinamide and ethambutol together resulting in more reliable results within the same runtime.…”

Section: Introductionmentioning

confidence: 99%

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Quantification of isoniazid, pyrazinamide and ethambutol in serum using liquid chromatography-tandem mass spectrometry

Sturkenboom¹,

Lijke²,

Jongedijk³

et al. 2015

J Appl Bioanal

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Clinical studies on tuberculosis have shown a correlation between low drug exposure and treatment failure and acquired drug resistance. Objective was to develop a LC-MS/MS method for the quantification of isoniazid, pyrazinamide and ethambutol. Stable isotope-labelled isoniazid-D4 and ethambutol-D4 were used as internal standards. Protein binding of isoniazid, pyrazinamide and ethambutol was investigated and proved low. Therefore, sample preparation using ultrafiltration could be applied, resulting in linear calibration curves in the range of 0.2-8 mg/L for isoniazid and ethambutol and 2-80 mg/L for pyrazinamide. The method was validated according to the guidelines of the FDA. A fast, simple and reliable LC-MS/MS method has been developed for the simultaneous determination of isoniazid, pyrazinamide and ethambutol in human serum for therapeutic drug monitoring and pharmacokinetic studies.

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Section: Discussioncontrasting

confidence: 96%

Section: Discussionmentioning

confidence: 99%

Section: Protein Binding and Ultrafiltrationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Quantification of isoniazid, pyrazinamide and ethambutol in serum using liquid chromatography-tandem mass spectrometry

Sturkenboom¹,

Lijke²,

Jongedijk³

et al. 2015

J Appl Bioanal

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“…4 Since RIF is a Biopharmaceutics Classification System class II member possessing low aqueous solubility and high permeability, its dissolution rate and hence bioavailability are limited. 5 However, a recent report revealed the low permeability of RIF through the intestinal cell, proposing a new classification for the drug to class IV. 6 In addition, oral administration of RIF causes undesirable side effects, including nausea, flu-like syndrome associated with acute renal failure, hepatotoxicity, and agranulocytosis.…”

mentioning

confidence: 99%

The relevancy of controlled nanocrystallization on rifampicin characteristics and cytotoxicity

Mohyeldin

Mehanna

Elgindy

2016

IJN

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Purpose This article investigated the influence of novel rifampicin nanosuspension (RIF NS) for enhancing drug delivery properties. Methods RIF NS was fabricated using the antisolvent precipitation technique. The impact of solvent type and flow rate, stabilizer type and concentration, and stirring time and apparatus together with the solvent–antisolvent volume ratio on its controlled nanocrystallization has been evaluated. NSs were characterized by transmission electron microscopy, particle size and zeta potential analysis, solubility, and dissolution profiles. The compatibility between RIF and the stabilizer was investigated via Fourier transform infrared spectroscopy and the differential scanning calorimetry techniques. The shelf-life stability of the RIF NS was assessed within a period of 3 months at different storage temperatures. Cell cytotoxicity was evaluated using 3(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on lung epithelial cells. Results Polyvinyl alcohol at 0.4% w/v, 1:15 methanol to deionized water volume ratio and 30-minutes sonication were the optimal parameters for RIF NS preparation. Nanocrystals were obtained with a nanometeric particle size (101 nm) and a negative zeta potential (−26 mV). NS exhibited a 50-fold enhancement in RIF solubility and 97% of RIF was dissolved after 10 minutes. The RIF NS was stable at 4±0.5°C with no significant change in particle size or zeta potential. The MTT cytotoxicity assay of RIF NS demonstrated a good safety profile and reduction in cell cytotoxicity with half maximal inhibitory concentration values of 0.5 and 0.8 mg/mL for free RIF and RIF NS, respectively. Conclusion A novel RIF NS could be followed as an approach for enhancing RIF physicochemical characteristics with a prominence of a safer and better drug delivery.

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Biowaiver monographs for immediate release solid oral dosage forms: Doxycycline hyclateA project of the International Pharmaceutical Federation (FIP), BCS and Biowaiver, www.fip.org/bcs.This article reflects the scientific opinion of the authors and not the policies of regulating agencies, the International Pharmaceutical Federation (FIP) and the World Health Organization (WHO).

Jantratid

Becker

Dressman

et al. 2010

Journal of Pharmaceutical Sciences

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Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing doxycycline hyclate are reviewed. According to the Biopharmaceutics Classification System (BCS), doxycycline hyclate can be assigned to BCS Class I. No problems with BE of IR doxycycline formulations containing different excipients and produced by different manufacturing methods have been reported and hence the risk of bioinequivalence caused by these factors appears to be low. Doxycycline has a wide therapeutic index. Further, BCS-based dissolution methods have been shown to be capable of identifying formulations which may dissolve too slowly to generate therapeutic levels. It is concluded that a biowaiver is appropriate for IR solid oral dosage forms containing doxycycline hyclate as the single Active Pharmaceutical Ingredient (API) provided that (a) the test product contains only excipients present in doxycycline hyclate IR solid oral drug products approved in the International Conference on Harmonization (ICH) or associated countries; and (b) the comparator and the test products comply with the BCS criteria for "very rapidly dissolving" or, alternatively, when similarity of the dissolution profiles can be demonstrated and the two products are "rapidly dissolving.".

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Biowaiver monographs for immediate release solid oral dosage forms: Rifampicin

Cited by 73 publications

References 80 publications

Quantification of isoniazid, pyrazinamide and ethambutol in serum using liquid chromatography-tandem mass spectrometry

Quantification of isoniazid, pyrazinamide and ethambutol in serum using liquid chromatography-tandem mass spectrometry

The relevancy of controlled nanocrystallization on rifampicin characteristics and cytotoxicity

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