Ascorbic acid improves stability and pharmacokinetics of rifampicin in the presence of isoniazid

Rajaram, Subashini; Vemuri, Venkata Deepthi; Natham, Rajendran

doi:10.1016/j.jpba.2014.07.027

Cited by 24 publications

(15 citation statements)

References 21 publications

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“…The remaining doses are maintained above 90% of the initial dose for both APIs when ascorbic acid is used as an antioxidant in a proportion of 0.1% w/v during three days of storage at 5 • C of storage. Our results are in accordance with the results obtained for ascorbic acid by Rajaram et al [28] and Aliabadi et al [36]. The first studied its effect in the stability and pharmacokinetics of RFP in the presence of INH in the stomach acid environment [28].…”

Section: Discussionsupporting

confidence: 93%

“…Our results are in accordance with the results obtained for ascorbic acid by Rajaram et al [28] and Aliabadi et al [36]. The first studied its effect in the stability and pharmacokinetics of RFP in the presence of INH in the stomach acid environment [28]. They demonstrate that this co-administration with these antiTBs in combination protect RFP from degradation but not in an acid environment.…”

Section: Discussionsupporting

confidence: 93%

“…HPBCD proportion (5.6% p/v, corresponding with a concentration of 0.040 M) used is under the threshold of 200 mg/kg/day given by EMA for children under two years [26,27]. An antioxidant as ascorbic acid was added in different proportions at F2 and F3 in order to improve the RFP stability under presence of INH [28]. The proportions used were the minimum and maximum concentration to be used as an antioxidant [29], and these values are under the recommended dietary allowances for children under six months [30].…”

Section: General Standard Operating Procedures (Sop)mentioning

confidence: 99%

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Stability Study of Isoniazid and Rifampicin Oral Solutions Using Hydroxypropyl-Β-Cyclodextrin to Treat Tuberculosis in Paediatrics

et al. 2020

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(1) Background: First-line antituberculosis treatment in paediatrics entails the administration of Isoniazid, Pyrazinamide, and Rifampicin. This study examines the possibility of developing a combined dose liquid formulation for oral use that would facilitate dose adjustment and adherence to treatment for younger children. (2) Methods: The active pharmaceutical ingredients stability under in vitro paediatric digestive pH conditions have been checked. The samples were studied as individual or fixed combined paediatric dosages to determine the pH of maximum stability. The use of hydroxypropyl-β-cyclodextrin to improve Rifampicin solubility and the use of ascorbic acid to increase the stability of the formulation have been studied. (3) Results: Maximum stability of combined doses was determined at pH 7.4, and maximum complexation at pH 8.0. Taking this into account, formulations presented the minimum dose of two active pharmaceutical ingredients dissolved. The addition of ascorbic acid at 0.1% w/v enables the detection of a higher remaining quantity of both drugs after three days of storage at 5 °C. (4) Conclusions: a formulation which combines the minimum paediatric dosages dissolved recommended by WHO for Isoniazid and Rifampicin has been developed. Future assays are needed to prolong the stability of the formulation with the aim of incorporating Pyrazinamide to the solution.

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Section: Discussionsupporting

confidence: 93%

Section: Discussionsupporting

confidence: 93%

Section: General Standard Operating Procedures (Sop)mentioning

confidence: 99%

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Stability Study of Isoniazid and Rifampicin Oral Solutions Using Hydroxypropyl-Β-Cyclodextrin to Treat Tuberculosis in Paediatrics

et al. 2020

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“…1. As an optimal method for separation, RPLC has been used in the analysis of rifampicin and its impurities [4][5][6][7].…”

Section: Introductionmentioning

confidence: 99%

Development of a sensitive and rapid method for rifampicin impurity analysis using supercritical fluid chromatography

Wang

Yan

2015

Journal of Pharmaceutical and Biomedical Analysis

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“…Ascorbic acid was added to the dissolution media to prevent rifampicin degradation. 33 Samples were taken at certain intervals and replaced with a fresh medium. The concentration of released rifampicin was determined using a UV-visible spectrophotometer (Beckman, DU 7500i) at 475 nm.…”

mentioning

confidence: 99%

<p>ArtinM Grafted Phospholipid Nanoparticles for Enhancing Antibiotic Cellular Uptake Against Intracellular Infection</p>

Suciati

Nafisa

Nareswari

et al. 2020

IJN

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Background and Aim An antimicrobial delivery in the form of surface-modified lectin of lipid nanoparticles was proposed to improve cellular accumulation. ArtinM, an active toll-like receptor 2 (TLR2) agonist lectin isolated from cempedak ( Arthocarpus integrifolia) seeds, was selected to induce cellular engulfment of nanoparticles within infected host cells. Materials and Methods Lipid nanoparticles were prepared using the emulsification technique before electrostatic adsorption of artinM. The formula comprising of rifampicin, soy phospholipid, and polysorbate 80 was optimized by Box-Behnken design to produce the desired particle size, entrapment efficiency, and drug loading. The optimum formula was characterized for morphology, in vitro release, and cellular transport. Results and Discussion Soy phospholipid showed a profound effect on controlling drug loading and entrapment efficiency. Owing to its surface activity, polysorbate 80 contributed significantly to reduce particle size; however, a higher ratio to lipid concentration resulted in a decrease of rifampicin encapsulation. The adsorption of artinM on the surface of nanoparticles was accomplished by electrostatic binding at pH 4, where this process maintained the stability of encapsulated rifampicin. A high proportion of artinM adsorbed on the surface of the nanoparticles shown by haemagglutination assay, zeta potential measurement, and transmission electron microscopy imaging. Cellular uptake revealed by confocal microscopy showed the success in transporting Nile-red labelled nanoparticles across fibroblast cells. Conclusion The delivery system of nanoparticles bearing artinM becomes a potential platform technology for antibiotic targeting in the treatment of life-threatening chronic diseases caused by intracellular infections.

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Ascorbic acid improves stability and pharmacokinetics of rifampicin in the presence of isoniazid

Cited by 24 publications

References 21 publications

Stability Study of Isoniazid and Rifampicin Oral Solutions Using Hydroxypropyl-Β-Cyclodextrin to Treat Tuberculosis in Paediatrics

Stability Study of Isoniazid and Rifampicin Oral Solutions Using Hydroxypropyl-Β-Cyclodextrin to Treat Tuberculosis in Paediatrics

Development of a sensitive and rapid method for rifampicin impurity analysis using supercritical fluid chromatography

<p>ArtinM Grafted Phospholipid Nanoparticles for Enhancing Antibiotic Cellular Uptake Against Intracellular Infection</p>

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