Preformulation studies of ceftriaxone for pediatric non-parenteral administration as an alternative to existing injectable formulations

Kauss, Tina; Marchivie, Mathieu; Phoeung, Thida; Gaubert, Alexandra; Désiré, Amélie; Tonelli, Giovanni; Boyer, Cinda M.; Langlois, Michel; Cartwright, Anthony C.; Gomes, Melba; White, Nicholas J.; Gaudin, Karen

doi:10.1016/j.ejps.2017.04.010

Cited by 9 publications

(7 citation statements)

References 22 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A human bile salt, sodium chenodeoxycholate (NaCDC) in a ratio 1/4 with CTX, has previously been shown as the optimal absorption enhancer for CTX 22 . Pre-formulation studies of CTX have been performed 23 and these confirmed poor compatibility with most of liquid excipients but good compatibility with NaCDC, thus supporting the development of solid drug dosage formulations 23 .…”

Section: Introductionmentioning

confidence: 89%

“…Granules with a LOD around 7% were considered as dried, as some CTX levels of moisture (3.5 hydrate equivalent to approximately 9% w/w) had been shown to be more labile 23 .…”

Section: Granulationmentioning

confidence: 99%

“…These did not improve flowability of CTX or the CTX-NaCDC mixture which was infinite according to European Pharmacopoeia standards. Dry and wet granulation were evaluated to solve flowability problems provided that drying was carried out rapidly after wetting and that moderate compression forces were used 23 . Wet granulation provided optimal results if precise control and a short CTX wetting time was used; to limit crystal damage a moderate compression using 80MPa obviated the significant PXRD broadening, which was seen with 150MPa compression 23 .…”

Section: Design and In Vitro Evaluation Of Recto-dispersible Tablets ...mentioning

confidence: 99%

See 2 more Smart Citations

Development of Rectodispersible Tablets and Granulate Capsules for the Treatment of Serious Neonatal Sepsis in Developing Countries

Kauss

Langlois

Guyonnet-Dupérat

et al. 2019

Journal of Pharmaceutical Sciences

Self Cite

View full text Add to dashboard Cite

Section: Introductionmentioning

confidence: 89%

“…Granules with a LOD around 7% were considered as dried, as some CTX levels of moisture (3.5 hydrate equivalent to approximately 9% w/w) had been shown to be more labile 23 .…”

Section: Granulationmentioning

confidence: 99%

Section: Design and In Vitro Evaluation Of Recto-dispersible Tablets ...mentioning

confidence: 99%

See 1 more Smart Citation

Development of Rectodispersible Tablets and Granulate Capsules for the Treatment of Serious Neonatal Sepsis in Developing Countries

Kauss

Langlois

Guyonnet-Dupérat

et al. 2019

Journal of Pharmaceutical Sciences

Self Cite

View full text Add to dashboard Cite

“…As none of the batch has highest drug release so from the studies we can conclude that increase in the polymer amount and crosslinking agent amount shows negative effect with the drug release. [16] The Table 4 is the cumulative drug release of all the formulations.…”

Section: In-vitro Drug Releasementioning

confidence: 99%

Formulation Evaluation and Optimization of Chitosan Coated Ceftriaxone Loaded Microparticles

Jain

Choudhary

Islam

2020

Int. J. Pharm. Sci. Drug Res.

View full text Add to dashboard Cite

Ceftriaxone, a third generation cephalosporin antibiotic is an important antibiotic used in the treatment of invasive infections caused by the certain bacteria such as the penicillin-resistant microorganisms like Staphyloccocus aureus, strains of S. pneumonia, S. aureus and Enterobacteriaceae , particularly among E. coli. There is increasing antimicrobial resistance of Ceftriaxone in particular against these strains of bacteria. This study has been conducted to formulate, evaluate and optimize chitosan coated ceftriaxone loaded microparticles with better efficacy and also observes the MIC against strains of bacteria. Emulsion crosslinking method was used for the formulation of microparticles of ceftriaxone by using chitosan as a polymer and glutraldehyde as a cross linking agent which is optimized by using Box-Behnken Design. Three independent variables were taken; effect of drug and the polymer ratio, effect of the stirring speed and effect of crosslinking agent and dependent variables were microparticles entrapment efficiency and the In vitro drug release. Following optimization of the formulations, physical characterization as well as entrapment efficiency and ultimately in-vitro evaluation was performed. Physical characterization include optical microscopy, SEM and DLS to check there physical properties. The method used for the formulation of microparticle had the optimum entrapment efficiency of 61.7% which was increase with the increase in the addition of the more amount of chitosan and glutraldehyde and method also achieved the good in vitro release. MIC studies of microparticles were done against Klebsiella pneumonia, Staphylococcus aureus, Streptococcus mutans, Escherichia coli and it was found that the formulations showed decrease in MIC.

show abstract

“…15 CEF is poorly absorbed through mucosal membranes, [16][17][18] which indicates that in this pharmaceutical form it is intended only for intravenous, intramuscular or subcutaneous injections, and this limits its therapeutic use in other modes of administration. 19 The use of the encapsulated form of CEF in the form of microcarriers and nanocarriers will increase the stability and bioavailability of the drug, provide a reduction in undesirable systemic effects and also allow for oral, nasal, and inhalative administration into the body. [20][21][22] The literature describes examples of delivery systems for cephalosporin based on various materials.…”

Section: Introductionmentioning

confidence: 99%

Development and characterization of ceftriaxone-loaded P3HB-based microparticles for drug delivery

et al. 2018

View full text Add to dashboard Cite

In this study, polymer-based microparticles are used to improve the therapeutic properties of ceftriaxone (CEF) and render them safer. Poly-3-hydroxybutyrate (P3HB) and poly-3-hydroxybutyrate/polyethylene glycol (P3HB-PEG)based microparticles were prepared by two methods: a double emulsification technique and spray-drying. The microparticles were characterized in terms of size and zeta potential, morphology, total drug loading and drug release. The microparticles had spherical shapes with diameters of a size range from 0.74 to 1.55 m (emulsification technique) and from 3.84 to 6.51 m (spray-drying); CEF encapsulation efficiency was around 63% and 49% for these methods respectively. The CEF release from microparticles obtained by spray-drying reached 100% after 150h, while for microparticles obtained by emulsification technique the total release of CEF did not exceed 34% after 312 h. The release profiles could be best explained by Zero order kinetics model, Higuchi and Korsmeyer-Peppas models, as the plots showed high linearity. Antibacterial activity of the microparticles was evaluated against gram-positive and gram-negative bacterial strains. In general, CEF encapsulation in polymeric microparticles preserves the therapeutic efficacy of the CEF and provides its prolonged effect.

show abstract

Preformulation studies of ceftriaxone for pediatric non-parenteral administration as an alternative to existing injectable formulations

Cited by 9 publications

References 22 publications

Development of Rectodispersible Tablets and Granulate Capsules for the Treatment of Serious Neonatal Sepsis in Developing Countries

Development of Rectodispersible Tablets and Granulate Capsules for the Treatment of Serious Neonatal Sepsis in Developing Countries

Formulation Evaluation and Optimization of Chitosan Coated Ceftriaxone Loaded Microparticles

Development and characterization of ceftriaxone-loaded P3HB-based microparticles for drug delivery

Contact Info

Product

Resources

About