Kinetic measurements of the hydrolytic degradation of cefixime: effect of Captisol complexation and water-soluble polymers

Mallick, Subrata; Mondal, Arijit; Sannigrahi, Santanu

doi:10.1211/jpp.60.7.0004

Cited by 25 publications

(11 citation statements)

References 51 publications

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“…This unique structure allows for the formation of inclusion complexes, where lipophilic compounds are noncovalently bound within the cavity. CDs and a number of derivatives have been widely used in oral and parenteral drug delivery systems to improve aqueous solubility and chemical stability of drugs (2,(16)(17)(18)(19). Topical applications of CDs have also been investigated (20)(21)(22).…”

Section: Introductionmentioning

confidence: 99%

Experimental and Computational Studies of Physicochemical Properties Influence NSAID-Cyclodextrin Complexation

Felton

Popescu²,

Wiley

et al. 2014

AAPS PharmSciTech

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Abstract. The objective of this research was to investigate physicochemical properties of an active pharmaceutical ingredient (API) that influence cyclodextrin complexation through experimental and computational studies. Native β-cyclodextrin (B-CD) and two hydroxypropyl derivatives were first evaluated by conventional phase solubility experiments for their ability to complex four poorly watersoluble nonsteroidal anti-inflammatory drugs (NSAIDs). Differential scanning calorimetry was used to confirm complexation. Secondly, molecular modeling was used to estimate Log P and aqueous solubility (S o ) of the NSAIDs. Molecular dynamics simulations (MDS) were used to investigate the thermodynamics and geometry of drug-CD cavity docking. NSAID solubility increased linearly with increasing CD concentration for the two CD derivatives (displaying an A L profile), whereas increases in drug solubility were low and plateaued in the B-CD solutions (type B profile). The calculated Log P and S o of the NSAIDs were in good concordance with experimental values reported in the literature. Side chain substitutions on the B-CD moiety did not significantly influence complexation. Explicitly, complexation and the associated solubility increase were mainly dependent on the chemical structure of the NSAID. MDS indicated that each NSAID-CD complex had a distinct geometry. Moreover, complexing energy had a large, stabilizing, and fairly constant hydrophobic component for a given CD across the NSAIDs, while electrostatic and solvation interaction complex energies were quite variable but smaller in magnitude.

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Section: Introductionmentioning

confidence: 99%

Experimental and Computational Studies of Physicochemical Properties Influence NSAID-Cyclodextrin Complexation

Felton

Popescu²,

Wiley

et al. 2014

AAPS PharmSciTech

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“…The drug release data was analyzed by applying different kinetic models as First order, Higuchi, Korsmeyer-Peppas kinetics. [33][34][35] These controlled release has been followed ( Figure 7). The kinetic parameters as per model are presented in the Table 3.…”

Section: Resultsmentioning

confidence: 99%

Solvent-free Hot Melt Extrusion Technique in Improving Mesalamine Release for Better Management of Inflammatory Bowel Disease

Sahoo¹,

De²,

Kataria³

et al. 2019

IJPER

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Background: Poor oral bioavailability of mesalamine (Mes) is due to extensive metabolism in the intestinal epithelial cells in addition to the liver. Purpose: Improved mesalamine release by Hot-Melt Extrusion (HME) technique could be utilized for better management of Inflammatory Bowel Disease (IBD). Methods: Mes and hydrophilic polymers like Eudragit-EPO, KollidonVA-64 and PEG 6000 were hot-melt extruded using a co-rotating twin-screw laboratory extruder. Results: The minor shifting with significantly reduced intensity and disappearance of peak in the Differential Scanning Calorimetry (DSC) thermogram could be attributed to some solid-solid interaction and not necessarily any incompatibility. Fourier-Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM) confirmed the transformation of individual drug crystal into accumulations of small crystallites due to partial or almost complete amorphization. Continuous manufacturing of stable amorphous solid dispersion by solvent-free drug loading Hot-melt extrusion technique has been found feasible in improving drug release compared to mesalamine alone in simulated gastric fluid (f 1 = 0.3 to 11.1 and f 2 = 26 to 49). Conclusion: Melt dispersion samples have exhibited significantly improved mesalamine release and could be utilized for better management of Inflammatory Bowel Disease (IBD).

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“…It is clear that the estimations of the lag time (Lt) followed a decreasing pattern with respect to temperature. The concurrent estimation of activation energy of permeation, partition, and diffusion coefficient as a component of temperature portrayed the thermodynamic approach of the drug permeation kinetic (Mallick, Mondal, & Sannigrahi, ). Here it has been found that the rising temperature lead to increase in partition, diffusion coefficients of permeation which implied the abatement in the activation energy (Mohapatra, Senapati, Sahoo, & Mallick, ).…”

Section: Discussionmentioning

confidence: 99%

Temperature‐dependent mucosal permeation kinetics of stigmasterol microspheres: In vivo mice model antioral candidiasis study

et al. 2019

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Evaluation of mucosal permeation of stigmasterol from the glutaraldehyde cross linked chitosan microspheres at increasing experimental temperatures was performed. The activation energy of permeation, partition, and diffusion were estimated to understand the permeation kinetic with respect to the temperature. The formulation depicting least activation energy possessed the increased permeation thresholds of drug at the site of application. The encapsulation efficacy and mucoadhesive strength were found to be directly proportional to the polymer‐emulsifier ratio. Decreased intensity in crystallography directed the molecular dispersion of microencapsulated drug. The depleted enthalpic phase transition in thermogram affirmed the stigmasterol encapsulation. The sphericity and the size of microspheres were determined by scanning electron photo micrograph. The in vivo quantification of oral Candida infection with different statistical approach and histopathological observation of infected tongue of mice on treatment with the stigmasterol encapsulated microspheres showed significant anti oral candidiasis activity by reduction of fungal colony count and recovery of papillae, reorganization of basal cell layer and newly formed papillae during 21–28 days of treatment.

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Kinetic measurements of the hydrolytic degradation of cefixime: effect of Captisol complexation and water-soluble polymers

Cited by 25 publications

References 51 publications

Experimental and Computational Studies of Physicochemical Properties Influence NSAID-Cyclodextrin Complexation

Experimental and Computational Studies of Physicochemical Properties Influence NSAID-Cyclodextrin Complexation

Solvent-free Hot Melt Extrusion Technique in Improving Mesalamine Release for Better Management of Inflammatory Bowel Disease

Temperature‐dependent mucosal permeation kinetics of stigmasterol microspheres: In vivo mice model antioral candidiasis study

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