Stability of Vancomycin Hydrochloride Solutions at Various PH Values as Determined by High-Performance Liquid Chromatography

Mathew, Mary; Gupta, V. Das

doi:10.3109/03639049509048108

Cited by 24 publications

(9 citation statements)

References 2 publications

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“…It is reported that vancomycin undergoes base-catalyzed hydrolysis at pH 8 to form a succinimide degradant (succinimide 11) [ 28 ]. Between pH 1 and 3, the acid-catalyzed reaction of vancomycin has been observed in aqueous solution [ 29 ]. The water-catalyzed reaction has been observed between pH 3 and 5.7, and between pH 5.7 and 7.0, vancomycin degradation was faster in phosphate-buffered solution, where HPO 4 2- (K 5 ) had the dominating catalytic effect [ 29 ] and K 5 was the second order rate constant for the acid/base catalysis of vancomycin hydrochloride.…”

Section: Resultsmentioning

confidence: 99%

Glycopeptide antibiotic drug stability in aqueous solution

Jakaria

Budil

Murtagh³

2022

AAPS Open

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Glycopeptide antimicrobials are a class of naturally occurring or semi-synthetic glycosylated products that have shown antibacterial activity against gram-positive organisms by inhibiting cell-wall synthesis. In most cases, these drugs are prepared in dry powder (lyophilized) form due to chemical and physical instability in aqueous solution; however, from an economic and practical point of view, liquid formulations are preferred. Researchers have recently found ways to formulate some glycopeptide antibiotic therapeutic drugs in aqueous solution at refrigerated or room temperature. Chemical degradation can be significantly slowed by formulating them at a defined pH with specific buffers, avoiding oxygen reactive species, and minimizing solvent exposure. Sugars, amino acids, polyols, and surfactants can reduce physical degradation by restricting glycopeptide mobility and reducing solvent interaction. This review focuses on recent studies on glycopeptide antibiotic drug stability in aqueous solution. It is organized into three sections: (i) glycopeptide antibiotic instability due to chemical and physical degradation, (ii) strategies to improve glycopeptide antibiotic stability in aqueous solution, and (iii) a survey of glycopeptide antibiotic drugs currently available in the market and their stability based on published literature and patents. Antimicrobial resistance deaths are expected to increase by 2050, making heat-stable glycopeptides in aqueous solution an important treatment option for multidrug-resistant and extensively drug-resistant pathogens. In conclusion, it should be possible to formulate heat stable glycopeptide drugs in aqueous solution by understanding the degradation mechanisms of this class of therapeutic drugs in greater detail, making them easily accessible to developing countries with a lack of cold chains.

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Section: Resultsmentioning

confidence: 99%

Glycopeptide antibiotic drug stability in aqueous solution

Jakaria

Budil

Murtagh³

2022

AAPS Open

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“…For each hydrogel/drug combination, at least 65% of the drug loaded into the gels was released within 168 h. Cumulative release of cefazolin was over 85% from PNDJ gels, and as low as 65% from PND gels, whereas only 70–85% of vancomycin was measured as having been released from any of the gel formulations. Incomplete release over this timeframe may be due to some combination of drug retention within the gel or degradation of the drugs—vancomycin36, 37 and cefazolin38, 39 both are known to be unstable under conditions similar to those used in these studies. PNDJ30 gels became translucent by 72 h and were dissolved in the release media by 120 or 168 h. Both PNDJ15 and PND gels remained intact throughout the studies.…”

Section: Resultsmentioning

confidence: 99%

Concanavalin A immobilized magnetic poly(glycidyl methacrylate) beads for antibody purification

Akkaya

Yavuz

Candan

et al. 2012

J of Applied Polymer Sci

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Concanavalin A (Con A) immobilized magnetic poly(glycidyl methacrylate) (mPGMA) beads in monosize and spherical for (1.62 μm in diameter) were used for the purification of human immunoglobulin G (IgG) from human plasma. Con A was immobilized by covalent binding onto the mPGMA beads. The maximum IgG adsorption on the mPGMA‐Con A beads was observed at pH 6.0. The nonspecific IgG adsorption onto the plain mPGMA beads was very low (0.22 mg/g). Scatchard analysis of the adsorption isotherm for IgG on mPGMA‐Con A beads showed an affinity constant (Ka) of 1.39 × 105 M−1 and a theoretical maximum adsorption capacity of 109.1 mg/g. An apparent IgG adsorption capacity of 66.2 mg/g was observed under the experimental conditions. IgG adsorption capacity from human plasma was observed as 48.0 mg/g. The adsorption of human serum albumin from plasma was 2.0 mg/g. The total protein adsorption was determined to be 50.0 mg/g. IgG molecules could be repeatedly adsorbed and eluted with the mPGMA‐Con A beads without noticeable loss in the IgG adsorption capacity. © 2012 Wiley Periodicals, Inc. J Appl Polym Sci, 2012

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“…The results getting from the vehicle control proved the absence of toxicity of the vehicle used in the tested solution. This liquid vehicle was formulated at a pH of 5.0 to find the best compromise between the VAN stability and lung tolerance but also to avoid possible bronchospasms that may occur at lower pH (Mathew & Das Gupta, 1995). Propylene glycol at 25% and phosphate buffer at the concentrations tested have been already used in human by nebulization (Bisgaard et al, 1987; Corcoran, 2006).…”

Section: Discussionmentioning

confidence: 99%

In vitro and in vivo local tolerability of a synergistic anti‐tuberculosis drug combination intended for pulmonary delivery

Ravon

Menchi

Lambot

et al. 2022

J of Applied Toxicology

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A drug combination, vancomycin (VAN) plus tetrahydrolipstatin (THL), has demonstrated an effective synergistic action in vitro against Mycobacterium tuberculosis (Mtb). The poor oral bioavailability of VAN and THL and the predominant tropism of Mtb infection to the lungs make their pulmonary administration very attractive. To evaluate their local tolerability, bronchial cells, alveolar cells and monocytes were exposed to concentrations around and above their minimal inhibitory concentration (MIC). The VAN had no inhibitory activity on the tested human cell lines, even at a concentration 125 times higher than its MIC, whereas the THL, alone or in combination with VAN, presented a cytostatic action. Monolayer epithelium showed no significant irreversible damage at concentrations up to 100 times the combination MIC.BALB/cAnNRj mice exposed to concentration of 50 times the combination MIC delivered endotracheally 3 times a week for 3 weeks showed no clinical signs or significant weight loss. The increase of proinflammatory biomarkers (i.e., IL-1, IL-6, TNFα and proportion of inflammatory cells) and cytotoxicity in bronchoalveolar lavage fluid (BALF) were non-significant. Lung histopathology did not show significant tissue damage. The VAN/THL combination at doses up to 50 times the combination MIC is found to be thus well tolerated by pulmonary route. This study is a promising result and encouraging further investigations of pulmonary administration of VAN/THL combination as dry powder for anti-tuberculosis treatment.

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Stability of Vancomycin Hydrochloride Solutions at Various PH Values as Determined by High-Performance Liquid Chromatography

Cited by 24 publications

References 2 publications

Glycopeptide antibiotic drug stability in aqueous solution

Glycopeptide antibiotic drug stability in aqueous solution

Concanavalin A immobilized magnetic poly(glycidyl methacrylate) beads for antibody purification

In vitro and in vivo local tolerability of a synergistic anti‐tuberculosis drug combination intended for pulmonary delivery

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