Aztreonam

Florey, Klaus

doi:10.1016/s0099-5428(08)60215-4

Cited by 12 publications

(12 citation statements)

References 19 publications

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“…The product was dried under vacuum to furnish 174.2 g (yield 86%) of aztreonam 1 , HPLC AP 97.8 . The product was identical ( 1 H NMR) to aztreonam prepared by method A …”

Section: Methodsmentioning

confidence: 99%

Regioselective Activation of Aminothiazole(iminoxyacetic acid)acetic Acid: An Efficient Synthesis of the Monobactam Aztreonam

Singh

Denzel

Fox

et al. 2002

Org. Process Res. Dev.

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An efficient synthesis of the monobactam aztreonam [[2S-[2r,3β(Z)]]-3[[(2-amino-4-thiazolyl)[(1-carboxy-1-methylethoxy)imino]acetyl]amino]-2-methyl-4-oxo-1-azetidinesulfonic acid] (1) by acylation of r-aminoazetidinone 22 with the regioselectively activated aminothiazoleiminoxyacetic diacid 15 or 18 is described. Reaction of benzhydryl ester 10 with N-hydroxybenzotriazole and dicyclohexylcarbodiimide followed by ester deprotection formed the monoacid amide 15. Alternatively, chemoselective transient silylation of the diacid 9 followed by activation with N-hydroxysuccinimide formed active ester 18. Acylation of r-aminoazetidinone 22 with amide 15 or ester 18 produced aztreonam (1) in 75-85% yield.

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“…The product was dried under vacuum to furnish 174.2 g (yield 86%) of aztreonam 1 , HPLC AP 97.8 . The product was identical ( 1 H NMR) to aztreonam prepared by method A …”

Section: Methodsmentioning

confidence: 99%

Regioselective Activation of Aminothiazole(iminoxyacetic acid)acetic Acid: An Efficient Synthesis of the Monobactam Aztreonam

Singh

Denzel

Fox

et al. 2002

Org. Process Res. Dev.

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“…Meropenem and cefuroxime have better stability yet have to be replaced every 8-12 h. Cold ice packs have been used to increase the stability of meropenem in order to allow replacement every 24 h (Kuti et al 2004). In contrast, anti-pseudomonal beta-lactams for continuous infusion, such as ceftazidime, cefpirome, cefepime and aztreonam, are stable at room temperature for at least 24 h and when refrigerated for at least 4-7 days (Vinks et al 1996b;Stiles et al 1989;Viaene et al 2002;Baririan et al 2003;Servais and Tulkens 2001;Sprauten et al 2003;Florey 1988) and cefotaxime is also stable for 24 h. Prolonged exposure to temperatures above 25 °C however may drastically reduce stability making several these antibiotics less suited for delivery via an ambulatory pump carried close to the body or underneath clothing (Viaene et al 2002;Baririan et al 2003;Servais and Tulkens 2001). For several other β-lactams used in the ICU setting, stability of intravenous fluids for prolonged infusion is not well documented (Trissel 2006).…”

Section: Stabilitymentioning

confidence: 99%

Continuous Infusion of Beta-lactam Antibiotics

Muller

Mouton

2013

Fundamentals of Antimicrobial Pharmacokinetics and Pharmacodynamics

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For beta-lactam antibiotics continuous infusion can be used to optimise antibiotic therapy. Pre-clinical studies in rodents and in vitro studies have shown the benefits of continuous infusion when compared to intermittent dosing. Pharmacokinetic studies in humans have shown an improved probability of target attainment for continuous infusion. However, the relationship between continuous infusion and improved clinical outcome is ambiguous. The superiority of continuous infusion over intermittent dosing in clinical outcome studies is most often documented in special subgroups, such as critically ill patients or patients infected with less-susceptible micro-organisms. Methods to calculate doses during continuous infusion and practical issues, such as stability of antimicrobial solutions, are described.

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“…Propylene glycol (PG) and polyethylene glycol-400 (PEG-400) were selected as plasticizer. [ 6 7 ] The mucoadhesive vaginal films were evaluated for percentage elongation, tensile strength, folding endurance, drug content, in vitro disintegration time, in vitro dissolution study, percentage swelling index, bioadhesive strength, in vitro diffusion study, ex vivo diffusion study, and in vitro antifungal activity.…”

Section: Introductionmentioning

confidence: 99%

Formulation, development and characterization of mucoadhesive film for treatment of vaginal candidiasis

Mishra

Joshi

Mehta

2016

Int J Pharma Investig

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Objective:The objective of the present investigation was formulation, optimization and characterization of mucoadhesive film of clotrimazole (CT) which is patient-convenient and provides an effective alternative for the treatment of vaginal candidiasis. CT is an antimycotic drug applied locally for the treatment of vaginal candidiasis.Materials and Methods:Mucoadhesive vaginal films were prepared by solvent casting technique using hydroxyl propylcellulose and sodium alginate as polymers. Propylene glycol and polyethylene glycol-400 were evaluated as plasticizers. The mucoadhesive vaginal films were evaluated for percentage elongation, tensile strength, folding endurance, drug content, in vitro disintegration time, in vitro dissolution study, swelling index, bioadhesive strength, and diffusion study.Results:Among various permeation enhancers used, isopropyl myristate was found to be suitable. To evaluate the role of the concentration of permeation enhancer and concentration of polymers in the optimization of mucoadhesive vaginal film, 32 full factorial design was employed. Optimized batch showed in vitro disintegration time, 18 min; drug content, 99.83%; and tensile strength, 502.1 g/mm2. In vitro diffusion study showed that 77% drug diffusion occurred in 6 h. This batch was further evaluated by scanning electron microscopy indicating uniformity of the film. In vitro Lactobacillus inhibition and in vitro antifungal activity of optimized batch showed an inhibitory effect against Candida albicans and no effect on Lactobacillus, which is a normal component of vaginal flora.Conclusion:Mucoadhesive vaginal film of CT is an effective dosage form for the treatment of vaginal candidiasis.

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Aztreonam

Cited by 12 publications

References 19 publications

Regioselective Activation of Aminothiazole(iminoxyacetic acid)acetic Acid: An Efficient Synthesis of the Monobactam Aztreonam

Regioselective Activation of Aminothiazole(iminoxyacetic acid)acetic Acid: An Efficient Synthesis of the Monobactam Aztreonam

Continuous Infusion of Beta-lactam Antibiotics

Formulation, development and characterization of mucoadhesive film for treatment of vaginal candidiasis

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