Determination of non-protein-bound N-acetylcysteine in plasma by high-performance liquid chromatography

K»gedal, Bertil; Källberg, Magnus; M»rtensson, Johannes

doi:10.1016/s0378-4347(00)84705-2

Cited by 26 publications

(4 citation statements)

References 6 publications

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“…Another potential reason for the differences between the findings of the present study and those by Borgström et al could be the fact that, in the latter study, proteins in the plasma samples were precipitated before disulfide bonds were reduced, which could have affected their findings [4,13]. Furthermore, in the studies by Borgström et al and Olsson et al, samples were collected for 12 h after NAC administration, while, in the study by Liu et al, samples were collected for 24 h [4,5,10].…”

Section: Discussioncontrasting

confidence: 90%

Pharmacokinetics and Safety of Single and Multiple Doses of Oral N-Acetylcysteine in Healthy Chinese and Caucasian Volunteers: An Open-Label, Phase I Clinical Study

2020

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Introduction Few studies have evaluated whether the pharmacokinetics of N -acetyl-cysteine (NAC) are different in Chinese and Caucasian individuals. Methods This single- and multiple-dose, single-centre, open-label, phase I clinical study was conducted in healthy adult volunteers. All participants received oral NAC 600-mg uncoated tablets, which were administered first as a single dose and, following a 48-h wash-out period, twice daily for 3 days. Blood and urine were collected after single- and multiple-dose NAC administration. Adverse event (AE) data were collected throughout the study. Results Fifteen Chinese and 15 Caucasian (mostly Italian) individuals (males 66.7%, mean age 36.8 years) participated in the study. Pharmacokinetic characteristics of NAC were similar in the two cohorts. Following both single- and multiple-dose administration, plasma concentration of NAC increased rapidly, reaching a peak at approximately 1.0 h. Maximum plasma concentration and extent of exposure were higher after multiple doses than after a single dose. The accumulation ratio was relatively consistent in both Chinese (mean ± standard deviation 1.5 ± 0.4) and Caucasian (1.4 ± 0.2) participants. The half-life was 15.4 h in Chinese and 18.7 h in Caucasian participants, and the fraction of NAC excreted in urine in the 36 h following administration was 3.7% in Chinese and 3.8% in Caucasian participants. Two Caucasian participants had a total of 3 AEs (headache, presyncope and dysmenorrhoea). No AEs occurred in Chinese participants. Conclusions The pharmacokinetic characteristics of NAC are similar in healthy Chinese and Caucasian individuals after single and repeated administration. NAC has a favourable tolerability profile.

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Section: Discussioncontrasting

confidence: 90%

Pharmacokinetics and Safety of Single and Multiple Doses of Oral N-Acetylcysteine in Healthy Chinese and Caucasian Volunteers: An Open-Label, Phase I Clinical Study

2020

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“…More pronounced fluorescence responses were observed with probes where the maleimide moiety was directly connected to the aromatic core of the fluorophore (6–286× in brightness, and 21–350× in quantum yield) than those having an aliphatic spacer (5–45× for the brightness, and 3–20× for the quantum yield). − While these probes are mostly used for the in vitro, in cellulo, or in plasma detection of biothiols, peptides, proteins, or antibodies, some of these probes can be used for biothiol recognition by HPLC with fluorescence monitoring. To this end, pyrene, − coumarin, BODIPY, , and N -[4-(2-phthalimidyl) phenyl] maleimide (PPM) were used for their good fluorescence responses to biothiols.…”

Section: Fluorogenic Maleimide-based Probesmentioning

confidence: 99%

“…78−120 While these probes are mostly used for the in vitro, in cellulo, or in plasma detection of biothiols, peptides, proteins, or antibodies, some of these probes can be used for biothiol recognition by HPLC with fluorescence monitoring. To this end, pyrene, 113−115 coumarin, 116 BODIPY, 106,117 and N-[4-(2-phthalimidyl) phenyl] maleimide (PPM) 118 were used for their good fluorescence responses to biothiols.…”

Section: Stability Of Reagents In the Context Of Oligonucleotidementioning

confidence: 99%

Covalent Modification of Biomolecules through Maleimide-Based Labeling Strategies

et al. 2018

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Since their first use in bioconjugation more than 50 years ago, maleimides have become privileged chemical partners for the site-selective modification of proteins via thio-Michael addition of biothiols and, to a lesser extent, via Diels-Alder (DA) reactions with biocompatible dienes. Prominent examples include immunotoxins and marketed maleimide-based antibody-drug conjugates (ADCs) such as Adcetris, which are used in cancer therapies. Among the key factors in the success of these groups is the availability of several maleimides that can be N-functionalized by fluorophores, affinity tags, spin labels, and pharmacophores, as well as their unique reactivities in terms of selectivity and kinetics. However, maleimide conjugate reactions have long been considered irreversible, and only recently have systematic studies regarding their reversibility and stability toward hydrolysis been reported. This review provides an overview of the diverse applications for maleimides in bioconjugation, highlighting their strengths and weaknesses, which are being overcome by recent strategies. Finally, the fluorescence quenching ability of maleimides was leveraged for the preparation of fluorogenic probes, which are mainly used for the specific detection of thiol analytes. A summary of the reported structures, their photophysical features, and their relative efficiencies is discussed in the last part of the review.

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“…Plasma samples were analysed by HPLC for concentration of non-protein-bound NAC according to previously described methods [8]. Urine was appropriately diluted and NAC was determined by a procedure similar to that used for plasma NAC determinations.…”

Section: Nac Determinationsmentioning

confidence: 99%

No effect of oral N-acetylcysteine on the bioavailability of erythromycin and bacampicillin

Paulsen

Borgström²,

Kågedal³

et al. 1988

Eur Respir J

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In vitro studies with N-acetylcysteine (NAC) solutions used for inhalation treatment have demonstrated inactivation of some antibiotics by NAC. Oral NAC treatment is increasingly common for long-term prophylaxis in chronic bronchitis. During exacerbations, treatment with oral antibiotics will often be given simultaneously. We assessed the effect of simultaneous oral administration of NAC on the bioavailability of two antibiotics in ten healthy volunteers. No effect of NAC was found on the bioavailability of ampicillin, after administration of the prodrug bacampicillin. A slight, but not significant statistical increase in erythromycin serum levels was seen with NAC. Acetylator phenotype did not influence the absorption of NAC, which seemed slightly reduced by bacampicillin, but significantly increased by erythromycin. No decrease of antibacterial activity of sera was found in vitro after the addition of NAC or the related thiol glutathione, employing micrococcus luteus and staphylococcus aureus as indicator organisms.

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Determination of non-protein-bound N-acetylcysteine in plasma by high-performance liquid chromatography

Cited by 26 publications

References 6 publications

Pharmacokinetics and Safety of Single and Multiple Doses of Oral N-Acetylcysteine in Healthy Chinese and Caucasian Volunteers: An Open-Label, Phase I Clinical Study

Pharmacokinetics and Safety of Single and Multiple Doses of Oral N-Acetylcysteine in Healthy Chinese and Caucasian Volunteers: An Open-Label, Phase I Clinical Study

Covalent Modification of Biomolecules through Maleimide-Based Labeling Strategies

No effect of oral N-acetylcysteine on the bioavailability of erythromycin and bacampicillin

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