Carbasalate calcium

Quantitative determination of carbasalate calcium derived metabolites, acetylsalicylic acid and salicylic acid, in six animal foods using liquid-liquid extraction method coupled with liquid chromatography-tandem mass spectrometry

This work describes a simple screening protocol for quantification of carbasalate calcium derived metabolites, acetylsalicylic acid (ASA) and salicylic acid (SA), in animal and aquatic food matrices using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The analytes were extracted from porcine muscle, milk, egg, shrimp, eel, and flatfish using acetonitrile, with the addition of formic acid as well as trifluoroacetic acid, followed by liquid-liquid purification with saturated n-hexane. A reverse-phase analytical column was employed with a mobile phase comprising (A) 1 mM ammonium acetate in distilled water and (B) methanol to achieve the best chromatographic separation. Matrix-matched calibration curves (R2 ≥ 0.9817) were constructed using six concentrations of 5, 10, 20, 30, 40, and 50 ?g/kg in porcine muscle, milk, egg, shrimp, eel, and flatfish matrices. The calculated limits of quantification (LOQ) were 10 and 7 ?g/kg, for ASA and SA, respectively. Recoveries of 67 to 102% with relative standard deviations (RSDs) of ≤9.0% (intra-day and inter-day) were obtained for all matrices at four spiking concentrations (5, 10, 20, and 50 ?g/kg). The method was feasibly applied for monitoring market samples. In conclusion, the developed method is versatile, accurate, and precise for detecting and quantifying acetylsalicylic acid and salicylic acid residues in animal-derived foods meant for human consumption.

Analytical determination and pharmacokinetics of major metabolites of carbasalate calcium in broilers following oral administration

As a newer anti-inflammatory agent, carbasalate calcium is used in various animal species. In this study, the pharmacokinetics of carbasalate calcium was investigated in broilers. Broilers, with body weight of 2.0 ± 0.3 kg, were administrated carbasalate calcium soluble powder at a single dose of 40 mg/kg body weight orally. The plasma concentrations of its metabolites, aspirin (ASA), salicylic acid (SA) and gentisic acid (GA) were determined by LC-MS/MS method and the pharmacokinetic parameters were calculated by noncompartmental analysis. After oral administration of carbasalate calcium, the plasma drug concentration for ASA, SA and GA reached a peak (C(max) ) of 8.88 ± 1.31, 42.6 ± 4.62 and 10.1 ± 2.16 μg/mL at 0.170, 2.00 and 2.00 h, respectively. The terminal half-life (t(1/2λz) ) of ASA, SA and GA was 11.2 ± 8.04, 23.7 ± 17.1 and 28.6 ± 4.90 h, respectively. In conclusion, analytical method for the quantification of ASA, SA and GA in plasma in the broilers was developed and validated. In broilers, carbasalate calcium is quickly metabolized in ASA and ASA is rapidly converted to SA and one of the metabolites of SA is GA.

Comparison of effects of calcium carbasalate and aspirin on gastroduodenal mucosal damage in human volunteers

Calcium carbasalate is a therapeutically active salicylate which seems to cause less gastroduodenal mucosal damage than aspirin in laboratory animals. This endoscopist-blinded, randomised, cross over trial aimed to compare acute gastric mucosal damage in 20 healthy volunteers treated with acetyl salicylic acid (ASA) (650 mg three times daily) and effervescent calcium carbasalate (ECC) (826.8 mg three times daily) bioequivalent to 650 mg ASA over a five day period. Endoscopy was performed immediately before treatment and on day 5 of each treatment. Serum salicylate, thromboxane B2, and gastric mucosal prostaglandin E2 (PGE2) concentrations were measured after endoscopy. ECC caused fewer gastric mucosal erosions than ASA. The total number of gastric erosions was 23.8 (16.1) in the ASA treated subjects compared with 9.1 (8.7) in ECC treated subjects (p = 0.004). Differences between ASA and ECC were significant for both the gastric antrum and body, and for both haemorrhagic and non-haemorrhagic erosions. The mean gastric body Lanza score for mucosal damage was lower after ECC than ASA (p = 0.003). The visual analogue score for gastric body damage was lower for ECC (16.9 mm (15.9)) than for ASA (32.7 mm (20.8)), p = 0.008. Serum salicylate concentrations were similar after both preparations (ASA: 66 (23) mg/l, versus ECC: 58 (17) mg/l, NS). Serum thromboxane B2 was similarly reduced using both preparations-97.2 (3.5)% inhibition with ASA, 95.2 (5.5)% inhibition with calcium carbasalate (NS). Suppression of gastric mucosal PGE2 synthesis was similar with both preparations (ASA: 83.4 (17.1)%; ECC 84.3 (12.9)%; NS). It is concluded that ECC causes significantly less gastroduodenal mucosal damage than ASA administered at bioequivalent doses as judged by serum salicylate, serum thromboxane, and mucosal PGE2 values. ECC may therefore be a less harmful alternative treatment to plain ASA.

Peptic ulcerations are related to systemic rather than local effects of low-dose aspirin

Background & aims: Effervescent calcium carbasalate is a calcium-salt of acetylsalicylic acid causing less local gastric damage than acetylsalicylic acid at high doses in healthy controls. The aim of the study was to investigate the incidence of peptic ulcers in a population-based cohort using bioequivalent low-dose acetylsalicylic acid (80 mg) or effervescent calcium carbasalate (100 mg).
Methods: Incident acetylsalicylic acid or effervescent calcium carbasalate users were identified from the Integrated Primary Care Information database. The study cohort comprised 19,819 subjects: 11,891 on acetylsalicylic acid and 7928 on effervescent calcium carbasalate. Incidence rates for documented peptic ulcer disease confirmed by endoscopy were calculated and time-dependent adjusted Cox regression analysis was used to compare the risk of peptic ulcers for patients using acetylsalicylic acid or effervescent calcium carbasalate.
Results: During an average 1.85 years of follow-up evaluation, 115 ulcers were found. The risk for developing a peptic ulcer during drug use was: 3.07 per 1000 person-years for acetylsalicylic acid and 4.31 for effervescent calcium carbasalate. The risk of peptic ulcers was not statistically significantly higher in patients using effervescent calcium carbasalate than in acetylsalicylic acid users (adjusted hazard ratio, 1.39; 95% confidence interval, 0.92-2.12).
Conclusions: The incidence rate of peptic ulcer disease is similar in patients using low-dose effervescent calcium carbasalate compared with regular low-dose acetylsalicylic acid. This implicates that peptic ulcers seem to be related to systemic rather than to local effects of low-dose acetylsalicylic acid.

Acetylsalicylic acid use is associated with reduced risk of out-of-hospital cardiac arrest in the general population: Real-world data from a population-based study

Aim: Activated blood platelet products facilitate myocardial intracellular Ca2+ overload, thereby provoking afterdepolarizations and increasing susceptibility of ischemic myocardium to ventricular fibrillation (VF). These effects are counteracted in vitro by acetylsalicylic acid (ASA), but no prior study investigated whether ASA is associated with decreased out-of-hospital cardiac arrest (OHCA) risk on a population level. Therefore, we studied whether ASA and other antiplatelet drugs (carbasalate calcium, clopidogrel) are associated with decreased risk of OHCA.
Methods: We conducted a population-based case-control study among individuals (772 OHCA-cases with documented VT/VF, 2444 non-OHCA-controls) who had used antiplatelet drugs in the year before index-date (OHCA-date), and studied the association between current antiplatelet drug use and OHCA-risk with multivariable logistic regression analysis.
Results: ASA use was associated with reduced OHCA-risk (adjusted odds ratio (ORadj) 0.6 [0.5-0.8]), and more so in women (ORadj 0.3 [0.2-0.6]) than in men (ORadj 0.7 [0.5-0.95], Pinteraction 0.021). Carbasalate calcium was associated with decreased OHCA-risk in women (ORadj 0.5 [0.3-0.9]), but not in men (ORadj 1.3 [0.96-1.7], Pinteraction 0.005). Clopidogrel was not associated with reduction in OHCA-risk. Risk reduction associated with ASA in patients with OHCA was similar in the presence of acute myocardial infarction (AMI) (ORadj 0.6 [0.4-0.9]) and in the absence of AMI (ORadj 0.7 [0.4-1.2]).
Conclusion: ASA use was associated with reduced OHCA-risk in both sexes, and more so in women, while carbasalate calcium only protected women. Clopidogrel was not associated with reduced OHCA-risk.