Enteric-coated aspirin in cardiac patients: Is it less effective than plain aspirin?

Jirmář, Radovan; Widimský, Petr

doi:10.1016/j.crvasa.2017.05.011

Cited by 12 publications

(11 citation statements)

References 21 publications

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“…Alternative NO-releasing prodrugs, diazenium-diolates (20) or furoxans (21). These compounds did not release significant levels of aspirin in human plasma stability studies.…”

Section: Figurementioning

confidence: 96%

“…EC-aspirin increases the exposure of the intestines to the drug by allowing it to pass through the stomach, prompting concerns that they increase irritation here instead, where symptoms are harder to detect [19]. EC-aspirin may also not be appropriate for use in the treatment of coronary heart disease [20]. The delayed absorption clearly also delays its therapeutic action.…”

Section: Introductionmentioning

confidence: 99%

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True or false? Challenges and recent highlights in the development of aspirin prodrugs

Willetts

Foley

2020

European Journal of Medicinal Chemistry

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“…Alternative NO-releasing prodrugs, diazenium-diolates (20) or furoxans (21). These compounds did not release significant levels of aspirin in human plasma stability studies.…”

Section: Figurementioning

confidence: 96%

Section: Introductionmentioning

confidence: 99%

True or false? Challenges and recent highlights in the development of aspirin prodrugs

Willetts

Foley

2020

European Journal of Medicinal Chemistry

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“…Up to 2 h delays were reported for enteric coated tablets and pellets to disintegrate post gastric emptying in vivo (Bogentoft et al, 1984;Ebel et al, 1993;HARDY et al, 1987;Liu and Basit, 2010). Clinically, this caused retarded absorption and onset of action of the active ingredient, or even ineffective therapy, as reported in the cases of enteric coated pancreatic enzymes and aspirin (Guarner et al, 1993;Jirmář and Widimský, 2018). Research has been carried out in speeding up the dissolution of enteric coated formulations in the proximal small intestine, for example the design of a double-coating system (DuoCoat TM ) that has a buffered inner coat to accelerate the dissolution of the outer enteric coating (Liu and Basit, 2010).…”

Section: Drug Release From Enteric Coated Prednisolone Microparticles Pellets and Tabletsmentioning

confidence: 99%

Regulating the pH of bicarbonate solutions without purging gases: Application to dissolution testing of enteric coated tablets, pellets and microparticles

Scott

Patel

Sithole

et al. 2020

International Journal of Pharmaceutics

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Dissolution media based on bicarbonate buffers closely mimic the environment of intestinal fluids and thus improve in vitro in vivo correlation compared to phosphate buffers. Purging gases into the medium is used as a method to stabilise bicarbonate buffers; however, this causes issues due to the disturbance of the hydrodynamics in the dissolution vessel. The aim of this study was to develop a novel system to regulate and stabilise the pH of bicarbonate buffers without purging gases for the application of dissolution testing of enteric coated products. A novel enclosure system was applied to the USP II dissolution vessel to supply N2 and CO2 gases above the dissolution medium without purging into the solution. Drug release from enteric coated predinisolone microparticles (216.9 µm), pellets (1.25 mm) and commercially available tablets was determined in 0.1M HCl and subsequently in pH 6.8 phosphate buffer or pH 6.2-6.8 bicarbonate buffers generated by titration of the acidic medium in situ using USP II apparatus. Supplying N2 at 3-4 bar and CO2 at 0.1 bar were able to increase the pH of the bicarbonate buffer from pH 6.2 to 6.8 within 45 min and subsequently stabilise the medium pH at 6.8 ± 0.05 pH units. Enteric coated microparticles showed much faster drug release in the physiological bicarbonate buffers than tablets and pellets. The novel bicarbonate-based dissolution system moves forward the application of the physiological bicarbonate buffers for testing pharmaceutical products to meet compendial requirements.

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“…Напомним, что pKa -значение pH, при котором диссоциировано 50% молекул вещества. В кислой среде желудка АСК слабо диссоциирует на ионы, оставаясь в нейтральном и, следовательно, более липофильном состоянии, что способствует ее быстрому прохождению через билипидный слой мембран клеток и всасыванию в портальный кровоток [16]. Максимальной стабильностью АСК обладает в среде с pH 2-3 [13].…”

Section: всасывание аск в жктunclassified

Antithrombotic effect of different acetylsalicylic acid drug formulations: is there a difference?

Сидоров

2021

Russ J Cardiol

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To date, a sufficient volume of clinical studies has been accumulated that have demonstrated a reduced antiplatelet effect of enteric-coated (EC) lowdose acetylsalicylic acid (ASA). Delayed and incomplete absorption from the intestinal alkaline medium, which significantly reduces the bioavailability of drug, is considered the main reason for laboratory aspirin resistance (pseudoresistance) to EC ASA. This phenomenon is of particular importance for patients with acute coronary syndrome, when a quick effect is required, as well as for patients with diabetes and obesity due to additional causes of increased platelet activity, on the one hand, and reduced bioavailability of ASA, on the other. Given the issue of efficacy, the dubious gastroprotective effect and the more pronounced damaging effect on the mucous membrane of small intestine, the use of EC ASA should be avoided, especially in patients with a multifactorial risk of insufficient response to therapy. A good alternative is buffered ASA, which quickly dissolves and is partially absorbed directly in the stomach, having antiplatelet activity comparable to simple ASA and a similar aspirin resistance, is associated with a lower risk of aspirin-induced enteropathy in comparison with ES ASA. In addition, according to a number of small studies and retrospective analyzes, buffered ASA is less likely to cause damage to gastric mucosa compared to EC ASA.

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Enteric-coated aspirin in cardiac patients: Is it less effective than plain aspirin?

Cited by 12 publications

References 21 publications

True or false? Challenges and recent highlights in the development of aspirin prodrugs

True or false? Challenges and recent highlights in the development of aspirin prodrugs

Regulating the pH of bicarbonate solutions without purging gases: Application to dissolution testing of enteric coated tablets, pellets and microparticles

Antithrombotic effect of different acetylsalicylic acid drug formulations: is there a difference?

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