From the pharmaceutical to the clinical: the case for effervescent paracetamol in pain management. A narrative review

Dubray, Claude; Maincent, Philippe; Milon, Jean Yves

doi:10.1080/03007995.2021.1902297

Cited by 12 publications

(7 citation statements)

References 62 publications

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“…Due to its benefits, effervescent delivery can be quite helpful for a variety of therapies. such as in the therapy of pain [24][25][26][27][28] , ulcers 29 , allergies 30,31 , osteoporosis, arthritis, inflammation, antimicrobial infections [32][33][34] and many more conditions 35 . Acetylsalicylic acid, also known to be aspirin, paracetamol 26,36,37 , ibuprofen 38 , ascorbic acids and other vitamins [39][40][41] , calcium carbonate, and other antacids like ranitidine 42,43 , famotidine 29 , etc.…”

Section: Effect Of Water On Effervescent Formulationsmentioning

confidence: 99%

A Comprehensive Review on Effervescent Tablets

Vanhere,

Derle,

Khatale

et al. 2023

J. Drug Delivery Ther.

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Effervescent tablets are becoming increasingly popular due to their ease of administration and rapid onset of action. They typically contain acidic materials and carbonates or bicarbonates that react quickly in the presence of water, releasing carbon dioxide and improving API solubility and flavour masking. However, effervescent tablets can be bulky, and the reaction rate is difficult to control due to water's catalytic effect. This article discusses the advantages and disadvantages of effervescent tablets, common effervescent reactions, active ingredients that can be formulated, and the preparation and manufacturing process. It also evaluates effervescent granules and tablets and explores the latest advancements in effervescent technology. Overall, effervescent tablets offer a promising option for drug delivery, and ongoing research will undoubtedly yield even more advanced formulations in the future. Keywords: Effervescent granules, Effervescent tablets, Hot melt granulation, Carbon dioxide content, Water activity

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Section: Effect Of Water On Effervescent Formulationsmentioning

confidence: 99%

A Comprehensive Review on Effervescent Tablets

Vanhere,

Derle,

Khatale

et al. 2023

J. Drug Delivery Ther.

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“…Since effervescence can quickly disperse active compounds and allows rapid dissolution, it is used in the administration of pharmaceuticals, particularly in patients who face difficulty in swallowing a tablet or capsule [ 66 ]. Another advantage of effervescence is that it also allows quick dispersion of the active compounds in the oral cavity as well as absorption through oral mucosal and, in this way, the first-pass effect can be avoided, leading to increased bioavailability of the drug and faster activity onset [ 5 , 67 ]. Effervescence may increase buccal absorption since the citric acid in the formulation sequesters calcium ions (Ca 2+ ), making the tight junctions more permeable, thereby promoting paracellular transport [ 35 ].…”

Section: Citric Acid In Formulationsmentioning

confidence: 99%

“…It is also used as a pH regulator [ 3 ]. Its effervescence in the presence of carbonates make it useful as tablet disintegrant, in instant drinks, and in personal care products, such as bath tablets [ 4 , 5 ]. Citric acid monohydrate is the usual form of citric acid sold on the commercial market.…”

Section: Introductionmentioning

confidence: 99%

Citric Acid: A Multifunctional Pharmaceutical Excipient

et al. 2022

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Citric acid, a tricarboxylic acid, has found wide application in the chemical and pharmaceutical industry due to its biocompatibility, versatility, and green, environmentally friendly chemistry. This review emphasizes the pharmaceutical uses of citric acid as a strategic ingredient in drug formulation while focusing on the impact of its physicochemical properties. The functionality of citric acid is due to its three carboxylic groups and one hydroxyl group. These allow it to be used in many ways, including its ability to be used as a crosslinker to form biodegradable polymers and as a co-former in co-amorphous and co-crystal applications. This paper also analyzes the effect of citric acid in physiological processes and how this effect can be used to enhance the attributes of pharmaceutical preparations, as well as providing a critical discussion on the issues that may arise out of the presence of citric acid in formulations.

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“…To address issues of elevated risk of hepatotoxicity and low systemic bioavailability in oral administration, an effervescent formulation of the drug with sodium bicarbonate was launched into the market. 1 , 2 …”

Section: Introductionmentioning

confidence: 99%

Sodium-based paracetamol: impact on blood pressure, cardiovascular events, and all-cause mortality

Rao,

Nazarzadeh,

Canoy

et al. 2023

European Heart Journal

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Background and Aims Effervescent formulations of paracetamol containing sodium bicarbonate have been reported to associate with increased blood pressure and a higher risk of cardiovascular diseases and all-cause mortality. Given the major implications of these findings, the reported associations were re-examined. Methods Using linked electronic health records data, a cohort of 475 442 UK individuals with at least one prescription of paracetamol, aged between 60 and 90 years, was identified. Outcomes in patients taking sodium-based paracetamol were compared with those taking non–sodium-based formulations of the same. Using a deep learning approach, associations with systolic blood pressure (SBP), major cardiovascular events (myocardial infarction, heart failure, and stroke), and all-cause mortality within 1 year after baseline were investigated. Results A total of 460 980 and 14 462 patients were identified for the non–sodium-based and sodium-based paracetamol exposure groups, respectively (mean age: 74 years; 64% women). Analysis revealed no difference in SBP [mean difference −0.04 mmHg (95% confidence interval −0.51, 0.43)] and no association with major cardiovascular events [relative risk (RR) 1.03 (0.91, 1.16)]. Sodium-based paracetamol showed a positive association with all-cause mortality [RR 1.46 (1.40, 1.52)]. However, after further accounting of other sources of residual confounding, the observed association attenuated towards the null [RR 1.08 (1.01, 1.16)]. Exploratory analyses revealed dysphagia and related conditions as major sources of uncontrolled confounding by indication for this association. Conclusions This study does not support previous suggestions of increased SBP and an elevated risk of cardiovascular events from short-term use of sodium bicarbonate paracetamol in routine clinical practice.

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From the pharmaceutical to the clinical: the case for effervescent paracetamol in pain management. A narrative review

Cited by 12 publications

References 62 publications

A Comprehensive Review on Effervescent Tablets

A Comprehensive Review on Effervescent Tablets

Citric Acid: A Multifunctional Pharmaceutical Excipient

Sodium-based paracetamol: impact on blood pressure, cardiovascular events, and all-cause mortality

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