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Effervescent Granulation
Published in Dilip M. Parikh, Handbook of Pharmaceutical Granulation Technology, 2021
Effervescence is the evolution of gas bubbles from a liquid, as a result of a chemical reaction. The most common reaction for pharmaceutical oral solid dosage forms is the autocatalytic acid–base reaction between sodium bicarbonate and citric acid.
From the pharmaceutical to the clinical: the case for effervescent paracetamol in pain management. A narrative review
Published in Current Medical Research and Opinion, 2021
Claude Dubray, Philippe Maincent, Jean Yves Milon
Although there appear to be no published studies showing that effervescence alters the metabolism of paracetamol, effervescent paracetamol formulations do offer a number of potential biopharmaceutical and pharmacokinetic advantages over conventional formulations. Effervescence accelerates the disintegration of tablets, increases paracetamol dissolution, and renders the drug more hydrophilic;18 in addition, effervescence increases gastric pH, thereby reducing drug contact time with the gastric mucosa and protecting the active drug from inactivation in the stomach19,20. Together, these properties result in a faster onset of action. However, the need to achieve rapid analgesia should be weighed against the need to facilitate appropriate use of the drug, avoiding the risk of overdose.
Assessment of the effect of polymers combination and effervescent component on the drug release of swellable gastro-floating tablet formulation through compartmental modeling-based approach
Published in Drug Development and Industrial Pharmacy, 2020
Syaiful Choiri, T. N. Saifullah Sulaiman, Abdul Rohman
The integrity of the system was assessed through assessing the performance of the drug release. Integrity disruption because of gas from effervescent reaction promotes burst release effect or higher rate of the drug release [19,24]. Percentage of the drug release from 2 to 7 h depicted the maintenance the integrity of the system. The IPC (CR of 58.31) was responsible to maintain the system integrity by reducing the drug release. Meanwhile, effervescent component promoted the system disruption due to porous system formed by gas from effervescent reaction [9,10]. Neither interaction of two factors nor three factors had significant effect on the tablet system integrity. Contour plot of DE2–7h (Figure 2(D)) had contrast results of the initial burst release model (DE30min) which cubic pattern was found in the contour plot. Cubic model showed high interaction because of this polynomial model. Therefore, interaction (non-linear pattern in the contour plot) was governed by the effect of polymer combination. The highest DE value was obtained at a high proportion of effervescent components (15–20%), meanwhile the lowest DE2–7h was obtained at IPC proportion ranging from 5 to 12%. Interaction of polymer maintained the drug release in controlled manner while the concentration of effervescent component increased. This indicated the efficiency of IPC in maintaining the robustness of HPMC promoted by interaction of the two polymers [31].
Optimization of the process variables of roller compaction, on the basis of granules characteristics (flow, mechanical strength, and disintegration behavior): an application of SeDeM-ODT expert system
Published in Drug Development and Industrial Pharmacy, 2019
where IEffervescence time: In the context of SeDeM-ODT expert system, the term effervescence test does not mean the typical effervescence reaction between acidic and basic moieties. Rather it has been applied for determination of dispersion time of the powder compact, prepared under maximum pressure. Effervescence time was determined as per official monograph [25]. Granules were compressed into tablets under maximum pressure without any capping and lamination. One tablet was placed in a beaker containing 200 mL of purified water, at ambient temperature and time taken by the tablet to disperse completely was taken as its effervescence time.Disintegration time with disk: Granules were compressed under maximum pressure without capping and lamination and subjected to determination of disintegration time using USP disintegration apparatus. Six tablets were randomly selected and their disintegration time with disk was determined using de-ionized water as a medium at 37 ± 2 °C [25]. Mean of six determinations (n = 6) was taken as disintegration time.Disintegration time without disk: Disintegration time was determined as described in the previous section without any disk [25].