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Effervescent tablets: a safe and practical delivery system for drug administration

Authors:
  • Koru Hospitals Ankara

Abstract

Effervescence is defined as the evolution of gas bubbles from a liquid as a result of a chemical reaction. For medicinal use, effervescent tablets have specific characteristics that allow rapid adsorption of the intended drug. In this manner, a medication can be absorbed easily and effectively if it dissolves easily in water and is present at a sufficient dose. Common acids utilized for effervescent reactions are citric, malic, tartaric, adipic and fumaric acids. Citric acid is most commonly used for this application, which also adds a citrus-like taste to the products. Tartaric, adipic and fumaric acids are usually used in small amounts, due to their low water solubility. Effervescent tablets are used to simplify the handling of doses, provide optimal compatibility, promote superior and rapid absorption, increase a patient's liquid intake and circumvent the difficulty of swallow- ing large pills. This review defines effervescent tablets in terms of the technology and describes the advantages and disadvantages.
Effervescent tablets: a safe and
practical delivery system for drug administration
Ka¤an ‹pci1, Tu¤ba Öktemer2, Leman Birdane3, Niyazi Alt›ntoprak4, Nuray Bayar Muluk5, Desiderio Passali6,
Andrey Lopatin7, Luisa Bellussi6, Ranko Mladina8, Ruby Pawankar9, Cemal Cingi10
1Department of Otorhinolaryngology, Ankara Koru Hospital, Ankara, Turkey
2Department of Otorhinolaryngology, Polatl› Can Hospital, Ankara, Turkey
3Department of Otorhinolaryngology, Yunus Emre State Hospital, Eskiflehir, Turkey
4Department of Otorhinolaryngology, Tuzla State Hospital, Istanbul, Turkey
5Department of Otorhinolaryngology, Faculty of Medicine, K›r›kkale University, K›r›kkale, Turkey
6Department for Otorhinolaryngology, Head and Neck Surgery, Siena University, Siena, Italy
7ENT Department, State Policlinic No1, Business Administration of the President of Russian Federation, Moscow, Russia
8ENT Department, University Hospital Rebro-KBC Zagreb, Zagreb, Croatia
9Division of Allergy, Nippon Medical School, Tokyo, Japan
10Department of Otorhinolaryngology, Faculty of Medicine, Eskiflehir Osmangazi University, Eskiflehir, Turkey
Medications such as pills are the forms generally used,
whereas they have some disadvantages. Slow absorption is
the important disadvantage as the onset of action gets pro-
longed. In liquid forms of the medication, the delay is avoid-
ed. Many drugs do not have enough stability levels in the
suspension form. Gastric residence also affects drug delivery
Correspondence: Ka¤an ‹pci, MD. Department of Otorhinolaryngology, Ankara Koru Hospital,
Ankara, Turkey.
e-mail: entdrkagan@gmail.com
Received: January 4, 2016; Accepted: March 22, 2016
©2016 Continuous Education and Scientific Research Association (CESRA)
Online available at:
www.entupdates.org
doi:10.2399/jmu.2016001009
QR code:
Özet: Efervesan tabletler: ‹laç kullan›m› için güvenli ve
pratik bir uygulama sistemi
Efervesans, bir s›v› içinde oluflan kimyasal reaksiyon sonucu, çözünme
ve gaz kabarc›klar›n›n oluflmas› olarak tarif edilmektedir. T›bbi kulla-
n›mda efervesan tabletler, verilen ilac›n h›zl› emilimini sa¤lamaya yöne-
lik bir özellik tafl›maktad›r. Verilen ilaç, e¤er su içinde yeterli dozda ve
kolayca çözünürse daha h›zl› ve etkin flekilde emilim sa¤lanacakt›r. Kö-
pürme reaksiyonu için genellikle sitrik, malik, tartarik, adipik veya fu-
marik asitler kullan›lmaktad›r. En s›k tercih edilen, ürüne hafif bir li-
mon aromas› da veren sitrik asittir. Tartarik, adipik ve fumarik asitler,
suda çözünürlükleri daha düflük oldu¤u için daha az miktarlarda kulla-
n›l›rlar. Uygun ilaç dozu al›m›n›n sa¤lanmas›, ilaca uyumun kolaylaflt›-
r›lmas›, h›zl› ve daha iyi emilim, hastan›n s›v› al›m›n›n art›r›lmas› ve bü-
yük tabletlerin yutulma zorlu¤unun ortadan kald›r›lmas› için efervesan
tabletler kullan›lmaktad›r. Bu derlemede, teknolojik aç›dan efervesan
tabletler de¤erlendirilmifl, avantaj ve dezavantajlar› tan›mlanm›flt›r.
Anahtar sözcükler: Efervesan, tablet, avantaj, dezavantaj.
Abstract
Effervescence is defined as the evolution of gas bubbles from a liquid as a
result of a chemical reaction. For medicinal use, effervescent tablets have
specific characteristics that allow rapid adsorption of the intended drug.
In this manner, a medication can be absorbed easily and effectively if it
dissolves easily in water and is present at a sufficient dose. Common acids
utilized for effervescent reactions are citric, malic, tartaric, adipic and
fumaric acids. Citric acid is most commonly used for this application,
which also adds a citrus-like taste to the products. Tartaric, adipic and
fumaric acids are usually used in small amounts, due to their low water
solubility. Effervescent tablets are used to simplify the handling of doses,
provide optimal compatibility, promote superior and rapid absorption,
increase a patient’s liquid intake and circumvent the difficulty of swallow-
ing large pills. This review defines effervescent tablets in terms of the
technology and describes the advantages and disadvantages.
Keywords: Effervescent, tablet, advantages, disadvantages.
Review
ENT Updates 2016;6(1):46–50
doi:10.2399/jmu.2016001009
Volume 6|Issue 1|April 2016
Effervescent tablets: a safe and practical delivery system for drug administration
47
which is predicted before. Gastro-retentive preparations are
created to manage gastric residence. Another form of the
drugs is effervescent tablets.[1] Effervescent mixtures and
powders, and compound effervescent powders including
saline cathartics are also used.[2]
In effervescent technology, gas bubbles occur from the
liquid after chemical reaction. Alkali metal bicarbonates
and acids (mainly citric or tartaric) are used to make effer-
vescence. The reaction occurs after adding water.[3–5] The
main issue is acid-base reaction. The basic component is
sodium bicarbonate and acidic component is citric acid.[5]
Effervescent tablets have specific characteristics that
allow rapid adsorption of the drug. The drug can be
absorbed easily when it displays adequate dissolution in
water and is present at a sufficient dose.[6] Potassium citrate
has these characteristics. In case of kidney stones contain-
ing urate and calcium, Potassium citrate is used which is
helpful to decrease the prevalence of the stones.[7] Patients
with kidney stones should take too much water to use
effervescent easily. Potassium citrate powders are given
with packages and the dose is measured. Therefore, a
study has been aimed to design and formulate potassium
citrate effervescent tablets. They decrease calcium oxalate
and urate stones.[8]
Definition of Effervescent Tablets
The chemical reaction occurs in effervescent tablets. It is
related to acid-base reaction. At the end, carbon dioxide is
released. Tartaric, malic, fumaric, citric and adipic acids
are utilized. Due to the citrus-like taste, citric acid is usu-
ally preferred for effervescents. Malic acid is expensive,
whereas it adds smoother taste. The low water-soluble
agents are fumaric, malic and tartaric acids. So, they can be
consumed in small amounts.[9]
In effervescent technology, when organic acid and
bicarbonate get together in the water, carbon dioxide is
released. The solving process is seen in 17–20°C water.
They may be easily carried and used. Their taste is pleas-
ing. The foam of them helps to kill the local bacteria. In
traditional Chinese Medicine, similar techniques and
materials are used to prepare similar medicine.[10]
After the reaction of effervescent tablets, simultaneous
carbon dioxide is produced. Their contents are com-
pressed mixture of acids and sodium bicarbonate.[11] They
rapidly dissolve in the water. When the patients have
problem with capsule or tablet swallowing, these agents
can be used easily.[12,13] These tablets are also absorbed
faster.[14] The main acid used is citric acid. The other acids
of adipic, tartaric, malic and fumaric are also used. Alkali
sources are Potassium carbonate and bicarbonate, and
sodium carbonate and bicarbonate. When considering low
cost, high solubility and intensity of reaction, sodium car-
bonate is preferred.[15] Excipients, water-soluble lubricants
and colors, flavorings and sweeteners are also added.[15]
Polyvinylpyrrolidone (PVP) is used as binder in effer-
vescent. Its form is as dry powder or wet forms of aqueous
or hydroalcoholic solutions. Mannitol and PEG 6000 are
other effective binders.[15,16] When using tablet press
machine, relative humidity should be low (25%) and
temperature should be at room temperature (25°C).[5] To
obtain excellent flowability, production is made by direct
compression method. Size of the particles should be equal.
In granules, particle size should be small.[13,17] To achieve
agglomeration of the particles, monohydrate citric acid is
released in the fusion method (at 54°C). Using a nonreac-
tive solution, such as ethanol or isopropanol, granulation
is achieved. 0.1–0.5% water is enough for active solu-
tion.[15] The control of effervescent tablets is performed by
conventional similar tablets. The control parameters are
weight, hardness, pH, solution time and friability.[8,15]
Potassium citrate is soluble in water, but insoluble in
alcohol.[7] It is used in metabolic acidosis and replaces sodi-
um bicarbonate. It can also be used in urinary tract infec-
tions as an alkalizing agent. It decreases the formation of
kidney stone induced by calcium oxalate and urate.[18–21]
Therefore, oral supplements with potassium citrate pre-
vent hyperkalaemia, because it can be absorbed from gas-
trointestinal tract highly.[8,21]
Effervescent tablet solution was compared with stan-
dard tablets in 242 patients. The formulations contained
1000 mg acetaminophen. The patients had moderate or
severe pain due to the dental surgery. Both of them were
evaluated in terms of pain intensity and relief. They were
both effective compared to placebo. Onset of analgesia
was 20 min in effervescent tablet and 45 min in standard
tablet. Median pain relief time was 15 min faster in the
effervescent tablet.[22]
Recently, effervescent antibiotics have been launched
on the market. Consumption of the drug as a half glass of
liquid seems easier than swallowing a large tablet.
Particularly in patients with a sore throat or swallowing
disorder, this delivery method improves the quality of life
with easier and faster uptake of the drug. Furthermore,
effervescent tablets have storage advantages for keeping
the drug dry, stable and safe compared with syrup or sus-
pension forms.
ENT Updates
‹pci K et al.
48
Effervescent Tablet Technology
The technology of the effervescent tablets was based on
chemical reaction. Acid neutralize a carbonate salt. At the
end, carbon dioxide gas is released which produce the
fizzing.[23] To initiate the reaction, water is important. If
there is no water in the medium, acid or carbonate cannot
dissociate and the reaction cannot be initiated. After the
reaction begins, more water is generated. Effervescent
tablets should be produced in optimum environment and
packaged carefully. Therefore, stability is created. During
the production, anhydrous raw materials are used. They
should be kept in dry environment. Relative humidity
ratio must be less than 10%. In effervescent tablets, the
source of carbon dioxide is carbonate. Sodium carbonate
and bicarbonate are the commonly used carbonate salts.[23]
In sodium carbonate, CO2percentage is lower than
bicarbonate. In bicarbonate, CO2proportion is higher
than soda ash. Its’ reaction time is more quickly and it is
less stable. In most of the products, both carbonate and
bicarbonate are used in 50/50 ratio. Reaction time and sta-
bility are acceptable in this form. In effervescent products,
magnesium and potassium carbonate are also used. Acids
are the other and important part in effervescent which
react with carbonates.[23] Citric acid is a trivalent and has
good neutralizing effect. Fumaric acid is a divalent and
more effective than citric acid. Fumaric acid reacts slowly
and less soluble than citric acid. Stability of the fumaric
acid is more than citric acid. The other acids are malic acid
and adipic acid.[23] The weight ratio of the acid and total
carbonate is 1:1 for ideal for effervescents. When this ratio
is 1:10, the system will be highly soluble and reactive.
Essential oils and fragrances are included as 0.5–3% in
effervescent. The oil should not contain glycol solvents
which can cause instability.[23]
Dyes or lake pigments can be added to produce colored
solutions or products. Color stability is also important.
They should be chosen as anhydrous material. Dried
flower bud, herbs, chamomile extract maybe used for this
purpose. The percentage may be lower than 1–2%.
Another 0.1–2% of the effervescent should be consisted of
vitamin E, squalene, almond oil and cosmetic esters.
Foamers are surfactants. PEG-30 castor oil, laureth 4,
polysorbate 80 or 85 are emulsifiers.[23]
Polymers are added as 0.2–4 percentage. PEG or
polyquaternium are usually used. For solid effervescent
tablets, binders are used as 10–20% (maltodextrin, lactose
and sorbitol). The materials that help flowing are calcium
silica, talc, fumed silica or cornstarch.[23] Production is
completed with exact ratios of different materials.[3]
During production, hydroscopic materials are used to
absorb moisture. Moisture may cause effervesvent reac-
tion. The production is performed in closed systems and
ended by split valve technology. To achieve high level
safety, low moisture should be present in ventilated air.[3]
Granulation and drying
The tablets are produced as equal weight and homoge-
neous. They compressed in high-speed rotary presses. Wet
granulation is avoided, because it may initiate reaction.[3]
Roller compaction and direct compression are used for dry-
ing.[2] Ventilation of the machines is also controlled.[3]
Wet granulation
The wet granulation is performed by two steps. Initial step
is done by alkaline or acid components, subsequently dry
blending is performed.[2] A high shear granulator is used
for drying.[2] These methods need running time and clean-
ing processes. This is a critical step and homogeneity of
the tablets is obtained with this method.[3]
Organic solvents
Effervescent reaction is not started in inorganic solvents.
These agents are used as a granulation fluid. In this method,
evaporation occurs at lower heat. Drying is obtained at
lower temperatures. The fluid bed is necessary because of
created organic gas and non-condensable process.[3]
Water
Water is used as a granulation fluid. It is used in very small
amount, because water may initiate pre-effervescent reac-
tion. In this reaction, carbon dioxide is released. Drying
process of the production reduces the water amount. A
high shear granulator is used for this purpose. In larger
bath sizes, the drying time takes longer.[3] For drying,
microwave technology or batches (small or medium) are
used. In larger batches, the process takes more time.[3]
Fluid bed spray granulation
In this process, simultaneous granulation and drying are per-
formed. Low moisture levels are obtained and the risk of
pre-effervescent reaction is limited to minimum. For more
granulation fluid, it is necessary to have high shear process.[3]
Lubricants
After granulation, lubricant should be added to the tablets.
To improve flowing, magnesium stearate is used. It pre-
vents tablets from sticking. When magnesium stearate is
used, a film will be present on the water after dissolving of
Volume 6|Issue 1|April 2016
Effervescent tablets: a safe and practical delivery system for drug administration
49
the tablets. L-leucine plus polyethylene glycol mixture are
also used for this purpose.[4,5]
Tablet compression
Moisture ratio is different in effervescent tablets and normal
tablets. It is <0.3% and 2%, respectively. Effervescent
tablets are commonly larger than normal tablets; and they
may be easily broken or damaged. For the packaging, these
details are very important to keep in mind. Dwell time
should be increased to solve this problem.[3]
During filling, powder pressure is obtained by rotary
valves. When lubricant is absent, the tablets can stick the
walls. Lubricants may be solid or liquid.[3] During press pro-
cedure, surface materials are forced to be pressed into the
tablets and moisture, absorbed from the air, is decreased.[3]
Blister packs and tube arrangements used
for packaging
Packing materials have a relatively stable shelf life.
Aluminum is used instead of polymer blister materials.
Because its water permeability is lower. In a package, ten
or more tablets are placed. Environment should have low
humidity, because humidity may destroy the tablets.
Drying agents such as silica gel is incorporated into the
tubes.[3]
Advantages and Disadvantages of
Effervescent Tablets
Oral forms are more preferred way of medication. In this
form, slow absorption maybe the most important disad-
vantages. When taking the liquid form, the lower dosages
can be used. Stability of active pharmaceutical ingredients
is lower in liquid form. As effervescent tablets are dis-
solved in water just before administration, it provides
advantage for the stability of these medications.[9]
Taking big tablets of capsules is difficult for the
patients. Effervescent technology provides an alternative
to them. Dissolving and break-down of standard tablets
also takes additional time in the stomach. In effervescents,
ingredients are distributed in the solution and they are not
localized in certain point.[9] They can be taken in liquids
and promotes patients to take more liquid. Absorption is
improved and usage is easy in effervescent tablets.[9]
Advantages of effervescent tablets:[3] Improved taste,
faster absorption, presentable fizzy tablets.
Disadvantages of effervescent tablets: Larger tablets,
complex production process, delicate packaging process.
Fundamentals of effervescent: There are organic
acid and alkali metal carbonate salts.[3]
Why Effervescent Tablets Are Used?
The doses can be taken easily. The ingredients (carbonate
and acid) serve as buffer for the stomach with optimum
pH. The absorption occurs at 15 min.[24] Effervescent
tablets are uncoated tablets.[6,25,26] They are susceptible to
the stomach.[25,27] They may be taken in liquid form. If
patients have swallowing difficulty, they can take these
medications easily. It is well-tolerated in the stomach.
After effervescent reaction, CO2is produced and it
increases the penetration of active substances into the
paracellar spaces.[28,29]
Lubricants are used to prevent adhesion of the tablets.
Sucrose is added as hydroscopic material and cause to
increase the tablet bulk. Aspartame and sucralose are the
other sweeteners.[1,30] Aspirin is the most commonly used
effervescent tablet.[6,31]
Effervescent tablets are used for:
Rapid and enhanced absorption: It is dissolved in
liquid and the ingredients are absorbed quickly.
Conventional tablets are dissolved slowly and absorp-
tion is reduced.[24]
Optimal compatibility: The effervescent tablet con-
tains a balanced ratio of acids and carbonates forming
a buffer. It has optimal compatibility with the stom-
ach.[24]
Increase in liquid intake: Effervescent tablets provide
both the medicinal value intended and additional liquid
intake. In diarrhea and high temperature in summer,
intake of effervescent table with water contributes to
daily liquid intake.[24]
Advantages in case of swallowing problems:
Effervescent tablets present an alternative for these
patients.[24]
Simple handling and measuring into exact doses:
Effervescent tablets are dissolved quickly and the
patients can obtain exact doses.[24]
Acknowledgement
Preparation of this paper including design and planning
was supported by Continuous Education and Scientific
Research Association (CESRA), Turkey.
Conflict of Interest: No conflicts declared.
ENT Updates
‹pci K et al.
50
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This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-
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Please cite this article as: ‹pci K, Öktemer T, Birdane L, Alt›ntoprak N, Bayar Muluk N, Passali D, Lopatin A, Bellussi L, Mladina R, Pawankar R, Cingi C.
Effervescent tablets: a safe and practical delivery system for drug administration. ENT Updates 2016;6(1):46–50.
... People who have trouble swallowing capsules or pills, especially youngsters and the elderly, are administered effervescent tablets. In comparison to normal tablets, this formulation facilitates swallowing, masks flavor, and provides quicker onset and absorption [8]. Furthermore, as compared to syrup or suspension forms, effervescent tablets offer storage benefits for keeping the medicine dry, stable, and safe. ...
... This administration strategy enhances the quality of life for people with a sore throat or a swallowing issue by allowing for simpler and quicker medication intake. Furthermore, as compared to syrup or suspension forms, effervescent tablets offer storage benefits for keeping the medicine dry, stable, and safe [8]. Because of their greater flavor, tendency to rapidly form solution and acceptance, effervescent pills of some medications, such as paracetamol, are more acceptable for children. ...
... Because of their greater flavor, tendency to rapidly form solution and acceptance, effervescent pills of some medications, such as paracetamol, are more acceptable for children. The appearance of effervescent paracetamol tablets could as well simplify ease of administration, and the utilization of appealing colors and tastes in this formulation can all help to promote paediatric compliance to the drug [8]. Furthermore, its tendency to rapidly form solution prior to oral administration has been exploited to improve the absorption of the drug compared to oral tablets. ...
Article
Full-text available
Aims: This study was aimed to determine the effect of varying parameters on the properties of effervescent paracetamol tablets for paediatrics. Study Design: This analytical study was carried out on effervescent paracetamol tablets formulated with differing formulation parameters. Place and Duration of Study: This study was carried out in the Methodology: Different formulations of effervescent paracetamol tablets were produced through wet granulation method using varied concentrations of citric acid (15, 20 and 25 %) and sodium bicarbonate (15, 20 and 25 %) as the major effervescent ingredients. The powder blends were evaluated for angle of repose, tapped and bulk density to determine its flow property. The prepared tablets were further evaluated using the unofficial test for hardness, friability and thickness as well as the official tests for weight uniformity, disintegration time, carbon dioxide (CO 2) content, water content and pH. Results: Angle of repose ranged from 23.96 ± 1.97 o-28.84 ± 0.91 o , Hausner's ratio ranged from 1.16 ± 0.02-1.25 ± 0.02 while Carr's index ranged from 14 ± 1.73-20 ± 1.15. All the granules had good flow properties while granules for F3 was the optimized formulation. Friability values were Original Research Article Agbamu et al.; JPRI, 34(27A): 52-58, 2022; Article no.JPRI.84485 53 from 0.38-0.39 %. Tablets disintegrated between 3 ± 43.06 to 5 ± 16.3 min. The effervescence time in all formulations was between 3 to 5 mins with batch F3 giving the best effervescence time. Conclusion: Granules made with Formulation F3 had the optimized flow characteristics. Effervescent paracetamol tablets containing 25% each of citric acid and sodium bicarbonate had the most desired properties as increase in both the concentration of the citric acid and sodium bicarbonate led to a decrease in the disintegration and effervescence time.
... Повышение растворимости и скорости растворения ФЗ вследствие использования метода ТД позволит создать быстрорастворимые шипучие ЛФ ФЗ, что расширит удобство и возможности применения данного соединения вследствие возможности получения раствора нужной концентрации менее, чем за 5 минут [20]. Ускорение процесса растворения ДВ достигается в результате протекания кислотноосновной реакции с выделением углекислого газа, выступающего в роли супер-разрыхлителя [21,22]. ...
... При этом шипучие ЛФ выгодно отличаются высокой стабильностью и удобством при хранении и транспортировке по сравнению с жидкими ЛФ [23]. Высокая скорость растворения ДВ, скорость и полнота проявления фармакологического эффекта, точность дозирования, микробиологическая и физико-химическая стабильность, экономическая целесообразность, а главное удобство применения обеспечивают высокую приверженность пациентов к приёму шипучих ЛФ [20,[24][25][26]. Учитывая многочисленные преимущества шипучих ЛФ, целесообразно расширение их ассортимента. ...
Article
Taking into account the current Product specification file, the aim of the work was to develop the composition and technology for obtaining effervescent tablets based on solid dispersions of furazolidone in the form of an aqueous solution for external use. Materials and methods. The used substances were: furazolidone, anhydrous sodium carbonate (chemically pure), polyvinylpyrrolidone-24000±2000 (chemically pure), malic acid (analytically pure), tartaric acid (chemically pure), citric acid (chemically pure), sodium benzoate (chemically pure), ethyl alcohol 96% (chemically pure), purified water. Preparation of granulates is separate wet granulation in a fluidized bed (Mycrolab, BOSCH, Germany). Obtaining tablets is the process of pressing on a manual hydraulic test press (“PRG”, VNIR, Russia). The dependence of disintegration, abrasion capacity and crushing resistance on compacting pressure was investigated. Technological parameters of granulates, еру obtained effervescent tablets, shelf life and storage conditions were investigated according to the State Pharmacopoeia of the Russian Federation XIV th ed. Results. Two compositions of effervescent tablets containing solid dispersions of furazolidone as an active substance were obtained, which, when dissolved in 100 ml of water at room temperature (20°C), form a solution of furazolidone with a concentration of 0.004% in less than 5 minutes. The method of quantitative determination of the furazolidone content in the effervescent tablets was validated. A complex of physicochemical methods for the analysis of tablets was carried out. Quality standards have been developed. The developed compositions stability of instant tablets during storage during accelerated and long-term tests has been experimentally confirmed. The preliminary shelf life and storage conditions have been determined. Conclusion. The result of technological and chemical-pharmaceutical research is the creation and evaluation of the quality of a new instant furazolidone dosage form as effervescent tablet formulations.
... The tablet is rapidly broken away from each other by internal liberation of carbon dioxide (CO2) in water (H2O) due to reaction between tartaric acid and citric acid with alkali metal carbonates or bicarbonates in presence of water. 1,2,3 Effervescent tablet defined as the uncoated tablet in general containing acid and carbonates or hydrogen carbonate which react quickly in the presence of water (H2O) release carbon dioxide(CO2) Or Effervescent tablets known as the evaluation of gas bubbles From a water as a result of chemical reaction 4,5 . A commonly used as acid in effervescent tablet is citric acid because of its citrous test bicarbonate is the commonly used base but potassium bicarbonate, sodium carbonate and potassium carbonate are used. ...
Research
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The oral dosage forms are the most popular way of taking medicine although having some disadvantages like deliberate absorption and thus onset of action is extend. This can be overcome by administrating the drug in a liquid form i.e. effervescent tablet. The research is a formulation of diclofenac sodium as a effervescent tablet by wet granulation method. The bitter tastes of the drug are masked by added sweetening agent (lactose, glucose etc.) In the present work we are prepared effervescent tablet in that we are used active drug diclofenac sodium and other active ingredient acid like tartaric acid and base sodium bicarbonate in different concentrations. The formulation of tablet was done by using wet granulation, wet granulation is found to be acceptable method of effervescent tablet formulation. The various pre-formulation studies were performed hardness, weight variation, disintegration, dissolution etc.
... Usually, the acid is citric acid, and the base is sodium bicarbonate or sodium carbonate [64]. While several other acids can be used in place of citric acid, such as malic, fumaric, tartaric, and adipic acids, citric acid is most widely used in effervescence formulations because it imparts a pleasant citrus-type flavor and acts as a flavor enhancer [65]. Effervescent tablets or powders in the presence of water or another liquid, such as saliva, release gas as carbon dioxide (CO 2 ) and can be used to produce carbonated liquid drinks. ...
Article
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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.
... The tablet is rapidly broken away from each other by internal liberation of carbon dioxide (CO2) in water (H2O) due to reaction between tartaric acid and citric acid with alkali metal carbonates or bicarbonates in presence of water. 1,2,3 Effervescent tablet defined as the uncoated tablet in general containing acid and carbonates or hydrogen carbonate which react quickly in the presence of water (H2O) release carbon dioxide(CO2) Or Effervescent tablets known as the evaluation of gas bubbles From a water as a result of chemical reaction 4,5 . A commonly used as acid in effervescent tablet is citric acid because of its citrous test bicarbonate is the commonly used base but potassium bicarbonate, sodium carbonate and potassium carbonate are used. ...
Article
Full-text available
The oral dosage forms are the most popular way of taking medicine although having some disadvantages like deliberate absorption and thus onset of action is extend. This can be overcome by administrating the drug in a liquid form i.e. effervescent tablet. The research is a formulation of diclofenac sodium as a effervescent tablet by wet granulation method. The bitter taste of the drug are masked by added sweetening agent (lactose, glucose etc.) In the present work we are prepared effervescent tablet in that we are used active drug diclofenac sodium and other active ingredient acid like tartaric acid and base sodium bicarbonate in different concentrations. The formulation of tablet was done by using wet granulation, wet granulation is found to be acceptable method of effervescent tablet formulation. The various pre-formulation studies was performed hardness, weight variation, disintegration, dissolution etc.
... Some geriatric patients have difficulty in swallowing solid forms such as tablets and capsules. Solid dosage forms of such preparations may be formulated as granules in sachets to be reconstituted into solution for their use when required [11]. Under proper storage conditions, it is expected that the granular dosage form will have an improved shelf life and longer lasting effect of the active ingredients. ...
Article
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Herbal medicines are currently being adopted as alternatives to orthodox medicines for the management of drug-resistant and emerging multidrug-resistant microbial strains of various diseases, including typhoid fever. A herbal decoction, MA 001, manufactured by the Centre for Plant Medicine Research (CPMR), has been used for the treatment of typhoid fever for at least two decades in Ghana with desirable outcomes. MA 001 is formulated from Citrus aurantifolia, Spondias mombin, Latana camara, Bidens pilosa, Trema occidentalis, Psidium guajava, Morinda lucida, Vernonia amygdalina, Persea americana, Paulina pinnatta, Momordia charantia and Cnestis ferruguinea medicinal plants. The low palatability and compliance to treatment due to the bulky nature of the decoction poses challenges in its optimum use. This study sought to design and formulate the therapeutic components of the aqueous herbal decoction of MA 001 into an optimal solid dosage form of effervescent granules to improve the delivery of MA 001 as well as increase patient compliance and convenience of product handling. The methods involved pre-formulation studies on the suitability of effervescent vehicles, formulation and evaluation of effervescent granules for drug excipient interactions using high performance liquid chromatography analysis. The findings indicate that the effervescent granules were suitable for use in the delivery of the therapeutic constituents for the treatment of typhoid fever as done with the decoction due to minimal herbal extract-excipient interaction.
... The oral dosage forms are the most popular method of drug administration, in spite of some disadvantages, like slow absorption, and thus the onset of action is time consuming. This can be overcome by administrating the drug in liquid form, but many active pharmaceutical ingredients have limited level of stability in liquid form [1]. Hence, effervescent granules are formulated to reduce these effects which are intended to be dissolved or dispersed in water before use. ...
Article
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Background: Many patients like elderly people, pediatric and persons with dysphagia find difficulty swallowing the tablets and thus do not comply with prescriptions. Objective of this study was to prepare salbutamol sulfate and evaluate as effervescent granules in-vitro using superdisintegrant agent (Explotab) and traditional one (Avecil) for comparison study. Methods: Three formulations (F1-F3) of effervescent Salbutamol Sulfate granules were formulated by the wet granulation method. Avecil, Explotab, Polyvinylpyrrolidone and other ingredients used in the formulation of effervescent granules. Evaluation tests were carried out for all three formulations include (particle size distribution, Flowability, effervescent time and percentage of drug release in 5 minutes). Results: Formula that contain Avecil (F3) has better flow properties (angle of repose, carr's index and hausner's ratio) than other formula. The formula that contain Explotab (F2) has more effervescent time than others while the formula without disintegrant (F1) had more amount of drug dissolved than others. Conclusion: Salbutamol sulfate was successfully prepared as effervescent granules to improve patient compliance. ‫تأثير‬ ‫دراسة‬ ‫المفككة‬ ‫المواد‬ ‫انواع‬ ‫على‬ ‫ال‬ ‫تحضير‬ ‫ال‬ ‫و‬ ‫تقييم‬ ‫الجسم‬ ‫خارج‬ ‫لل‬ ‫سالبيو‬ ‫تامول‬ ‫بشكل‬ ‫فوارة‬ ‫حبيبات‬ ‫إبراهيم‬ ‫أحمد‬ ‫محمد‬ ، ‫علوان‬ ‫سالم‬ ‫زهراء‬ ‫الخالصة‬ ‫الهدف‬ : ‫الدوائية‬ ‫الجرع‬ ‫أشكال‬ ‫صياغة‬ ‫في‬ ‫مهمة‬ ‫المريض‬ ‫وامتثال‬ ‫الدواء‬ ‫اخذ‬ ‫سهولة‬ ‫ان‬ , ‫السن‬ ‫كبار‬ ‫مثل‬ ‫المرضى‬ ‫من‬ ‫العديد‬ ‫كان‬ ‫الطبية.‬ ‫للوصفات‬ ‫يمتثلون‬ ‫ال‬ ‫وبالتالي‬ ‫أالقراص‬ ‫ابتالع‬ ‫في‬ ‫صعوبة‬ ‫يجدون‬ ‫البلع‬ ‫عسر‬ ‫من‬ ‫يعاني‬ ‫الذي‬ ‫والشخص‬ ‫واألطفال‬ ‫المريض‬ ‫امتثال‬ ‫لتحسين‬ ‫فوارة‬ ‫كحبيبات‬ ‫سلفيت‬ ‫السالبوتامول‬ ‫هواعداد‬ ‫الدراسة‬ ‫هذه‬ ‫من‬ ‫الهدف‬ ‫للدواء‬. ‫الطريق‬ ‫ة‬ : ‫الت‬ ‫بطريقة‬ ‫حضرت‬ ‫الفوارة‬ ‫سلفيت‬ ‫السالبيوتامول‬ ‫حبيبات‬ ‫من‬ ‫صيغ‬ ‫ثالثة‬ ‫ح‬ ‫باستخد‬ ‫وذلك‬ ‫الرطب‬ ‫بيب‬ ‫االفسيل‬ ‫ام‬ , , ‫االكسبلوتاب‬ ‫بايروليدون‬ ‫فنيل‬ ‫بولي‬ ‫تتضمن‬ ‫الثالثة‬ ‫الصيغ‬ ‫لجميع‬ ‫اجريت‬ ‫التي‬ ‫التقييم‬ ‫دراسة‬ ‫وان‬ ‫المكونات‬ ‫من‬ ‫وغيرها‬ ‫(توزيع‬ ‫الجسيمات‬ ‫حجم‬ ‫و‬ ‫التدفق‬ ‫قابلية‬. ‫دقائق)‬ ‫خمسة‬ ‫في‬ ‫الدواء‬ ‫النطالق‬ ‫المئوية‬ ‫والنسبة‬ ‫الحبيبات‬ ‫فوران‬ ‫ووقت‬
... 95 The use of effervescent granules to be applied to the scalp was tested as a strategy to improve the permeation of minoxidil sulfate. 96 This formulation, when deposited on the skin and moistened, triggers the formation of bubbles resulting from the reaction between an organic acid and an alkali salt, 96,97 increasing the mobility in situ of the minoxidil particles and leading to an accumulation of the product in the cutaneous appendages. 96 In fact, the effervescent formulation demonstrated a 2.7-fold increase drug accumulation into hair follicles after 6 h of treatment compared to the control in permeation studies using porcine skin. ...
Article
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Camila O Cardoso,1 Seila Tolentino,1 Tais Gratieri,1 Marcilio Cunha-Filho,1 Renata FV Lopez,2 Guilherme M Gelfuso1 1Laboratory of Food, Drugs, and Cosmetics (LTMAC), University of Brasilia, Brasília, 70910-900, DF, Brazil; 2School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, 14040-903, SP, BrazilCorrespondence: Guilherme M GelfusoUniversity of Brasília, Department of Pharmacy, Campus Universitário Darcy Ribeiro, Brasília, 70910-900, DF, BrazilTel +55 61 3107-1990Email gmgelfuso@unb.brAbstract: Alopecia is a clinical condition related to hair loss that can significantly affect both male and female adults’ quality of life. Despite the high market demand, only few drugs are currently approved for alopecia treatment. Topical formulations still bring drawbacks, such as scalp irritation with frequent use, and low drug absorption to the site of action, which limits the efficacy. The most recent research points out that different formulation technology could circumvent the aforementioned flaws. Such technology includes incorporation of drugs in rigid or deformable nanoparticles, strategies involving physical, energetical and mechanical techniques, such as iontophoresis, sonophoresis, microneedling, and the use of solid effervescent granules to be hydrated at the moment of application in the scalp. In this paper, the progress of current research on topical formulations dedicated to the treatment of alopecia is reviewed and discussed.Keywords: alopecia, drug delivery, hair follicle, iontophoresis, nanoparticles, topical treatment
Article
Near-infrared (NIR) and Raman spectroscopy are analytical methods which are used increasingly for qualitative and quantitative at- or in-line measurements in the pharmaceutical industry. With the published quality guidelines of the Food and Drug Administration (FDA), these technologies are becoming popular, especially for ensuring high product quality and process monitoring. After a development of multivariate methods in this study, the best models were selected based on various quality parameters and the applicability of these in the routine process was presented. Calcination is a partial conversion to sodium carbonate, which increases compressibility and stability of effervescent tablets. Fluid bed granulation and drying oven processing were available as calcination technologies in this study. To determine the decomposition level spectroscopically, an analytical method was required. For this purpose, two standard methods (hydrochloric acid titration and a thermogravimetric analysis method) were compared. Thermogravimetric analysis was chosen due to a better determination of separately weighed binary mixtures of sodium hydrogen carbonate and sodium carbonate. Changes of water content, powder density and particle size showed influences on spectra and chemometric models. This impact was consistently avoided or reduced by reproducible sample handling and by using pre-processing operations. With a well understood standard method available, the main part of this study deals with diverse model developments of NIR and Raman data. The Raman technology was found to be superior to the NIR to determine the decomposition level of sodium hydrogen carbonate. The NIR demonstrated a low robustness and routine capability, higher number of factors, and poorer Root Mean Square Errors.
Research
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Investigating the percentage purities of the 0.100 g aspirin tablets of the brands of Bayer, Ecotrin, Equate, GenCare and Tesco in terms of the mass of the acetylsalicylic acid (pure aspirin), which is found by performing a back titration with them, 1.00 mol dm-3 sodium hydroxide and 1.00 mol dm-3 hydrochloric acid, present in the total mass of them (impure aspirin)
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Background: Amoxicillin is a semisynthetic antibiotic, which is used as an antimicrobial drug. This study was designed to formulate amoxicillin effervescent tablets, aimed at improved patient compliance and increased drug stability. Materials and Methods: In this study, nine effervescent tablet formulations were prepared from amoxicillin trihydrate. The effervescent base was comprised of various amounts of citric acid and sodium bicarbonate. Powders and granules were evaluated for their particle size, bulk density, tapped density, compressibility index, Hausner's ratio and angle of repose. The effervescent tablets were then prepared from powders and granules of acceptable quality by direct compression and fusion methods. The tablets were evaluated for weight variation, friability, pH of solution, carbon dioxide (CO2) content, hardness, effervescence time, thickness, assay, content uniformity, water content and equilibrium moisture content. Results: The results indicated better flowability of granules prepared by fusion method as compared with the direct compression. The percent weight variations of tablets were within the acceptable limit of 0.5%. The friability was less than 1% in all formulations. The solution pH of tablets prepared by direct compression and fusion methods ranged from 4.55 to 5.74 and 4.74-5.84, respectively. The CO2 amounts generated by of fusion method tablets were smaller as compared to the direct compression method. The hardness of tablets was 40.66-56 for direct compression method and 60.6-74.6 for fusion method. The tablets produced by the fusion method had a larger thickness and lower water content than tablets produced by direct compression method. Conclusion: Tablets prepared by the fusion method exhibited superior pre- and post-compression characteristics as compared to tablets prepared by direct compression method.
Article
Effervescent tablets are an interesting pharmaceutical dosage form, offering some unique advantages when compared with simple tablets. However, the manufacturing process involves some critical steps that need to be addressed carefully during formulation and factory design.
Article
In the present study, the design of an oral effervescent tablet of diclofenac potassium was carried out. Six different formulations were prepared using different diluents, carbonates by wet granulation and direct compression method. The prepared tablets were evaluated for various pre compression characteristics (like angle of repose, bulk density, tapped density, cars index and hausner's ratio) and post compression characteristics (like weight variation, hardness friability ,drug content, disintegration, CO 2 content, effervescent time, particle size and in vitro dissolution studies). The dissolution test was carried out in SIF without enzymes, 0.1N HCl and pH 4.8 acetate buffer. Among all the formulations, its F3 formulations were better in all the terms of precompression and post compression parameters. In F3 formulations, F3A (by direct compression) and F3B (by wet granulation method) were there. F3B (composed of active dextrates (Emdex), citricacid, tartaric acid, effersoda and arginine) had given good pre formulation and post compression studies as F3A. Even the drug release in the medium SIF pH6.8 without enzymes was 99.2% when compared to F3A (98.7%) and marketed tablet (98%).It had all the qualities of a good effervescent tablet, based on this F3B formulation was selected as the best formulation, and it was charged for stability studies. It had given better release profile in all the mediums when compared to marketed conventional tablet (SUPANAC). A better therapeutic objective can be obtained by formulating effervescent tablet of diclofenac potassium that may help in obviating the demerits of slow release and slow absorption, gastrointestinal side effects of normal tablets.
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Editorial Reviews Product Description Now complete in 17 volumes, the Encyclopedia of Pharmaceutical Technology presents authoritative and contemporary articles on all aspects of drug development, dosage forms, manufacturing, and regulation;enabling the specialist and novice alike to keep abreast of developments in this rapidly evolving and highly competitive field. A dependable reference tool and a solid investment for years to come--maintaining currency through its supplements (Volume 18/Supplement 1 due to be published in the Fall, 1998)! The Encyclopedia contains interdisciplinary contributions in a wide array of subjects, including Drugs decomposition metabolism pharmaceutical incompatibilities pharmacokinetics physicochemical properties preformulation stability Drug Delivery Systems and Devices;Development and Manufacture analysis and controls bioavailability use of computerization formulation and processing alternatives national and international registration packaging patents process validation scale-up safety and efficacy stability standards Post-Production and Practical Considerations governmental/industrial/professional organizations legal aspects national and international agencies patent life of drugs patient compliance …and much, much more! Special Discount Offer New Subscribers ... save $415.00 off the subscription price of $3315.00! Purchase the entire 17-volume set for $2900.00 (only $171.00 per volume) offer expires 3/31/98 Missing volumes? For a limited time, complete your set at the special price of $171.00 per volume. offer expires 3/31/98 --This text refers to an alternate Hardcover edition.
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Purpose: The aim of this study was to design and formulation of potassium citrate effervescent tablet for reduction of calcium oxalate and urate kidney stones in patients suffering from kidney stones. Methods: In this study, 13 formulations were prepared from potassium citrate and effervescent base in different concentration. The flowability of powders and granules was studied. Then effervescent tablets were prepared by direct compression, fusion and wet granulation methods. The prepared tablets were evaluated for hardness, friability, effervescent time, pH, content uniformity. To amend taste of formulations, different flavoring agents were used and then panel test was done by using Latin Square method by 30 volunteers. Results: Formulations obtained from direct compression and fusion methods had good flow but low hardness. Wet granulation improves flowability and other physicochemical properties such as acceptable hardness, effervescence time ≤3 minutes, pH<6, friability < 1%, water percentage < 0.5% and accurate content uniformity. In panel test, both of combination flavors; (orange - lemon) and (strawberry - raspberry) had good acceptability. Conclusion: The prepared tablets by wet granulation method using PVP solution had more tablet hardness. It is a reproducible process and suitable to produce granules that are compressed into effervescent tablets due to larger agglomerates.
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Abstract The equilibrium moisture content (EMC) was determined for thirty pharmaceutical excipients. These data are to be included in the forth-coming publication of the Handbook of Pharmaceutical Excipients. This work was undertaken as a collaborative effort under the sponsorship of the Academy of Pharmaceutical Sciences. The results of this study are being reported herein prior to publication of the Handbook. The experimental procedure for determining equilibrium moisture content is included along with a method for classifying the hygroscopic property of solids.
Article
The aim of this work was to benefit from the advantageous technique of tablet manufacture by direct compression for the easy preparation of stable effervescent tablets. In order to overcome the bad flowability and low compressibility of sodium bicarbonate, a common carbon dioxide source in effervescent tablet formulation, a spray-drying technique was applied. The adjustment to achieve different conditions when operating the spray-dryer was described. Some additives such as polyvinylpyrrolidone and silicon oil were found to be essential to obtain direct compressible spray-dried sodium bicarbonate. The prepared spray-dried sodium bicarbonate showed good compression characteristics and excellent compressibility without being transformed into sodium carbonate.