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

April 2016
ENT Updates

DOI:10.2399/jmu.2016001009

Authors:

Kagan Ipci

Koru Hospitals Ankara

Leman Birdane

Niyazi Altıntoprak

Maltepe University

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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.

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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

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

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.

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

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.

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NC-ND3.0) Licence (http://creativecommons.org/licenses/by-nc-nd/3.0/) which permits unrestricted noncommercial use, distribution, and reproduc-

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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.

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Full-text available

Aug 2023

Introduction: Red beetroots (Beta vulgaris L.) are a natural ingredient rich in nutrients and provide various notable health benefits. In dentistry, red beetroots have the potential to act as a plaque-disclosing agent. Previous studies showed that red beetroot preparation in gelform is more effective compared to chewable tablets, but has significant drawbacks in taste. Effervescent granules have the potential to conceal the unpleasant taste of beetroot substances. This study aims to determine the ideal formula and evaluate the physical properties and stability of effervescent granules made from red beetroot extract. Methods: This was an experimental design study with descriptive analysis. The maceration method was used to extract the red beetroot constituents. Fresh fruits were collected, air-dried, and macerated with 96% ethanol twice. The filtrates were then concentrated. The wet granulation method was used to formulate effervescent granules. The samples were grouped into formula 1 (F1), formula 2 (F2), and formula 3 (F3) using 1%, 3%, and 4% red beetroot extract, respectively. All sample groups were analyzed for physical stability, namely: organoleptic, flowability, density, dissolving time, and pH tests. Results: All samples surpassed the sensory evaluation for physical properties. Formula 1 (1%) and formula 2 (3%) models passed all the physical stability tests. Meanwhile, the 4% formula (F3) failed two physical tests. F1 (1%) samples also showed lighter brown color for its lower beetroot extract concentration, indicating under-qualification as dental plaque staining materials. Therefore, 3% concentration (F2) has the best formulation regarding physical properties and stability. Conclusion: Formulas F1 and F2 have the best physical properties and stability by passing all the tests, while Formula 3 failed the organoleptic and flow rate tests.KEYWORDSformulation, physical stability, Beta vulgaris L, effervescent granules

ARTIKEL REVIEW : FORMULASI DAN EVALUASI SEDIAAN EFERVESEN HERBAL SEBAGAI ANTIOKSIDAN

Article

May 2021

Besarnya pengaruh radikal bebas terhadap kesehatan manusia membuat masyarakat saat ini banyak mengkonsumsi buah dan sayur serta bahan alam lain tinggi antioksidan. Untuk mendapat dan mengefisiensikan manfaat antioksidan dari herbal dibutuhkan adanya suatu teknologi yang tepat salah satunya dibuat dalam sediaan efervesen. Sediaan efervesen memiliki beberapa keunggulan yaitu memiliki rasa yang enak, mudah dikonsumsi dan diabsorbsi cepat oleh tubuh. Review ini akan memberikan informasi mengenai formulasi dan evaluasi sediaan efervesen dari berbagai herbal sebagai antioksidan. Pencarian jurnal dilakukan secara online melalui situs pencarian jurnal yang terakreditasi. Sebanyak 17 jurnal dari 121 jurnal pencarian awal memenuhi kriteria inklusi. Kombinasi asam sitrat dan asam tartrat serta natrium bikarbonat dengan metode granulasi basah menjadi formulasi yang paling banyak digunakan. Evaluasi waktu larut, pH, dan kadar air sediaan menjadi indikator kualitas sediaan efervesen. Metode DPPH menjadi pilihan yang paling banyak digunakan untuk menguji aktivitas antioksidan dalams sediaan. Sediaan efervesen dapat menjadi bentuk penghantar antioksidan dari berbagai herbal.

Pharmacokinetic profile of novel multi-layer stable effervescent tablet: a cross-over study with an established European brand in healthy young male adults

Article

Full-text available

Nov 2024

Effervescent formulation helps in faster and better absorption of drugs, especially those that are rapidly soluble in water. However, these tablets require special packaging in order to prevent them from absorbing moisture, hence increasing cost. We compared an effervescent tablet prepared using an in-house developed method (multi-layer tablet with acid and base part separated by an inert layer) to a European effervescent tablet (Efferalgan®) in a single-center, randomized cross-over study among twelve healthy volunteers. Blood samples were collected for 8 h and analyzed for paracetamol concentration using HPLC. Our results showed that both the products have similar pharmacokinetic profiles with no significant difference observed for Clast, Thalf, Kelim, and MRT (p-value > 0.05). Moreover, to assess bioequivalence we did not find any significant difference (p-value > 0.05) in AUC (27.12 ± 6.02 vs. 27.29 ± 2.64 µg.h/ml), Cmax (7.42 ± 1.06 vs. 7.83 ± 1.19 µg/ml) and tmax (0.85 ± 0.22 vs. 0.83 ± 0.25 h). The TR ratios for AUC, Cmax, and tmax were 0.99, 0.95, and 1.02 respectively, and were all within the specified FDA limits i.e., 0.8–1.25. We found our test tablet to be bioequivalent to that of Efferalgan®. Graphical Abstract

Strategies for Formulation of Effervescent Granules of an Herbal Product for the Management of Typhoid Fever

Article

Jan 2021

Limon Kabuğu Tozundan Efervesan Tablet Yapımı Sürecinde Fiziksel, Kimyasal Değişikliklerin Ve Antimikrobiyal Etkinin Araştırılması

Article

Aug 2024

Serpil Korkmaz

Turunçgillerin kabuğu genellikle kalın ve lifli yapıdadır. Bu özellik, meyveleri koruyarak uzun süre taze kalmasını sağlar. Ayrıca biyoaktif bileşen bakımından meyve içeriğine göre daha zengin olması nedeniyle değerlendirilmesine yönelik çalışmalar artmıştır. Bitkisel kökenli gıda takviyeleri daha çok tercih edilmekte olup; özellikle suda çözünür efervesan tabletlerin, yutma güçlüğünü ortadan kaldırması ve hızlı emilim gibi avantajları bilinmektedir. Bundan dolayı limon kabukları uygun koşullarda kurutulup efervesan tablet haline getirilerek yapısındaki faydalı etken maddelerden daha verimli bir şekilde yararlanmak hedeflenmiştir. Sitrik asit ve NaHCO3 bazının nötrleşmesi efervesan tabletin prensibini oluşturmaktadır. Bu bileşenler önce kübik sonra V karıştırıcıda karıştırılıp homojenize edilmiş; ısıl işlemle de partiküllerin kaynaşması sağlanmıştır. Limon kabukları, 50°C’de etüvde kurutularak toz haline getirilip, standart boyut büyüklüğü için eleme işlemi yapılmıştır. Limon kabuğu tozu da eklenen içerik manuel tablet basma makinasında el yordamıyla preslenip tablet eldesi gerçekleşmiştir. Limon kabuğunun efervesan tablete dönüşümü sırasında içerik ve etki değişiminin yararlanılabilir olduğunu kanıtlamak için analizler yapılmıştır. Fenolik madde, Askorbik asit, mineral madde miktar analizi ve antioksidan özellik tayini kimyasal analizleri; renk ve pH değişimi fiziksel analizleri yanı sıra limon kabuğu tozu ve tablet içeriklerinin antibakteriyel ve antifungal özellikleri araştırılmıştır. Bunun için disk difüzyon yöntemi kullanılmış ve Müller-Hinton besiyerinde enfeksiyon etkeni bakteri türleri ve C. albicans mantarı için inhibe edici etkileri ölçülüp; antibiyotik diskleri ile karşılaştırılmıştır. Tüm test mikroorganizmaları üzerinde üremeyi durdurucu etki tespit edilmiştir. Köpürme testi efervesan tablet standardında; pH değerinde azalma, renk analizinde b* değeri dışında artış, fenolik bileşiklerde artış diğer kimyasal içeriklerde kabul edilebilir ölçüde azalma olduğu tespit edilmiştir. Tüm analiz sonuçları limon kabuğu tozunun efervesan tablet formunda bir gıda takviyesi şeklinde değerlendirilebileceği fikrini desteklemiştir. Anahtar Sözcükler: Limon kabuğu tozu, efervesan tablet, biyoaktif bileşen, gıda takviyesi.

Pharmaceutical technologies and applications over additive manufacturing

Chapter

Jan 2024

Do effervescent vitamin tablets affect the surface roughness, microhardness, and color of human enamel and contemporary composite resins?

Article

May 2024

Purpose To compare the impact of four effervescent vitamin tablets on the surface roughness, microhardness, and color of human enamel and contemporary composite resins. Material and Methods Sixty enamel and a total of 240 anterior (Gradia Direct Anterior), posterior (Gradia Direct Posterior), and universal composite resin (Filtek Ultimate) specimens ( n = 60 per group) were fabricated. Each group was subdivided into five subgroups ( n = 12, per subgroup). The specimens were subsequently immersed in YOUPLUS, Redoxon, Sunlife Immuvit, and Sambucol effervescent vitamin solutions for 2 min per day over 30 days. Distilled water was used as control. Subsequently, surface roughness (Ra) was detected using a profilometer, and microhardness (VHN) was measured using a microhardness tester. A spectrophotometer device was used to record the L,a,b color coordinates of the specimens after 24 h, 7 days, and 30 days, and the color changes (Δ E 00 ) of the groups were calculated. The data were analyzed by ANOVA, two‐way ANOVA, Kruskal‐Wallis, Levene's, and Fisher's least significant difference (LSD) tests ( p < 0.05). SEM analysis was conducted on one randomly selected specimen per group (×1000). Results In terms of surface roughness, material X vitamin interactions were found significant ( p < 0.05). The increase in Ra from 24 h to 30 days was found significant ( p < 0.05) except for Gradia Direct Anterior X Redoxon, Sunlife Immuvit and Sambucol, Filtek Ultimate X Sunlife Immuvit and Sambucol, and all control groups. Ra changes were also concluded by SEM. Regarding VHNs, material X vitamin interactions were significant ( p < 0.005), except for all Filtek Ultimate subgroups. The changes in VHNs of the groups from 24 h to 30 days were significant for all enamel and Gradia Direct Anterior X YOUPLUS, Gradia Posterior X YOUPLUS, Sunlife Immuvit, and Sambucol groups ( p < 0.05). In terms of Δ E 00 , significant differences were observed between the 7 days and 30 days in the enamel ( p = 0.047), Gradia Direct Anterior ( p = 0.019), and Gradia Direct Posterior groups ( p = 0.038). Conclusions Daily consumption of effervescent vitamin tablets can increase surface roughness, decrease microhardness, and influence the color of human enamel and contemporary anterior, posterior, and universal composite resins after a 30‐day period.

Preparation and evaluation of a functional effervescent powder based on inclusion complexes of orange oil and β -cyclodextrin derivatives

Article

Jul 2023

Design, formulation, optimization and stability studies of paracetamol effervescent tablets

Article

Full-text available

Jan 2023
PAK J PHARM SCI

The purpose of the current study was to develop stable effervescent-tablets without controlling area relative-humidity; temperature and no requirement of special packaging. Current 3 2 factorial-design experimental studies were conducted in the Research Laboratory of Pharmaceutics, Hamdard University. Duration of study is from December-2021 to November-2022. Various paracetamol based effervescent formulations (F1-F9) were prepared with different molar-ratio of citric-acid anhydrous and sodium-bicarbonate as independent variables. Design-Expert ® software was used to graphically express the influence of each factor. By novel approach; tablets were compressed at ambient temperature and relative-humidity; acid components were kept on one-side and basic ingredients on another side; both sides were separated by an inert-layer. Tablets were kept at accelerated humidity and temperature in normal packing for six months; after six months, F6 formulation was found acceptable based on effervescence-time (120 sec), pH-value (5.5) and other quality criterion. Parameters of assay, effervescence-time, pH-value and carbon-dioxide content were found within the set-limit. Hence; novel approach for developing effervescent formulation by separating acid components at one-side and basic ingredients on another side of tablet through inert-layer is workable under room temperature and humidity. It is expected that commercial production of tablets by this technique may reduce cost of effervescent products and no requirement for special packaging.

Formulation, Characterization and Physicochemical Evaluation of Ranitidine Effervescent Tablets

Article

Full-text available

Dec 2013

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.

Formulation, Characterization and Physicochemical Evaluation of Potassium Citrate Effervescent Tablets

Article

Full-text available

Dec 2013

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.

Effervescent: Dosage manufacturing

Article

Apr 2003

H. Stahl

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.

AHFS drug information

Article

Jan 2004

Effervescent tablets

Article

Jan 1989

R. Mohrle

The Theory and Practice of Industrial Pharmacy

Article

Jan 1976

Formulation and evaluation of diclofenac potassium effervescent tablets

Article

Jan 2011

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.

Encyclopedia of Pharmaceutical Technology

Article

Nov 1999

James Swarbrick

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

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Equilibrium Moisture Content of Pharmaceutical Excipients

Article

Oct 2008

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.

Preparation of direct compressible effervescent components: spray-dried sodium bicarbonate

Article

Jul 1988
INT J PHARMACEUT

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.