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gaining more patients compliance, attractive, easy to pH of the solution was within the range of 5.65 to
use in known measured doses convenient to the users 5.85. Dissolution profile comparison with the
S. B. Shirsand Et. Al 2010 Fast disintegrating conventional formulation was carried out and
tablets of lorazepam were prepared by effervescent maximum drug release by the trial formulation was
method with a view to enhance patient compliance. A observed within 15min. spectrophotometric
3² full factorial design was applied to investigate the determination of drug content was found to be 99.82
combined effect of two formulation variables: ± 1.754. Stability characterization was also conducted
amount of crospovidone and mixture of sodium on the formulations under stress (40 °C/75 % R.H.)
bicarbonate, citric acid and tartaric acid (effervescent that showed formulations remained stable throughout
material) on in vitro dispersion time. Crospovidone the study duration with acceptable difference in
(2-8% w/w) was used as superdisintigrant and physical and chemical characteristics. Such
mixture of sodium bicarbonate, citric acid and tartaric formulations increases patient compliance and have
acid (6-18% w/w) was used as effervescent material, possibly improved bioavailability. The work also
along with directly compressible Mannitol to enhance emphasizes on the benefit of using direct
mouth feel. The tablets were evaluated for hardness, compression method as a cost effective technique in
friability, thickness, drug content uniformity and in terms of process, materials handling with
vitro dispersion time. Based on in vitro dispersion productivity
time (approximately 13 s); the formulation containing Basawaraj S.Patil et. al 2011 Granisetron
8% w/w crospovidone and 18% w/w mixture of hydrochloride is a selective 5-HT3 receptor
sodium bicarbonate, citric acid and tartaric acid was antagonist, which may have beneficial therapeutic
found to be promising and tested for in vitro drug effects in the treatment of vomiting and nausea
release pattern (in pH 6.8 phosphate buffer), short- resulting from cancer therapy. In the present work
term stability and drug-excipient interaction. Surface attempts were made to prepare fast dissolving tablets
response plots are presented to graphically represent (FDT) of Granisetron hydrochloride by effervescent
the effect of independent variables (concentrations of technique with a view to enhance patient compliance.
crospovidone and effervescent material) on the in sodium starch glycolate used as super disintegrant
vitro dispersion time. The validity of the generated along with sodium bicarbonate, anhydrous citric acid
mathematical model was tested by preparing two and tartaric acid in different ratios(as effervescent
extra-design check point formulations. The optimized material) were used. The prepared formulations were
tablet formulation was compared with conventional evaluated for pre-compressional and post-
marketed tablet for drug release profiles. This compressional parameters. The compatibility of drug
formulation showed nearly eleven-fold faster drug with other ingredients was checked by FTIR studies,
release (t50% 2.8 min) compared to the conventional these results revealed that there was no interaction
commercial tablet formulation (t50% >30 min). between dug and other excipients. The values of
Short-term stability studies on the formulation precompressional parameters were within prescribed
indicated that there were no significant changes in limits and indicated good free flowing properties. In
drug content and in vitro dispersion time (P<0.05). all the formulations the hardness test indicates good
M. Harris shoaib et. Al 2011 Effervescent tablets mechanical strength. Friability of all formulations
have always been convenient, simple and measured was less than1. Drug content was found to be high (≥
dosage form. They enhance the bioavailability of the 100.10%) and uniform in all the formulations. The
drug and the addition of flavorant also masks the tablet thickness was found to be 3.08 to 3.25 mm.
objectionable taste of the medicament in a more The weight variation results revealed that average
patient compliant way. The present study focuses on percentage deviation was less then ± 7.5%, which
developing a new, simple, cost effective formulation provides good uniformity in all formulations. The
of naproxen sodium 250 mg as an effervescent tablet disintegration time of the tablets decreased
using direct compression technique. Nine different significantly with increase in the concentration of
trial formulations of naproxen 250 mg were assigned effervescent agents. The formulations GE4, GE8 and
with varying proportions o sodium carbonate, sodium GE12 50 % of drug released in 3.15, 2.11, 2.61 min,
bicarbonate, citric acid and PEG 6000 and were and 90 % of drug released in 7.23, 7.25, 6.25 min.
prepared by direct compression method, and Stability study carried out as per ICH guidelines for
evaluated for pharmaceutical quality attributes. three months and results revealed that upon storage
Quality assessment proved formulations F8 as a disintegration time of tablets decreased significantly
satisfactory one showing respectively mean weight of (p<0.05).The release of drug from the GE12
2200 ± 50.52 having hardness and friability formulation was quick when compared to other
of14.78421 ± 1.3791 kg and 1.241 %. Tablets took 4 formulation
min and 36 s to disintegrate completely. The average
Sagar A Adichwal, et. al 2012 The purpose of this Ibuprofen inhibit prostaglandin (PG) synthesis in
research was to develop a novel gastroretentive drug peripheral tissue so in this study Paracetamol and
delivery system based on effervescent technology for Ibuprofen combination used for analgesic, anti-
controlled delivery of active agent. Glipizide, a pyretic and anti-inflammatory action simultaneously.
poorly soluble drug has been used as a model drug The aim of this study was to formulate effervescent
and an attempt has been made to improve the tablet with sufficient mechanical integrity and to
solubility of drug by the incorporation of accelerating achieve faster disintegration in the water.
agents, such as dispersant, alkalising agent in Effervescent tablets are uncoated tablets that
conjunction with hydrophilic swellable polymer such generally contain acid substances and carbonates or
as hydroxypropylmethylcellulose and present it in the bicarbonates and which react rapidly in the presence
form of gastroretentive floating tablets, which are of water by releasing carbon dioxide. They are
designed to provide the desired controlled and intended to be dissolved or dispersed in water before
complete release of drug for prolonged period of use. Effervescent compositions in the form of tablets
time. Floating tablets were prepared by direct are comprising a therapeutic agent, granulating agent,
compression method. Hydroxypropylmethylcellulose and an effervescent system which dissolve rapidly in
(HPMC K15M, HPMC K100M), Carbopol 940P, water to yield an effervescent solution containing a
were incorporated for gelforming properties. completely dissolved therapeutic agent and a process
Buoyancy was achieved by adding an effervescent for their preparation. In this study different ratio of
mixture of sodium bicarbonate and anhydrous citric Citric acid and Sodium bicarbonate was used,
acid. The optimized formulation (F7) exhibited superdisintegrant like SSG and cross-providone was
98.60% drug release in 24 hrs, while the buoyancy used, compared to cross-providone SSG decreases
lag time was 140sec. In-vitro drug release kinetics the Solution time of tablet. Granules prepared by Wet
was found to follow both the Zero order and the granulation technique and from the result it was
Korsmeyer and Peppas equation (Table 7). The found that the Particle size 355-500 μm of granules
release of glipizide from the formulations was found show good Solution time and Hardness property
to be non-fickian type. Evaluation of Gastric K.R.Srinath, et. al 2012 The oral dosage forms are
Retention Using X-Ray Imaging studies were the most popular way of taking medication despite
performed on rabbit to justify the increased gastric having some disadvantages like slow absorption and
residence time of the dosage form in the stomach, thus onset of action is prolong. This can be overcome
based on the floating principle. Optimized by administrating the drug in liquid from but, many
formulation (F7) showed no significant change in APIs have limited level of stability in liquid form. So,
physical appearance, drug content, total buoyancy Effervescent Tablets acts as an alternative dosage
time, or in vitro dissolution pattern after storage at form. The tablet is added into a glass of water just
40°C/75% (Figure 5) relative humidity for 1 month before administration and the drug solution or
Niraj Upmanyu, et. al 2012 Levofloxacin dispersion is to be drunk immediately. The tablet is
effervescent sustained release tablets were developed quickly broken apart by internal liberation of CO2 in
in eight different formulations (F1 to F8) by water due to interaction between tartaric a acid and
employing different grades of polymers and citric acid with alkali metal carbonates or
effervescent agents such as sodium bicarbonate and bicarbonates in presence of water.Due to liberation in
citric acid. The formulations were evaluated for CO2 gas, the dissolution of API in water as well as
various physical parameters, dissolution parameters taste masking effect is enhanced. The advantages of
and drug released mechanisms. F8 formulation effervescent tablets compared with other oral dosage
showed maximum floating time of 12 hours and gave forms includes an opportunity for formulator to
slow and maximum drug release of Levofloxacin improve taste, a more gentle action on patient’s
spread over 12 hours and whereas Levofloxacin stomach and marketing aspects. In present work an
released from marketed tablet was rapid and attempt has been made to formulate an effervescent
maximum within 8 hours tablet containing immediate release of paracetamol
Chauhan P, et. al 2012 Recently, fast-dissolving using various acids and bases. In present work we are
drug delivery system have started gaining popularity used different acids and bases in different
and acceptance as new drug delivery system, because concentration. In the preformulation study,
they are easy to administer and lead to better compatibility evaluation was performed which
compliance. Usually, elderly people experience implies that drug; acids, bases and other excipient are
difficulty in swallowing the tablet. Paracetamol compatible with each other. The formulation of
having analgesic, antipyretic effect, they inhibit tablets was done by using wet granulation as well as
cyclooxygenase enzyme involved in prostaglandin dry granulation in that technique wet granulation
(PG) synthesis but not in peripheral tissue while which was found acceptable. The total nine placebo
tablets were prepared and evaluated for hardness, grades of polymers with Sodium bicarbonate and
disintegration time, weight variation and solubility. citric acid. All the ingredients were accurately
All the formulation shows hardness and weight weighed and passed through different mesh sieves
variation with in limit but the combination of citric accordingly. Then, except Magnesium stearate all
acid (12.56%), tartaric acid (25.17%), sodium other ingredients were blended uniformly in glass
bicarbonate (38.20%), sodium carbonate (6.41%) mortar After sufficient mixing of drug as well as
,binding agent PVP-K-30 (2.94%) and sodium other components, Magnesium stearate was added, as
benzoate (0.52%). for the final formulation,(F7) post lubricant, and further mixed for additional 2-3
Because these ingredients shows the good \ minutes. The tablets were compressed using rotary
effervescent reaction and has no problem in capping tablet machine. The weights of all the tablets were
and sticking like other formulation kept constant for all formulation.
M. Karthik raja et. al 2012 Any drug delivery
system was designed to provide a therapeutic PREFORMULATION EVALUATION:
amount of drug to a proper site in the body with It includes different tests like Bulk density, tapped
intestinally to achieve desired release and thereby to density, Carr’s index, hausner’s ratio, Angle of
maintain the desired drug concentration. Multiple- repose.
unit floating drug delivery systems has several
advantages over monolithic ones, like avoiding all- Evaluation of Caffeine Effervescent Tablets:
or-nothing emptying, more predictable drug release Weight variation:
kinetics. In addition to drug formulations that deliver 20 tablets were selected randomly from the lot and
the drug for a prolonged or extended period, itwas weighted individually to check for weight variation.
important for efficient therapy to achieve spatial and
determined placement of the dosage form in the Weight Variation Specification as per IP
gastrointestinal tract. A gastroretentive effervescent Table 1: Weight Variation Specification
tablet of tinidazole by direct compression was
Average Weight of Tablet % Deviation
formulated in two different concentration of HPMC
along with Sodium bicarbonate and citric acid. The 80 mg or less <10
gas forming agent’s sodium bicarbonate was added in More than 80 mg but less <7.5
same concentrations. The formulated tablets were than 250 mg
then evaluated for pre formualative studies, 250 mg or more <5
solubility, and post formulation evaluation like drug
content, floating properties and invitro dissolution. Hardness
The invitro release study showed about 80-84% of The limit of hardness for the effervescent tablet is
drug release at the end of 7 hrs with good buoyancy usually kept in a lower range to facilitate early
effect for the batch formulated with the combination disintegration in the mouth. The hardness of the
of high concentration of HPMC. The above study tablet may be measured using conventional hardness
demonstration EF1 formulation could be successfully testers (Monsanto tablet hardness tester). It is
employed for good Controlled release action and it expressed in kg/cm2 or pound.
was planned to effervescent Floating tablets
formulation by using direct compression. Direct Friability
compression proves to be one of the best method of Friability of the tablet determined using Roche
preparation of floating tablets friabilator. This device subjects the tablet to the
combined effect of abrasion and shock in a plastic
MATERIALS AND METHODS: chamber revolving at 25 rpm and dropping a tablet at
MATERIALS: Caffeine, Superdisintegrants (sodium I height of 6 inches in each revolution. Pre weighted
bicarbonate, citric acid, spray dried lactose, sample of tablets was placed in the friabilator and
magnesium carbonate, sodium starch glycolate, were subjected to the 100 revolutions. Tablets were
sodium benzoate ), sugar based excipients, fillers or dusted using a soft muslin cloth and reweighed. The
diluents, colours, sweeteners, Lubricants, glidants friability (F) is given by the formula.
and preservatives.
Direct Compression
Direct compression normally requires careful Winitial - Wfinal
selection of raw materials to achieve a free-flowing, F = --------------------´ 100
non-segregating, compressible mixture. Effervescent Winitial
tablets were prepared by direct compression
technique using varying concentrations of different
Parameters F1 F2 F3 F4 F5 F6
Caffeine 100mg 100mg 100mg 100mg 100mg 100mg
RESULTS:
STANDARD GRAPH
Table 3: Standard graph
S.NO CONCENTRATION ABSORBANCE
1 0 0
2 1 0.139
3 2 0.256
4 3 0.365
5 4 0.478
6 5 0.584
Formulation Bulk density Tapped density Hausner’s Carr’s index Angle of repose
code gm/cc gm/cc ratio
parameters
F1 166.6 300 0.55 80 0.67
F2 166.6 375 0.47 112.5 0.67
F3 176.4 375 0.47 112.5 0.74
F4 176.4 333 0.55 100 0.74
F5 187.5 428 0.43 128.5 0.64
F6 187.5 428 0.43 128.5 0.64