FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF PROCHLORPERAZINE MALEATE - REVIEW OF LITERATURE
REVIEW OF LITERATURE
Few methods were reported in literatures which are as
follows:
3.1 Fast
Dissolving Tablet of Anti-Emetic Drugs
Gudas GK et al., (2010), prepared FDT of chlorpromazine. The tablets were prepared with sodium starch glycolate, crospovidone, croscarmellose, L-HPC, pre-gelatinised starch. The blends were examined for angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio. The tablets were evaluated for hardness, friability, disintegration time, dissolution rate and drug content.1
Kumar DN et al., (2010), prepared fast dissolving tablets of granisetron HCl using novel coprocessed superdisintegrants consisting of crospovidone and sodium starchglycolate in the different ratios (1:1, 1:2 & 1:3). The developed superdisintegrants were evaluated for angle of repose, carr’s index and Hausner’s ratio in comparison with physical mixture of superdisintegrants. The angle of repose of the developed excipients was found to be < 250, carr’s index in the range of 10-15% and Hausner’s ratio in the range of 1.11-1.14. Short-term stability studies on promising formulation indicated that there were no significant changes in drug content and in vitro dispersion time (p<0.05).2
Randale SA et al., (2010), masked the intensely bitter taste of metoclopramide and formulated a rapid disintegrating tablets of the taste masked drug. Taste masking was done by complexing metoclopramide with Eudragit in different ratio by the extrusion-precipitation method. Drug-polymer complexes (DPCs) were tested for drug content, in vitro taste in simulated salivary fluid, taste evaluation in oral cavity. The complex having drug-polymer ratio of 1: 2 shows significant taste masking, confirmed by drug. Prepared tablets were evaluated for various parameters like tensile strength, wetting time, water absorption ratio, in vitro disintegration time and disintegration in oral cavity.3
Goel H et al.,
(2010), developed a disintegrating system that could be used for preparing
fast disintegrating tablets of highly water soluble drug metoclopramide without
compromising on the mechanical strength. For this purpose disintegrating system
consisting of chitosan-alginate (CTN-ALG) complex (1:1): glycine and chitin was
developed. The results revealed that when CTN-ALG and glycine were mixed in the
ratio of 30:70, the granules exhibited a minimum water sorption time and
maximum effective pore radius. The results suggested incorporation of chitin
(5-10%w/w) while preparing FDTs of
metoclopramide to enhanced the disintegration without compromising their
mechanical strength.4
Shirshand SB et al., (2010), developed fast disintegrating tablets of
proclorperazine maleate with a view to enhance patient compliance by direct
compression method. In this method, crospovidone and croscarmellose sodium in
combination were used as superdisintigrant.5
Dahima R and Sharma R, (2010), masked the intensely bitter taste of metoclopramide
hydrochloride and to formulate orodispersible tablets of taste mask drug.
Drug-resin complex were optimize by considering parameters such as optimization
of resin concentration, optimization of swelling time, optimization of stirring
time, optimization of pH and optimization of temperature on maximum drug
loading. In vitro drug release study of taste masked tablets showed that
more than 85% of the drug release within 10 min. Thus, results conclusively
demonstrated successful masking of taste and rapid disintegration of the
formulated tablets in the oral cavity.6
Mahamuni SB et al., (2009), prepared fast dissolving tablets, which can rapidly
disintegrate in the saliva using taste-masked granules of drugs with a bitter
taste, Promethazine HCl. The taste masked granules were prepared using gastro
erodible Eudragit E-100 by extrusion method. Fast dissolving tablets were
prepared using taste-masked granules and a mixture of excipients containing
optimized level of microcrystalline cellulose and starch. The effect of various
superdisintegrants crospovidone, sodium starch glycolate, croscarmellose sodium
was also studied. The prepared tablets were evaluated for taste, crushing
strength, disintegration time and dissolution.7
Singh SK et al., (2009), prepared fast disintegrating combination tablets of
omeprazole and domperidone by using pertinent disintegrant. The tablets were
prepared using mannitol as diluent and sodium saccharin as sweetening agent
along with three different levels of disintegrant. The superdisintegrant used
in this study were Kollidon CL, Ac-di-sol and SSG. The tablets were evaluated
for weight variation, hardness, friability, wetting time, water absorption
ratio, disintegration time and dissolution study. Using the same excipients,
the tablets were prepared by direct compression and were evaluated in the
similar way. Drug content was estimated by using HPLC. Tablet formulation
prepared with 4.76% Ac-di-sol i.e. 10 mg showed disintegration time 15 s. Also
the hardness, friability, dissolution rate and assay of prepared tablets were
found to be acceptable according to standard limits.8
Shirsand SB et al., (2009), designed fast disintegrating tablets of
prochlorperazine maleate by direct compression method. Mucilage of plantago
ovata and crospovidone were used as superdisintegrants (2-8% w/w) along with
microcrystalline cellulose (20-60% w/w) and directly compressible mannitol to
enhance mouth feel. The prepared batches of tablets were evaluated for
hardness, friability, drug content uniformity, wetting time, water absorption
ratio and in vitro dispersion time. Formulation prepared by using 8% w/w
of plantago ovata mucilage and 60% w/w of microcrystalline cellulose emerged as
the overall best formulation.9
Fars KA, (2007), formulated
metoclopramide FDT with sufficient mechanical strength and fast disintegration
from bases prepared by both spray and freeze drying techniques. Different
disintegration accelerators were utilized to prepare the proper FDT using
various superdisintegrants (Ac-di-sol, kollidon and sodium starch glycolate), a
volatilizing solvent (ethanol) and an amino acid (glycine).10
3.2
Fast Dissolving Tablet of Other Drugs
Khemariya P et al., (2010), developed mouth dissolving tablet of meloxicam by
sublimation technology. The tablets were prepared by wet granulation procedure.
The tablets were evaluated for friability, wetting and disintegration time.
Sublimation of camphor from tablets resulted in better tablets as compared to
the tablets prepared from granules that were exposing to vacuum.11
Bhardwaj S et al., (2010), developed fast disintirating tablets of accelofenac.
Tablets were prepared by sodium starch glycolate following by direct
compression technique. The tablets were evaluated for hardness, friability,
weight variation, disintegration time, water absorption ratio and wetting time.
All the formulation showed disintegration time in range of 12.2 to 27.5 s along
with rapid in vitro dissolution.12
Abed KK et al., (2010), prepared orodispersible tablets of diazepam using
different types of superdisintegrants (Ac-di-sol, sodium starch glycolate and
crospovidone and different types of subliming agents camphor and ammonium
bicarbonate at different concentrations and two methods of tablets preparations
(wet granulation and direct compression methods). The formulations were
evaluated for flow properties, wetting time, hardness, friability, content
uniformity, in vivo disintegration time, release profiles and buccal
absorption tests. All formulations showed satisfactory mechanical strength
except formulation which contains camphor and formulation which was prepared by
direct compression method. The results revealed that the tablets containing
crospovidone as a superdisintegrant had good dissolution profile with shortest
disintegration time.13
Chandira RM et al., (2010), prepared FDT of etoricoxib using variety of super
disintegrants like primogel, kollidone, Ac-di-sol, L-HPMC, L-HPC. The prepared
tablets were evaluated for weight variation, hardness, friability, in vitro disintegration
time, wetting time and in vitro dissolution study. Formulation contain
L-HPC 8% shows the lowest disintegration time (44 s) and wetting time (52 s).14
El-Massik MA et al., (2010), utilized a maltodextrin to prepare orally
disintegrating tablets of meclizine. Tablets were prepared by both direct
compression and wet granulation techniques. The effect of maltodextrin
concentrations on ODT characteristics-manifested as hardness and disintegration
time-was studied. The effect of conditioning as a post-compression treatment on
ODT characteristics was also assessed. Maltodextrin-pronounced hardening effect
was investigated using differential scanning calorimetry (DSC) and X-ray
analysis.15
Keny RV et al., (2010), developed mouth disintegrating tablets of rizatriptan
benzoate to produce the intended benefit. Mouth dissolving tablets of
rizatriptan benzoate were prepared using superdisintigrant crospovidone,
carboxymethylcellulose calcium, indion 414 and indion 234 using direct
compression method. The tablets prepared were evaluated for thickness,
uniformity of weight, content uniformity, hardness, friability, wetting time, in
vivo and in vitro disintegration time, mouth feel, in vitro drug
release and assay by high performance liquid chromatography.16
Parikh BN et al., (2010), developed solid oral formulations of telmisartan which
can be prepared using less complicated and expensive processes and fulfill all
prerequisites for pharmaceutical use, i.e. long-lasting stability of the
formulation under different climatic conditions and sufficient solubility of
the active substance for sufficient gastrointestinal absorption in the slightly
acidic and neutral pH region. Preferably, the formulations should have
immediate release characteristics and a dissolution showing no essential pH
dependency within the physiological relevant pH interval of the gastrointestinal
tract. Tablets were evaluated for various parameters like, weight variation,
content uniformity, in-vitro dissolution studies were performed using United
States Pharmacopeia (USP) apparatus type II.17
Shid SL et al., (2010), prepared orodispersible tablets of flurbiprofen
using various superdisintegrants such as croscarmellose sodium, sodium starch
glycolate, crospovidone and camphor (as subliming agent) in different ratio and
subjected for evaluation. Results revealed that the tablets of all formulations
have acceptable physical parameters.18
Rajalakshmi G et al., (2010), formulated pheniramine maleate a selective H1 receptor
antagonist into orodispersible tablets. The tablets were prepared by direct
compression method using superdisintegrants like croscarmellose sodium,
crospovidone, sodium starch glycolate, low hydroxylpropyl cellulose and
pre-gelatinized starch in different ratios. The blends examined for various pre
compression parameters. Tablets were evaluated by measuring hardness,
friability, content uniformity, weight variation and drug release pattern.19
Kalia A et al., (2009), prepared mouth dissolving tablets of oxcabazepine
using two different technologies, direct compression method and solid
dispersion technology. Tablets produced by direct compression method contain
crospovidone as a superdisintegrant and aspartame as a sweetener. Solid
dispersions of oxcarbazepine with polyvinylpyrrolidone K-30 and polyethylene
glycol 6000 in different weight ratios were prepared with a view to increase its
water solubility. Oxcarbazepine solid dispersions with polyvinylpyrrolidone
K-30 in 1:2 ratios of drug: carrier showed maximum drug release and hence,
compressed along with other excipients into mouth dissolving tablet. The
results compared for both the technologies showed that the oxcarbazepine
tablets prepared using solid dispersion technology was found to have good
technological properties and satisfying and reproducible drug dissolution
profiles.20
Rao NG et al., (2009), developed rapidly disintegrating oral tablets by
direct compression using cogrinding and solid dispersion methods by using
chlorthalidone as a model drug. The tablet formulation containing polyvinyl
pyrrolidone K-12 solid dispersion showed maximum drug release than the
chlorthalidone polyvinyl pyrrolidone K-12 co-grinding method. The prepared
tablets were evaluated for hardness, friability, wetting time, disintegration
time and in vitro drug release. DSC and FTIR studies revealed that no
chemical interaction between the drug and the carrier. The stability studies
were conducted as per the ICH guidelines and the formulations were found to be
stable with insignificant change in the hardness, and disintegration time.21
Kumar DN et al., (2009), prepared fast dissolving tablets of fexofenadine by
effervescent method with a view to enhance patient compliance. Three
super-disintegrants viz., crospovidone, croscarmellose sodium and sodium starch
glycolate along with sodium bicarbonate and anhydrous citric acid in different
ratios were used and directly compressible mannitol to enhance mouth feel
property of tablets. The prepared batches of tablets were evaluated for
hardness, friability, drug content uniformity and in vitro dispersion
time. Among the three promising formulations, the formulation containing 8% w/w
of crospovidone and mixture of 24% w/w sodium bicarbonate, 18% w/w of anhydrous
citric acid emerged as the best based on the in vitro drug release
characteristics compared to conventional commercial tablet formulation.
Short-term stability studies on the formulations indicated that there were no
significant changes in drug content and in vitro dispersion time
(P<0.05).22
Swamy PV et al., (2009), designed orodispersible tablets of pheniramine maleate
by effervescent method. Mixture of sodium bicarbonate and tartaric acid were
used along with superdisintegrants pregelatinized starch, sodium starch
glycolate, croscarmellose sodium and crospovidone. The prepared batches of
tablets were evaluated for hardness, friability, drug content uniformity and in
vitro dispersion time. Formulation containing 4% w/w crospovidone and
mixture of sodium bicarbonate and tartaric acid emerged as the overall best
formulation.23
Devireddy SR et al., (2009), formulated orally disintegrating tablets of levocetirizine
dihydrochloride with different superdisintegrants (sodium starch glycollate,
croscarmellose sodium, and crospovidone) using mannitol as a diluent.
Tulsion-335, Indion-204 and poly kyron T-134 cation exchange resins were used
as taste-masking agents. The drug and resin complex was prepared by the
kneading method. Ten formulations were prepared with varying combinations of
superdisintegrants and ion-exchange resins by the wet granulation technique,
using polyvinylpyrrolidone K-30 as the binder. The prepared tablets were
evaluated for degree of taste masking, weight variation, hardness, friability, in
vitro and in vivo disintegration time, content uniformity and water
absorption ratio.24
Okuda Y et al., (2009), designed a new orally disintegrating tablet that has
high tablet hardness and a fast oral disintegration rate using a new
preparation method. To obtain rapid disintegration granules (RGD), a
saccharide, such as trehalose, mannitol, or lactose, was spray-coated with a
suspension of corn starch using a fluidized-bed granulator. As an additional
disintegrant, crospovidone, light anhydrous silicic acid, or hydroxypropyl
starch was also included in the suspension. The RDGs obtained possessed
extremely large surface areas, narrow particle size distribution, and numerous
micro-pores. When tabletting these RDGs, it was found that the RDGs increased
tablet hardness by decreasing plastic deformation and increasing the contact
frequency between granules. In all tablets, a linear relationship was observed
between tablet hardness and oral disintegration time.25
Giri TK and Sa B, (2009), described the formulation of rapidly disintegrating,
diazepam tablets. The tablets were prepared by the conventional wet granulation
method using solid dispersion of the drug with PEG-4000 and/or PEG-6000. A 32
factorial design was used to reduce the number of experimental runs and to
obtain several formulations by which tablets disintegrated within 3 min and
released 85% of the drug in less than 30 min. Several tablet formulations
prepared with different amounts of PEGs in solid dispersion met the above two
criteria. However, tablets which were prepared with PEG-4000 alone at the
lowest concentration disintegrated in the shortest time (32.12 s) and released
85% of the drug most rapidly (11.03 min).26
Gupta A et al., (2009), investigated correlation between disintegration and
dissolution for immediate release tablets containing a high solubility drug and
to identify formulations where disintegration test, instead of the dissolution
test, may be used as the acceptance criteria based on International Conference
on Harmonization Q6A guidelines. A statistical design of experiments was used
to study the effect of filler, binder, disintegrating agent and tablet hardness
on the disintegration and dissolution of verapamil hydrochloride tablets. All
formulation variables, i.e., filler, binder and disintegrating agent were found
to influence tablet dissolution and disintegration, with the filler and
disintegrating agent exerting the most significant influence.27
Jacob S et al., (2009), prepared fast dissolving effervescent tablets were
prepared by the modification of nonreactive liquid based wet granulation
technique. Citric acid was coated with plastic materials such as polyethylene
glycol (PEG), which provide a physical barrier to the reaction. The inherent
hygroscopic nature of PEG could decrease the affinity for moisture of
effervescent mixtures and can provide a stabilizing effect. Sodium bicarbonate
was blended with sugar alcohol like mannitol, which would give a protective
coating. PEG 1000 melts at body temperature and thereby does not delay the
reaction between the acid source and base.28
Singh J and Singh R, (2009), formulated and optimized orodispersible tablets of
meloxicam using a 22 factorial design for enhanced bioavailability. The tablets
were made by non-aqueous wet granulation using crospovidone and mannitol. A 22
factorial design was used to investigate the amount of crospovidone and taste
masking, soothening hydrophilic agent (mannitol), as independent variables and
disintegration time as dependent response.29
Madan J et al., (2009), prepared fast dissolving tablets of the nutraceutical,
freeze-dried aloe vera gel by dry granulation method. The tablets were
evaluated for crushing strength, disintegration time, wetting time, friability,
drug content and drug release. A 32 full factorial design was applied to
investigate the combined effect of two formulation variables - amounts of
microcrystalline cellulose and mannitol. The results of multiple regression
analysis revealed that in order to obtain fast dissolving tablets of the aloe
vera gel, an optimum concentration of mannitol and a higher content of
microcrystalline cellulose should be used.30
Late SG et al., (2009), investigated effects of calcium silicate
(disintegration-promoting agent) and various lubricants on an optimized
cyclodextrin-based fast disintegrating tablets formulation. Effects of moisture
treatment were also evaluated at 75, 85 and 95% relative humidities. A two
factors at three levels (32) full factorial design were used to optimize
concentrations of calcium silicate and lubricant. Magnesium stearate, being
commonly used lubricant, was used to optimize lubricant concentration in
optimization study. Results of multiple linear regression analysis revealed
that concentration of calcium silicate had no effect; however concentration of
lubricant was found to be important for tablet disintegration and hardness.31
Fujii M et al., (2009), investigated the factors affecting disintegration time
in the mouth (DTM) of rapidly disintegrating tablets. The relation between DTM
and stationary time of upper punch displacement (STP) was examined using a
tabletting process analyzer. Results indicated that the bulk density of mixed
excipient powder used for tablet preparation affects both DTM and STP. As the
value of bulk density increased, STP became longer and DTM shorter. The results
of a combination of granules and powder with or without drug showed linear
relation between apparent volume and DTM (r2 = 0.7332). For a DTM less than 60
s, a formulation with a bulk density greater than 0.5 g/mL should be chosen
with a compression force of 5 kN. The hardness of tablets could be greater than
3 kg if at least one high-compressibility excipient was used in the
formulation.32
Madgulkar et al., (2009), developed novel taste masked mouth-dissolving tablets
of tramadol that overcomes principle drawback of such formulation which was
inadequate mechanical strength. In this work, the bitter taste of tramadol HCl
was masked by forming a complex with an ion exchange resin Tulsion335. The
novel combination of a superdisintegrant and a binder that melts near the body
temperature was used to formulate mechanically strong tablets that showed fast
disintegration. A 32 full factorial design and statistical models were applied
to optimize the effect of two factors, i.e., superdisintegrant (crospovidone)
and a mouth-melting binder (gelucire 39/01). It was observed that the
responses, i.e., disintegration time and percent friability were affected by
both the factors. The statistical models were validated and can be successfully
used to prepare optimized taste masked mouth-dissolving tablets of tramadol HCl
with adequate mechanical strength and rapid disintegration.33
Zade PS et al., (2009), prepared bitterless fast dissolving tablet of
tizanidine hydrochloride using Eudragit E 100 as a taste masking agent. Mass
extrusion was the technique used for preparing taste masked granules. The
tablets were prepared with three superdisintegrants e.g. sodium starch
glycolate, crosscarmellose sodium and crospovidone.34
Chaulang G et al., (2009), prepared solid dispersion of furosemide in SSG in
ratios of 1:1 and 1:2 by kneading method. The solid dispersion was
characterized FTIR, DSC and XRD to ascertain if there were any physicochemical
interactions between drug and carrier that could affect dissolution. Tablets
containing the solid dispersion were formulated and their dissolution
characteristics compared with commercial furosemide tablets.35
Furtado S et al., (2008), prepared orodispersible tablets of famotidine using
camphor as subliming agent and sodium starch glycollate together with
crosscarmellose sodium as superdisintegrants. The formulations were evaluated
for weight variation, hardness and friability, drug content, wetting time, in
vitro and in vivo dispersion time, mouth feel and in vitro dissolution.
The results revealed that the tablets containing subliming agent had a good
dissolution profile.36
Mohapatra A et al., (2008), prepared the tablets of metformin using starch RX1500
and microcrystalline cellulose by direct compression. The tablets showed
erosion behavior rather than disintegration. Then lactose was incorporated
which created pores to cause burst release of drug. But these tablets did not
give good mouth feel. Thus, Pearlitol SD 200 (spray dried mannitol) was used to
prepare tablets by wet granulation (10% polyvinylpyrrolidone in Isopropyl
alcohol as binder). The optimized batches of tablets not only exhibited desired
mouth feel but also disintegration time, in vitro dispersion time, water
absorption ratio and in vitro drug release. All the batches contained
15% starch and 4% of croscarmellose sodium.37
Kuno Y et al., (2008), evaluated the effect of lubricants on the
characteristics of orally disintegrating (OD) tablets manufactured using the
phase transition of sugar alcohol. OD tablets were produced by directly
compressing a mixture containing lactose–xylitol granules, disintegrant,
glidant and lubricant and subsequent heating. The effect of the type of
lubricant on the tablet characteristics was evaluated using magnesium stearate,
sodium stearyl fumarate (SSF) and talc as lubricants.38
Seong HJ and Kinam P, (2008), investigated complex formation between drugs and
ion-exchange resins and the effects of coating by various aqueous polymeric
dispersions on the complexes were evaluated for developing new
sustained-release fast-disintegrating tablets. Complexes of ion-exchange resin and
dextromethorphan, a model drug, were prepared using different particle sizes of
the resins. Based on drug loading, release profiles and scanning electron
microscopy images, the coated particles were granulated with suitable tablet
excipients and then compressed into the tablets. As the particle size of resins
increased, the drug loading and release rate decreased due to the reduced
effective diffusion coefficient and surface area.39
Patel IM and Patel MM, (2008), developed fast dissolving tablets of etoricoxib.
Granules containing etoricxib, crospovidone, aspartame and menthol prepared by
wet granulation technique. Menthol was sublimed from the granules by exposing
the granules to vacuum. The porous granules were then compressed into tablets.
Alternatively, the tablets were prepared and later exposed to vacuum. The
tablets were evaluated for percentage friability and disintegration time. A 32
full factorial design was applied to investigate the combined effect of two
formulation variables; amount of menthol and crospovidone. The result of
multiple regression analysis indicated that for obtaining for fast dissolving
tablet optimum amount of menthol and higher percentage of crospovidone should
be used.40
Masareddy RS et al., (2008), studied two different methods direct compression and
sublimation in formulation of mouth dissolving tablets of clozapine. Total four
formulations using various superdisintegrants and subliming agents were
prepared. All prepared formulations were evaluated for physico-chemical parameters.
The formulations exhibited good disintegration properties with total
disintegration time in the range of 25 to 35 s. Comparative evaluation of two
methods showed direct compression method was a better alternative to
sublimation method as its formulations rapidly disintegrate in oral cavity.
Kinetic studies indicated that all the formulations followed first order
release with diffusion mechanism.41
Shen YC et al., (2007), designed an orally disintegrating tablet formulation
of olanzapine to dissolve rapidly upon contact with saliva also described a
manic patient who has an esophageal stricture and chronic pharyngitis, two
conditions that impede the swallowing of medications. She was successfully
treated for her mania with this orally disintegrating formulation.42
Mohammad BJ et al., (2007), prepared carbamazepine solid dispersions by the
co-grinding technique using an insoluble but highly hydrophilic crospovidone
and soluble hydroxypropylmethylcellulose (HPMC) as the carriers. The ratios of
drug to carrier were 1:1, 1:5 and 1:10. Comparison of the dissolution of the
drug from its cogrounds with that of the unground drug, its ground form and the
corresponding physical mixtures revealed considerable differences. The
percentage of drug dissolved during the first 30 min (% D30), for the ground
and coground drug was 75-95, whereas the % D30 for ungrounded drug and its
physical mixtures ranged from 41-62.43
Malke S et al., (2007), prepared fast dissolving tablets of oxycarbazepine
containing Avicel PH 102 as a diluent and Ac-di-sol as a superdisintegrant by
wet granulation process. All the formulations were evaluated for
characteristics such as hardness, friability, weight variation, wetting
ability, disintegration time and dissolution rate.44
Pandey PV and Amarnath R, (2007), investigated performance of three disintegrants,
sodium starch glycolate, croscarmellose sodium and crospovidone using
intragranular and extragranular methods, both in the same quantity of 2% w/w.
Chloroquine phosphate was the drug of choice for the present study. Other
excipients used in the formulation of tablets were lactose monodehydrate,
polyvinylpyrolidone K-30 (PVP K-30), aerosil and magnesium stearate.45
Modi A and Tayade P, (2006), investigated enhancement of the dissolution profile of
valdecoxib using solid dispersion with polyvinylpyrrolidine. They also
described the preparation of fast-dissolving tablets of valdecoxib by using a
high amount of superdisintegrants. A phase solubility method was used to
evaluate the effect of various water-soluble polymers on aqueous solubility of
valdecoxib.46
Ahmed IS et al., (2006), developed ketoprofen tablets which dissolve rapidly in
the mouth. The solubility and dissolution rate of poorly water-soluble
ketoprofen was improved by preparing a lyophilized tablet of ketoprofen using
freeze-drying technique.47
Cirri M et al., (2006), developed a tablet formulation based on an effective
flurbiprofen-cyclodextrin system, able to allow a rapid and complete
dissolution of this practically insoluble drug. Three different cyclodextrins
were evaluated the parent beta-cyclodextrin (previously found to be the best
partner for the drug among the natural cyclodextrins) and two amorphous, highly
soluble beta-cyclodextrin derivatives, i.e., methyl-beta-cyclodextrin and
hydroxyethyl-beta-cyclodextrin.48
Shishu and Bhatti A, (2006), formulated compressed tablets of diazepam using
microcrystalline cellulose as directly compressible filler and sodium starch
glycolate as superdisintegrant. The taste masked microspheres were prepared
using amino alkyl methacrylate copolymer (Eudragit E-100) by solvent
evaporation technique. Taste evaluation of these microspheres was done by both
spectrophotometric taste evaluation technique and panel testing.49
Takagi H et al., (2005), established a pharmaceutical composition useful for
rapid disintegration, which comprises of a sparingly soluble medicament held on
a gel-forming water-soluble polymer as a solid dispersion.50
Francesco C, (2005), studied the feasibility of preparing fast-dissolving
mucoadhesive microparticulate delivery systems containing amorphous piroxicam
to improve drug residence time on sublingual mucosa and drug dissolution rate.
The two new mucoadhesive carriers Eudragit L 100 and Eudragit S 100 sodium
salts, both characterized by a fast intrinsic dissolution rate, have selected.51
Rasetti EC and Grange V, (2005), developed new non-steroidal anti-inflammatory drugs
(NSAID) formulations with faster onset of analgesic action like fast dissolving
tablets. An open-label, randomized, single dose, crossover study with a 18 days
washout period was conducted in 16 healthy volunteers to compare the
pharmacokinetic profile of 20 mg piroxicam freeze-dried tablet (Proxalyoc,
Cephalon) with that of 20 mg piroxicam capsule (Feldene, Pfizer).52
Abdelbary G et al., (2005), assessed the in vitro disintegration profile
of rapidly disintegrating tablets (RDT) was very important in the evaluation
and the development of new formulations of this type. So far neither the US
Pharmacopoeia nor the European Pharmacopoeia has defined a specific
disintegration test for RDT; currently, it was only possible to refer to the
tests on dispersible or effervescent tablets for the evaluation of RDT's
disintegration capacity. In the present study, they have evaluated the
disintegration profile of RDT manufactured by main commercialized technologies,
using the texture analyzer .53
Yoshio K et al., (2005), studied the properties of rapidly disintegrating (RD)
tablets manufactured by the phase transition method. RD tablets were produced
by compressing powder containing erythritol (melting point: 122°) and xylitol
(melting point: 93-95°) and then heating at about 93° for 15 min. The hardness
and oral disintegration time of the heated tablets increased with an increase
of the xylitol content.54
Kuchekar BS et al., (2004), in the present work, an attempt was made to formulated
and evaluated mouth dissolving tablets of salbutamol sulphate. Formulations
were prepared by factorial design technique. Different disintegrates were used
to formulate fast dissolving tablets.55
Abu-Izza et al., (2004), formulated tablets which dissolve rapidly in the mouth
and provide an excellent mouth feel. The tablets of the invention comprise a
compound, which melts at about 37o or lower, have a low hardness, high
stability and generally comprise few insoluble disintegrants which may cause a
gritty or bulky sensation in the mouth. Convenient and economically feasible
processes by which the tablets of the invention may be produced were also
provided.56
Mizumoto T et al., (2004), developed a quick disintegrating tablet in buccal
cavity, comprising a mixture of drug, a sugar (A) and an amorphous sugar (B)
and after forming a tablet, it was humidified and dried. The tablet in the
present invention was to provide stability against moisture at preserved,
because the amorphous sugar changed to the crystalline state in a
non-reversible reaction after it was humidified and dried in a manufacturing
process.57
Johnson ES and Lacy J, (2004), formulated a composition for oral administration
comprising a carrier and as active ingredient, an opioid (μ-receptor) agonist,
such as fentanyl or a salt thereof, characterized in that the composition was
in the form of a fast-dispersing dosage form designed to release the active
ingredient rapidly in the oral cavity.58
Luber J and Bunick FJ, (2004), studied an immediate release tablet capable of being
chewed or disintegrated in the oral cavity, which comprises a pharmaceutically
active ingredient and a matrix comprising polyethylene oxide having a weight
average molecular weight of from about 500,000 to about 10,000,000. The tablets
possesses exceptionally good mouth feel and stability.59
Hall M et al., (2004), developed a composition comprising a carrier and an
active ingredient, wherein the carrier was fish gelatin and the composition was
a fast-dispersing dosage form designed to release the active ingredient rapidly
on contact with a fluid. In one embodiment, the composition was designed for
oral administration and releases the active ingredient rapidly in the oral
cavity on contact with saliva. The fish gelatin can be obtained from cold water
fish sources and was preferably the non-gelling, non-hydrolyzed form. A process
for preparing such a composition and a method of using fish gelatin in a fast
dispersing dosage form were also provided.60
Lalla JK and Mamania HM, (2004), studied the inclusion complex of rofecoxib, an NSAID
with β-cyclodextrin using ball milling technique has been prepared and
evaluated using differential scanning calorimetry thermograph. The fast
dissolving tablet composition with 25 mg equivalent rofecoxib showed complete
release of rofecoxib in 12 min as compared to 20% drug release from the
conventional release marketed tablets during the same period.61
Shirwaikar AA and Ramesh A, (2004), formulated atenolol as fast disintegrating tablets
using three superdisintegrants, croscarmellose sodium (Ac-di-sol), crospovidone
(Polyplasdone XL) and sodium starch glycolate (Explotab). All the
superdisintegrants were used at different concentration levels to assess their
efficiency and critical concentration level.62
Valleri M et al., (2004), investigated the possibility of developing glyburide
tablets, allowing fast, reproducible and complete drug dissolution, by using
drug solid dispersion in polyethylene glycol. The glyburide dissolution profile
from the newly developed tablets was clearly better than those from various
commercial tablets at the same drug dosage.63
Drooge DJ et al., (2004), studied anomalous dissolution behavior of tablets
consisting of sugar glass dispersions was investigated. The poorly aqueous
soluble diazepam was used as a lipophilic model drug. The release of diazepam
and sugar carrier was determined to study the mechanisms governing dissolution
behavior.64
Gohel M et al., (2004), developed mouth dissolving tablets of nimesulide.
Granules containing nimesulide, camphor, crospovidone and lactose were prepared
by wet granulation technique. Camphor was sublimed from the dried granules by
exposure to vacuum. The porous granules were then compressed. Alternatively,
tablets were first prepared and later exposed to vacuum. The tablets were
evaluated for percentage friability, wetting time, and disintegration time. In
the investigation, a 32 full factorial design was used to investigate the joint
influence of 2 formulation variables: amount of camphor and crospovidone.65
Schroeder M and Steffens K, (2003), prepared rapidly disintegrating preparations
containing at least one active pharmaceutical ingredient and at least one
excipient by a simple process in which the predominant part of the complete
composition of the ingredients was granulated, the resulting granules and where
appropriate, the remainder of the ingredients were shaped in the presence of
liquid virtually without pressure, and the resulting shaped articles were
dried.66
Zakarian N et al., (2003), invented dispersible tablets containing macrolides as
active ingredients either on their own or associated with other active
ingredients, in addition to a method for the production thereof. The
dispersible tablets were characterized in that the macrolide was chosen from a
group that was made up of pristinamycin, azithromycin, roxithromycin,
clarithromycin and spiramycin.67
Murray OJ et al., (2003), studied fast dispersing solid dosage forms that
preferably dissolve in the oral cavity within sixty, more preferably within
thirty, most preferably within ten seconds. A novel feature of the solid dosage
forms according to the invention resided in the fact that the composition was
essentially free or absolutely free of mammalian gelatin.68
Laruelle C et al., (2003), established pharmaceutical dosage forms with rapid
disintegration in the mouth and to their process of preparation. The
pharmaceutical dosage forms comprised of at least one active principle
dispersed in a mixture of excipients and were characterized in that the mixture
of excipients comprised at least one weakly compressible diluting agent other
than trehalose and a copolymer of 1-vinylpyrrolidin-2-one and of vinyl acetate.69
Murali M et al., (2002), designed nimodipine tablets with fast in vitro release
rates using nimodipine-modified gum karaya co-grinding mixtures. Co-grinding
mixtures of nimodipine and gum karaya were also prepared to highlight the
efficiency of modified gum karaya.70
El-Arini SK and Clas SD, (2002), studied in vitro disintegration behavior of
fast dissolving system, manufactured by the main commercialized technology,
using the texture analyzer instrument.71
Simone S and Peter CS, (2002), prepared two types of tablets containing coated
ibuprofen as a high dosed model drug. The properties of the water dispersible
tablet, such as porosity, hardness, disintegration time and increase in
viscosity after dispersion, were investigated. The selected tablet formulation,
containing 26% galactomannan and 5% crospovidone, disintegrated before the
galactomannan started to swell. These tablets dispersed in water within 40 s
and showed a crushing strength of 95 N.72
Sunanda H and Bi Y, (2002) developed rapidly disintegrating tablets using both
direct compression and wet compression methods. Tablet properties such as
porosity, tensile strength, wetting time and disintegration time were evaluated
and the formulation and disintegration time of the tablets were elucidated.
Formulation and preparation conditions were optimized using polynomial
regression or artificial neural network.73
Khankari et al., (2001), formulated a rapidly dissolving robust dosage form.
The invention was directed to a hard tablet that can be stored, packaged and
processed in bulk. The tablet dissolved rapidly in the mouth of the patient
with a minimum of grit. The tablet was created from an active ingredient mixed
into a matrix of no direct compression filler and a relatively high lubricant
content.74
Gilis P and De Conde V, (2000), formulated a fast-dissolving tablets for oral
administration comprising of an active ingredient, a therapeutically effective
amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier,
characterized in that the said carrier comprised a spray-dried mixture of
lactose monohydrate and microcrystalline cellulose as diluents, and a
disintegrant; and direct compression process for preparing such fast dissolving
tablets was used.75
3.3
Formulations of Prochlorperazine Maleate
Obata Y et al., (2010), developed transdermal drug delivery system for
prochlorperazine (PCPZ) and performed an in vitro skin permeation study
with hairless mouse skin. When the concentration of L-menthol in the hydrogel
was 0-0.5%, the PCPZ flux was small; on the other hand, the flux was increased
remarkably when the L-menthol concentration was higher than 1%. The optimal
formulation of hydrogel would be contained 20% isopropanol (IPA), 10%
N-methyl-2-pyrrolidone (NMP), 2% L-menthol and 1% PCPZ. The strong inhibitory
effects to stereotyped behavior were observed at 4 h after administration of
PCPZ hydrogel, and the efficacy was sustained for at least 8 h after the
administration in mice in vivo. Thus, it was considered that PCPZ was
delivered to brain via systemic circulation by the administration of PCPZ
hydrogel.81
Suresh S et al., (2010), designed fast disintegrating tablets of
prochlorperazine maleate with crospovidone (upto 3% w/w) and croscarmellose
sodium (upto 5% w/w) in combination were used as superdisintegrants. The
prepared formulations were evaluated for hardness, friability, drug content
uniformity, dispersion time, wetting time and water absorption ratio. Among the
formulations tested, formulation containing 5% w/w of croscarmellose sodium and
3% w/w of crospovidone as superdisintegrant emerged as the overall best based
on drug release characteristics in pH 6.8 phosphate buffer compared to
commercial conventional tablet formulation.82
Misao N et al., (2009), developed oral disintegrating film containing
prochlorperazine using microcrystalline cellulose, polyethlene glycol and
hydroxypropylmethyl cellulose as the base materials. The uniformity of dosage
units of the preparation was acceptable according to the criteria of JP15 or
USP27. The film showed an excellent stability at least for 8 weeks when stored
at 40° and 75% in humidity. The dissolution test revealed a rapid
disintegration property, in which most of prochlorperazine dissolved within 2
min after insertion into the medium.83
Finn A et al., (2005), developed buccal dosage form of prochlorperazine and
also conducted two clinical studies to characterize the single-dose and
multiple-dose pharmacokinetics of prochlorperazine and its metabolites after
buccal administration. The results of these studies demonstrate that buccal
administration of prochlorperazine produces plasma concentrations more than
twice as high as an oral tablet, with less than half the variability. In
addition to the metabolites, N-desmethyl prochlorperazine and prochlorperazine
sulfoxide, 2 new metabolites, prochlorperazine 7-hydroxide and prochlorperazine
sulfoxide 4-N-oxide, were identified and quantitated. Exposure to metabolites
after the buccal prochlorperazine formulation was approximately half that
observed after the oral tablet. Buccal administration of prochlorperazine,
twice daily, should enhance the therapeutic role of prochlorperazine in
preventing and treating nausea and vomiting. 84
Singh S et al., (1999), prepared and evaluated buccal prochlorperazine
(Bukatel) for its efficacy and tolerability with commonly used metoclopramide.
Bukatel was well tolerated and well rated by both patients and investigators
with no adverse effects on buccal mucosa and causing less drowsiness and
sedation. Results indicated that Bukatel was safe and effective for the
treatment of nausea and/or vomiting in patients suffering from vertiginous
disorders and could be safely and strongly recommended as an alternative to
less bioavailable and indiscriminately used oral metoclopramide tablets.85
Nagarsenker MS et al., (1998), prepared coevaporates of prochlorperazine maleate
(PCPM) by using different polymers by solvent evaporation technique. Ethyl
cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose phthalate
were used in preparation of coevaporates. The coevaporates were characterized
by X-ray diffraction studies, IR spectrophotometry and Differential scanning
calorimetry. Dissolution behavior of coevaporates was studied using buffer
solution with pH 1.2 and 6.8 by half change method. A two level, two factor
factorial design was used to quantitate effect of polymers on dissolution
profile of PCPM. Dissolution of drug in pH 6.8 buffer improved with increasing
content of hydroxypropyl methylcellulose phthalate in coevaporates. 86
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