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Gandhi et al Journal of Drug Delivery & Therapeutics.

2019; 9(2):507-513

Available online on 15.03.2019 at http://jddtonline.info

Journal of Drug Delivery and Therapeutics


Open Access to Pharmaceutical and Medical Research
© 2011-18, publisher and licensee JDDT, This is an Open Access article which permits unrestricted
non-commercial use, provided the original work is properly cited

Open Access Review Article


Comparative study on effect of natural and synthetic superdisintegrants in
the formulation of orodispersible tablets
Lavika Gandhi* and Md. Semimul Akhtar
Shri Ram Murti Smarak College of Engineering & Technology (Pharmacy), Bareilly (U.P) India

ABSTRACT
Now-a-days, Orodispersible drug delivery systems are extensively used to improve bioavailability and patient compliance. Over the past three
decades, Orodispersible tablets (ODTs) have gained considerable attention as a preferred alternative to conventional tablets and capsules due to
better patient compliance, improved solubility and stability profiles. ODTs are solid dosage forms containing medicinal substances which
disintegrate rapidly, usually in a matter of seconds, when placed on the tongue. New ODT technologies address many pharmaceutical and patient
needs, ranging from enhanced life-cycle management to convenient dosing for paediatric, geriatric, and psychiatric patients with dysphagia. The
therapeutic activity of these formulations is obtained through a typical manner like disintegration followed by dissolution. Hence disintegration
has major role for facilitating drug activity. In recent years, several newer agents have been developed known as superdisintegrants. The
objective of the present article is to highlight the various kinds of superdisintegrants (Natural & Synthetic) along with their role in tablet
disintegration and drug release, which are being used in the formulation to provide the safer, effective drug delivery with patient compliance.
Keywords: ODTs, Orodispersible tablets, Disintegrants, Superdisintegrants, Natural, and Synthetic.

Article Info: Received 28 Jan 2019; Review Completed 03 March 2019; Accepted 06 March 2019; Available online 15 March 2019
Cite this article as:
Gandhi L, Akhtar MS, Comparative study on effect of natural and synthetic superdisintegrants in the formulation of
orodispersible tablets, Journal of Drug Delivery and Therapeutics. 2019; 9(2):507-513
http://dx.doi.org/10.22270/jddt.v9i2.2404

*Address for Correspondence:


Lavika Gandhi, Shri Ram Murti Smarak College of Engineering & Technology (Pharmacy), Bareilly (U.P) India

INTRODUCTION conventional tablets, but are composed of super


disintegrants, which help them to dissolve the tablets within
Drug delivery through oral route is the most common and a minute in the mouth in the presence of saliva without any
preferred route of drug administration both for solid and difficulty of swallowing.4-8
liquid dosage forms. However, solid dosage forms are
popular because of the ease of administration, accurate Due to the presence of super disintegrants, it gets dissolved
dosage, self-medication, pain avoidance, and most quickly, resulting in rapid absorption of drug which in turn
importantly the patient compliance.1 Tablets and capsules provides rapid onset of action.8 Since the absorption is
are the most popular solid dosage forms. However, many taking place directly from the mouth, so, bioavailability of
people face difficulty in swallowing tablets and hard gelatin the drug increases.9 Drugs present in orodispersible tablets
capsules. This difficulty in swallowing is called dysphasia.2 It are also not suffering from first pass metabolism. This type
has been found that this problem has been encountered in all of drug delivery is becoming popular day by day due to its
groups of patient, but especially with pediatric and geriatric numerous advantages.
populations. Thus, these conventional dosage forms result in
high incidence of noncompliance and ineffective therapy
Advantages of ODTS 10, 11
with respect to swallowing specially in the case of pediatric, 1. Quick onset of action and improved bioavailability.
geriatric, or any mentally retarded persons. Orodispersible
tablets are also called as orally disintegrating tablets, mouth- 2. Useful for patients who cannot swallow the dosage forms
dissolving tablets, rapid dissolving tablets, fast- and for pediatric, geriatric and mentally retard patients.
disintegrating tablets, fast-dissolving tablets. Recently, 3. Improved patient compliance.
European Pharmacopoeia has used the term orodispersible
tablets. This may be defined as uncoated tablets intended to 4. Frequently administered when water is not available.
be placed in the mouth where they disperse readily within 3 5. Accurate dose can be given as compared to oral liquids.
min before swallowing.3 United States Pharmacopoeia has
also approved these dosage forms as orodispersible tablets.
Thus, orodispersible tablets are solid unit dosage forms like
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Gandhi et al Journal of Drug Delivery & Therapeutics. 2019; 9(2):507-513

6. Pleasant mouth feel of the tablet helps to change the 6. It allows high drug loading.
perception of medication as bitter pill particularly in
7. It should exhibit low sensitivity to environmental
pediatric patients.
conditions such as temperature and humidity.
7. Allow high drug loading.
8. Stability of drug is improved as compared to oral dosage
forms like suspensions.
9. Disintegrates rapidly which may result in rapid release of
drugs.
10. High production capacity as compared to suspensions.
Properties of Orodispersible tablets 10
1. No need of water for oral administration.
2. Should have adequate taste-masking properties.
3. Pleasant mouth-feel properties, adequate hardness.
4. Leave little or no residue in mouth after oral
administration.
Figure 1: Showing process of fast drug release involving
5 It should be compatible with taste masking. superdisintegrants.

Table 1: Common reasons and conditions for using ODT 12


Medication type Indication
Fast – acting Pain , fever, heartburn, diarrhoea, migraine, anxiety, insomnia
Parkinson’s disease, Alzheimer’s disease, psychosis, Schizophrenia, Hypertension,
Compliance critical
Cholesterol, Transplantation
Paediatric Cough/cold/allergy, Pain, fever, ADHD

Mechanisms of fast dissolving tablets 3. There are some under mentioned mechanisms by which
the tablet is broken down into the smaller particles and then
To achieve the tablets fast dissolving properties: subsequently result a solution or suspension of the drug.
1. Water must quickly enter into the tablet matrix to cause The mechanisms are
rapid disintegration and instantaneous dissolution of the
tablet. •High swellability of disintegrants
2. Incorporation of an appropriate disintegrating agent or •Chemical reaction
highly water soluble excipients in the tablet formulation.
•Capillary action

• COLOUR • LUBRICANT
• FLAVOR • GLIDANT
• SWEETENER • ANTIADHESIVES

ORGANOLEPTIC
PROCESS AIDS
PROPERTIES

EXCIPIENTS

DOSE
ACCURACY DRUG RELEASE
AND OTHER
EXCIPIENTS

• FILLERS • SUPERDISINTEGRAN
• SURFACE ACTIVE TS
AGENTS • NATURAL
• POLYMERS WITH TASTE • SYNTHETIC
MASKING • CO-PROCESSED

Figure 2: Classification of excipients used in orodispersible tablets13

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Gandhi et al Journal of Drug Delivery & Therapeutics. 2019; 9(2):507-513

Superdisintegrants 5) Particle repulsive forces


6) Deformation recovery
Disintegrating agents are substances routinely included in 7) Enzymatic reaction
the tablet formulations to aid in the break-up of the
compacted mass into the primary particles to facilitate the
dissolution or release of the active ingredients when it is put
into a fluid environment. They endorse moisture penetration
and dispersion of the tablet matrix. The major function of
disintegrants is to oppose the efficiency of the tablet binder
and physical forces that act under compression to structure
the tablet.
Recently new materials termed as “superdisintegrants” have
been developed to improve the disintegration processes. 14
Superdisintegrants are another version of super-absorbing
materials with tailor-made swelling properties. These
materials are not planned to absorb significant amounts of
water or aqueous fluids, but planned to swell very fast.
Superdisintegrants are used as a structural weakener for the
disintegrable solid dosage forms. They are physically
dispersed within the matrix of the dosage form and will Figure 3: Disintegration mechanism of
expand when the dosage form is exposed to the wet superdisintegrant materials
environment. 15 These newer substances are more effective Swelling:
at lower concentrations with greater disintegrating
efficiency and mechanical strength. Superdisintegrants are Although water penetration is a necessary first step for
generally used at a low level in the solid dosage form, disintegration, swelling is probably the most widely accepted
typically 1 - 10 % by weight relative to the total weight of the mechanism of action for tablet disintegrants. Particles of
dosage unit. Their particles are generally small and porous, disintegrants swell on coming in contact with suitable
which allow for rapid tablet disintegration in the mouth medium and a swelling force develops which leads to break-
without an objectionable mouth-feel from either large up of the matrix. Tablets with high porosity show poor
particles or gelling. The particles are also compressible disintegration due to lack of adequate swelling force. On the
which improves tablet hardness and its friability. Effective other hand, sufficient swelling force is exerted in the tablet
superdisintegrants provide improved compressibility, with low porosity. It is worthwhile to note that if the packing
compatibility and have no negative impact on the mechanical fraction is very high, fluid is unable to penetrate in the tablet
strength of formulations containing high-dose drugs. and disintegration is again slows down.
Generally, one gram of superdisintegrant absorbs 10-40 g of
Porosity and capillary action (Wicking):
water or aqueous medium. After absorption, swelling
pressure and isotropic swelling of the superdisintegrants Effective disintegrants that do not swell are believed to
particles create stress concentrated areas where a gradient impart their disintegrating action through porosity and
of mechanical properties will exist due to which whole capillary action. Tablet porosity provides pathways for the
structure will break apart.15 penetration of fluid into tablets. When we put the tablet into
suitable aqueous medium, the medium penetrates into the
Selection of Superdisintegrants 16, 17
tablet and replaces the air adsorbed on the particles, which
Since superdisintegrant is used as an excipient in the tablet weakens the intermolecular bond and breaks the tablet into
formulation, it has to meet certain criteria other than its fine particles. Water uptake by tablet depends upon
swelling properties. The requirement placed on the tablet hydrophilicity of the drug/excipient and on tableting
disintegrants should be clearly defined. The ideal conditions. For these types of disintegrants maintenance of
disintegrants should have: porous structure and low interfacial tension towards
aqueous fluid is necessary which helps in disintegration by
1. Poor solubility. creating a hydrophilic network around the drug particles.
2. Poor gel formation. Fig. 4 shows the disintegration of tablet by swelling and
wicking mechanism.
3. Good hydration capacity.
4. Good moulding and flow properties.
5. No tendency to form complexes with the drugs.
6. Good mouth feel.
7. It should also be compatible with the other excipients and
have desirable tableting properties.
Mechanism of Superdisintegrants: 18, 19, 20, 21, 22
Superdisintegrants are used to improve the efficacy of solid
dosage forms. This is achieved by various mechanisms. The
mechanism by which the tablets are broken into small pieces
and then produces a homogeneous suspension is based on:
1) Swelling
2) Porosity and capillary action (Wicking)
3) Heat of wetting Figure 4: disintegration of tablets by swelling and wicking
4) Chemical reaction (Acid-Base reaction) mechanism
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Gandhi et al Journal of Drug Delivery & Therapeutics. 2019; 9(2):507-513

Heat of wetting
When disintegrants with exothermic properties get wetted, Such a phenomenon may be an important aspect of the
localized stress is created due to capillary air expansion, mechanism of action of disintegrants such as Crospovidone
which aids in disintegration of tablet. This explanation, and starch that exhibit little or no swelling. Fig. 5 illustrates
however, is limited to only a few types of disintegrants and the repulsion and deformation mechanism in tablet
cannot describe the action of most modern disintegrating disintegration.
agents.
Enzyme reaction
Chemical reaction (acid base reaction)
Enzymes present in the body also act as disintegrants. These
The tablet is quickly broken apart by internal liberation of enzymes dearth the binding action of binder and helps in
CO2 in water due to interaction between tartaric acid and disintegration. Due to swelling, pressure is exerted in the
citric acid (acids) with alkali metal carbonates or outer direction that causes the tablet to burst or the
bicarbonates (bases) in presence of water. The tablet accelerated absorption of water leads to an enormous
disintegrates due to generation of pressure within the tablet. increase in the volume of granules to promote disintegration.
Due to liberation in CO2 gas, the dissolution of active
pharmaceutical ingredients in water as well as taste masking Type of Superdisintegrant and their example
effect is enhanced. As these disintegrants are highly sensitive Two types of Superdisintegrant:
to small changes in humidity level and temperature, strict
control of environment is required during preparation of the A) Synthetic superdisintegrant
tablets. The effervescent blend is either added immediately B) Natural superdisintegrant
prior to compression or can be added in two separate
fraction of formulation. The effervescent blend is added A) Natural superdisintegrant
immediately prior to compression or can be added into two These superdisintegranting agents are natural in origin and
separate fraction of formulation. are preferred over synthetic substances because they are
Particle repulsive forces/ due to disintegrating particle comparatively cheaper, abundantly available, non-irritating
and nontoxic in nature. The natural materials like gums and
This is another mechanism of disintegration that attempts to mucilage’s have been extensively used in the field of drug
explain the swelling of tablet made with non-swellable delivery for their easy availability, cost effectiveness, Eco
disintegrants. According to Guyot-Hermann’s particle- friendliness, emollient and non-irritant nature, non-toxicity,
particle repulsion theory, water penetrates into tablet capable of multitude of chemical modifications, potentially
through hydrophilic pores and a continuous starch network degradable and compatible due to natural origin. There are
is created that can convey water from one particle to the several gums and mucilage’s are available which have super-
next, imparting a significant hydrostatic pressure. The water disintegrating activity.
then penetrates between starch grains because of its affinity
for starch surfaces, thereby breaking hydrogen bonds and Mucilages as Superdisintegrants
other forces holding the tablet together. The electric Plantago ovata Seed Mucilage (Isapgula)
repulsive forces between particles are the mechanism of
disintegration and water is required for it. Researcher found Isapghula consists of dried seeds of the plant Plantago ovata
that particle repulsion force is secondary to wicking. and it contains mucilage which is present in the epidermis of
the seeds. The seeds of Plantago ovata were soaked in
Deformation Recovery: distilled water for 48 hrs and then boiled for few minutes for
Deformation recovery theory implies that the shape of complete release of mucilage into water. The material was
disintegrant particles is distorted during compression and squeezed through muslin cloth for filtering and separating
the particles return to their pre-compression shape upon out the marc. Then, an equal volume of acetone was added to
wetting, thereby this increase in size of the deformed the filtrate so as to precipitate the mucilage. The separated
particles causing the tablet to break apart. mucilage was dried in oven at temperature less than 60°C.
The mucilage of Plantago ovata is a recent innovation for its
superdisintegration property when compared with
Crosspovidone. It shows faster disintegration time than the
superdisintegrant, Crosspovidone.
Lepidium sativum Mucilage
Lepidium sativum (family: Cruciferae) is known as asaliyo
and is widely used as herbal medicine in India. It is widely
available in market and has very low cost. Parts used are
leaves, root, oil, seeds etc. Seeds contain higher amount of
mucilage, dimeric imidazole alkaloids lepidine B, C, D, E and
F and two new monomeric imidazole alkaloids
semilepidinoside A and B. Mucilage of Lepidium sativum has
various characteristic like binding, disintegrating, gelling.
Gum Karaya
Gum Karaya is a negative colloid and a complex
polysaccharide of high molecular weight. On hydrolysis it
yields galactose, rhamnose and galacturonic acid. Gum
Karaya occurs as a partially acetylated derivative. It is a
Figure 5: Disintegration of tablets by repulsion and dried exudation of Sterculia Uren tree (Family-
deformation Sterculiaceae). Its synonyms are Karaya, sterculia, Indian
tragacanth, Bassora tragacanth, kadaya, Kadira, katila. Gum
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Gandhi et al Journal of Drug Delivery & Therapeutics. 2019; 9(2):507-513

Karaya is compatible with other plant hydrocolloids as well side chain. Carboxymethylation as well as
as proteins and carbohydrates. carbamoylethylation of Cassia gum is reported to improve
cold water solubility, improve viscosity and increase
Fanugreek Seed Mucilage
microbial resistance as compared to native gum Therefore,
Trigonella Foenum-graceum, commonly known as an attempt was made to incorporate calcium or sodium salts
Fenugreek, is an herbaceous plant of the leguminous family. of carboxymethylated or carbamoylethylated C. fistula gum
It has found wide applications as a food, a food additive, and as superdisintegrant in the formulation development of FDT.
as a traditional medicine. The leaves and both the ripe and
Locust Bean gum
unripe seeds of Trigonella Foenum-graceumare used as
vegetables. Fenugreek has been used in treating colic Locust bean gum is extracted from the endosperm of the
flatulence, dysentery, diarrhea, dyspepsia with loss of seeds of the carob tree Ceretonia siliqua, which grows in
appetite, chronic cough, dropsy, enlargement of liver and Mediterranean countries. It is also called Carob bean gum.
spleen, rickets, gout, and diabetes. It is also used as gastro Some other familiar polysaccharides are starch and cellulose,
protective, antiurolithiatic, diuretic, antidandruff agent, Anti- which are made of long chains of the sugar glucose. In locust
inflammatory agent and as antioxidant. The seed is stated to bean gum, the ratio of mannose to galactose is higher than in
be a tonic. It also is used in post-natal care and to increase guar gum, giving it slightly different properties, and allowing
lactation in nursing mothers. Fenugreek seeds contain a high the two gums to interact synergistically so that together they
percentage of mucilage (a natural gummy substance present make a thicker gel than either one alone. It shows as a binder
in the coatings of many seeds). Although it does not dissolve and as a disintegrants property at different concentration.
in water, mucilage forms a viscous tacky mass when exposed Pharmaceutical application of locust bean gum in various
to fluids. Like other mucilage-containing substances, novel drug delivery systems. Locust bean gum has been
fenugreek seeds swell up and become slick when they are widely used in food industry as a thickening and gelling
exposed to fluids. The resulting soft mass is not absorbed by agent. Locust bean gum has also been reported to have
the body, but instead passes through the intestines and bioadhesive and solubility enhancement properties. There
triggers intestinal muscle contractions. are various reports that Locust bean gum can be used in
pharmaceutical and biotechnological purpose.
Guar gum
Hibiscus rosa-sinensis Linn. Mucilage
Guar gum is a galactomannan, commonly used in cosmetics,
food products and in pharmaceutical formulations. Guar gum Hibiscus rosa-sinensis Linn of the Malvaceae family is also
is mainly consisting of the high molecular weight known as the shoe‐flower plant, China rose, and Chinese
(approximately 50,000-8,000,000) polysaccharides hibiscus. The plant is available in India in large quantities
composed of galactomannans and is obtained from the and its mucilage has been found to act as a
endosperm of the seed of the guar plant, Cyamopsis superdisintegrant. The plant contains cyclopropanoids,
tetragonaloba (L) Taub (Synonym-Cyamopsispsoraloides). It methyl sterculate, methyl‐2‐ hydroxysterculate,
is used as thickener, stabilizer and emulsifier, and approved 2‐hydroxysterculate malvate and β‐rosasterol. The leaves
in most areas of the world (e.g. EU, USA, Japan, and contain carotene (7.34 mg/100 g of fresh material) moisture,
Australia). Its synonyms are Galactosol; guar flour; jaguar protein, fat, carbohydrate, fibers, calcium, and phosphorus.
gum; meprogat; meyprodor. It has also been investigated in Mucilage of Hibiscus rosa-sinensis contains L‐rhamnose,
the preparation of sustained release matrix tablets in the D‐galactose, D‐-galactouronic acid, and D‐glucuronic acid.
place of cellulose derivatives such as methylcellulose. In
Mango Peel Pectin
pharmaceuticals, guar gum is used in solid-dosage forms as a
binder and disintegrant, and in oral and topical products as a Dried mango peel powder is use for extracting pectin. Rather
suspending, thickening, and stabilizing agent, and also as a mango peel pectin cannot be used for promising the
controlled-release carrier. Guar gum has also been examined behavior of superdisintegrants, but due to its good swelling
for use in colonic drug delivery. index and good
Cassia fistula gum solubility in biological fluids it can be used to prepare fast
dispersible tablets (Shihora H & Panda S, 2011; Mangal M et
Seeds of Cassia fistula gum obtained from Cassia fistula tree.
al., 2012). Various Natural Superdisintegrant along with
Gum obtained from the seeds of Cassia fistula comprises β-
different drugs and method adopted for their preparation as
(1→4) linked d-mannopyranose units with random
described in table 2.
distribution of α (1→6) linked d-galactopyranose units as

Table 2: A list of natural Superdisintegrants used in formulation


Name of drug Superdisintegrants Method of compression
Glimepride Ocimum tenuiflorum Direct compression
Lisinopril Plantago Ovata mucilage, Alovera mucilage, Mucilage of hibiscus rosasinesis Direct compression
Nimesulide Lipidium sativum (Cruceferae) Direct compression
Ondensetron HCl Plantago ovate husk Direct compression
Fexofenadine HCl Plantago ovate mucilage, Seed Direct compression

Synthetic Superdisintegrants: Cross-linked polyvinyl Pyrrolidone (Crospovidone):


Synthetic super- disintegrants are frequently used in tablet Unlike other superdisintegrants, which rely principally on
formulations to improve the rate and extent of tablet swelling for disintegration, crospovidone use a combination
disintegration thereby increasing the rate of drug of swelling and wicking. Due to its high crosslink density,
dissolution. The most widely used synthetic crospovidone swells rapidly in water without gelling.
superdisintegrants are illustrated below. Crospovidone particles are found to be granular and highly
porous which facilitates wicking of liquid into the tablet and
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particles to generate rapid disintegration. Larger particles made by crosslinking of potato starch as it gives the product
provide a faster disintegration than smaller particles. with the best disintegrating properties 31. The degree of
Crospovidone disintegrants are highly compressible cross-linking and substitution are important factors in
materials as a result of their unique particle morphology. determining the effectiveness of these materials as
Crospovidone can also be used as solubility enhancer. It is superdisintegrants 30. The effect of the crosslinking is to
available in two particle sizes in the form of Polyplasdone XL reduce both the water soluble fraction of the polymer and
and Polyplasdone XL-10. the viscosity of dispersion in water. The natural predried
starches swell in water to the extent of 10-20 percent and
Croscarmellose Sodium:
the modified starches increase in volume by 200-300
It is an internally cross linked polymer of carboxymethyl percent in water.
cellulose sodium. It has high swelling capacity with minimal
The mechanism by which this action takes place involves
gelling resulting in rapid disintegration. Due to fibrous
rapid absorption of water leading to an enormous increase in
structure, croscarmellose particles also show wicking action.
volume of granules that result in rapid and uniform
In tablet formulations, croscarmellose sodium may be used
disintegration. These are available as explotab and primogel
in both direct compression and wet-granulation processes. which are low substituted carboxy methyl starches 24. The
When used in wet-granulation, the croscarmellose sodium
effect of introduction of the large hydrophilic carboxymethyl
should be added in both the wet and dry stages of the
groups is to disrupt the hydrogen bonding within the
process (intra- and extra-granularly) so that the wicking and
polymer structure. This allows water to penetrate the
swelling ability of the disintegrant is best utilized.
molecule and the polymer becomes cold water soluble 30.
Sodium Starch Glycolate: Table 3 shows a brief description on properties of synthetic
superdisintegrants.
Sodium Starch Glycolate is the sodium salt of a
carboxymethyl ether of starch. These are modified starches

Table 3: Characteristics of synthetic superdisintegrants employed in formulation of ODTS 23, 24, 25


Synthetic Superdisintegrants Properties Effective Concentration for disintegration
It is completely insoluble in water. Rapidly
disperses and swells in water. Greatest rate of
swelling compared to other disintegrants. It is used in the range of 1-3% w/w.
Greater surface area to volume ratio than other
disintegrants. Available in micronized grades if
Crospovidone needed for improving state of dispersion in the
powder blend. Swelling index- 58±1.5% v/v.
It is insoluble in water, although it rapidly swells It may be used as a tablet disintegrant at
to 4-8 times its original volume on contact with concentration upto 5% w/w, although
water. Specific surface area- 0.81-0.83 m2/g. normally 2 % w/w is used in tablets
Croscarmellose sodium
Swelling index- 65±1.7% v/v. prepared by direct compression and 3 %
w/w in tablets prepared by wet-granulation
process.
Absorbs water rapidly, resulting in swelling up It is used in the range of 4-6%. Above 8%,
to 6%. High concentration causes gelling and loss disintegration times may actually increase
Sodium starch glycolate
of disintegration. Swelling index- 52±1.2% v/v. due to gelling and its subsequent viscosity
producing effects.

Advantages of Synthetic Superdisintegrants: as a better alternative to overcome the shortcomings of these


superdisintegrants.
 Effective in lower concentrations than starch.
CONCLUSION
 Less effect on compressibility and flow ability.
With the increase demand of novel drug delivery, the fast
 More effective intragranularly. However, there are a disintegrating drug delivery system has become one of the
number of limitations that superdisintegrants mile stone of present investigations. Although, there are
practically impose in pharmaceutical applications. For many superdisintegrants, the search for newer
example More hygroscopic (may be a problem with disintegrating agents is ongoing and researchers are
moisture sensitive drugs) experimenting with modified natural products like formalin
Some are anionic and may cause some slight in-vitro binding casein, chitin, chitosan, polymerized agar acrylamide, xylan,
with cationic drugs (not a problem in-vivo) [26]. An acidic smecta, key-jo-clay, crosslinked carboxymethyl guar, mango
medium significantly reduces the liquid uptake rate and peel pectin, cassia tora, cassia nodosa and modified tapioca
capacity of sodium starch glycolate and croscarmellose starch etc. Studies have suggested that the water insoluble
sodium, but not crospovidone. The degree of swelling of superdisintegrants show better disintegration property than
Primojel1 (sodium starch glycolate) and Polyplasdone XL101 the slightly water soluble agents, since they do not have a
(crospovidone) is minimized following wet granulation tendency to swell. The comparative studies concluded that
formulation. Finally, the medium ionic strength was found to the use of Natural Superdisintegrant is more advantageous
have an adverse effect on the swelling capacity of over the synthetic superdisintegrants in the formulation of
croscarmellose. Therefore, natural superdisintegrants serve Orodispersible Tablets.

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Gandhi et al Journal of Drug Delivery & Therapeutics. 2019; 9(2):507-513

The use of Natural superdisintegrants serves as a best 15. Omidian H and Park K, Swelling agents and devices in
alternative in the formulation of Fast dissolving tablets. oral drug delivery, Journal of Drug Delivery Science and
Technology 2008; 18 (2): 83-93.
REFERENCES
16. Iyad R, Mayyas AR, Eftaiha AA and Badwan A, Chitin-
1. Chein YW, Oral drug delivery and delivery systems. 2nd silicon dioxide coprecipitate as a novel superdisintegrants,
ed, New York: Marcel Dekker; 2015. Journal of Pharmaceutical Sciences 2008; 97(11):4955-69.
2. Lindgren S, Janzon L. Dysphagia, Prevalence of swallowing 17. Uddhav S Bagul, (2006), Current status of tablet
complaints and clinical finding. Med Clin North Am 2014; disintegrants: a review, Retrieved March 5, 2011 from
77:3-5. Pharmainfo.net.
3. Fu Y, Yang S, Jeong SH, Kimura S, Park K. Orally fast http://www.pharmainfo.net/reviews/current-status-tablet-
disintegrating tablets, Developments, technologies, taste- disintegrantsa-review
masking and clinical studies. Crit Rev Ther Drug Carrier 18. Konapure AS, Chaudhari PS, Oswal RJ, Kshirsagar SS,
System, 2014; 21:433-76. Antre RV and Chorage TV, Mouth dissolving tablets-an
4. Bandari S, Mittapalli RK, Gannu R, Rao YM. Orodispersible innovative technology. International Journal of Applied
tablets, An overview. Asian J of Pham. 2009; 2:2-11. Biology and Pharmaceutical Technology, 2011; 2(1):496-
503.
5. Habib W, Khankari RK, Hontz J, Fast dissolve drug delivery
systems. Crit Rev Ther Drug Carrier Syst 2015; 17:61-72. 19. Pahwa R, Piplani M, Sharma PC, Kaushik D and Nanda S:
Orally disintegrating tablets, friendly to pediatrics and
6. Brown D, Orally disintegrating tablets-taste over speed, geriatrics. Archives of Applied Science Research, 2010;
Drug Del Technol 2012; 3:58-61 2(2):35-48.
7. Seager H, Drug delivery products and Zydis fast-dissolving 20. Bhatt P, Khatri N, Kumar M, Baradia D, Misra A.
forms, J Pharm Pharmacol 2014; 50:375-82. Microbeads mediated oral plasmid DNA delivery using
8. Behnke K, Sogaard J, Martin S, Bauml J, Ravindran AV, polymethacrylate vectors: an effectual groundwork for
Agren H. Mitrazapine orally disintegrating tablet versus colorectal cancer. Drug delivery. 2015; 22(6):849-61.
sertraline, A prospective onset of action study, J Clin 21. Bhowmik D, Chiranjib B, Yadav J, Chandira RM and
Psychopharmacol 2013; 23:358-64. Kumar S, Emerging trends of disintegrants used in
9. Clarke A, Brewer F, Johnson ES, Mallard N, Hartig F, Taylor formulation of solid dosage form. Scholars Research Library
S, et al, A new formulation of selegilline, Improved Der Pharmacia Lettre 2010; 2 (1):495-504
bioavailability and selectivity for MAO-B inhibition, J Neural 22. Mohanachandran PS, Sindhumol PG and Kiran TS:
Transm 2014; 110:1241-55. Superdisintegrants: an overview. Journal of Pharmaceutical
10. Bradoo, R, Fast dissolving drug delivery systems, JAMA Sciences Review and Research, 2011; 6(1):105-109
India, 2013; 4(10):27-31. 23. Raymond CR, Handbook of Pharmaceutical Excipients,
11. Kuchekar, B., Atul, S., Badhan, C., Mahajan, HS, Mouth APhA Publishers, Fifth Edition, 2008.
Dissolving Tablets: A novel drug delivery system, 24. Goel H, Rai P, Rana V and Tiwary AK, Orally
Phramaceutics, 2012, 35:7-9. disintegrating systems, innovations in formulation and
12. Harmon TM. Orally Disintegrating Tablets: a valuable life technology. Recent Patents on Drug Delivery & Formulation,
cycle Management Strategy”. Pharmaceutical commerce, 2014; 2:258-274.
march 2007, available online 25. GK Bolhuis, AW Arends-Scholte, GJ Stuut and JA de Vries,
www.pharmaceuticalcommerce.com. Disintegration efficiency of sodium starch glycolates
13. Loyd VA, Nicholas GP, Ansel HC, Ansel's pharmaceutical prepared from different native starches, European Jounal of
dosage forms and drug delivery systems. Edn 9, Wotters Pharmaceutics and Biopharmaceutics, 2015; 40(5):317 –
Kluwer (India) Pvt Ltd, New Delhi, 2014, 300-15. 320.

14. Belet MH and Derle DV, Analysis of patents pertaining to 26. Tandel H, Bhatt P, Jain K, Shahiwala A, Misra A. In-Vitro
superdisintegrants used in tablet manufacturing, Journal of and In-Vivo Tools in Emerging Drug Delivery Scenario:
intellectual Property Rights, 2008; 13:601-604. Challenges and Updates. In: Misra ASA, editor. In-vitro and
in-vivo tools in drug delivery research for optimum clinical
outcomes. Boca Raton: CRC Press; 2018.

ISSN: 2250-1177 [513] CODEN (USA): JDDTAO

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