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THE KIND OF

DISINTERGRANT

Amalia Dwi Ayuningtyas (1800023086)


01 Definition of Disintegrant

02
Mechanism of Tablet Disintegrants

03
Types of Disintegrant

04
Advantages and Disadvantages
“ The Disintegrant is added to most of the preparation
to encourage a break up of the tablet when it comes in contact
with water in the stomach. Tablet fragmentation may be critica
l for dissolution of drug and attainment of drug bio-availability.
The distinegranting agents may be mixed at two stages :
1. During the formation of granules, prior to wetting with the granul
ating fluid and is known intra-granular. It break down the granules
giving a finer product.
2. During compaction of granules into tablets. It cause tablet to disi-
ntegrate quickly into granules.

Mechanism of Tablet Disintegrants
DUE TO RELEASE OF GASES
BY CAPILLARY ACTION
01 04 Carbon-dioxide released o wetting within tablets due
The tablet is placed in a suitable aqueous medium,
to interaction between carbonates and bicarbonates
then the medium penetrates into the tablet and rep
with citric acid. In this pressure is generated and is
lace the air adsorbed on the particles, which weak
used to formulate very rapidly dissolving tablet and
ens the inter-molecular bond and finally tablet is br
are highly sensitive to small changes in humidity level
eaks into fine powder.
and temperature.
BY SWELLING
02 The mostly used general mechanism of action for
tablet disintegration is swelling tablets with high porosi
05 BY ENZYMATIC REACTION
Enzymes present in the body act as disintegrants.
ty show poor disintegration due to lack of swelling forc These enzymes destroy the binding action of binders
e. If the packing fraction is very high, fluid is unable to and help in breaking of tablet.
enter in the tablet and disintegration is again slow. Enzim :
AIR EXPANSION - Selulase
03 When disintegrants with exothermic properties gets
- Amilase
- Protease
wet and, localized stress is generated due to capilla
ry air expansion.
Types of Disintegrant
1. STRACH

• It is widely used in tablet manufacturing and also have the lowest cost. However, native starches have cer
tain limitation and is replaced by modified starches.
• Starch used in concentration of 5-20% of the total weight.
• Modified starches are Primogel and Explotab, which are low substituted carboxymethyl starches and is us
ed in lower concentration of 1-8%.
• Pre-gelatinized starches are also used in 5-10% concentration. The main mechanism of action is through
swelling and it is directly compressible

2. ALGINATES
• They are hydrophillic colloidal substances which has high sorption capacity.
• It is insoluble in water and is slightly acidic in reaction, so, it is only used in acidic and neutral granulation.
Types of Disintegrants

3. ION EXCHANGE RESIN

• It has highest water uptake capacity than other and has a tendency to adsorb certain drugs.

4. MICRO CRYSTALLINE CELLULOSE

• It has very good disintegrant properties and also serves as excellent binder.Sometimes, it causes separ
ation in granulation. To overcome this problem, removal of moisture by drying of cellulose is done.
• It is also an effective tablet disintegrant when used in a concentration of between 10-20%.
Super Disintegrants
Because of the increased demands for faster dissolution requirements, there are no
w available, a new generation of “Super Disintegrants” in addition to the disintegran
ts discussed earlier.

Three major groups of compounds have been developed which swell to many times th
eir original size when placed in water while producing minimal viscosity effects:

01 Modified Starches

• Sodium Carboxymethyl Starch (Chemically treated Potato Starch)


• Mechanism of Action: Rapid and extensive swelling with minimal gelling.
• Effective Concentration: 4-6%. Above 8%, disintegration times may actually increase due to gelling and its
subsequent viscosity producing effects.
Super Disintegrants
02 Cross-linked polyvinylpyrrolidone

• Water insoluble and strongly hydrophilic.


• Mechanism of Action: Water wicking, swelling and possibly some deformation recovery.
• Effective Concentration: 2-4%

03 Modified Cellulose

• Internally cross-linked form of Sodium carboxymethyl cellulose.


• Mechanism of Action: Wicking due to fibrous structure, swelling with minimal gelling.
• Effective Concentrations: 1-3% (Direct Compression), 2-4% (Wet Granulation)
Advantages & Disadvantages of Super Disintegrants

• More hygroscopic (may be a problem with moisture sen


sitive drugs)
• Some are anionic and may cause some slight in-vitro bi
nding with cationic drugs (not a problem in-vivo.)
Disadvantages

Adavantages
• Effective in lower concentrations than starch
• Less effect on compressibility and flow ability
• More effective intragranularly
Thank you