Factor affecting the strength of the tablets.ppt

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About This Presentation

various factors affecting strength of tablets


Slide Content

A seminar on A seminar on
compaction and compressioncompaction and compression

Presented By:-Presented By:-
Sureja Sunil B.Sureja Sunil B.
11
stst
M.Pharm M.Pharm
Dept. of Dept. of
PharmaceuticsPharmaceutics
PESCPPESCP
Bangalore-50Bangalore-50

Facilitated By:-Facilitated By:-
Dr. UmadeviDr. Umadevi
Asst. ProffesorAsst. Proffesor
Dept. of Dept. of
pharmaceuticspharmaceutics
PESCPPESCP
Bangalore-50Bangalore-50

Factor affecting the strength of Factor affecting the strength of
the tablets:-the tablets:-
1.1.Particle sizeParticle size
2.2.Moisture contentMoisture content
3.3.LubricantsLubricants
4.4.Applied pressureApplied pressure

1.1.Particle size:-Particle size:-
A decrease in particle size resulted in the increase A decrease in particle size resulted in the increase
in the tablet strength in the tablet strength
very large particle often exists as agglomerates of very large particle often exists as agglomerates of
small crystal on compression such as small crystal on compression such as
agglomerates , being more friable than the crystal, agglomerates , being more friable than the crystal,
breakdown in smaller units the strength of the breakdown in smaller units the strength of the
tablets prepared from such aggregates is higher. tablets prepared from such aggregates is higher.
With very fine particle , such as those produced by With very fine particle , such as those produced by
a fluid energy mill , the powder are very cohesive a fluid energy mill , the powder are very cohesive
even in the uncompressed state. On compaction even in the uncompressed state. On compaction
strong compact of tablet can be formedstrong compact of tablet can be formed . .
At a given pressure the use of a very small At a given pressure the use of a very small
particle increases the chances of grapping & the particle increases the chances of grapping & the
volume of air entrapped also increases.volume of air entrapped also increases.


general equation formed for the effect of general equation formed for the effect of
particle size is :particle size is :

Here, Here,
K= constant K= constant
a= material constant lies between (0.2 to a= material constant lies between (0.2 to
0.47)0.47)
Fc= hardness of the impactFc= hardness of the impact
d= diameter of the granuled= diameter of the granule

2. 2. moisture content:-moisture content:-
in the preparation of the pharmaceutical in the preparation of the pharmaceutical
tablet , it is generally accept that a small tablet , it is generally accept that a small
proportion of the moisture is present and in proportion of the moisture is present and in
some cases this is required to form a some cases this is required to form a
coherent tablets.coherent tablets.
Wet granulation of the powder material with Wet granulation of the powder material with
hydrophilic adhesive was shown to yield tablet hydrophilic adhesive was shown to yield tablet
whose mechanical strength is dependant on whose mechanical strength is dependant on
the optimum content above or below with the the optimum content above or below with the
tablets strength was reduced tablets strength was reduced


With the optimum moisture content there With the optimum moisture content there
is :is :
Die wall lubricationDie wall lubrication
Inter-particulate lubricationInter-particulate lubrication
Hydro-dynamic resistance to consolidationHydro-dynamic resistance to consolidation
Expression of intestinal liquid to the die wallExpression of intestinal liquid to the die wall

3. Lubrication :3. Lubrication :

Lubricating agent assist particle movement and Lubricating agent assist particle movement and
consolidation of the tablet by reducing die wall consolidation of the tablet by reducing die wall
friction. friction.
But during compression the lubricant is spread But during compression the lubricant is spread
over the surface of the particles and therefore over the surface of the particles and therefore
reduce the strength of the bond between the reduce the strength of the bond between the
particles. particles.
By proper selection of the lubricating agent and By proper selection of the lubricating agent and
adding adequate quantity of granules leads to the adding adequate quantity of granules leads to the
increase in the strength of the tablet. increase in the strength of the tablet.

4. 4. Effect of applied pressureEffect of applied pressure
 At higher forces due to fragmentation new surfaces At higher forces due to fragmentation new surfaces
are formed causing an increase in surface area, are formed causing an increase in surface area,
hence more area is available for bond formation, hence more area is available for bond formation,
hence more will be the hardness of the compacthence more will be the hardness of the compact

Fc = FcFc = Fc
00 V V
rr
-m-m
Where, Where,
Fc0 = strength of the tablet when Vr =1 (i.e. Fc0 = strength of the tablet when Vr =1 (i.e.
completely consolidated)completely consolidated)
m = is a constant for particular systemm = is a constant for particular system
(here Vr is the relative volume defined as Vr = 1/1-ε(here Vr is the relative volume defined as Vr = 1/1-ε
Where ε is the porosity of the compact Where ε is the porosity of the compact


And, shotton and Ganderton gave a general And, shotton and Ganderton gave a general
equation for the effect of applied pressure on the equation for the effect of applied pressure on the
strength of the compact.strength of the compact.

Log P = nFe + CLog P = nFe + C

Where,Where,

P= applied pressureP= applied pressure

Fe= strength of the compactFe= strength of the compact

C= constantC= constant

STUDY ON FORMULATION STUDY ON FORMULATION
ASPECT OF TABLETS SUCH ASPECT OF TABLETS SUCH
AS SUBLINGUAL, BUCCAL AS SUBLINGUAL, BUCCAL
CHEWABLE AND CHEWABLE AND
MEDICATED LOZENGESMEDICATED LOZENGES

Sublingual tabletsSublingual tablets:-:-

In addition to good adsorption, the ideal drug for In addition to good adsorption, the ideal drug for
sublingual use should be small in dose, usually sublingual use should be small in dose, usually
not more then 10 to 15 mg. not more then 10 to 15 mg.

. The ideal compound should not have any . The ideal compound should not have any
undesirable taste, since bitter or bad tasting undesirable taste, since bitter or bad tasting
compound will stimulate saliva flow. compound will stimulate saliva flow.

It will be absorbed by the highly vascular It will be absorbed by the highly vascular
mucosal lining of the mouth.mucosal lining of the mouth.


Objective:-Objective:-
1.1.Take drug for absorption directly through the Take drug for absorption directly through the
mucosamucosa
2.2.Drugs administered to produce systemic effect fast Drugs administered to produce systemic effect fast
3.3.To overcome first pass metabolism.To overcome first pass metabolism.
Two type:-Two type:-
1.1.Molded sublingual tabletMolded sublingual tablet
2. 2. Compressed sublingual tabletsCompressed sublingual tablets

Molded sublingual tablet:-Molded sublingual tablet:-

Sublingual tablets are intended to be Sublingual tablets are intended to be
placed beneath to the tongue and held placed beneath to the tongue and held
there until absorption taking place. there until absorption taking place.

They must dissolve or disintegrate quickly, They must dissolve or disintegrate quickly,
allowing the medicament to be rapidly allowing the medicament to be rapidly
absorbed, there fore, sublingual tablet are absorbed, there fore, sublingual tablet are
frequently formulated as molded tablets.frequently formulated as molded tablets.

IngredientsIngredients Quantity par tablets Quantity par tablets
1. Codeine phosphate (powder)1. Codeine phosphate (powder) 30.0mg30.0mg
2. Lactose2. Lactose 17.5 mg17.5 mg
3. Sucrose( powder) `3. Sucrose( powder) ` 1.5 mg1.5 mg
Alcohol-water (60:40)Alcohol-water (60:40)
Q.s.Q.s.
FormulationFormulation :- :-
Molded sublingual tablets are usually formulated with soluble Molded sublingual tablets are usually formulated with soluble
ingredients only, So They contain lactose, dextrose, sucrose, ingredients only, So They contain lactose, dextrose, sucrose,
mannitol or other rapidly soluble material or the mixtures of mannitol or other rapidly soluble material or the mixtures of
these ingredientsthese ingredients
To insure rapid solubility of the soluble tablets, the excipients To insure rapid solubility of the soluble tablets, the excipients
put through a fine screen or 120 mesh blotting cloth.put through a fine screen or 120 mesh blotting cloth.
Excipient:Excipient: Mainly beta-lactose is used as diluents. Mainly beta-lactose is used as diluents.
 Antioxidant-sodium sulfite, sodium tri sulfate and buffer added Antioxidant-sodium sulfite, sodium tri sulfate and buffer added
to improve physical and chemical stability of the product.to improve physical and chemical stability of the product.
Formula for codeine phosphate tablet (30 mg).Formula for codeine phosphate tablet (30 mg).

Compressed sublingual tablets:-Compressed sublingual tablets:-
compressed sub lingual tablet have been compressed sub lingual tablet have been
prepared which disintegrate quickly and allow prepared which disintegrate quickly and allow
the active ingredient to dissolve rapidly and the active ingredient to dissolve rapidly and
allow the active ingredient to dissolve rapidly allow the active ingredient to dissolve rapidly
to saliva and to be available for absorption to saliva and to be available for absorption
with out requiring the complete solution of all with out requiring the complete solution of all
the ingredient of the formula . Compared to the ingredient of the formula . Compared to
molded tablets, compressed tablets have less molded tablets, compressed tablets have less
weight variation and better content uniformity.weight variation and better content uniformity.

Ingredients Quantity par tablets
1. Nitro glycerin 3.0 mg
2. Mannitol 2.0 mg
3. Microcrystalline cellulose29.0 mg
4. Flavor Q.s.
5.sweetener Q.s.
6.coloring agent Q.s.
Formula for nitro glycerin tablets (0.3 mg) direct Formula for nitro glycerin tablets (0.3 mg) direct
compressioncompression

Buccal tablets:Buccal tablets:
The purpose of buccal tablets is the same The purpose of buccal tablets is the same
as that of sublingual tablets, i.e. Absorption as that of sublingual tablets, i.e. Absorption
of the drug through the lining of the mouth .of the drug through the lining of the mouth .
Buccal tablets are most often used when Buccal tablets are most often used when
replacement hormonal therapy is the goal.replacement hormonal therapy is the goal.
Flat, elliptical or capsule shaped tablets are Flat, elliptical or capsule shaped tablets are
usually selected for buccal tablets, since usually selected for buccal tablets, since
they can be most easily held between the they can be most easily held between the
gum and cheeks.gum and cheeks.

Formulation:-Formulation:-
Formula for methyl Formula for methyl
testosterone buccal testosterone buccal
tablets (10 mg):-tablets (10 mg):-
IngredientsQuantity par
tablets
1. Methyl
testostero
ne
10 mg
2. Lactose 86mg
3. Acacia 87mg
4.talc 10 mg
5.magnessiu
nm state
6 mg
6.water Q.s.

Chewable tablet:Chewable tablet:
Chewable tablet mean chewing in the Chewable tablet mean chewing in the
mouth prior to the swallowing and are not mouth prior to the swallowing and are not
intended to be swallowed intact .intended to be swallowed intact .
Chewable dosage form, such as soft pill, Chewable dosage form, such as soft pill,
tablets, gums, and new chewy squares .tablets, gums, and new chewy squares .
The main purpose of this formulation is to, The main purpose of this formulation is to,
more easy administration of medicament more easy administration of medicament
to the infant, children’s and old people to the infant, children’s and old people
where they face problem of swallowing.where they face problem of swallowing.


Advantage:-Advantage:-
Large tablet is difficult to Large tablet is difficult to
swallow swallow
the particle size is the particle size is
reduced in the mouth it reduced in the mouth it
also increases the also increases the
dissolution rate dissolution rate
Better bioavailability Better bioavailability
through bypassing through bypassing
disintegrationdisintegration
Patient convenience Patient convenience
patient acceptance patient acceptance
through pleasant taste through pleasant taste
and having better and having better
stabilitystability

Disadvantage:-Disadvantage:-
No suitable for the No suitable for the
drugs those are bitter drugs those are bitter
in taste & which in taste & which
irritate the mucosa of irritate the mucosa of
the mouththe mouth
These chewable These chewable
tablets may contain tablets may contain
vitamin, antacids, vitamin, antacids,
analgesics, cold analgesics, cold
remediesremedies so not so not
suitablesuitable


Formulation:-Formulation:-
In these formulations, importance is given to In these formulations, importance is given to
Amount of active substanceAmount of active substance
Flow propertiesFlow properties
Compatibility-stabilityCompatibility-stability
Organoleptic propertiesOrganoleptic properties
CompressibilityCompressibility
DisintegrationDisintegration
LubricationLubrication
Here, desired product attribute:Here, desired product attribute:

good taste and mouth feel good taste and mouth feel

Acceptable bioavailability and bioactivityAcceptable bioavailability and bioactivity

Acceptable stability and qualityAcceptable stability and quality

Economic formula and progressEconomic formula and progress


Direct compression vehiclesDirect compression vehicles:- Sucrose, :- Sucrose,
dextrose, fructose, sorbitol, mannitoldextrose, fructose, sorbitol, mannitol

Lubricant:Lubricant: magnesium, calcium salt of stearic magnesium, calcium salt of stearic
acid acid

Sweeteners:Sweeteners: Sucrose, saccharine, and mannitol Sucrose, saccharine, and mannitol

Flavoring agentFlavoring agent :- :-
•For antacids: -For antacids: - chocolate, mint, orange, vanilla, chocolate, mint, orange, vanilla,
butterscotch butterscotch
•For cough/cold: -For cough/cold: - black current, spice vanilla, wild cheery, black current, spice vanilla, wild cheery,
clove, and menthol and eucalyptusclove, and menthol and eucalyptus
•For vitamins: -For vitamins: - fresh pineapple, grape, raspberry, almond, fresh pineapple, grape, raspberry, almond,
blueberry, strawberryblueberry, strawberry


There are three types of chewable There are three types of chewable
tablets:tablets:
1.1.Multivitamin chewable tabletsMultivitamin chewable tablets
2.2.Antacids chewable tabletsAntacids chewable tablets
3.3.Analgesic chewable tabletsAnalgesic chewable tablets

Medicate Lozenges:-Medicate Lozenges:-

Lozenges are the flavored medicated dosage Lozenges are the flavored medicated dosage
forms intended to the sucked and held in the forms intended to the sucked and held in the
mouth.mouth.

. They may contain Vitamins, Antibiotic, . They may contain Vitamins, Antibiotic,
Antiseptics, Local Anesthetics, Aromatic, Anti Antiseptics, Local Anesthetics, Aromatic, Anti
Histamines, Decongestants, and Histamines, Decongestants, and
Corticosteroids, Astringent, Analgesics, And Corticosteroids, Astringent, Analgesics, And
Demulcents or combination of these Demulcents or combination of these
ingredients.ingredients.

There are 2 types of lozengesThere are 2 types of lozenges
1.1.Hard candy lozengesHard candy lozenges
2.2.Compressed tablets lozengesCompressed tablets lozenges

1.1.Hard Candy LozengesHard Candy Lozenges:-:-

It is a mixture of sugar and other It is a mixture of sugar and other
carbohydrates that are kept in amorphous carbohydrates that are kept in amorphous
or glossy condition. These are solid syrup or glossy condition. These are solid syrup
of sugar having moisture content from of sugar having moisture content from
0.5-1.5%0.5-1.5%

raw material used:raw material used:

Sugar, Corn syrup, Invert sugar, Reducing Sugar, Corn syrup, Invert sugar, Reducing
sugar, Acidulent, Flavor, Medicament:sugar, Acidulent, Flavor, Medicament:

Ingredient % used Quantity
1. Liquid sugar 67%w/w 88.90lb
2. Corn syrup 80.5% w/w 49.70lb
3. Ground candy
salvage
3.00lb
4.chlorphenirami
ne male ate
72.75gm
5. Wild cherry
flavor
72.75gm
6. Benzyl alcohol 72.75gm
7. Citric acid red (
fine granules)
3.00gm
8. Red color
cubes
10.00gm

2.2.Compressed tablet lozenges Compressed tablet lozenges
With the desired area of activity on the With the desired area of activity on the
mucous membrane of the mouth and mucous membrane of the mouth and
pharynx, are usually large diameter tablets pharynx, are usually large diameter tablets
(5/8-3/4 in.) Compressed in a weight range (5/8-3/4 in.) Compressed in a weight range
of 1.5 to 4.0 gm and formulated with a goal of 1.5 to 4.0 gm and formulated with a goal
of slow, uniform and smooth disintegration of slow, uniform and smooth disintegration
or erosion over an extended time period (5 or erosion over an extended time period (5
to 10 min)to 10 min)
Raw materialRaw material :- Tablet base, binder, flavor, :- Tablet base, binder, flavor,
colors, lubricants, and medicaments colors, lubricants, and medicaments

Formulation:-Formulation:-
Wet granulation techniqueWet granulation technique
Ex. Anti tussive Anesthetic lozengesEx. Anti tussive Anesthetic lozenges
Ingredients Quantity
1. Dextromethorphen hbr-
10% adsorb ate
4.0 %
2. Benzocaine 2.0%
Filler
1. Confectioners sugar 6(3%
corn starch)
53.0%
2. Polyethylene
glycol6000(powdered)
15.0 %