TABLET

Definition of Tablet: - Tablet is a defined as a compressed solid dosage form

containing medicament with or without excipients.

Or,

According to IP “Pharmaceutical tablets are solid, flat or biconvex dishes, unit

dosages form, prepared by compressing a drugs or a mixture of drugs, with or
without excipients.

Advantage:-

1. Unit dosage form

2. Microbial contamination low
3. Easy to performulate
4. High stability
5. Cost low & easy transport

Disadvantage:-

1. Bioavailability are low

2. Disintegration time is high
3. Not suitable for children or unconscious patients
4. Low solubility
5. Low permeability

Different types of Tablet:-

1. On the basis of route of administration

(A) Tablet ingested orally:
(i) Compressed tablet- e.g. Paracetamol tablet
(ii) Multiple compressed tablet-
(iii) Sugarcoated tablet- e.g. Multivitamin tablet
(iv) Film coated tablet- e.g. Metronidazole tablet
(v) Chewable tablet- e.g. Antacid tablet
(B) Tablet used in oral cavity:-
(i) Buccal tablet- e.g. Vitamin –C tablet
(ii) Sublingual tablet- e.g. Vicks, menthol tablet
(iii) Troches or lozenges
(iv) Dental cone

(C) Tablet administrated by other route:-

(i) Suppositories or Inserts- e.g. Clortrimazole tablet
(ii) Implantation tablet

(D) Tablet used to prepared solution:-

(i) Effervescent tablet- e.g. Disprin tablet ( Aspirin)
(ii) Dispensing tablet – e.g. Enzyme tablet (Digiplex)
(iii) Hypodermic tablet
(iv) Tablet triturates- e.g. Enzymes

2. On the basis of drug release tablet:

(i) Immediate release tablet
(ii) Modified release tablet
(iii) Extended release tablet
(iv) Delayed release tablet

3. On the basis of method of manufacturing:

(i) Compressed tablet
(ii) Molded tablet

Excipients are used for tablets formulation:

In addition to active pharmaceutical ingredients is API (Drugs), Tablet contain a
number of inert material are known as additives or Excipients.

1. Diluents: - The diluents is needed to increase the bulk when quantity of

medicament is very small in each tablet. E.g. Lactose, sucrose, sodium
chloride, mannitol etc...
2. Binding agents: - These substance or agents is a material used to form
materials into a cohesive whole, as means provide binding stability to each
other. E.g. Gum, tragacanth, methyl cellulose etc...
3. Disintegrating agents: - are the substances which are generally used in the
formulation to breakdown the tablet into a small particle. E.g. Starch, clays
(Bentonite), cellulose derivative etc…
4. Glidants: - to improve the flow properties of granules. E.g. Talc, corn starch,
etc…
5. Lubricants: - To reduce the interparticle friction during compression and
between tablet and die wall during ejection of tablet. E.g. Magnesium
stearate, stearic acid, talc, etc…
6. Sweetening agents- e.g. Mannitol, sugar, fructose, etc…
7. Coloring agents: - all coloring agents must be approved and certified by FDA.
E.g. FD&C yellow 6- sunset yellow, Green3- Fast green, etc…

Tablet formulation Method

There are two general methods of tablet preparation.

1. Direct Compression
2. Granulation Method

Direct Compression: - this method can be classified as basically mixing and

processing of formulation ingredients than compressing into tablets.

There are Two types of direct compression method:-

1. Powder Compression: suitable for drugs that are sensitive to moisture
and heat, fill material possessing, good flowbility and compressibility.
2. Crystal Compression: suitable for drugs with proper crystal form and
good flowbility.

Process:-
Raw Material Weighing Screening Mixing Compression

Advantage: - Stability good, cost effective, fast dissolution, etc…

Granulation Method: - may be defined as a size enlargement process which
convert small particle into stronger, larger, uniform.

There are two important different types of granulation method:-

1. Dry Granulation
2. Wet Granulation

Dry Granulation: - suitable for drugs that are sensitive in moisture and heat.

Process: - Raw material weighing screening mixing slugging

Milling/Screening Mixing Compression

Uses: - Slugging compression machine- Chilsonator roller compactor

Wet Granulation: - suitable for drugs that are stable to moisture and heat.

Process:-

Raw material Weighing Screening Mixing Wet massing

Milling Drying Milling/Screening Mixing Compression

Compression Machine
Tablets are made by the drug & excipients on stamping machine called Presses.
Tablet compression machine or tablet presses are designed with the following
component.

1. Hopper: - for holding the granules.

2. Dies: - define the size & shape of tablet.
3. Punches: - compress the granules within a dies.
4. Cam tracks: - guiding the movement of the punches.
5. Feeding machine: - moving granules from hopper to the die cavity.
Tablet presses are classified:-

1. Single punch
2. Multi-station Rotary Presses.

Compression Machine Tooling:-

Tooling types Punch diameter(mm) Die diameter(mm)/inch

B 19 30.5 / 1.187
BB 19 24 / 0.945
D 25.4 38.1 / 1.50
DB 25.4 30.15 / 1.187
Note: - The dies and punches and their setup on compression machine is called
Tooling.

Tablet Manufacturing problems or Defects

An industrial pharmacy usually encounters number of problems during
manufacturing. An ideal tablet should be free from any visual defect or functional
defects. The Imperfections known as ‘VISUAL DEFECT’ are either related to
Imperfections in any one or more of the following factors.

1. Formulation design
2. Table ting process
3. Machine

The defects related to Tablet ing process...

1. Capping: is the term used, when the upper or lower segment of the tablet
separates horizontally during ejection from the tablet press, or during
subsequent.

Normal tablet capping

 2. Lamination: is the separation of a tablet into two or more distinct
horizontal layers.

Normal Tablet Lamination

3. Cracking: Small, fine cracks observed on the upper and lower

central surface of tablet, or very rarely on the sidewall are referred
to as Cracks.
4. Chipping: Breaking of tablet edges.

The defects related to formulation…

1. Sticking: refers to the tablet material adhering to the die wall.
2. Picking: is a more specific term that describes product sticking only within
the letters, logos, or designs on the punch faces.
3. Binding: Sticking of the tablet to the die and does not eject properly out of
the die.

The defects related to Machine…

Double Impression: Due to free rotation of the punches, having some
engraving on their faces.

The defects related to more than one factor…

Mottling: Unequal distribution of color on a tablet with light or dark areas.
 Tablet Coating
Definition: - Tablet coating is defined as “covering the tablets with
one or more layers of mixture of various substances such as natural or
synthetic resins, gums, inactive and insoluble filler, sugar, plasticizer,
waxes, authorized color and sometimes flavor.”
Objective of tablet coating:-
1. Mask the odour, taste or color of the drug.
2. Provides physical and chemical protection for drug.
3. Controls the release of drug from the tablet.
4. Avoid chemical incompatibility.
5. Protects the drug from gastric environment of stomach in case of acid
sensitive drug.

Types of tablet coating

1. Sugar coating
2. Film coating
3. Enteric coating
4. Compressed coating
5. Dip coating

Sugar coating:- is the most conventional multistep coating process.

This process involves application of sugar based coating solution to
the tablets.
Advantages:-
- Cheap, safe coating material
- Cheap coating machine
- Good patient compliance
- Require less hardness core
Disadvantages:-
- Time consuming process.
- High weight gain.
- Increase in packaging & shipping
Raw material for sugar coating;-
Sugar & its substituent’s:- Glucose, lactose, sugar alcohol

Binders: - Acacia, gelatin, PVP

Coloring agents: - Water soluble (dyes), Water insoluble (lakes)

Anti-Adherents:- Talcum, colloidal silica

Fillers: - CaCO3, starch, TiO2

Polishing agents: - beeswax, carnauba wax, paraffin

Steps involved in Sugar coating:-

- Seal coating
- Sub-coating
- Grossing/Smoothing
- Coloring
- Polishing/Finishing
- printing

Film coating:-
1. Modern approach to coating
- Tablets
- Capsules
2. By surrounding them with thin layer of polymeric material.
Raw material for film coating:-

1. Polymer
2. Solvents
3. Plasticizers
4. Colorants

Process:-

- Single stage process, which involves spraying a coating solution.

- The solution is sprayed onto a rotating tablet bed followed by drying, which
facilitates the removal of the solvent leaving behind the deposition of thin
film of coating materials around each tablet.

Evaluation of Tablets:-
Various Unofficial & Official tests are performed to evaluate the tablet.

Un-Official test:-
- Organoleptic
- Size & Shape
- Hardness
- Friability
Official tests:-
- Wight variation
- Content uniformity
- Dissolution
- Disintegration
 HARDNESS TEST
- This test is also known as “Crushing Strength Test”.
- Tablets require a certain amount of strength, o hardness to with
stand mechanical shocks of handling in manufacturing, packaging,
and shipping.
- Tablet hardness has been defined as the force required to break a
tablet in a diametric compression test.
Factor affecting of hardness:-
- Moisture content
- Concentration of binder
- Compression force

Equipment used to measure the hardness of tablet:-

- Monsanto tester
- Pfizer tester
- Strong cob hardness tester
- Erweka hardness tester
The hardness measured in Kg/cm2.

Figure- Monsanto hardness tester

 FRIABILITY TEST
Definition of Friability test: - Defined as the % of weight loss by tablet due
to mechanical action during the test.

Or,

Friability is the phenomena where the surface of tablet damage due to mechanical
action.

Friability tester is known as the Roche friabilator

Process:-
- Pre weighed tablet sample placed in friabilator.
- Operated 100 revolutions (25rpm for 4min).
- Dropping tablet a distance 6 inches.
- Tablet are damage then reweighed.

Figure:- Friabilator

Note: - Compress tablet lose less than 0.5 to 1% of their weight are generally
acceptable.
Formula:-
%Friability = (W0-Wf/W0)*100

Where, W0= Initial weight Wf= final weight

Wight Variation Test

- Take 20 tablets and weighed individually.
- Calculate average weight.
- The tablet pass the U.S.P test if no more that 2 tablet are out of %limit and
if no tablet differs by more than 2 times of % limit.

Formula:-
Wt. Variation=(Individual wt / Average wt)*100

Note:-
USP STANDARD:-
Average weight Percent difference
130 mg or less 10
More than 130mg through 324mg 7.5
More than 324mg 5

IP STANDARDS:-
Average wt. of tablet(mg) Max. %different
allowed
84 or less 10%
84- 250 7.5%
 More than 250 5%

Disintegration test
Definition of disintegration: - Is the process in which tablet breakdown
into smallest particles or granules.
Tablet Granules Small particles
Disintegration Disintegration

Apparatus:-
- 6glass tubes – 3 inches length
- 10 mesh screen at the bottom
- Temperature: 37±2°C
- Speed : 28-32 rpm

FIGURE :- Disintegration test apparatus

Liquids used in disintegration:-
- Water
- Gastric fluid (pH = 7.5,KH2PO4+Pancreatic enzyme + NaOH)

Process:-
Put one tablet into each tube, suspend the assembly in the beaker containing 0.1 M
hydrochloric acid and operate without the disc for 2 hrs. No tablet show sign of
cracks that would allow the disintegration. Replace the liquid in the beaker with
mixed with phosphate buffer pH 6.8, add a disc to each tube operate the apparatus
for further 60 minute.

Acceptable criteria:- this test is met if Not less than 16 of the total 18 dosage
units tested are disintegration.

Disintegration time:-

- Uncoated tablet : 5-30min

- Coated tablet : 1-2 hrs

DISSOLUTION TEST
- Dissolution is the process by which a solid solute enters a solution.
- It may be defined as the amount of drug substances that goes into a solution
per unit time.
- It is important for determine Bioavailability of drug.

Dissolution apparatus:-

Type 1 – Basket type

Types 2 – Paddle type

 Figure:- Dissolution test apparatus

Standards:-

Stage No. of units Acceptable criteria

S1 6 tablet All unit “6” not less than
Q+5%

S2 6 tablet Average of 12 tablets

equal to or not >Q and Q-
25%
S3 12 tablet Average of 24 tablets
equal to or not >Q and Q-
25%
Where, Q= % Drug dissolved

NOTE: - 75% of drug should be dissolved within 45 min as per U.S.P.