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PRACTICAL-3

AIM: To prepare and evaluate IR tablet formulation by wet granulation method

using ascorbic acid as model drug and to study the effect aqueous and non-aqueous
granulating agents.
A. Tablets using aqueous granulating agent (hydrophilic binder).
B. Tablets using non-aqueous granulating agent (hydrophobic binder).
FORMULA:
Each tablet contains 250 mg Ascorbic acid I.P.
Excipients: Quantity sufficient
Batch size: 20 tablets
Packaging: Aluminium strip of 10 tablets
FORMULATION:
A. Tablets using aqueous granulating agent (hydrophilic binder).
INGREDIENTS

QUANTITY PER QUANTITY PER ROLE OF EACH

TABLET
20 TABLETS
INGREDIENTS
Ascorbic acid
250 mg
5g
Vitamin
C
supplement
Starch
paste q.s.
q.s.
Binder
(10%W/V)
Microcrystalline
30 mg
0.6 g
Diluent
and
cellulose (Avicel)
disintegrant
Magnesiun stearate 10 mg
0.2 g
Lubricant
and
glidant
Aerosil
(Silicic 5 mg
0.1 g
Lubricant
and
acid)
antiadherent

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OBSERVATION TABLE:
A. Tablets using aqueous granulating agent (hydrophilic binder).
1. Weight variation:
No. of Weight (mg)
tablets
1
2
3
4
5
6
7
8
9
10
11
12
13
14
15
16
17
18
19
20
MEAN
2. Hardness:
No.
of Hardness (Kg/cm2)
tablet
1
2
3
4
5
MEAN

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B.Tablets using non-aqueous granulating agent (hydrophobic binder).

INGREDIENTS

QUANTITY PER QUANTITY PER ROLE OF EACH

TABLET
20 TABLETS
INGREDIENTS
Ascorbic acid I.P. 250 mg
5g
Vitamin
C
supplements
Ethyl cellulose 5% q.s.
q.s.
Binder
solution in ethanol
Microcrystalline
30 mg
0.6 g
Diluent
and
cellulose (Avicel)
disintegrant
Magnesiun stearate 10 mg
0.2 g
Lubricant
and
glidant
Aerosil
(Silicic 5 mg
0.1 g
Lubricant
and
acid)
antiadherent
PROCEDURE:
1. METHOD OF PREPARATION:
A. Tablets using aqueous granulating agent (hydrophilic binder).
PREPARATION OF STARCH PASTE (10%W/V):
10 g of starch powder was weighed accurately and dissolved in 100 ml hot
boil water (60c) with continuous heating until thick paste was obtained.
PREPARATION OF TABLETS:
Weighed accurately API and microcrystalline cellulose and transferred to
mortar to mix properly.
Added sufficient quantity of starch paste (10%W/V) slowly and made up a
wet dump mass with suitable consistency.
Passed through it 10 # sieve and dried granules in hot air oven.
Dried granules were passed through the arrangements of sieve No, 22 # and
44 # sieves. Granules were collected on 44 # sieve and fines were collected
below the 44 # sieve.
Suitable proportion of fines and granules were compressed to tablet under
rotary tablet machine with proper tooling.

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3. Friability:
No. of tablet

% weight loss

4. Disintegration:
No.
tablet
1
2
3
4
5
MEAN

of Disintegration
time

%DR

Total
(mg/900ml)

Total
mcg/900ml

Cum.conc
(mcg/5ml)

Conc.
(mcg/900ml)

conc(mcg/5ml)

Conc. * dil.
Factor

Conc(mcg/ml)

Absrbance

Time

5. Dissolution rate profile:

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B. Tablets using non-aqueous granulating agent (hydrophobic binder).

Preparation of ethyl cellulose (5%w/v) solution:
2.5 g ethyl cellulose was weighed accurately and dissolved in 50 ml ethanol.
Preparation of tablets:
Weighed accurately API and microcrystalline cellulose and transferred to
mortar to mix properly.
Added sufficient quantity of ethyl cellulose (5%W/V) solution slowly and
made up a wet dump mass with suitable consistency.
Passed through it 10 # sieve and dried granules in hot air oven.
Dried granules were passed through the arrangements of sieve No, 22 # and
44 # sieves. Granules were collected on 44 # sieve and fines were collected
below the 44 # sieve.
Suitable proportion of fines and granules were compressed to tablet under
rotary tablet machine with proper tooling.
2. METHOD OF CHARACTERIZATION:
1. Weight variation: It was performed by using 20 tablets by
alternatively weighing of each tablet on weighing machine.
2. Hardness: It was characterized for each tablet by using the Monsanto
tester.
3. Friability: It was performed by subjecting a weighed No. of tablets to
Roche Friabilator that revolved at 25 rpm and dropping the tablets.
4. Disintegration: It was performed using USP disintegrating test
apparatus.
5. Dissolution rate profile: It was performed by using USP type
apparatus.

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Tablets using non-aqueous granulating agent (hydrophobic binder).
1. Weight variation:
No. of Weight (mg)
tablets
1
2
3
4
5
6
7
8
9
10
11
12
13
14
15
16
17
18
19
20
MEAN

2. Hardness:
No.
of Hardness (Kg/cm2)
tablet
1
2
3
4
5
MEAN

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Comments:
1. If the API is moisture sensitive /hygroscopic, then aqueous granulating agent
is not advisable because it may degrade API by hydrolysis/oxidation
If the given API is heat sensitive then drying is necessary which can be
achieved non-aqueous granulation easily.
2. In the formulation where the wet granulation method is only advisable
method when choice of granulating agent is critical depending on the
sensitivity of API.
3. In present study, the effect of aqueous and non- aqueous binder solution on
stability of moisture sensitive API is investigated by key parameters like
content and dissolution profile.
NOTE: The formulation characterizes after 6-8 hours of the formulation.
The observations show that the hydrophobic granulating agent for the moisture
sensitive API is important as binding agent which increase the stability of
formulation.

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3. Friability:
No. of tablet

% weight loss

4. Disintegration:
No.
tablet
1
2
3
4
5
MEAN

of Disintegration
time

%DR

Total
(mg/900ml)

Total
mcg/900ml

Cum.conc
(mcg/5ml)

Conc.
(mcg/900ml)

conc(mcg/5ml)

Conc. * dil.
Factor

Conc(mcg/ml)

Absrbance

Time

5. Dissolution profile

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REFERENCE :
Pharmaceutical dosage forms: Tablet volume 1, edited by Herbert A Liebermann
and Leon Lachmann.