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PRACTICAL-1

Aim: To prepare conventional tablet formulation containing

hydrophilic and hydrophobic API and to study effect on
dissolution rate
a) Hydrophilic API by wet granulation
b) Hydrophilic API by direct compression
c) Hydrophobic API by direct compression
Formula:
a) Each tablet contains 500 mg Metformin, Excipients quantity sufficient.
b) Each tablet contains 500 mg Metformin, Excipients quantity sufficient.
c) Each tablet contains 300 mg Aspirin, Excipients quantity sufficient.
Batch size: 20 tablets
Packaging: Aluminum strips of 10 tablets.
Formulation:
a) Metformin by wet granulation.
INGREDIENTS

QUANTITY
PER TABLET

Metformin
Polivinyl
pyrollidon
Microcrystalline
cellulose
Starch
Magnesium
Stearate
Starch paste
Total

500 mg
62.5 mg

QUANTITY
PER
TABLETS
10 g
1.25 g

ROLE
OF
20 INGREDIENTS

62.5mg

1.25 g

Filler

12.5 mg
6.25 mg

0.25 g
0.125 g

Disintegrant
Lubricant

q.s.
643.75 mg

q.s
12.875 g

Granulating fluid

Drug
Binder

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Observations:
i .Observation table for weight variation test
Sr.
Weight of tablets(x)
no.
a
b
c
1
2
3
4
5
6
7
8
9
10
11
12
13
14
15
16
17
18
19
20
Avg.
ii. Hardness of tablet:
a.)
b.)
c.)

iii. Disintegration time:

a.)
b.)
c.)

x-x avg
a
b

x-x avg /x avg *100

a
b
c

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b) Metformin by direct compression.

INGREDIENTS

QUANTITY
PER TABLET

Metformin
Hydroxy
Propyl
Methyl Cellulose
Povidone
Colloidal Sillica
Micro Crystalline
Cellulose
Magnesium
Stearate
Total

500 mg
77.90 mg

QUANTITY
PER
TABLETS
10 g
1.558 g

ROLE
OF
20 INGREDIENTS

26.8 mg
3.25 mg
36.85 mg

0.536 g
0.065 g
0.737 g

Binder
Glident
Diluent

5.2 mg

0.104 g

Lubricant

650 mg

13 g

Drug
Diluent

c) Aspirin by direct compression

INGREDIENTS

QUANTITY
PER TABLET

Aspirin
Starch
Starch paste
Lactose
DCP
Talc
Mg stearate
Aerosil
Total

300 mg
15.8 mg
q.s
15.8 mg
13.8 mg
8 mg
4 mg
0.148 mg
357.55 mg

QUANTITY
ROLE
OF
PER
20 INGREDIENTS
TABLETS
15 g
Analgesic
0.79 g
Diluent
q.s
Binder
0.79 g
Diluent
0.69 g
Disintegrant
0.4 g
Lubricant
0.2 g
Glidant
0.074 g
Glidant
18 g

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iv. Observation table of Friability

Formulation Initial
Final
(a)-(b)
weight of weight of
tablet(a)
tablets(b)
A
B
C

(a)-(b)*100
(a)

Total
(mg/900ml)

%DR

Total
(mg/900ml)

%DR

Total
mcg/900ml

Cum.conc
(mcg/5ml)

Conc.
(mcg/900ml)

conc(mcg/5ml)

dil.
Conc. *
Factor

Conc.(mcg/ml)

Absrbance

Time

v. Observation table of Dissolution study

a. Hydrophilic API by wet granulation

Total
mcg/900ml

Cum.conc
(mcg/5ml)

Conc.
(mcg/900ml)

conc(mcg/5ml)

dil.
Conc. *
Factor

Conc.(mcg/ml)

Absrbance

Time

b. Hydrophilic API by direct compresssion

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Procedure:
2. Method of preparation
a) Hydrophilic API by wet granulation
All the ingredients were weighed accurately.
Metformin and Polivinyl pyrollidon, Microcrystalline cellulose
were taken in mortar and pestle and grinded together to obtain
uniform mixing and obtain fine powder.
Lump mass was obtained by using starch paste as granulating
agent.
This lump mass was passed through 10# sieve and granules
were obtained.
The granules were collected on the paper and allowed to dry in
oven at 45C for 1 hour.
After drying the mass was passed through 20# sieve and
granules were retained on 40# sieve.
At the end, 2% w/w of the lubricant magnesium stearate was
added and mixed for 5 minutes.
Fines obtained were weighed.
15% of fines were added to the dried granules and pack in zip
lock bag and punched into tablets using tablet punching
machine.
Tablets were then evaluated.
b) Hydrophilic API by direct compression
All the ingredients were weighed accurately and mixed
thoroughly.
Prepared powder mixture was subjected to direct compression.
Tablets were then evaluated.
c) Hydrophobic API by direct compression
All the ingredients were weighed accurately.
Aspirin, starch powder, lactose, DCP, were taken in mortar and
pestle and grinded together to have uniform mixing and obtain
fine powder.
10% of starch paste was prepared and sufficient quantity was
added to the fine powder to obtain the lump mass.
This lump mass was then passed through 10# sieve to obtain
granules and were allowed to dry in oven at 60C.

dil.

%DR

Total
(mg/900ml)

Total
mcg/900ml

Cum.conc
(mcg/5ml)

Conc.
(mcg/900ml)

conc(mcg/5ml)

Conc. *
Factor

Conc.(mcg/ml)

Absrbance

Time

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c. Hydrophobic API by direct compression

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Granules were then passed through 20# sieve and retained on
40# sieve.
Fines obtained were weighed.
15% of fines were added to the dried granules and pack edt in
zip lock bag and punched into tablets using tablet punching
machine.
Tablets were then evaluated.

3. Method of characterization
ii. Weight variation:
A total of 20 tablets were taken and each tablet were weighed
accurately.
Average of 20 tablets was calculated and percentage weight
variation was calculated using following formula.
Percentage weight variation = x-x avg /x avg *100

iii.

iv.

Hardness:
Hardness of tablet was determined by using Monsanto hardness
tester.
Friability:
20 tablets were weighed and placed in the apparatus where they
were exposed to rolling and repeated shocks.
They fell 6 inches in each turn within the Roche apparatus.
After 100 revolutions of apparatus the tablets were weighed and
the weighed to compare with initial weight.
The loss due to abrasion was used to measure friability.

The value was expressed in percentage

v.

Disintegration time
One tablet was put into each tube, assembly was suspended
in the beaker containing distilled water and operated with the
10# discs.
Time was recorded required to disintegrate tablet and its
pattern.
Remove the assembly from the liquid.

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vii.

Dissolution study
In vitro dissolution study of metformin tablets was
performed using phosphate buffer pH 6.8 maintained at a
temperature of 37 0.5C in USP II dissolution test
apparatus and at rotation speed of 100 rpm.
Samples were withdrawn time interval (5, 10, 15, 20, 30, 45
and 60 min), and filtered through Whatman filter paper.
Absorbance of suitably diluted samples was determined by
UV spectrophotometer at 236 nm and the percentage of drug
release was calculated.

Comments:
1.) Hydrophilic API can be crystalline powder having average to good
flowability. It can be formulated by direct compression or wet granulation
method. While hydrophobic API has poor flow and can only be
formulated by wet granulation method which will improve flow.
2.) Physicochemical nature of API affects sets of disintegration,
deaggregation and also dissolution. In case of hydrophilic API steps are
not rate limiting while for hydrophobic API formulation should facilitate
sequences of steps. This can be achieved by wet granulation method
using proper binder.
3.) In present study effects of method of preparation on rate limiting step is
investigated. Observation show

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