Aim: To prepare conventional tablet formulation containing

hydrophilic and hydrophobic API and to study effect on

dissolution rate
a) Hydrophilic API by direct compression
b) Hydrophilic API by wet granulation
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)
Batch size: 20 tablets
Packaging: Aluminum strips of 10 tablets.
Formulation:
a) Metformin by wet granulation.
Ingredients
Metformin
Polivinyl
pyrollidon
Microcrystalline
cellulose
Crosscarmalose
Sodium
Magnesium
Stearate
Purified water
Total

Formula for one

tablet
500 mg
62.5 mg

Formula for 20
tablets
10 gm
1.25gm

Role of each
ingredient
Drug
Binder

62.5mg

1.25gm

Filler

12.5 mg

0.25gm

6.25 mg

0.125gm

Superdisintegran
t
Lubricant

q.s.

q.s

643.75 mg

12.875 gm

Granulating
fluid

b) Metformin by direct compression.

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

Formula for one

tablet
500 mg
77.90 mg

Formula for 20
tablets
10 gm
1.558 gm

Role of each
ingredient
Drug
Diluent

26.8 mg
3.25 mg
36.85 mg

0.536 gm
0.065 gm
0.737 gm

Binder
Glident
Diluent

5.2 mg

0.104 gm

Lubricant

650 mg

13 gm

Procedure:
1. Method of preparation
All the ingredients were weighed accurately.
Metformin and Polivinyl pyrollidon, Microcrystalline cellulose were
taken in mortar and pestle and grinded together to have uniform mixing
and obtain fine powder.
Lump mass was obtained by using purified water as granulating agent.
Pass this lump mass through 10# sieve and granules 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, 1% w/w of croscarmellose sodium and 2% w/w of the
lubricant magnesium stearate were 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.
2. Method of characterization
i. 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.
% weight variation = x-x avg /x avg *100
ii.

iii.

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 a measured of table friability.

The value was expressed in percentage.

Observations:
i .Observation table of weight variation
Sr.
no.
1
2
3
4
5
6
7
8
9
10
11
12
13
14
15
16
17
18
19
20
Avg.

Weight of tablets(x)
a
B
c

x-x avg
b

x-x avg /x avg *100

a
b
c

iv.

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.

v.

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.

ii. Hardness of tablet:

a.)
b.)
c.)
iii. Disintegration time:
a.)
b.)
c.)
iv. Observation table of Friability
Formulation Initial
weight of
tablet(a)
a
b
c

Final
weight of
tablets(b)

(a)-(b)

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

%DR

(mg/900ml) Total

Total mcg/900ml

(mcg/5ml) Cum.conc

(mcg/900ml) Conc.

conc(mcg/5ml)

Factor Conc. * dil.

Conc.(mcg/ml)

Absrbance

Observation table of Dissolution

Time

vi.

Sr.no. Time(min.) absorbance Conc.per Conc.in Cumulative % drug

ml.
900 ml conc.
release
a b c a b c a B c a b c a b c
1
0
2
10
3
20
4
30
5
40
6
50
7
60

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