RESULTS AND DISCUSSION

RESULTS AND DISCUSSIONS

PRE-FORMULATION STUDIES

Description

These tests were performed and the results were illustrated in the
following table:

Table no-11: Table showing the description of loratadine (API)

Test Description
Colour White to off white powder

Result

The results were found as per specifications.

Solubility
These tests were performed and the results are illustrated in the table
Table no-12: Table showing the Solubility of loratadine (API) in various
solvents.

Solvents Solubility
Water In soluble
pH6.8 Phosphate Soluble
buffer
Methanol Soluble
Chloroform Soluble

Table No-13: . Standard graphs for loratadine

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 RESULTS AND DISCUSSION

Absorbance at 245nm
SD, n=3
Concentration in mcg

0.0550.011
2

0.1050.012
4

0.1650.014
6

0.2120.012
8

0.2660.016
10

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 RESULTS AND DISCUSSION

0.3

f(x) = 0.03x + 0
0.25 R = 1

0.2

0.15 Abs
Linear (Abs)

0.1

0.05

0
1 2 3 4 5 6 7 8 9 10 11

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 RESULTS AND DISCUSSION

Figure No: Standard graph of loratadine

Melting Point

This test is performed and the result was illustrated in the following table

Table no-14: Table showing the melting point of APIs

Material Melting Point

Loratidine 1340

Drug excipient compatibility studies

Fig no: FTIR Spectra of Loratidine pure drug

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 RESULTS AND DISCUSSION

Fig no: FTIR Spectra of Loratidine optimized formulation

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 RESULTS AND DISCUSSION

PREFORMULATION STUDIES

Table no-15- Pre-compression parameters for formulation batches

Bulk Tapped Compressibil Hausners Angle of
Formulati
density density ity index (%) ratio repose
on code
(gm/mL) (gm/mL)

F1 0.7210.0 0.87 17.1260.6 1.2060.06 36.620.2

45 0.01 1

F2 0.7100.0 0.8730.0 19.7140.7 1.2510.04 37.460.1

43 4 1

F3 0.410.04 0.4830.5 15.1130.8 1.1780.08 38.320.3

5 1
0.450.04 0.52 28.060.3
F4 15.600.2 1.150.02
5 0.09 1
0.450.04 0.50 27.580.1
F5 12.230.6 1.110.04
5 0.07 5
0.440.04 0.50 28.440.1
F6 12.580.8 1.130.08
4 0.09 1

F7 0.410.04 0.4830.4 15.1130.9 1.1780.07 38.320.3

8 9 3

F8 0.7100.0 0.8730.0 19.7140.6 1.2510.05 37.460.1

32 36 5

Result: All the formulations were evaluated for bulk density, tapped density, %

compressibility, hausners ratio and angle of repose. The results of %

compressibility, hausners ratio and angle of repose were found to be between 12-

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 RESULTS AND DISCUSSION

20, 1.11-1.26 and 30-40 respectively. These results show that the formulations

have fair to very good flow properties.

Conclusion: From the above Table, Preformulation studies of powder blend had
shown that the blends had passable parameters like Angle of Repose, Bulk density,
Tapped density, Carrs index and Hausners ratio. From the Table, it is observed
that based on compressibility index and it was concluded that the blend showed
passable flow characteristics.

EVALUATION PARAMETERS OF TABLETS

The prepared tablets were subjected to preliminary characterization such as

hardness, thickness, % weight variation, friability and drug content. The
evaluated parameters were within acceptable range for all the formulations.

Table no-16: Evaluation parameters of formulations of porous tablets before

drying
Formula

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 RESULTS AND DISCUSSION

Average Drug Disintegra

Thickne Hardnes content tion
Friabi weight (%) Time
tion code ss (mm) s (KP) variation
lity S.D.
(mg)
(%) (min)

F1 3.29 99.130. 4.2

5.0 0.54 202.1
53
F2 3.05 205.6 96.270. 3.3
3.5 0.45 64
F3 3.38 201.8 97.630. 4.5
3.5 0.35 55
F4 3.50 201.9 98.360. 3.4
3.5 0.41 58
F5 3.43 205.4 98.330. 4.3
4.0 0.42 62
3.27 203.6 98.640. 2.9
F6 3.5 0.31 84

3.38 2016 99.2 7 mins 10

F7 4.1 0.26 secs

3.36 202.0 98.6 7 mins 5

F8 4.1 0.23 secs

Observations:

From the above Table, it is observed that the thickness, hardness, friability, weight
variation and content uniformity of the porous tablets before drying were in the
passable range. The F1, F3, F5 formulations containing camphor as the subliming
agent didnt show much effect on the disintegration time. The disintegration of F6
formulation was found to be of 2.9mins which is satisfactory. The disintegration
of F7 & F8 was found to be more than 7 mins.

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 RESULTS AND DISCUSSION

Table no-17. Evaluation parameters for formulations of porous tablets after

drying

Average Drug Disintegrat

Thickness Hardness
Formulati weight content ion
S.D. S.D.
on code variation (%) Time
(mm) (Kp)
(mg) S.D.

F1 3.29 3.7 201.3 99.26 1min 10sec

F2 3.05 3.8 203.2 96.38 43sec

F3 3.38 4.1 200.9 97.03 1min

F4 3.50 4.1 200.00 98.26 36sec

F5 3.43 4.2 203.4 98.29 57sec

3.27 201.8 98.60 20sec
F6 4.8
3.38 200.9 99.36 5 mins
F7 4.3
3.36 200.3 99.56 5 mins 34
F8 4.3
secs

Observations:

From the above Table, it is observed that the thickness, hardness, weight variation
and drug content of the porous tablets were in the passable range. The F1, F3, F5
formulations containing camphor as the subliming agent didnt show much effect
on the Disintegration time where as the optimized formulation F6 10% camphor
and CCS 10 % showed better results The Disintegration time of F6 formulation
after drying was found to be of 20 sec ( 20sec) which is satisfactory.F7 and F8
trails were with crospovidone as disintegrant but the disintegration time was more
than 5 mins.

RESULTS OF IN-VITRO RELEASE PROFILE

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 RESULTS AND DISCUSSION

Tableno-18. In-Vitro Release Profile of Loratidine from formulations F1-F8

Time F1 F2 F3 F4 F5 F6 F7 F8
10
mins 32.56 38.26 42.52 48.96 50.38 58.92 12.56 18.26
15
mins 46.28 48.03 50.36 56.48 61.94 69.52 26.28 28.03
20
mins 55.23 60.58 62.85 68.92 70.56 77.89 35.23 40.58
30
mins 60.65 65.92 70.59 74.56 77.89 82.56 40.65 50.92
45
mins 72.36 74.82 75.62 80.82 83.56 98.94 52.36 54.82
60
mins 80.56 80.49 82.51 85.45 88.95 100.59 60.56 60.49

120

100
F1
80
F2
60 F3
%CDR
F4
40 F5

20 F6
F7
0 F8
0 10 20 30 40 50 60 70

time in mins

In-Vitro Release Profile of Loratidine from formulations F1-F8

Observations: The in-vitro drug release profiles of Loratidine from all the
formulations F1 to F8 are shown in the above Tables. From the results, it is
observed that the dissolution profiles of the formulated products (F1, F2, F3, F4&
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 RESULTS AND DISCUSSION

F5) didnt meet the proper dissolution profile of Loratidine i.e 85% of drug release
in 45mins. The formulations F6 showed 98.45% of drug release within 45mins.The
formulationsF7, F8 showed 60% in 60 mins after change in disintegrant i.e
Crospovidone even with increase in concentration of the crospovidone.

STABILITY STUDIES:

Loratidine tablets of F6 formulation were packed in HDPE (High density

polyethylene) container with child resistant caps (CRC) and induction sealed.
These bottles were charged for stability study at 400C &75% RH.

After one month:

Table no-19: Physical evaluation of Tablets for stability studies of Optimized

formulation:

Parameter Initial 400C / 75%RH

Colour White White
Surface Smooth Smooth
Disintegration 20sec 22sec
Assay 98.60 98.0

Observation: The Loratidine porous tablets were subjected to stability studies at

40oC and 75% RH for 1 month and from the above results, it was found that there
is no significant effect on the tablets.

After Three months:

Table no-20-: Physical evaluation of Tablets for stability studies of optimized

formulations:

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 RESULTS AND DISCUSSION

Parameter Initial 400C / 75%RH

Colour White White
Surface Smooth Smooth
Disintegration 20sec 25sec
Assay 98.60 96.70

Observation: The Loratidine porous tablets were subjected to stability studies at

40oC and 75% RH for 3 months and from the above results, it was found that there
is no effect on the tablets and was found to be within the limits according to ICH
guidelines.

DISCUSSION
Immediate release tablets of Loratidine were formulated by direct
compression method using Camphor and Menthol as subliming agents,

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 RESULTS AND DISCUSSION

Microcrystalline cellulose, Lactose monohydrate as diluents, CCS as super

disintegrant, Magnesium stearate as lubricant.

Compatibility studies were performed using IR spectrophotometer. The IR

spectrum of pure drug and physical mixture of drug and excipients were studied as
shown in Figures. The peaks obtained in the spectras of each formulation
correlates with the peaks of drug spectrum. This indicates that the drug is
compatible with the formulation components.

The blends were analyzed for parameters such as Bulk density, Tapped
density, Compressibility index and Hausners ratio and the results were found to be
within limits.

Bulk density and tapped density values were found to be within limits.
Compressibility index has been proposed as an indirect measure of bulk density,
size and shape, surface area and cohesiveness of material. The powdered blend has
required flow property.

After compression, all the tablets were dried at 60oC for 12hrs and were
evaluated for various parameters like weight variation, hardness, thickness,
friability, disintegration and in-vitro drug release.

All formulations were found to have good hardness so they were taken for
further studies. The measured hardness of tablets of each batch are in the range of 3
to 3.5kg/cm2.

Tablets mean thickness were almost uniform in all formulations and were found to
be in the range of 3.05 mm to 3.50mm.

Friability values are found to be less than 1% in all the cases and considered to be
satisfactory.

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 RESULTS AND DISCUSSION

The total weight of each formulation was maintained constant and the weight
variation of the tablets was within limits of 5%.

All the tablets passed the pharmacopoeial specifications for disintegration of

Loratidine porous tablets within 5 minutes.

The optimized formulation F6 containing 10% of menthol showed in-vitro drug

release of almost 98.06% of Lovastatin in 45mins and the disintegration time was
found to be 20sec. The tablets loaded for stability at 40oC and 75% RH for 1 month
and 3 months respectively did not show much effect on the disintegration time and
drug content and are within the limits as per ICH guidelines therefore ensuring that
the formulation F6 is a stable formulation.

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