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2008,
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ISSN 0974-3618
RESEARCH ARTICLE
ABSTRACT
Amlodipine besylate effervescent floating tablets were developed in ten different formulations (F1 to F10) by employing
different grades of polymers and effervescent agents such as sodium bicarbonate and citric acid. The formulations were
evaluated for various physical parameters, buoyancy studies, dissolution parameters and drug released mechanisms. F10
formulation showed maximum floating time of 24 hours and gave slow and maximum drug release of Amlodipine
besylate spread over 24 hours and whereas Amlodipine besylate released from marketed tablet was rapid and maximum
within 12 hours.
KEY WORDS
INTRODUCTION:
EXPERIMENTAL
Materials
Amlodipine besylate was procured from Signa Pharma Pvt.
Ltd. Kanpur. HPMC K100 M, HPMC K15 M, Carbapol 934
p, Sodium biacarbonate, Citric acid, poly vinyl pyrrolidine
and Talc were obtained from Colorcon Asia Pvt. Ltd and
Loba chemicals. Amlosafe 10 (marketed brand of
Amlodipine besylate) tablets were purchased from local
market.
Received on 20.07.2008
Accepted on 25.08.2008
Modified on 23.08.2008
RJPT All right reserved
Methods
Effervescent Floating tablets containing Amlodipine
besylate were prepared by direct compression technique
using varying concentrations of different grades of polymers
with Sodium bicarbonate and citric acid. All the ingredients
were accurately weighed and passed through different mesh
sieves accordingly. Then, except Magnesium stearate all
other ingredients were blended uniformly in glass mortar
After sufficient mixing of drug as well as other components,
Magnesium stearate was added, as post lubricant, and further
mixed for additional 2-3 minutes. The tablets were
compressed using rotary tablet machine. The weights of the
tablets were kept constant for all formulation.
Evaluation of effervescent floating tablet formulations
Hardness of the tablets was tested using a Monosanto
hardness tester. Friability of tablets was determined in Roche
friabilator. Ten tablets were selected randomly from each
batch and weighed individually to check for weight
variation. The results are given in table no. 2
526
120
F1
F2
F3
F4
F5
F6
F7
F8
F9
100
80
60
40
20
y = -0.0729x + 2.0996
R2 = 0.9475
2
1.5
1
0.5
0
0
10
15
20
25
30
Time (hrs)
0
10
15
20
25
30
Time(hrs)
100
120
Cumulative % Drug Release
120
80
60
40
F10
20
0
0
10
15
20
25
30
y = 23.761x - 12.922
R2 = 0.9924
100
80
60
40
20
0
Time (Hrs)
Root Of Time
100
80
y = 4.2369x + 11.403
2
R = 0.9528
60
40
20
0
0
10
Cum % Release
15
20
25
30
y = 0.6901x + 1.0848
R2 = 0.9959
2.5
2
1.5
1
0.5
0
0
0.5
Time (hrs.)
Log Cum % Drug Release
The buoyancy lag time (BLT) and total floating time (TFT)7
On immersion of tablets of different formulations in
0.1N HCl solution at 375C, the tablets floated, and
remained buoyant without disintegration, the results of
the buoyancy lag time (BLT) and total floating time
(TFT) were shown in Table 3.
Estimation of Amlodipine besylate8
Amlodipine besylate content in the tablets was
estimated by using UV spectrophotometric method
based on the measurement of absorbance at max 239
1.5
Log Time
Linear (Log Cum % Drug Release)
527
F4
10
50
100
--50
60
30
10
10
5
5
330
F5
10
--100
50
50
60
30
10
10
5
5
330
F6
10
100
--50
50
60
30
10
10
5
5
330
F7
10
100
50
--50
60
30
10
10
5
5
330
F8
10
100
50
50
--60
30
10
10
5
5
330
F9
10
110
40
50
--60
30
10
10
5
5
330
F10
10
125
40
40
--60
30
10
5
5
5
330
100
80
60
40
F 10
20
Marketed Product
0
0
10
Time (hrs)
20
30
528
ACKNOWLEDGMENT:
The authors are grateful to Centre for development action
and community research (CDACR) for help in literature
survey and procurement of drug sample.
REFERENCES:
1. Deshpande AA, Shah NH, Rhodes CT and Malick W.
Development of a novel controlled release system for gastric
retention. Pharm. Res. 1997; 14(6): 815-819.
2. Klausner EA, Lavy E, Friedman M and Hoffman A. Expandable
gastroretentive dosage form. J. Control. Rel. 2003; 90: 143-162.
3. Singh BN and Kim HK. Floating drug delivery systems: an
approach to oral controlled drug delivery via gastric retention. J.
Control. Rel. 2000; 63: 235-59.
4. Barar FSK. Essentials of pharmacotherapeutis.3rd S. Chand and
Company Ltd. New Delhi. 246
5. Gutierrez-rocca J, Omidian H and Shah K. Progress in
Gastroretentive Drug Delivery System Bussiness Briefing,
Pharmatech. 2003: 152-156.
529
F5
13.5
28.2
39.8
51.5
62.9
73.7
84.9
95.3
98.7
F6
12.8
27.4
38.3
50.2
61.1
72.4
84.1
94.5
98.4
F7
13.6
22.3
35.2
48.4
59.2
69.3
78.8
89.2
98.3
F8
10.7
15.8
24.6
32.4
42.7
55.2
70.8
84.7
96.2
98.8
F9
10.2
16.1
23.5
30.3
41.6
53.1
68.7
79.8
95.5
98.9
F10
7.3
11.7
19.4
25.9
32.1
43.2
52.8
72.1
85.8
96.8
98.6
Slope
4.2369
-0.729
23.761
0.6901
R2value
0.9528
0.9475
0.9924
0.9959
530