Escolar Documentos
Profissional Documentos
Cultura Documentos
ISSN 2349-7750
ISSN: 2349-7750
PHARMACEUTICAL SCIENCES
Available online at: http://www.iajps.com
Research Article
Corresponding Author:
Karthik Thammera,
Department of Pharmaceutics,
Nalanda Institute of Pharmaceutical Sciences,
Kantepudi, Sattenapalli, Andhra Pradesh,
India.
QR code
Please cite this article in press as Karthik et al , Formulation and Evaluation of Naftopidil Immediate
Release Tablets, Indo Am. J. Pharm. Sci, 2015;2(10).
www.iajps.com
Page 1441
Methods Used
Pre Formulation Studies
Preformulation testing is an investigation of
physical and chemical properties of a drug
www.iajps.com
Karthik et al
ISSN 2349-7750
Page 1442
Karthik et al
ISSN 2349-7750
Estimation of Naftopidil
A spectrophotometric method based on the
measurement of absorbance at 423 nm in 0.1N HCl
was used in the present study for the estimation of
Naftopidil.
Reagents
Preparation of 0.1N Hcl
8.5ml of concentrated HCl was taken in a
volumetric flask and it was made up to 1000ml
with distilled water.
Standard Solution
100 mg of Naftopidil pure drug was dissolved in
100 ml of 0.1 N HCl (stock solution-1000 g/ml),
from this 10 ml of solution was taken and the
volume was adjusted to 100 ml with 0.1 N HCl
(100 g/ml).
Procedure:
The above solution was subsequently diluted with
0.1N HCl to obtain the series of dilutions
containing 2,4,6,8,10,12,16,20,24,30, and 100g/ml
of Naftopidil. The absorbance of the above
dilutions was measured at 423 nm by using the
UV-Spectrophotometer using 0.1N HCl as the
blank. Then a graph was plotted by taking
Concentration on X-Axis and Absorbance on YAxis
which
gives
a
straight
line.
Absorbance
0.097
0.202
0.308
0.415
10
0.525
12
0.628
14
0.744
16
0.823
www.iajps.com
Page 1443
Karthik et al
ISSN 2349-7750
RESULTS
Table 2: Composition of Naftopidil Immediate Release Tablets
S.NO
1.
2.
3.
4.
5.
INGREDIENTS
F1
A. Dry mix
Naftopidil
75.00
Lactose
130.20
monohydrate
Microcrystalline
55.80
Cellulose 101
Aerosil 200 pharma
Sodium Starch
6.00
Glycollate
F2
75.00
180.00
F3
F4
F5
Quantity (mg/tab)
75.00
75.00
75.00
195.00
189.00
195.00
F6
75.00
175.00
6.00
6.00
6.00
6.00
6.00
Continue
www.iajps.com
Page 1444
Karthik et al
5.
6.
Povidone K30
Purified Water
7.
Microcrystalline
Cellulose 102
Sodium Starch
Glycollate
Aerosil 200 pharma
8.
9.
10.
Magnesium stearate
Average weight (mg)
B. Binder Solution
9.00
9.00
9.00
q.s
q.s
q.s
C. Blending
15.00
21.00
6.00
6.00
1.50
1.50
300.00
6.00
6.00
1.50
1.50
D. Lubrication
1.50
1.50
300.00
300.00
ISSN 2349-7750
15.00
q.s
9.00
q.s
6.00
q.s
6.00
6.00
30.00
6.00
6.00
3.50
1.50
1.50
3.00
1.50
300.00
1.50
300.00
1.50
300.00
INGREDIENTS
F7
F8
F9
F10
A. Dry mix
Quantity (mg/tab)
Naftopidil
75.00
75.00
75.00
75.00
Lactose
175.00
175.00
189.00
150.00
monohydrate
3.
Microcrystalline
45.00
Cellulose 101
4.
Aerosil 200 pharma
1.50
3.00
6.00
5.
Sodium Starch
6.00
6.00
6.00
12.00
Glycollate
B.BINDER SOLUTION
5.
Povidone K30
6.00
6.00
15.00
9.00
6.
Purified Water
q.s
q.s
q.s
q.s
C. BLENDING
7.
Microcrystalline
30.00
30.00
6.00
Cellulose 102
8.
Sodium Starch
3.50
3.50
6.00
Glycollate
9.
Aerosil 200 pharma
1.50
1.50
1.50
D. LUBRICATION
10.
Magnesium stearate
1.50
1.50
1.50
3.00
Average weight (mg)
300.00
300.00
300.00
300.00
Table 4: Solubility data of Naftopidil across pH
1.
2.
www.iajps.com
F11
F12
75.00
150.00
75.00
150.00
45.00
45.00
6.00
12.00
6.00
12.00
9.00
q.s
9.00
q.s
3.00
300.00
3.00
300.00
Medium
Solubility at 25 C (mg/ml)
0.110-3
1110-3
1.910-3
0.610-3
< 0.110-3
< 0.110-3
< 0.110-3
Page 1445
Karthik et al
ISSN 2349-7750
Ratio
API: Expt
Initial
Observation
Final observation
Conclusion
Compatible
Compatible
1
2
API (Naftopidil)
API+ Lactose monohydrate
--1 :1
Off-White
Off-White
40C/75% RH
2nd week
4th week
Off-White
Off-White
Off-White
Off-White
3
4
1:1
1:1
Off-White
Off-White
Off-White
Off-White
Off-White
Off-White
Compatible
Compatible
5
6
7
1:1
1:1
1:1
Off-White
Off-White
Off-White
Off-White
Off-White
Off-White
Off-White
Off-White
Off-White
Compatible
Compatible
Compatible
1:1
Off-White
Off-White
Off-White
Compatible
www.iajps.com
B.D (gm/ml)
T.D (gm/ml)
0.490.013
0.620.061
0.6130.008
Blend Property
C.I (%)
H.R
Angle of Repose
20.972.445
1.260.028
44.912.05
0.7950.025
22.950.009
1.2980.009
26.521.32
0.660.003
0.750.165
9.560.009
1.180.165
29.561.64
0.780.012
0.860.231
9.360.156
1.140.156
27.461.52
0.720.011
0.790.013
9.241.447
1.100.018
28.411.69
0.620.028
0.690.009
7.910.124
1.080.015
29.251.39
0.680.009
0.740.011
8.200.098
1.890.001
28.540.42
0.700.089
0.770.011
8.290.089
1.090.021
29.962.18
0.620.015
0.5440.014
0.67 0.006
0.6970.018
7.600.075
220.224
1.080.005
1.2820.011
29.931.70
0.580.012
0.5840.015
0.760.231
0.7350.015
8.360.156
20.5130.226
1.240.156
1.2580.014
24.461.52
260.014
28.470.70
Page 1446
Karthik et al
S.
No
1
2
3
4
5
Physical
parameter
Weight
variation
Hardness
(KP)
Thickness
(mm)
Friability
%
Disintegrati
on time
ISSN 2349-7750
F1
F 10
F 11
F 12
1.65
1.57
1.42
1.54
1.18
1.35
1.44
1.23
1.48
1.54
1.63
1.38
8.8
8.4
8.2
9.4
9.1
8.8
9.4
8.8
8.5
8.8
9.0
8.6
4.41
4.40
4.50
4.37
4.37
4.85
4.89
4.90
4.93
4.12
4.02
4.14
0.05
0.12
0.10
0.18
0.12
0.07
0.06
0.14
0.15
0.18
0.10
0.15
3min
25sec
2min
30sec
2min
24sec
1min
29sec
1min
45sec
1min
20sec
1min
30sec
1min
40sec
1min
20sec
1min
18sec
1min
10sec
1min
10sec
Parameter
F1
F2
F3
F4
F5
F6
F7
F8
F9
F 10
F 11
F12
1
2
Assay (%)
Dissolution
study(NLT
75% in 45
mins)
99.9
63.9
98.6
62.4
98.5
59.6
100.7
63.6
98.7
60.0
99.5
72.8
98.7
58.7
99.6
67.4
100.6
65.7
98.7
85.5
98.9
75.7
98.7
86.7
F1
F2
0
44.0
49.5
53.9
61.4
63.9
70.0
74.3
0
40.1
47.5
53.0
58.4
62.4
67.4
72.4
120
79.4
76.2
www.iajps.com
Page 1447
Karthik et al
ISSN 2349-7750
www.iajps.com
0
39.8
43.7
49.1
54.8
60.0
62.8
68.3
70.3
0
49.2
57.6
59.7
67.7
72.8
77.8
77.5
77.6
Page 1448
Karthik et al
ISSN 2349-7750
www.iajps.com
Page 1449
Karthik et al
ISSN 2349-7750
www.iajps.com
TIME
INITIAL
15 DAYS
0
5
10
15
30
45
60
90
120
0
70.5
77.2
79
80.9
86.1
86.8
86.2
85.5
0
65
73.5
77.8
79.2
84.6
85
84.7
84.4
Page 1450
Karthik et al
ISSN 2349-7750
TIME
www.iajps.com
0
62
72.5
77.8
79.2
84.6
85
84.7
84.4
Page 1451
Karthik et al
ISSN 2349-7750
www.iajps.com
Page 1452