Upload
vuongtruc
View
239
Download
1
Embed Size (px)
Citation preview
127
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
7.0 Formulation and evaluation of ASA suppositories, Suppositories
loaded ASA-nanoparticulates
7.1 Preparation of ASA-suppositories
ASA containing glycerinated gelatin suppository formulations prepared based on
fusion method. Variable concentrations of gelatin and glycerin were weighed accurately.
The concentration of glycerin and gelatin were varied for each formulation to select the
best optimized formulation1.
Twenty four formulations were prepared (Fs1-Fs24) by fusion method. The
amount of drug and base required was calculated based on the displacement. Glycerin,
gelatin and water melted to 60 ⁰C, over water bath followed by the addition of
micronized ASA under stirring to have content uniformity. The mixture was cooled to
50 ⁰C and poured in to the pre calibrated metallic mould and placed into the refrigerator
for solidification shown in table 7.1.
7.2 Preparation of gelatin suppositories loaded ASA- nanoparticles
ASA-nanoparticles loaded in to the suppositories as discussed in the literature.
Glycerinated gelatin was selected as the base for loading nanoparticles. Based on
literature drug diffusion efficiency was comparatively more in glycerinated gelatin.
Based on the previously performed characterization studies for the nanoparticles and
ASA suppositories, best formulations were selected, and based on displacement value
100 mg of ASA nanoparticles were added to the molten base and suppositories were
prepared by fusion process in metallic mould2. The base which was fused at 60⁰C, then
128
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
the nanoparticles was added and stirred with glass rod to have content uniformity and
poured in to the one gram metallic mould and solidified in refrigerator by keeping
overnight. Composition of suppositories loaded ASA- nanoparticles was shown in table
7.2.
Table 7.1 Representing different formulation and their composition of ASA-
suppositories
Formulation
code
Gelatin
(gm)
Glycerin(gm)
Water(gm)
ASA(mg)
FS1 0.663
5.96 Q.S 600
FS2 0.828
5.80 Q.S 600
FS3 0.994
5.636 Q.S 600
FS4 1.16
5.2 Q.S 600
FS5 1.326
5.31 Q.S 600
FS6 1.65
4.98 Q.S 600
FS7 2.33 4.30 Q.S 600
FS8 1.99 4.64
Q.S
600
FS9 1.83
4.80 Q.S
600
FS10 1.66 4.97
Q.S
600
FS11 1.5 5.13
Q.S
600
FS12 1.33
5.30
Q.S
600
FS13 2.86 3.77 Q.S
600
FS14 2.33 4.30 Q.S
600
FS15 1.86 4.77 Q.S
600
FS16 1.66 4.97 Q.S
600
FS17 1.53 5.10 Q.S
600
FS18 1.33 5.30 Q.S
600
FS19 0.39 6.24 Q.S 600
FS20 0.66 5.97 Q.S
600
FS21 0.79 5.84 Q.S
600
FS22 0.99 5.64 Q.S
600
FS23 1.32 5.31 Q.S
600
FS24 1.65 4.98 Q.S 600
129
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
*Table representing formula for six suppositories
Table 7.2 Composition of suppositories loaded ASA nanoparticles
Formulation code Fas2 Fas4 Fas9 Fas11 Fbs1 Fbs3 Fbs4 Fbs8 Fbs11 Fbs12
Gelatin (gm)
0.828
1.16
1.83
1.5
2.86
1.86
1.66
0.66
1.32
1.65
Glycerin(gm)
5.80
5.2
4.80
5.13
3.77
4.77
4.97
5.97
5.31
4.98
Water(gm)
Q.S
Q.S
Q.S
Q.S
Q.S
Q.S
Q.S
Q.S
Q.S
Q.S
ASA
nanoparticles(mg)
600
600
600
600
600
600
600
600
600
600
*Table representing formula for one suppository
Figure 7.1 Prepared ASA-suppositories
Evaluation methods for ASA-Suppositories and suppositories loaded ASA-
nanoparticles
7.3 Appearance and physical integrity of suppositories
Appearance of the prepared ASA-suppositories and suppositories loaded ASA-
nanoparticles was evaluated with naked eye physical integrity of the suppositories was
evaluated by slicing the suppositories with stainless steel blade in to two half’s and
130
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
observed to find out the presence of fissure and pits3.
7.4 Weight variation
Twenty suppositories were weighed and average weight was calculated. Each
suppository was then individually weighed by using digital balance. Not more than two
of the individual masses deviate from the average mass by more than 5% and non deviate
by more than twice4.
7.5 Mechanical Strength
The breaking strength or crushing strength was determined for measuring fragility
or brittleness of suppositories, which assess whether the suppositories will be able to
withstand the hazards of packing, transporting and normal handling or not. Suppositories
were randomLy selected and subjected for crushing using (Erweka hardness tester)4.
Figure 7.2 Erweaka hardness tester
131
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
7.6 Content uniformity
Content uniformity test was determined by spectrophotometric method. The
suppository and suppositories loaded nanoparticles was individually melted, dissolved in
100 mL of phosphate buffer pH 7.2 in separate volume flask and the solution was filtered
using 0.45 µ membrane. After suitable dilution the sample was measured using U.V.
spectrometry at a wave length of 225 nm5.
7.7 Disintegration Test
The disintegration time is a critical factor in the determination of the release rate
of the active ingredient(s) from the suppository. During this test, the time taken for the
suppository to melt or disperse is measured when immersed in a water bath maintained at
constant temperature (37±10C). The time required for the suppository to melt or disperse
in the surrounding water was noted6.
7.8 Liquefaction time
Liquefaction time of the suppositories was determined based on the procedure
discussed in literature7. Glass cylinder with external diameter 50 mm, internal diameter of
20 mm and length 30 mm, two ends of the cylinder was fixed with circulating pump;
temperature of circulating medium was maintained at 37±10C. Inside the cylinder
cellophane dialyzer tubing was used to hold the suppository and then the rubber tubing
from water circulation pump was attached to one end of the glass cylinder separate
provision is provided in to the glass cylinder for thermometer arrangement7.
132
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Figure 7.3 Liquefaction assembly
7.9 Stability studies
Satiability studies were conducted based on the procedure discussed in literature,
to assess the stability of nanoparticles, suppositories and suppositories loaded
nanoparticles the samples are stores at room temperature (22⁰C - 27⁰C) and at
refrigerator conditions 5 ⁰C for three months, sampling was done at 1, 2, 3 months and
evaluated for FTIR and DSC to find out the changes during storage8.
7.10 In-vitro dissolution for ASA suppositories and suppositories loaded ASA
nanoparticles
In-vitro drug release has performed by placing the suppository in a dialysis bag
whose molecular weight was cut 10 kDa and 5 mL of dissolution medium pH 7.2
phosphate buffer and glass beads were added in to the bag and sealed and the bag was
placed in the receptor compartment containing 50 mL of phosphate buffer at 37 ± 5ºC
over a magnetic stirring at 50 rpm samples were withdrawn at regular intervals and
133
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
replaced with equal amount of buffer for a period of 24 h9. The assemblage was designed
as shown in the represented in figure below.
Figure 7.4 Diagrammatic representation of suppositories and suppositories loaded
nanoparticles in-vitro drug release assemblage.
7.11 Mathematical modeling
Drug release mechanisms and kinetics are the two important characteristics of a
delivery systems in describing the drug dissolution profile. A number of mathematical
models have been developed to analyze the drug release from types of controlled release
drug delivery systems10
.
The korsmeyer-peppas power law equation predicts that the fraction release of
drug of exponentially is related to the release time and adequately describes the release of
drug from slabs, cylinders and spheres.
134
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Kinetics of in-vitro drug release
To study the release kinetics of in-vitro drug release, data was applied to kinetic
models such as zero order, first order, Higuchi and Korsmeyer- Peppas.
Zero order
Where K0 - is the zero-order rate constant expressed in units of concentration/time
t -is the time in hrs.
First order
Where C0 - is the initial concentration of drug,
K - is the first order constant
t - is the time in hrs.
Higuchi
Where Qt - is the amount of the release drug in time t,
K- is the kinetic constant and t- is time in hrs
Korsmeyer Peppas
C = K0t
LogC = LogC0 – Kt / 2.303
Qt = Kt1/2
Mt/ M∞ = Kt n
135
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Where Mt - represents amount of the released drug at time t,
M∞- is the overall amount of the drug (whole dose) released
K- is the diffusional characteristic of drug/ polymer system constant
n- is a diffusional exponent that characterizes the mechanism of release of drug.
A plot of the log (Drug released) Vs. log time yields slope “n” having the value –
n= 0.5 indicates fickian diffusion
n= 0.5 to 1 or n= 0.5 to 0.89 indicates anomalous non fickian diffusion.
In this the rate of solvent penetration and drug release are in the same range. This
deviation is due to increased drug diffusion from the matrix by the solvent induced
relaxation of the polymer.
n= 0.89 or n=1 indicates zero order release which can be achieved when
drug diffusion is rapid compared to the constant rate solvent induced
relaxation and swelling in the polymer.
Use of the power law equation to analyze the rate of drug release from a porous
system will probably lead to n > 0.5, since the combined mechanism will shift the release
exponent towards the smaller values.
136
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Table 7.3 Physiochemical evaluation results of ASA- suppositories (Fs1-Fs24)
Formulation
code
Weight
variation
(gm± S.D)
Mechanical
strength
(kg ± S.D)
Content
uniformity
(% content ±
S.D)
Disintegration
time
(minutes ± S.D)
Liquefaction
Temperature
(⁰C)
Fs1 1.01 ± 0.012 1.71 ± 0.01 95.06 ± 1.4 8.9 ± 1.7 29 ⁰C
Fs2 1.01 ± 0.013 0.88 ± 0.01 95.33 ± 1.1 8 ± 0.7 29 ⁰C
Fs3 1.004 ± 0.001 1.107 ±0.01 96.4 ± 0.5 8.5 ± 0.8 30 ⁰C
Fs4 1.06 ± 0.01 1.31 ± 0.01 96.2 ± 1 8.4 ± 1 29 ⁰C
Fs5 1.01 ± 0.01 2.11 ± 0.01 96.16 ± 1.04 10 ± 1.2 31 ⁰C
Fs6 1.02 ± 0.005 1.91 ± 0.03 93.5 ± 0.5 9 ± 1.1 31⁰C
Fs7 1.02 ± 0.005 1.53 ± 0.01 96.66 ± 2.3 8.9 ± 0.1 30 ⁰C
Fs8 1.02 ± 0.001 1.61 ± 0.02 97.66 ± 0.5 8.8 ± 0.8 30 ⁰C
Fs9 1.05 ± 0.06 0.82 ± 0.01 98.56 ± 0.5 8.2 ± 0.6 29 ⁰C
Fs10 1.01 ± 0.006 1.9 ± 0.01 97.1 ± 1 9.5 ± 1 30 ⁰C
Fs11 1.003 ± 0.007 1.61 ± 0.01 94.2 ± 1 8.7 ± 1.2 29 ⁰C
Fs12 1.002 ± 0.006 1.53 ± 0.02 95.16 ± 1.6 8.4 ± 0.3 29 ⁰C
Fs13 1.04 ± 0.02 2.3 ± 0.15 96±2 9.83±0.28 31⁰C
Fs14 1.08 ± 0.015 1.7 ± 0.1 94.6±1.5 8.6±0.57 28⁰C
Fs15 1.04± 0.03 1.6 ± 0.15 93.3±3.2 8.96±0.057 28⁰C
Fs16 1.1 ± 0.011 1.1 ± 0.1 94±2 10.1±0.17 30⁰C
Fs17 1.07 ± 0.02 1.1 ± 0.05 94.3±2.5 8.56±0.6 29⁰C
Fs18 1.06 ± 0.03 1 ± 0.05 94.4±2.25 8.23±0.25 28⁰C
Fs19 1.07 ± 0.03 0.8 ± 0.26 95.6±3.5 8.26±0.2 28⁰C
Fs20 1.05 ± 0.02 1.1 ± 0.2 94.3±3.5 8.56±0.81 28⁰C
Fs21 1.06 ± 0.04 1.2 ± 0.05 97.6±1.5 8±0.1 28⁰C
Fs22 1.05 ± 0.04 1.1 ± 0.11 96.3±2.08 8.76±0.41 28⁰C
Fs23 1.04 ± 0.05 0.7 ± 0.11 96.3±1.52 9.2±0.1 29⁰C
Fs24 1.07 ± 0.05 2.3 ± 0.05 94.3±2.3 11.06±0.8 31⁰C
Table 7.4 Physiochemical evaluation results of suppositories loaded ASA-
nanoparticles
Formulation
code
Weight
variation
(gm± S.D)
Mechanical
strength
(kg ± S.D)
Content
uniformity
(% content ±
S.D)
Disintegration
Time
(minutes ± S.D)
Liquefaction
Temperature(⁰C)
Fas2 1.02 ± 0.008 0.78 ± 0.4 82.3 ± 0.5 7.2 ± 0.3 29 ⁰C
Fas4 1.02 ± 0.004 1.10 ± 0.1 76 ± 1.1 8.1 ± 2 30 ⁰C
Fas9 1.05 ± 0.2 0.81 ± 1.2 88.9 ± 1.8 7.8 ± 1.2 29 ⁰C
Fas11 1.01 ± 0.4 1.21 ± 1.4 74.2 ± 0.8 8.5 ± 2.3 30 ⁰C
137
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Table 7.5 In-vitro characterization of suppositories loaded ASA-nanoparticles
Formulation
code
Weight
variation
(gm ± S.D)
Melting
point
(⁰C)
Disintigration
time
(minutes ±
S.D)
Mechanical
strength
(kg ± S.D)
Content
uniformity
(%content
± S.D)
Fbs1 1.03±0.01 32 8.5±0.5 1.82±0.02 67.16±1.25
Fbs3 1.04±0.0208 31 8.6±2.08 1.66±0.02 77.16±4.01
Fbs4 1.037±0.04 32 9.6±1.15 1.59±0.005 55.33±3.05
Fbs8 1.02±0.023 31 8.3±1.52 1.64±0.03 76.73±4.6
Fbs11 1.117±0.16 30 8.2±2 1.81±0.011 73.66±3.05
Fbs12 1.04±0.02 31.5 9.2±2 1.65±0.02 56.33±1.52
Table 7.6 In-vitro drug release of ASA suppositories (Fs1-Fs12)
Cumulative Percentage Drug Release
Time
(minutes)
Fs1 Fs2 Fs3 Fs4 Fs5 Fs6 Fs7 Fs8 Fs9 Fs10 Fs11 Fs12
0 0 0 0 0 0 0 0 0 0 0 0 0
5 16.4
± 0.36
21.5
± 0.5
18.5
± 0.5
21.16
±1
12.16
± 0.28
13.93
± 0.3
20.83
± 0.76
19.6
±
0.52
26.4
± 0.36
18.5
± 0.5
21.5
± 0.5
22.63
± 0.5
15 46.5± 0.5 51.4±
0.5
50±1 50.1
± 0.85
23.96
± 0.25
26.9
± 0.36
44.13
± 0.32
40.6
±
0.55
58.4
± 0.35
44.5
± 0.5
48.2±
0.6
43±1
30 72.73
± 0.64
76.56
± 0.8
73.96
± 0.95
74.83
± 0.47
47.96
± 0.05
50.3
± 0.79
62.5±
0.5
68.5
± 0.5
83±1 71.7±1.1 75.6
± 0.5
71.63
± 0.5
45 85.43
± 0.51
92
±1
88.3
± 0.60
90.6
± 0.52
82.06
± 0.2
85.43
± 0.37
87.4
± 0.51
84.8
± 0.8
94.63
± 0.55
85.16
± 0.3
87.63
± 0.5
82.63
± 0.5
60 96.5
± 0.5
98.06
±1
96.9
± 0.1
99.3
± 0.45
91.06
± 0.1
95.16
± 0.37
97.5
± 0.45
95.6
±0.55
97.6
± 1.8
97.23
± 0.49
98.7
±1.5
97
±1
Figure 7.5 In-vitro drug release of ASA suppositories (Fs1-Fs12)
0
20
40
60
80
100
120
0 20 40 60 80
Pe
rce
nta
ge r
ele
ase
Time (minutes)
Fs1Fs2Fs3Fs4Fs5Fs6Fs7Fs8Fs9Fs10Fs11
138
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Figure 7.6 In-vitro drug release of optimized formulation of ASA-suppositories.
Table 7.7 In-vitro drug release Kinetics of ASA-suppositories
(Fs1-Fs12)
Formulation
code
Krosmayer’s
Peppas
equation
n r2
Higuchis
r2
First order
K1 r2
Zero order
K0
r2
Fs1 0.722 0.986 0.992 -0.052 0.968 1.847 0.788
Fs2 0.630 0.988 0.967 -0.028 0.968 1.939 0.682
Fs3 0.679 0.973 0.990 -0.025 0.973 1.893 0.737
Fs4 0.652 0.989 0.992 -0.034 0.899 1.934 0.729
Fs5 0.852 0.990 0.958 -0.018 0.949 1.625 0.971
Fs6 0.801 0.978 0.979 -0.022 0.932 1.697 0.969
Fs7 0.638 0.997 0.996 -0.057 0.967 1.823 0.84
Fs8 0.664 0.996 0.996 -0.049 0.986 1.807 0.830
Fs9 0.548 0.984 0.980 -0.089 0.961 2.017 0.465
Fs10 0.684 0.993 0.996 -0.057 0.973 1.848 0.809
Fs11 0.629 0.993 0.994 -0.076 0.935 1.910 0.734
Fs12 0.603 0.996 0.995 -0.051 0.970 1.818 0.772
Table 7.8 In-vitro drug release study of suppositories loaded ASA-nanoparticles
0
20
40
60
80
100
120
0 20 40 60 80
Cu
mm
ilati
ve
Pe
rce
nta
ge r
ela
se
Time (minutes)
Fs2
Fs4
Fs9
Fs11
139
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Cumulative Percentage Drug release
Time
(hr) Fas2 Fas4 Fas9 Fas11
0 0 0 0 0
1 0.014±0.004 0.017±0.003 0.014±0.002 0.0663±0.08
2 19.6±1.52 18.6±1.52 22±1 16.6±1.93
4 29.63±1.51 33±1.41 33.6±1.52 26.6±0.57
8 35.4±0.52 41±1 44±2 34.2±1.31
12 55±1 51±1.73 56.6±1.52 47.6±1.52
16 68±1 62.6±1.52 67.3±1.52 58±1
20 76.8±0.98 66.6±1.52 76±1 66±1
24 82.3±1.52 71±0.85 86.4±1.63 74.06±0.9
Figure 7.7 In-vitro drug release study of ASA form suppositories loaded
nanoparticles
Table 7.9 In-vitro drug release kinetics of suppositories loaded ASA-nanoparticles
(Fas2, Fas4, Fas9, Fas11)
Formulation
code
Korsmeyer’s Peppas
equation
n r2
Higuchis
r2
First order
K1 r2
Zero order
K0
r2
Fa2 0.310 0.637 0.886 -0.030 0.988 3.866 0.899
Fa4 0.315 0.627 0.968 -0.022 0.971 3.502 0.800
Fa9 0.304 0.619 0.923 -0.035 0.969 3.340 0.851
Fa11 0.477 0.666 0.983 -0.023 0.988 3.464 0.896
0
20
40
60
80
100
0 10 20 30
Pe
rce
nta
ge r
ele
ase
Time (Hours)
Fas2
Fas4
Fas9
Fas11
140
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Table 7.10 In-vitro drug release of ASA-suppositories (Fs13-Fs24)
Cumulative Percentage Drug Release (mean ± S.D)
Time
(min)
Fs13
Fs14
Fs15
Fs16
Fs17
Fs18
Fs19
Fs20
Fs21
Fs22
Fs23
Fs24
0 0 0 0 0 0 0 0 0 0 0 0 0
5
13.66±3.21
16±2
19±1
21.3±1.52
21.3±1.52
32.6±2.2.08
26.6±1.5
24.6±1.52
23.6±1.15
21.3±1.5
29±1
20±1
10
28±1
34.6±1.5
38.6±1.5
42±2
42.6±2.08
53±2
45.6±3.05
43.3±1.52
40.6±2.08
39±1
49.3±0.5
37.6±7.5
15
40.3±1.5
44±1
49±1
51±1`
52.6±0.5
74.6±1.5
60.3±2.08
58±1
55.6±1.15
53.3±1.5
69±1
55.6±1.5
30
71±1
74.33±1.15
77±1
83.6±3.51
84.3±3.2
87.3±1.5
73.6±2.08
70±1
68.6±1.52
64.3±2.5
80±1
74.3±3.2
45
85±2
86±1
90±1
93.3±1.52
93.8±1.19
92.6±1.5
86.6±1.52
84±1
83±1
76.6±1.5
91.3±1.5
87±1
60
95±2
92±1
96.3±1.5
96.06±3.71
94.06±1.1
94.3±3.5
94.3±2.08
96.6±2.5
92.6±2.08
90.6±1.5
99±1
97±1.7
Figure 7.8 In-vitro drug releases of ASA-suppositories
(Fs13-Fs24)
0
20
40
60
80
100
120
0 20 40 60 80
Fs13
Fs14
Fs15
Fs16
Fs17
Fs18
Fs19
Fs20
Fs21
Fs22
Fs23
Fs24
141
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Figure 7.9 In-vitro dissolution results of optimized formulation ASA-suppositories
Figure 7.10 In-vitro dissolution study of optimized formulation ASA from
nanoparticles and suppositories loaded nanoparticles Fb9, Fbs23
0
20
40
60
80
100
120
0 20 40 60 80
Pe
rce
nta
ge
Cu
mila
tive
pe
rce
nta
ge r
ele
ase
Time (minutes)
Fs13
Fs15
Fs16
Fs20
Fs23
Fs24
0
10
20
30
40
50
60
70
80
0 5 10 15 20 25 30
% P
erc
en
ate
gC
um
mila
tive
pe
rce
nta
ge r
ele
ase
Time (hours)
142
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Table 7.11 In-vitro kinetics of ASA- suppositories (Fs13-Fs24)
Formulation
code
Zero order
K0 r2
First order
K1 r2
Higuchi
r2
Krosmayer’s Peppas
n r2
Fs13 1.819 0.851 -0.022 0.985 0.909 0.557 0.809
Fs14 1.824 0.747 -0.018 0.996 0.926 0.723 0.969
Fs15 1.914 0.697 -0.024 0.996 0.949 0.662 0.949
Fs16 1.969 0.588 -0.024 0.986 0.927 0.626 0.962
Fs17 1.961 0.526 -0.022 0.939 0.912 0.62 0.95
Fs18 2.026 0.49 -0.018 0.92 0.815 0.426 0.883
Fs19 1.889 0.307 -0.019 0.986 0.953 0.504 0.954
Fs20 1.87 0.486 -0.022 0.927 0.969 0.53 0.963
Fs21 1.859 0.436 -0.017 0.995 0.957 0.553 0.958
Fs22 1.729 0.552 -0.015 0.957 0.965 0.557 0.956
Fs23 2.011 0.452 -0.03 0.921 0.912 0.484 0.929
Fs24 1.903 0.611 -0.024 0.962 0.958 0.626 0.953
Table 7.12 In-vitro dissolution of suppositories loaded ASA-nanoparticles
(Fbs13, Fbs15, Fbs16, Fbs20, Fbs23, Fbs24)
Cumulative Percentage Drug release
Time(hr) Fbs13 Fbs15 Fbs16 Fbs20 Fbs23 Fbs24
0 0 0 0 0 0 0
1 0.11±0.01 0.21±0.02 0.28±0.01 0.14±0.01 0.3±0.01 0.26±0.04
2 6.5±0.5 8.066±0.15 11.86±1.59 13.2±0.81 20.6±2.5 17±1
4 12.06±0.9 11.2±0.3 21.4±1.47 18.3±0.91 25.1±0.76 24.4±1.25
8 22±1 14.6±0.5 29.4±1.44 33.3±2.5 44±1 33.3±1.52
12 31.8±0.76 24.96±0.65 37.06±1.05 41.3±2.5 57±1 42.83±2.25
16 37.8±0.28 31±0.8 40.73±0.55 46.3±3.05 64.9±0.85 52±1
20 42.16±1.04 36.13±0.3 46.6±1.55 52.6±1.52 67.33±1.5 60±1
24 51.16±0.76 40.46±0.47 53.06±2 56±1 72.13±1.8 63.83±1.25
143
Chapter 7 Formulation, Evaluation of ASA-suppositories
Suppositories loaded ASA-nanoparticles
Figure 7.11 In-vitro drug release study of ASA form suppositories loaded
nanoparticles
Table 7.13 In-vitro kinetics of suppositories loaded ASA-nanoparticles
(Fbs13, Fbs15, Fbs16, Fbs20, Fbs23, Fbs24)
Formulation
code
Zero order
K0 r2
First order
K1 r2
Higuchi
r2
Krosmayer’s Peppas
n r2
Fbs13 2.098 0.986 0.029 -0.996 0.998 1.984 0.886
Fbs15 1.667 0.984 0.021 -0.993 0.989 1.597 0.861
Fbs16 2.027 0.962 0.029 -0.984 0.990 1.693 0.856
Fbs20 2.225 0.954 0.033 -0.978 0.989 1.947 0.851
Fbs23 2.975 0.946 0.056 -0.986 0.986 1.831 0.863
Fbs24 2.561 0.970 0.042 -0.991 0.991 1.826 0.837
0
10
20
30
40
50
60
70
80
0 5 10 15 20 25 30
% C
DR
Time (Hours)
Fbs13
Fbs15
Fbs16
Fbs20
Fbs23
Fbs24