Overactive bladder (OAB) is a combination of urinary symptoms that includes a sudden, strong need to urinate. The major symptom of OAB is a sudden, strong urge to urinate that you can't ignore. Leak urine or have “urge incontinence.” This means urine leaks when you feel the sudden urge to go. Urinate frequently. You may need to go to the bathroom many times during the day. Wake up at night to pass urine. The cost for (branded) oral tablet 10 mg is around $411 for a supply of 30 tablets. It indicates that there is strong need of generic version for affordable healthcare. The data shows that number of people affected with overactive bladder is 37 million.

1. Progress Seminar Presentation
Formulation and Evaluation of Immediate Release Tablet in
Treatment of Overactive Bladder
Presented by: Bhumin Nitin Jain Guided by:
M. Pharmacy 2nd Year Sem III Dr. Monika Ola
22MPH1007 Associate Professor
Dept. of Pharmaceutics
1
R. C. Patel Institute of Pharmaceutical Education & Research, Shirpur

2.  Contents
• Introduction
• Aim, Need and Objective
• Time Frame
• Plan of work
• Drug Profile
• Excipients Profile
• Preformulation Studies
• Formulation Studies
• Evaluation Studies
• Work Remaining
• References 2

3.  Introduction
• Overactive bladder (OAB) is a combination of urinary symptoms that includes a
sudden, strong need to urinate.
Figure 1 Normal and Overactive Bladder
• The major symptom of OAB is a sudden, strong urge to urinate that you can't ignore.
3
Reference:https://www.ever
ydayhealth.com/overactive-
bladder/causes/

4. • Leak urine or have “urge incontinence.” This means urine leaks when you feel the
sudden urge to go.
• Urinate frequently. You may need to go to the bathroom many times during the day.
• Wake up at night to pass urine.
 Risk Factors for OAB:
• Hormone changes
• Pelvic muscle weakness or spasms
• A urinary tract infection
• Side effects from a medication
4
Reference:https://www.myrbetriqhcp.com/combi
nation-treatment/#
Figure 2 MOA of Drug

5.  Aim, Need and Objective
• Aim: To formulate and evaluate immediate release tablet in treatment of Overactive
Bladder
• Need:
1. The cost for (branded) oral tablet 10 mg is around $411 for a supply of 30 tablets. It
indicates that there is strong need of generic version for affordable healthcare.
2. The data shows that number of people affected with overactive bladder is 37
million.
Figure 3 No. of people affected by OAB
5
Reference:https://www.urovantmed
icalaffairs.com/overview-of-
overactive-bladder

6. • Objective:
1. To formulate and evaluate immediate release tablets by Direct compression.
2. To study dissolution profile and to compare their drug-release profiles with
(innovator)
3. To study stability of optimized formulation.
6

7.  Time Frame
7
Plan of work Proposed time frame(duration in month)
1-2 2-3 3-4 4-5 5-6
Literature survey ,selection of
drugs ,excipients and chemicals
Preformulation studies
Formulation design
,development and optimization
Evaluation of formulation
Stability studies
Done Remaining

8.  Plan of work
1. Literature review
2. Selection of Drug and Excipients
3. Preformulation Studies
4. Formulation Development
5. Evaluation of Formulation
6. Stability Studies of Formulation
8

9.  Drug Profile
Drug Name Drug X
Category Antimuscarinic Antagonist
Molecular weight 362.465 g/mol
BCS class BCS class I
Half-life 45-68 hrs
Log P 1.69
Solubility It is freely soluble at room temperature
in water, glacial acetic acid, dimethyl
sulfoxide, and methanol.
9

10.  Excipients Profile
10
Parameter Lactose
Monohydrate
Corn Starch Hypromellose
2910
Magnesium
Stearate
Molecular
formula
C12H22O11 H2O C27H48O20 C56H108O30 C36H70MgO4
Molecular
weight g/mol
360.31 692.65 1261.45 591.27
Solubility Freely soluble in
water; practically
insoluble in ethanol,
diethyl ether and
chloroform.
Practically
insoluble in cold
ethanol and in
cold water.
Partially soluble
in DMSO.
Soluble in cold
water,practically
insoluble in hot
water and ether,
but soluble in
mixtures of
ethanol
Practically
insoluble in
ethanol, ether and
water; slightly
soluble in warm
benzene and
warm ethanol.
Melting point 201–2020 C 256-258OC 225–230oC 117–150o C
Function Diluent / filler Disintegrant Binder Lubricant

11.  Preformulation studies
• Organoleptic properties:
Table 1 Organoleptic Properties
• Melting point: Melting point of drug was found to be 145-151°C
• UV Analysis:
Test Results
Description White Powder
Taste and Odour Bitter and Odourless
Loss on Drying 1.50 %
Figure 4 UV Spectrum of Drug
11

12. Concentration
(µg/mL)
Absorbance
5 0.265
10 0.437
15 0.627
20 0.824
25 0.981
30 1.134
Table 2 Absorbance of Drug
Figure 5 Calibration curve of drug in water
• XRD :
Figure 6 XRD Pattern of API
2θ values
3.75
7.45
11.16
14.19
18.61
19.30
20.99
23.21
25.13
Table 3 2θ Values of X-Ray
12

13. • FTIR:
13
Figure 7 FTIR of Drug
Type of Vibrations
Standard
Peakcm-1
Observed
Peakcm-1
C=O 1730-1715 1716.95
C-H 3000-2500 2876.85
C≡N 2500-2000 2298.10
C=C 2000-1500 1578.61
C-N 1500-1000 1352.98
S-O 700-500 548.29
Table 4 Reported IR Frequency of Drug

14. • Drug-Excipient Compatibility Study
14
API Excipients Ratio used
Drug X - -
Drug X Lactose monohydrate (SuperTab 14SD) 1:21.4
Drug X Corn starch (Maize Starch B Pharma Grade) 1:6.3
Drug X Hypromellose 2910 (Methocel E5 Premium LV) 1:1.2
Drug X Magnesium stearate (Hyqual, Vegetable Source) 1:0.1
Drug X Opadry pink (03F540267) 1:0.45
Drug X Opadry yellow (03F520313) 1:0.90
Drug X All excipients (for 5 mg strength) 1:21.4:6.3:1.2:0.1:0.90
Drug X All excipients (for 10 mg strength) 1:21.4:6.3:1.2:0.1:0.45
Figure 8 Normal overlay diffractogram scan of
API, Drug X tablets , 5 mg and Drug X tablets ,
5 mg Placebo
Figure 9 Normal overlay diffractogram scan of
API, Drug X tablets, 10 mg and Drug X tablets,
10 mg Placebo
The X-ray diffractogram DrugX API,
Drug X tablets 5 and 10 mg, and Drug X
tablets 5 and 10 mg placebo has shown
sharp peaks at different angles (2ϴ)
13.5°, 15.5°, 17.6°, 18.1° and
21.8°.
Table 5 Ratio of API & Excipients used

15.  Formulation studies
Trial no. Trial name Observations
1. To take trial batch by DC
and to study
physicochemical
parameters
All parameters were
found satisfactory and
meet the specification.
Dissolution of generic
Drug X tablets, 10 mg
was observed more than
85% in 15 minutes.
2. To take trial batch using
reduced particle size to
study impact on
dissolution of drug
It was concluded that
reduced API PSD has no
impact on dissolution of
drug product.
3. To take trial batch 5mg
using reduced particle size
of API to study impact on
dissolution of drug
It was concluded that
reduced API PSD has no
impact on dissolution of
drug product.
15
Sr.
No.
Name of
Ingredient
Qty (mg) / tablet
T1 (10
mg)
T2 (10
mg)
T3 (5
mg)
Optimized
Batch
5 mg 10
mg
1. Drug X 10.00 10.00 5.00 5.00 10.00
2. Lactose
Monohydrate
102.00 125.00 130.00 130.
00
125.0
0
3. Corn Starch 31.50 7.50 7.50 7.50 7.50
4. Hypromellose
2910
6.00 6.00 6.00 6.00 6.00
5. Magnesium
Stearate
0.50 1.50 1.50 1.50 1.50
6. Opadry Pink 3.75 3.75 - - 3.75
7. Opadry
Yellow
- - 3.75 3.75 -
8. Purified Water q.s q.s q.s q.s q.s

16. • Optimized Batch
Product Solifenacin SuccinateTablets, 5 mg
Dissolution
condition
USPII/ 900mL
water /50rpm
USPII/ 900mL
0.1 N HCl / 50rpm
USPII/ 900mLpH
4.5acetatebuffer/
50rpm
USPII/ 900mL
pH 6.8phosphate
buffer/ 50rpm
Time
(minutes)
%
Release
% RSD
%
Release
% RSD
%
Release
% RSD
%
Release
% RSD
10 49 28.55 44 26.01 47 18.32 49 23.15
15 75 18.98 72 24.37 79 13.64 76 16.93
30 96 4.03 101 1.48 101 0.51 92 2.94
45 97 3.5 102 1.66 101 0.93 93 2.13
Table 6 Multimedia dissolution profiles of Drug
X tablets, 5 mg
Figure 10 Multimedia dissolution profiles of Drug
X tablets, 5 mg
Product Solifenacin succinate tablets, 10mg
Dissolution
condition
USPII/ 900mL
water /50rpm
USPII/ 900mL
0.1 N HCl / 50rpm
USP II/ 900mLpH
4.5acetatebuffer/
50rpm
USPII/ 900mL
pH 6.8phosphate
buffer/ 50rpm
Time
(minutes)
%
Release
% RSD
%
Release
% RSD
%
Release
% RSD
%
Release
% RSD
10 59 29.5 65 9.98 67 15.23 61 22.82
15 78 22.62 84 8.22 90 11.19 82 17.86
30 97 1.42 98 1.8 100 1.27 93 1.65
45 97 1.55 98 1.41 100 1.59 93 1.24
Table 7 Multimedia dissolution profiles of
Drug X tablets, 10 mg
0
20
40
60
80
100
120
0 10 20 30 40 50
%
Drug
release
TIme (min.)
Multimedia dissolution profile of solifenacin succinate tablets, 10 mg
Water
0.1N HCl
pH 4.5 acetate buffer
pH 6.8 phosphate buffer
Figure 11 Multimedia dissolution profiles of Drug
X tablets, 10 mg
16
0
20
40
60
80
100
120
0 10 20 30 40 50
%
Drug
release
TIme (min.)
Water
0.1N HCl
pH 4.5 acetate buffer
pH 6.8 phosphate buffer

17. • RLD Dissolution
17
Product Innovator drug , 5 mg
Dissolution
condition
USP II / 900 mL
water / 50 rpm
USP II / 900 mL 0.1
N HCl / 50 rpm
USP II / 900 mL pH
4.5 acetate buffer /
50 rpm
USP II / 900 mL pH
6.8 phosphate buffer
/ 50 rpm
Time
(minutes)
%
Release
% RSD
%
Release
% RSD
%
Release
% RSD
%
Release
% RSD
10 37 15.89 53 7.68 62 5.83 37 23.69
15 72 12.33 72 6.54 86 4.69 56 20.78
30 97 2.48 94 4.3 101 2.58 81 8.47
45 97 1.01 99 2.45 102 1.69 85 3.6
Table 8 Multimedia dissolution profile of Innovator
drug , 5 mg
0
20
40
60
80
100
120
0 10 20 30 40 50
%
Drug
Release
Time (min.)
Water
0.1N HCl
pH 4.5 acetate buffer
pH 6.8 phosphate buffer
Figure 12 Multimedia dissolution profile of
Innovator drug , 5 mg
Product Innovator drug , 10 mg
Dissolution
condition
USP II / 900 mL
water / 50 rpm
USP II / 900 mL 0.1
N HCl / 50 rpm
USP II / 900 mL pH
4.5 acetate buffer /
50 rpm
USP II / 900 mL pH
6.8 phosphate buffer
/ 50 rpm
Time
(minutes)
%
Release % RSD
%
Release % RSD
%
Release % RSD
%
Release % RSD
10 67 7.05 60 5.54 48 28.37 48 30.06
15 88 5.23 79 5.64 70 23.68 69 23.91
30 101 1.84 99 1.65 97 6.55 92 9.39
45 101 1.49 102 1.35 100 2.04 95 2.27
Table 9 Multimedia dissolution profile of Innovator
drug , 10 mg
0
20
40
60
80
100
120
0 10 20 30 40 50
%
Drug
Release
Time (min.)
Water
0.1N HCl
pH 4.5 acetate buffer
pH 6.8 phosphate buffer
Figure 13 Multimedia dissolution profile of
Innovator drug , 10 mg

18.  Evaluation Studies
18
Trial no Dose
Tablet wt.
(mg)
Thickness(
mm)
Diameter(
mm)
Hardness(
N)
Friability(
% w/w)
Assay(%
w/w)
T1 10 mg
146.0 -
153.0
3.35 -3.40 7.51 - 7.52 39 -55 0.22 99.0
T2 10 mg
149.1 –
152.3
3.46 – 3.49 7.52 – 7.54 45 -50 0.09 98.2
T3 5 mg
148.3 –
154.9
3.39 – 3.46 7.50 – 7.53 37 -47 0.11 96.9
Optimi-
zed
Batch
5 mg
149.00 –
156.00
3.44 - 3.52 7.49 -7.52 41 – 49 0.13 97.90
10 mg
146.00 –
154.00
3.40 – 3.47 7.53 -7.55 43- 51 0.10 98.0
RLD
5 mg
146.00-
157.00
3.44- 3.51 7.48- 7.53 40- 49 0.13 100.4
10 mg
145.00-
154.00
3.39-3.47 7.52-7.58 40- 50 0.10 100.4

19.  Work Remaining
• Stability Study of Drug X tablet, 5 mg .
• Stability Study of Drug X tablet, 10 mg.
19

20.  References
• Chapple, C.R., Cardozo, L., Steers, W.D. and Govier, F.E., 2006. Drug significantly
improves all symptoms of overactive bladder syndrome. International Journal of
Clinical Practice, 60(8), pp.959-966.
• Maniscalco, M., Singh-Franco, D., Wolowich, W.R. and Torres-Colón, R., 2006.
Drug for the treatment of symptoms of overactive bladder. Clinical therapeutics,
28(9), pp.1247-1272.
• Keane, D.P. and O'Sullivan, S., 2000. Urinary incontinence: anatomy, physiology and
pathophysiology. Best Practice & Research Clinical Obstetrics & Gynaecology,
14(2), pp.207-226.
• Sudha, R.K.V., Kishore, V.S., Babu, C.H. and Jitendranath, E., 2015. Design,
Development and Evaluation of Drug Tablets. Research Journal of Pharmaceutical
Dosage Forms and Technology, 7(2), pp.111-117.
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