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FORMULATION AND EVELUATION OF BUCCAL CAVITY

TABLETS OF IBUPROFEN

A project report submitted

In partial fulfillment of the requirement

For the award of the degree of

BACHELOR OF PHARMACY

Mohd Parvez
EnrollmentNo-131583

Under the guidance of

Dr Ritu Gupta

DEPARTMENT OF PHARMACEUTICS
INVERTIS INSTITUTE OF PHARMACY
INVERTIS UNIVERSITY
BAREILLY-LUCKNOW HIGHWAY, NH-24, BAREILLY, U.P

2016---2017
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CERTIFICATE

This is to certify that the project report entitled Formulation and Evaluation of
Buccal cavity Tablets of Ibuprofen is being submitted by Mohd Parvez bearing
a Enrollment no. 131559 in partial fulfillment of the requirement for the award of
the Degree of Bachelor of Pharmacy, for the elective subject Novel Drug
Delivery System at Invertis Institute of Pharmacy, Invertis University, Bareilly.
The Institute wishes him all the success in life
.

Supervisor Head of the department

Dr .Ritu Gupta Mr. Ajit Yadav
Associate professor

ACKNOWLEDGEMENT
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It is said that accomplishments must be credited to those who had put up

The foundations of the particular chore. In a work of this magnitude, it was natural to solicit

guidance, help and co-operation from many people and I like to acknowledge all those who

generously provided their time and expertise to maintain the quality of work.

First and foremost I express my profound gratitude and venerable regards to my guide

Dr .Ritu Gupta as a teacher she has always strived to inculcate the scientific attitude in me. I

am thankful to her for his guidance, vital encouragement, incisive criticism and dynamic

assistance. She was always present for me, whenever I needed him and I cherish the amount of

freedom I have enjoyed during this tenure under him.

I would like to express my sincere regards to Mr. Ajit yadav Head of the Department,

who is guardian figure to me. He supported me in my research and instilled confidence to reach

greater heights in my life and Mr. Vipin Agrwal for his help, fruitful knowledge, suggestions

and advice for the work.

This task would have been fruitless without the blessing, support, encouragement and

inspiration o f Mr.Himanshu Joshi and Mr.Shashank Chaturvedi. Here I pay tributes to my

parents for lifting me up in my life. I sincerely thank them for their love, trust, patience &

support without which I would have failed to stand where I am standing today. My deepest sense

of gratitude towards my father, Mr. Zahid Qureshi and my mother Mrs. Farzane Bee who has

always motivated and contributed towards the pursuance of my studies, without worrying about

all odds. My sincere thanks to my brother Dr. Javed Qureshi who has always played a role of a

wise advisor and he really deserves heartfelt thanks for her wishes, love and support.
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At this moment I really shall not forget my sister Shafia who always dreamed of me

reaching to this level. I would really thank all the rest of my family who have directly and

indirectly helped me to achieve my goals.

I am grateful to Dr .Umesh Gautam chancellor of Invertis University for his words of

encouragement and timely support.

I express my indebtedness to our vice chancellor prof. Jadish Rai for his help and

cooperation throughout my project work.

I express my sincere thanks to Dr. Y.D.S. Arya for his kindness, helpfulness and

motivating thoughts.

I really feel short of words when it comes in expressing my deep sense of gratitude

towards, Mohd Rizwan ,Amir khan , Kunwar Pal Singh, Rajat Gupta , Bharat Singh

,Anurag pdy , Keshav Sharma, and Nasreen khan, for all their cooperation, support and

making me believe that I am capable of doing even better.

Words fail to express my gratitude towards our M.pharm seniors Mr. Ashish Gangwar,

Mr. Akhil Chaudhary, and Ms. Sumbul Naaz helped me to achieve my targets.

Date:

Place: Mohd Parvez

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CONTENTS

CHAPTER NO. TITEL NO. PAGE NO.

I
NITRODUCTION 6-12

II 13-14
REVIEW OF LITERATURE

III PRE FORMULATION 15-17

IV FORMULATION 18-19

V EVALUATION 20-38

VI RESULT AND 39-41

DISCUSSION
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CHAPTER I
INTRODUCTION
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INTRODUCTION

The oral cavity is an attractive site for the administration of drugs because of ease of
administration. Various dosage forms like Tablets, Capsules, and Liquid preparations are
administered by oral route. In recent years delivery of therapeutic agents through buccal mucosa
has gained significant attention. There is a possibility for mucosal (local effect) and transmucosal
(systemic effect) drug Administration. In first case the mucosal administration of drugs is to
achieve site-specific release of drugs on the mucosa, whereas, in second case, transmucosal
administration involves drug administration through mucosal barrier to reach the systemic
circulation. Among the various transmucosal routes like nasal, rectal, vaginal, ocular, pulmonary
and buccal routes, the buccal mucosa is an attractive alternative to the oral route of drug
administration and it is a potential site for the delivery of drugs to the systemic circulation.
Therapeutic agents administered through buccal mucosa enters directly to the systemic
circulation and there by circumvent the first-pass hepatic metabolism gastric irritation and other
problems associated with conventional oral route. Among these the buccal mucosa has several
advantages like excellent accessibility, an expanse of smooth muscle, immobile mucosa,
moderate permeability, less enzymatic activity and suitable for the administration of retentive
dosage forms. Moreover, buccal drug absorption can be promptly terminated in case of toxicity
by removing the dosage form from the buccal cavity. It is also possible to administer therapeutic
agent to patients who cannot be dosed orally to prevent accidental swallowing. Therefore
adhesive mucosal dosage forms were suggested for oral delivery, which includes adhesive
tablets, adhesive gels and adhesive patches. So, buccal route is an attractive site for
administration of drugs. These buccal tablets are small, flat and are intended to be held between
the cheek and teeth or in the cheek pouch and an ideal buccal adhesive system must have the
following properties: should adhere to the site of attachment for few hours, should release the
drug in controlled manner and should provide the drug release in an unidirectional way in to the
mucosa.
Buccal drug delivery was introduced by Orabase in 1947, when gum tragacanth was mixed with
dental adhesive powder to supply penicillin to the oral mucosa (Sudhakar et al., 2006). Buccal
route of drug delivery is a good alternative, amongst the various routes of drug delivery. Oral
 Page No8

route is perhaps the most preferred for the patients. Within the oral mucosal cavity, the Buccal
region offers an attractive route of administration for systemic drug delivery. However, oral
administration of drugs has disadvantages such as hepatic first pass metabolism and enzymatic
degradation within the GI tract, that prohibit oral administration of certain classes of drugs
especially peptides and proteins. Buccal routes of drug delivery offer distinct advantages over
oral administration for systemic drug delivery. These advantages include possible bypass of first
pass effect, avoidance of pre-systemic elimination within the GI tract, these factors make the oral
mucosal cavity a very attractive and feasible site for systemic drug delivery. Considering the low
patient compliance of rectal, vaginal, sublingual and nasal drug delivery for controlled release,
the buccal mucosa has rich blood supply and it is relatively permeable. The buccal mucosa lines
the inner cheek and buccal formulations are placed in the mouth between the upper gingival
(gums) and cheek to treat local and systemic conditions.

Advantages of buccal tablets -

1. Larger surface area promotes rapid disintegration and dissolution in the oral cavity.
2. Enhanced oral bioavailability of molecules that undergo first pass Effect.
3. Precision in the administered dose.
4. With the help of Mouth dissolving film drug delivery system those Drugs can be given to
the patients that are not crushed and not injected to patients.
5. Better patient compliance.
6. Ease of swallowing and no need of water have led to better
7. Acceptability amongst the dysphasic patient.

Disadvantages of buccal tablets

1. Relatively small absorptive surface area (0.01 sq m vs. 100 sq m for GIT).
2. Movement affects mucoadhesive systems.
3. Less permeable than the small intestine.
4. Salivation and swallowing taste of the drug.

DRUG PROFILE

DESCRIPTION
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Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) used to treat mild to moderate

pain, and helps to relieve symptoms of arthritis (osteoarthritis, rheumatoid arthritis, or juvenile
arthritis), such as inflammation, swelling, stiffness, and joint pain

Chemical name: 2 (4-isobutyl phenyl) propanoic acid,

Structure:

Molecular formula: C13H8O2

Molecular weight: 206.29 g/mol

Melting point: 76 0C

Boiling point: 319.6 11.0 0C Half life: Ibuprofen is rapidly metabolized and eliminated in the
urine. The excretion of ibuprofen is virtually complete 24 hours after the last dose. The serum
half-life is 1.8 to 2.0 hours.
Ultra violet:
Bioavailability
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Ibuprofen is rapidly absorbed, and both peak plasma concentrations and maximal analgesic
onset are achieved within 1.5-2 hours of oral administration. The first is a
sodium ibuprofen formulation containing 256 mg of ibuprofen sodium dehydrate per tablet
(equivalent to 200 mg ibuprofen acid)

Volume of distribution
Protein binding is saturable and at concentrations >20 g/mL binding is non-linear. Based on
oral dosing data there is an age- or fever- related change in volume of distribution for ibuprofen.
Febrile children <11 years old have a volume of approximately 0.2 L/kg while adults have a
volume of approximately 0.12 L/kg.

Mechanism of action: Ibuprofen is a non-selective inhibitor of an enzyme called

cyclooxygenase (COX), which is required for the synthesis of prostaglandins via the arachidonic
acid pathway. COX is needed to convert arachidonic acid to prostaglandin H2 (PGH2) in the
body

Ibuprofen dosing information

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Usual Adult Dose for Dysmenorrheal:

200 to 400 mg orally every 4 to 6 hours as needed.

Usual Adult Dose for Osteoarthritis:

Initial dose: 400 to 800 mg orally every 6 to 8 hours. Maintenance dose: May be increased to a
maximum daily dose of 3200 mg based on patient response and tolerance.

Usual Adult Dose for Rheumatoid Arthritis:

Initial dose: 400 to 800 mg orally every 6 to 8 hours. Maintenance dose: May be increased to a
maximum daily dose of 3200 mg based on patient response and tolerance.

Usual Adult Dose for Headache:

Study (n=34) - Prevention of Electroconvulsive therapy (ECT)-induced headache. 600 mg orally

90 minutes prior to the initial ECT session

Usual Adult Dose for Pain:

Oral: Mild to moderate pain: 200 to 400 mg orally every 4 to 6 hours as needed. Doses greater
than 400 mg have not been proven to provide greater efficacy. IV: (Patients should be well
hydrated before IV ibuprofen administration) Pain: 400 to 800 mg intravenously over 30 minutes
every 6 hours as needed.

Usual Adult Dose for Fever:

Oral: 200 to 400 mg orally every 4 to 6 hours as needed. IV: (Patients should be well hydrated
before IV ibuprofen administration) Fever: Initial: 400 mg intravenously over 30 minutes
Maintenance: 400 mg every 4 to 6 hours or 100 to 200 mg every 4 hours as needed.

Usual Pediatric Dose for Fever:

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Greater than 6 months 12years, 5 mg/kg/dose for temperature less than 102.5 degrees F (39.2
degrees C) orally every 6 to 8 hours as needed.10 mg/kg/ dose for temperature greater than or
equal to 102.5 degrees F (39.2 degrees C) orally every 6 to 8 hours as needed. The recommended
maximum daily dose is 40 mg/kg. OTC pediatric labeling (analgesic, antipyretic): 6 months to
11 years: 7.5 mg/kg/dose every 6 to 8 hours; Maximum daily dose: 30 mg/kg

Usual Pediatric Dose for Pain:

Infants and Children: 4 to 10 mg/kg orally every 6 to 8 hours as needed. The recommended
maximum daily dose is 40 mg/kg. OTC pediatric labeling (analgesic, antipyretic): 6 months to 11
years: 7.5 mg/kg/dose every 6 to 8 hours; Maximum daily dose: 30 mg/kg

Usual Pediatric Dose for Rheumatoid Arthritis:

6 months to 12 years: Usual: 30 to 40 mg/kg/day in 3 to 4 divided doses; start at lower end of

dosing range and titrate; patients with milder disease may be treated with 20 mg/kg/day; doses
greater than 40 mg/kg/day may increase risk of serious adverse effects; doses greater than 50
mg/kg/day have not been studied and are not recommended. Maximum dose: 2.4 g/day

.
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CHAPTER II
REVIEW OF
LITERATURE

REVIEW OF LITERATURE

1. Bharat B.et al (2015) Formulated and emulated oral disintegrated tablets Celcoxbi
 Page No14

2. Jaffar I. S et al, (2014) formulated and in vitro evaluated buccal mucoadhesive tablets

Promethazine HCl

3. Bhattacharjee.S et al (2014) designed developmted and evaluated of mucoadhesive film

water insoluble drug using different Plasticizers

4. Arun R.R et al (2014) development of carbamazepine fast dissolving tablets effect of

functionality of hydrophillic carriers on solid dispersion technique

5. Krishna R.V et al (2011) formulation and Invitro evaluation of Buccoadhesive tablets of

Furosemide
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Chapter iii
Pre formulation

PRE FORMULATION

UV SPECTROSCOPY:
An U.V spectrophotometric method based on the measurement of absorbance at 245 nm in
phosphate buffer oh pH 5.8 was used for the estimation of paracetamol. The method obeyed
Beers law in the concentration range 0 - 10 g/ml.

Angle of repose:
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The angle of repose of powdered gum was determined by the funnel method. The accurately
weighed granules were taken in a funnel. The height of the funnel was adjusted in such a way
that the tip of the funnel just touched the apex of the heap of granules. The granules were
allowed to flow through the funnel freely onto the surface. The diameters of powder cone was
measured and angle of repose was calculated using the equation.
=tan1(h/r )

Bulk density
Both bulk density (BD) and tapped density (TBD) were determined. A quantity of 2 gm of
powder from each formula, previously lightly shaken to break any agglomerates formed, was
introduced into a 10 ml measuring cylinder. After the initial volume was observed, the cylinder
was allowed to fall under its own weight on to a hard surface form the height of 2.5 cm at 2
second intervals. The tapping was continued until no further change in volume was noted. LBD
and TBD were calculated using the formulas.
BD = Weight of the powder/volume of the packing
TBD = Weight of the powder/tapped volume of the packing

Compressibility index /Carrs index

The flow of property was also determined by measuring the compressibility index. It is an
important measure that can be obtained from the bulk and tapped densities. According to the
theory, the less compressible materials are more flowable. A material having values of less than
20 to 30% is defined as the free flowing martial, based on the apparent bulk density and tapped
density, the drug was determined by using the formulas.9
 Page No17

density
comperessibility index=bulk 100
tap density

Table1.precompression parameters of Aspirin floating tablets,

S Test F1 F2 F3 F4 F5 F6 F7 F8 F9 F10
N
o
1 Bulk 0.62 065 0.60 0.62 0.64 0.69 0.61 0.62 0.62 0.60
density
(gm/ml)

2 Tapped 0.87 0.87 0.86 0.80 0.873 0.87 0.89 0.85 0.876 0.85
density
(gm/ml)

3 Care 28.73 29.83 28.80 30.25 29.98 30.35 31.23 29.98 28.80 29.8
index 0
4 Angle 25 25 25 24 26 25 . 26 28 . 25 25
of . . . .4 .4 . .4 .
repose 56 30
(degree) 25 24 34 5 5 56 5 24
 Page No18

Chapter IV

Formulation

FORMULATION

Materials and Methods

Ibuprofen CDH New Delhi, CMC CDH New Delhi, Magnesium sterate CDH New Delhi, Talc
CDH New Delhi, HPMC CDH New Delhi, Microcrystalline cellulose CDH New Delhi, P V P
CDH New Delhi,

Table2: of Formulation
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Sr. Name of Amount (gm/tablet)

No. Ingredient
Formulation F1 F2 F3 F4 F5 F6 F7 F8 F9 F10
Code
1 Ibuprofen 200 200 200 200 200 200 200 200 200 200

2 CMC 50 75 100 - 50 75 60 70 100 50

3 HPMC - - - 100 50 25 25 - 15 35
4 PVP 9.5 9.5 9.5 9.5 9.5 9.5 9.5 9.5 9.5 9.5
5 Microcrystallin 235 210 185 185 185 185 200 215 170 200
e cellulose
6 Magnesium 10 10 10 10 10 10 10 10 10 10
sterate
7 Talc 5 5 5 5 5 5 5 5 5 5
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CHAPTER V
EVALUATION

EVALUATION

1. Weight variation test

The weight variation test for given tablet was successfully done

Formula
% deviation or % weight deviation =
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Indivsual weight Avrage weight

100
Avrage weight

Procedure
Taken 20 tablet to perform weight variation test.

Weighed 20 tablet collectively with the aid of electronic balance.

Calculated the average weight of 20 tablets collectively.

Now weighed the individual tablet by using electronic balance.

Calculation of deviation was done by using mentioned formula.

Table 3. Weight variation test for F1

S No Individual weight Average weight % Deviation Inference
1 510 500 2 Pass
2 520 500 4 Pass
3 490 500 -2 Pass
4 490 500 -2 Pass
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5 495 500 -1 Pass

6 495 500 -1 Pass
7 480 500 -4 Pass
8 480 500 -4 Pass
9 510 500 2 Pass
10 510 500 2 Pass
11 510 500 2 Pass
12 515 500 3 Pass
13 520 500 4 Pass
14 480 500 -4 Pass
15 490 500 -2 Pass
16 490 500 -2 Pass
17 495 500 -1 Pass
18 480 500 -4 Pass

19 480 500 -4 Pass

20 525 500 5 Pass

Table 4. Weight variation test for F2

S No Individual weight Average weight % Deviation Inference

1 525 500 5 Fail
2 530 500 6 Fail
3 530 500 6 Fail
4 531 500 6.2 Fail
5 526 500 5.2 Fail
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6 527 500 5.4 Fail

7 529 500 5.8 Fail
8 493 500 -1.4 Pass
9 493 500 -1.4 Pass
10 482 500 -3.6 Pass
11 472 500 -5.6 Fail
12 472 500 -5.6 Fail
13 493 500 -1.4 Pass
14 293 500 -1.4 Pass
15 492 500 -1.6 Pass
16 492 500 -1.6 Pass
17 499 500 -0.2 Pass
18 498 500 -0.4 Pass
19 499 500 -0.2 Pass
20 532 500 6.4 Fail

Table5. Weight variation test for F3

S No Individual weight Average weight % Deviation Inference

1 510 500 2 Pass
2 520 500 4 Pass
3 490 500 -2 Pass
4 490 500 -2 Pass
5 495 500 -1 Pass
6 495 500 -1 Pass
7 480 500 -4 Pass
8 480 500 -4 Pass
9 510 500 2 Pass
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10 510 500 2 Pass

11 525 500 5 Pass
12 530 500 6 Fail
13 530 500 6 Fail
14 531 500 6.2 Fail
15 526 500 5.2 Fail
16 527 500 5.4 Fail
17 529 500 5.8 Fail
18 493 500 -1.4 Pass
19 493 500 -1.4 Pass
20 482 500 -3.6 Pass

Table 7. Weight variation test for F4

S No Individual weight Average weight % Deviation Inference

1 510 500 2 Pass
2 510 500 2 Pass
3 515 500 3 Pass
4 520 500 4 Pass
5 480 500 -4 Pass
6 490 500 -2 Pass
7 490 500 -2 Pass
8 495 500 -1 Pass
9 480 500 -4 Pass
10 480 500 -4 Pass
11 472 500 -5.6 Fail
12 472 500 -5.6 Fail
13 493 500 -1.4 Pass
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14 293 500 -1.4 Pass

15 492 500 -1.6 Pass
16 492 500 -1.6 Pass
17 499 500 -0.2 Pass
18 498 500 -0.4 Pass
19 499 500 -0.2 Pass
20 532 500 6.4 Fail

Table 8.Weight variation test for F5

S No Individual weight Average weight % Deviation Inference

1 510 500 2 Pass
2 520 500 4 Pass
3 490 500 -2 Pass
4 490 500 -2 Pass
5 495 500 -1 Pass
6 495 500 -1 Pass
7 480 500 -4 Pass
8 480 500 -4 Pass
9 510 500 2 Pass
10 510 500 2 Pass
11 510 500 2 Pass
12 515 500 3 Pass
13 520 500 4 Pass
14 480 500 -4 Pass
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15 490 500 -2 Pass

16 490 500 -2 Pass
17 495 500 -1 Pass
18 480 500 -4 Pass
19 480 500 -4 Pass
20 525 500 5 Pass

Table 9.weight variation test for F6

S No Individual weight Average weight % Deviation Inference
1 525 500 5 Pass
2 530 500 6 Fail
3 530 500 6 Fail
4 531 500 6.2 Fail
5 526 500 5.2 Fail
6 527 500 5.4 Fail
7 529 500 5.8 Pass
8 493 500 -1.4 Pass
9 493 500 -1.4 Fail
10 482 500 -3.6 Fail
11 472 500 -5.6 Pass
12 472 500 -5.6 Fail
13 493 500 -1.4 Fail
14 293 500 -1.4 Pass
15 492 500 -1.6 Pass
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16 492 500 -1.6 Fail

17 499 500 -0.2 Fail
18 498 500 -0.4 Fail
19 499 500 -0.2 Pass
20 532 500 6.4 Pass

Table 10. Weight variation test for F7

S No Individual weight Average weight % Deviation Inference

1 525 500 5 Fail
2 530 500 6 Fail
3 530 500 6 Fail
4 531 500 6.2 Fail
5 526 500 5.2 Fail
6 527 500 5.4 Fail
7 529 500 5.8 Fail
8 493 500 -1.4 Pass
9 493 500 -1.4 Pass
10 482 500 -3.6 Pass
11 472 500 -5.6 Fail
12 472 500 -5.6 Fail
13 493 500 -1.4 Pass
14 293 500 -1.4 Pass
15 492 500 -1.6 Pass
16 492 500 -1.6 Pass
17 499 500 -0.2 Pass
18 498 500 -0.4 Pass
19 499 500 -0.2 Pass
20 532 500 6.4 Fail
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Table 11. Weight variation test for F8

S No Individual weight Average weight % Deviation Inference

1 510 500 2 Pass
2 520 500 4 Pass
3 490 500 -2 Pass
4 490 500 -2 Pass
5 495 500 -1 Pass
6 495 500 -1 Pass
7 480 500 -4 Pass
8 480 500 -4 Pass
9 510 500 2 Pass
10 510 500 2 Pass
11 525 500 5 Pass
12 530 500 6 Fail
13 530 500 6 Fail
14 531 500 6.2 Fail
15 526 500 5.2 Fail
16 527 500 5.4 Fail
17 529 500 5.8 Fail
18 493 500 -1.4 Pass
19 493 500 -1.4 Pass
20 482 500 -3.6 Pass
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Table 12. Weight variation test for F9

S No Individual weight Average weight % Deviation Inference

1 510 500 2 Pass
2 510 500 2 Pass
3 515 500 3 Pass
4 520 500 4 Pass
5 480 500 -4 Pass
6 490 500 -2 Pass
7 490 500 -2 Pass
8 495 500 -1 Pass
9 480 500 -4 Pass
10 480 500 -4 Pass
11 472 500 -5.6 Fail
12 472 500 -5.6 Fail
13 493 500 -1.4 Pass
14 293 500 -1.4 Pass
15 492 500 -1.6 Pass
16 492 500 -1.6 Pass
17 499 500 -0.2 Pass
18 498 500 -0.4 Pass
19 499 500 -0.2 Pass
20 532 500 6.4 Fail

Table 13.weight variation test for F10

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S No Individual weight Average weight % Deviation Inference

1 525 500 5 Pass
2 530 500 6 Fail
3 530 500 6 Fail
4 531 500 6.2 Fail
5 526 500 5.2 Fail
6 527 500 5.4 Fail
7 529 500 5.8 Pass
8 493 500 -1.4 Pass
9 493 500 -1.4 Fail
10 482 500 -3.6 Fail
11 472 500 -5.6 Pass
12 472 500 -5.6 Fail
13 493 500 -1.4 Fail
14 293 500 -1.4 Pass
15 492 500 -1.6 Pass
16 492 500 -1.6 Fail
17 499 500 -0.2 Fail
18 498 500 -0.4 Fail
19 499 500 -0.2 Pass
20 532 500 6.4 Pass

2. Friability test
Procedure
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Roche friabilatar A number and deducted tablets (usually 6mg) are placed in tumbling apparatus
made the plastic that revolves at 25 rpm and drops the tablets to distance of 6 niche with each
revaluation normally the tablet are subjected to free for 100 revolution or 10 minutes. The tablets
are then deducted and are weighed the friability is calculated by formula. 25 rpm for 25 min.

Inetial weightFinal weight

Freability= X 100
Initial weight

Fig Tablet Friability Tester (Roche Friabilatar)

 Page No32

Table10. Friability
S No Formulation Code Friability %
1 F1 0.8
2 F2 1.0
3 F3 1.2
4 F4 1.0
5 F5 0.8
6 F6 1.1
7 F7 1.2
8 F8 1.3
9 F9 1.0
10 F10 1.1

3. Hardness Test
In hardness test we Monsanto and Pfizer

We put the individual tablet in to the Monsanto and Pfizer,

We repeated the process 6 trims

Apply the force and when the tablet starts braking the records the reading from the points
 Page No33

PFIZER TESTER

Hardness which is now more appropriately called crushing strength determinations are made
during tablet production and are used to determine the need for pressure adjustment on tablet
machine.

Table 11. For Hardness

S No Formulation No Hardness kg/cm
1 F1 6
2 F2 7
3 F3 9
4 F4 8
5 F5 5
6 F6 6
7 F7 6
8 F8 8
9 F9 9
10 F10 6
4. Dissolution Test
Procedure
Placed the 900 ml of water which should be free from dissolution air and warm set up to
37 0C
 Page No34

Placed the tablets in the basket and set the apparatus

Start the motor and adjust rotation speed of 50 rpm

Now take the reading after 5 min 10, 15, 30, and 45 minutes by diluting 1 ml of sample
with 10 ml of water.

Table12. Dissolution
S No Time minutes % Amount release Cumulative % Release
1 5 2 2
2 10 4 6
3 30 3 9
4 60 7 16
5 120 12 28

Fig dissolution curve

5. Disintegration Test:
Disintegration test is widely used in the pharmaceutical industry for evalution of disintegration
capability of formulations (ex: tablets) and quality control of different dosage forms.
 Page No35

Applications of Disintegration test:

1. Disintegration test is a simple test which helps in the preformulation stage to the formulator.
2. It helps in the optimization of manufacturing variables, such as compression force time
3. This test is also a simple in-process control tool to ensure uniformity from batch to batch and
among different tablets.
4. It is also an important test in the quality control of tablets.
Advantages of Disintegration tests:
This test is simple in concept and in practice. It is very useful in preformulation, optimization
and in quality control.
Disadvantages:
Disintegration test cannot be relied upon for the assurance of bioavailability.

The disintegration test for each dosage form is given in the pharmacopoeia. There are some
general tests for typical types of dosage forms. However, the disintegration test prescribed in the
individual monograph of a product is to be followed. If the monograph does not specify any
specific test, the general test for the specific dosage form may be employed. Some of the types of
dosage forms and their disintegration tests are:

1. Uncoated tablets-
Tested using distilled water as medium at 37+/-2 C at 29-32 cycles per minute; test is completed
after 15 minutes. It is acceptable when there is no palpable core at the end of the cycle (for at
least 5 tablets or capsules) and if the mass does not stick to the immersion disc.

2. Coated tablets-
The same test procedure is adapted but the time of operation is 30 minutes.

3. Enteric coated/ Gastric resistant tablets-

The test is carried out first in distilled water (at room temperature for 5 min.; USP and no
distilled water per BP and IP), then it is tested in 0.1 M HCL(upto 2 hours; BP) or Stimulated
 Page No36

gastric fluid (1 hour; USP) followed by Phosphate buffer, pH 6.8 (1 hour; BP) or Stimulated
intestinal fluid without enzymes (1 hour; USP).

Fig Disintegration Apparatus

6. Content Uniformity
In this test, 20 tablets were randomly selected and the percent drug content was determined, the
tablets contained not less than 85% or more than 115% of the labeled drug content can be
considered as the test was passed.

7. Assay
The drug content in each formulation was determined by triturating 20 tablets and powder
equivalent to average weight was added in 100ml of 0.1N Hydrochloric acid, followed by
stirring. The solution was filtered through a 0.45 membrane filter, diluted suitably and the
absorbance of resultant solution was measured spectrophotometrically at 315nm using 0.1 N
Hydrochloric acids as blank.
 Page No37

CHAPTER VI
 Page No38

RESULTS
DISCUSSION

RESULTS AND DISCUSSION

The buccal cavity release tablets, each containing 200 mg of Ibuprofen were prepared using
Hydroxypropylmethylecelluse (HPMC) as polymers. And other ingredient show in table no 3.
Different tablet formulations were prepared by direct compression technique and formulations
were named as F-1, F-2, F-3, F-4, F-5, F-6, F-7, F-8, F-9, and F-10 respectively. Flow properties
of powder, resistance to particle to particle movement can be judged by using angle of repose.
 Page No39

The values for the angle of repose were found range of 250.25-250.24.the mentioned data is
also mention in the above given tables.

DISCUSSION

The solubility of drug was conducted in pH 6.6 phosphate buffer because it is the
average pH of the oral cavity defined the term bioadhesion as the attachment of a
synthetic or natural macromolecule to mucus and/or an epithelial surface. In
general, mucoadhesion/bioadhesion may be defined as the adhesion between a
bioadhesive polymer and mucus. Mucoadhesion is considered to occur in four
major stages: wetting, interpenetration, adsorption, and formation of secondary
chemical bonds between mucus membrane and polymer. The strength of
mucoadhesion is affected by different factors like molecular weight of the polymer,
contact time with membrane, degree of swelling of the polymer, and the type of
biological membranes used in the study. The adhesion will increase with the degree
of hydration until a point where over hydration leads to a sudden decline in BS,
which might be due to the disentanglement at the polymer/tissue interface. The
degree of swelling was increased with the increase in the concentration of
NaCMC; this led the formulations

CONCLUSION
 Page No40

Development of bioadhesive buccal drug delivery of tizanidine hydrochloride

tablets was one of the alternative routes of administration to avoid first-pass effect
and provide prolonged release. In addition, these formulations reduce the need of
frequent administration and enhance patient compliance. A combination of sodium
carboxymethyl cellulose and hydroxypropyl methylcellulose K4M results in
sustained buccal drug delivery. The in vitro drug release was found to be non-
Fickian. The results strongly suggest that increase in the permeation was due to the
effect of sodium deoxycholate on paracellular and transcellular pathways. From
healthy human volunteers, subjective parameters and mucoadhesive behavior were
found to be satisfactory

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