PRACTICE SCHOOL (BP706PS)

B. Pharm Final Year (Sem VII)

A Practice School Report Submitted to

Dr. Babasaheb Ambedkar Technological University, Lonere

For Partial fulfillment of Semester VII credits

of

BACHELOR OF PHARMACY

Under the faculty of

PHARMACY

By

Ms. Harshada Ashok Tribhuvan

Under the guidance of

Dr/ Mr./Mrs/Ms. Chaitali Ingawale Madam

Kasturi Shikshan Sansthan College of Pharmacy, Shikarapur (Pune)

2023-2024
 CERTIFICATE

This is to certify that the Practice School report entitled “Formulation Development” is
carried out by Ms. Harshada Ashok Tribhuvan under the guidance of Dr/Mr/Mrs. Chaitali
Ingawale Madam in the partial fulfillment of the requirement of Semester VII credits of the
degree of Bachelor of Pharmacy under faculty Pharmacy of Dr. Babasaheb Ambedkar
Technological University, Lonere.

Place: Shikarapur

Date: Principal
 DECLARATION

I, hereby declare that the Practice School report entitled “Formulation Development” is
completed and written by me.

Place: Shikarapur

Date: Signature of Student

 ASSESSMENT

Continuous Mode:
Sr. No. Criteria Out of Marks Marks Obtained

1 Attendance 05

2 Academic Activity 10

3 Student Teacher Interaction and 10

Perception of Guide

Total 25

End Semester Exam :

Sr. No. Criteria Out of Marks Marks Obtained

1 Presentation of Work 15

2 Communication Skill 15

3 Objective 10

4 Methodology adopted 40

5 Conclusion & Outcome 15

6 Question & Answer (Defense) 15

7 Compilation of report 15

Total 125

Name & Sign. Name & Sign.

Of of
External Examiner Internal Examiner
 INDEX

Sr. No. Content Page No.

1. Review of literature 01

2. Introduction to h- index 02

3. Dissolution Protocall 03-04

4. Preparation of Floating Tablet of Aspirin 05-07

5. Preparation & Evaluation of Aspirin Tablet by Wet Granulation 08-14

method
6. Preparation & Evaluation of Aspirin Tablet by Dry Granulation 15-16
method
7. Preparation of Aspirin Tablet by Direct Compression method 17-19

8. Mechanism of Action of Aspirin 20

9. Drug Interaction of Aspirin 21

10. Uses, Side effects, Precautions of Aspirin 22

11. Outcomes 23

12. Conclusion 23

13. References 24
Formulation Development

Review of Literature

A literature review is a survey of scholarly sources on a specific topic. It provides an

overview of current knowledge, allowing you to identify relevant theories, methods, and gaps
in the existing research that you can later apply to your paper, thesis, or dissertation topic.

There are five key steps to writing a literature review:

1) Search for relevant literature

2) Evaluate sources

3) Identify themes, debates, and gaps

4) Outline the structure

5) Write your literature review

A good literature review doesn’t just summarize sources—it analyzes, synthesizes, and
critically evaluates to give a clear picture of the state of knowledge on the subject.

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Formulation Development

Introduction to h-index

The h-index, or Hirsch index, measures the impact of a particular scientist rather than a journal.
The h-index is an author-level metric that measures both the productivity and citation impact of
the publications, initially used for an individual scientist or scholar. The index is based on the
set of the scientist’s most cited papers and the number of citations that they have received in
other publications. The index has more recently been applied to the productivity and impact of a
scholarly journal as well as a group of scientists, such as a department or university or country.
The index was suggested in 2005 by Jorge E. Hirsch, a physicist at UC San Diego, as a tool for
determining theoretical physicists' relative quality and is sometimes called the Hirsch index or
Hirsch number.

Definition
The h-index is defined as the maximum value of h such that the given author/journal has
published at least h papers that have each been cited at least h times. The index is designed to
improve upon simpler measures such as the total number of citations or publications. The index
works best when comparing scholars working in the same field, since citation conventions differ
widely among different fields.

Application
1. Indices similar to the h-index have been applied outside of author level metrics.
2. The h-index has been applied to Internet Media, such as YouTube channels. It is defined
as the number of videos with ≥ h × 105 views. When compared with a video creator’s
total view count, the h-index and g-index better capture both productivity and impact in a
single metric.

The h-index can be calculated automatically in Web of Science and Scopus or manually in
other databases that provide citation information (e.g. SciFinder, Google Scholar).

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Formulation Development

Dissolution Protocol

Dissolution is the process by which a solid substance enters into a solvent to form a
Solution. Pharmaceutical definition: Dissolution is a test used throughout the life cycle Of a
pharmaceutical product to evaluate the rate of release of a drug substance from The dosage
form.
Example : Voveron SR Tablet.

Principle of Dissolution Test Apparatus :

A dissolution test uses an apparatus with specific test conditions in combination with Acceptance
criteria to evaluate the performance of the product.
There are seven different types of dissolution apparatus defined in the United States
Pharmacopeia (USP) – Basket Type, Paddle Type, Reciprocating Cylinder, Flow Through Cell,
Paddle Over Disc, Rotating Cylinder, and Reciprocating Disc.

Importance of Dissolution of Drugs :

Dissolution is the process in which a substance forms a solution. Dissolution Testing measures
the extent and rate of solution formation from a dosage form, Such as tablet, capsule, ointment,
etc. The dissolution of a drug is important For its bioavailability and therapeutic effectiveness.

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Formulation Development

Dissolution Test Apparatus : USP TYPE – 2 – Paddle

Advantages : Easy to use, Robust, Long experience, pH change possible & Can be Easily
automated which is important for routine investigation.

Application :
USP Apparatus I and II are the most commonly used dissolution apparatus for Solid oral dosage
forms and are versatile in enabling the development of many Types of dissolution methods, from
those for formulation development Purposes to those used for QC testing of commercial batches,
confirms Clay

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Formulation Development

Preparation of floating tablets of Aspirin

Structure of Aspirin
Chemical Formula - C9H8O4

Aspirin :
Aspirin also known as acetylsalicylic acid, is a nonsteroidal anti-inflammatory drug used to
reduce pain, fever, and/or inflammation, and as an antithrombotic. Aspirin is used to relieving
pain, lowering fever and reducing inflammation,. It is sold under several brand names in India
such as Ecosprin, Sprin, Aspro, Eprin and Delisprin.

Classification of floating tablets

Floating Drug Delivery

Non-effervescent System Raft Forming (in situ gel

Effervescent System formation) system

Gas Generating System

(conventional single layer or Hydrodynamically balanced system
multilayer)  Matrix layered tablets
 Floating capsules  Alginate beds
 Floating pills Hollow microspheres / microbaloons
 Ring capsules
 Films
Magnetic System
Volatile liquid (Vaccum) System
 Intragastic osmotically controlled
 Gastrointestinal inflatable

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Formulation Development

Advantages of floating drug delivery system

Floating dosage systems are delivery systems with gastric retentive behavior and offer
several advantages in drug delivery. Some of these include:
1. Simple and conventional technique for formulation.
2. Site-specific drug delivery.
3. Controlled delivery of drugs.
4. Delivery of drugs for residual action at a specific site in the stomach.
5. Improved drug absorption with increased GRT and excess duration of contact of
dosage regimen at its target site.

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Formulation Development

Disadvantages of floating drug delivery system

1. The major disadvantage of a floating system is due to the necessity of a sufficient

level of gastric fluids to float without a sink. However, this limitation can be
overcome by coating the dosage form with bio adhesive polymers that easily
adhere to gastric mucosa.
2. The drugs those get significantly absorbed throughout gastrointestinal
tract, with significant first-pass metabolism, are desirable candidate
predominantly.
3. Certain drugs present in the floating system may causes irritation to gastric
mucosal linings.
4. Gastric emptying of floating systems may occur at random and highly
dependent on its dimensions. Therefore patients should not have dosage prior
going to bed.
Evaluation of floating tablets

1. Floating time: The total duration of tablet floating on the medium is

considered as floating time
2. Floating lag time: Time required for the tablets to rise on the surface of the
medium was considered as floating lag time
3. Content uniformity

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Formulation Development

Preparation & Evaluation of Aspirin Tablet by Wet Granulation method

Theory :

Aspirin Tablet is prepared by wet granulation method In this binders and Lubricants in
combination leads to better drug release kinetic. The in-vitro dissolution studies we got our
result our Formulation Follow zero order kinetics with the effect of lubricants using in
combination for better kinetic drug release.

Binders :

Binders hold the ingredient in a tablet together Binders ensure that tablet and granules can be
formed with required mechanical strength and give volume to low active dose tablets.

List of Binders used in Tablet Formulation

Sr. No. Binders Example

1 Saccharides Sucrose, Lactose
2 Polysaccharides Starches, Cellulose as Microcrystaline,
cellulosehydroxypropyl cellulose
3 Sugar Alcohols Xylitol, Sorbitol or Mannitol
4 Protein Gelatin
5 Synthetic Polymers Polyvinylpyrrolidone (PVP), Polyethylene glycol
(PEG)
6 Solution Binders Sucrose, Polythylene glyd, Water or Alcohol
7 Dry Binders Methyl Cellulose, Polyvinyl pyrrolidine and
polyethylene glycol

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Formulation Development

LUBRICANTS:
These are preventing ingredients from clumping together and from sticking to the tablet
punches or capsule filling machine. Lubricants also ensure that tablet formation and ejection
can occur with low resistance between the solid and die wall. lubricants in tablets or hard
gelatin capsules. Lubricants are agents added in small quantities to tablet and capsule
formulations to improve certain processing characteristics.

List of Lubricants used in Tablet Formulation

Sr. No. Lubricants Examples
1 Minerals Talc or silica
2 Fats Stearin, Magnesium, tearate or steric acid

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Formulation Development

Method

Wet granulation forms the granulation by binding the powders together with an adheshive
instead of by compaction.

Stages of granule development:

A. Pendular
B. Funicular
C. Capillary
D. Droplet Steps

Steps Involved:
Step 1: Weighing and mixing of formulation ingredients.
Step 2: Preparing the damp mass.
Step 3: Screening the damped powder into pellets or granules.
Step 4: Drying of moist granules

Step 5: Sizing the granulation by dry screening.

Step 6: Lubrication of granules
Step 7: Compression of granules into tablets.

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Formulation Development

Procedure

1) Tablets were prepared using wet granulation technique as per the composition given
earlier.
2) The calculated amount which was required to prepare 400 mg aspirin tablets,
containing 250 mg drug, HPMC polymer and PVP as a binder were mixed uniformly.
3) An enough granulating agent (water) was added slowly to prepare wet mass. Granules
were prepared by sieving method using a 20# sieve.
4) Further, granules were dried at 35-45°C for six hours. The dried granules were stored
in desiccators until compression of tablets.
5) The required amounts of granules were weighed and compressed using automatically
operated tablet punching machine having 12mm flat faced punch diameter and during
the tablet preparation to maintain the low resistance between the solid and die wall,
lubricants added in granules. Lubricant combinations are agents added in small
quantities to the tablet during the tablet preparation.
6) The compressed tablets were stored in airtight container at room temperature for
further evaluation.

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Formulation Development

EVALUATION OF ASPIRIN TABLET

A) Hardness
Hardness is tablet crushing strength. It is tested by Monsanto tester, Strong-Cobb tester,
Pfizer tester, Erweka tester and Schleuniger tester. Tablet requires a certain amount of
strength or hardness and resistance to friability to withstand mechanical shakes during
handling in the manufacture, packaging, and shipping.

Monsento Tester Strong-Cobb tester

Pfizer tester Erweka tester

Schleuniger tester

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Formulation Development

B) Friability
Friability tester known as Roche Friabilator. A number of tablets weighed and placed in
Roche Friabilator where they're exposed to repeated shocks and rolling. The tablets are
tumbled at a distance of 6 inches at each turn. After 100 revolutions and if cracked, cleaved
and broken tablets presents after tumbling then it fails the test and vice versa.

Roche Friabilator

C) Weight Variation Test

Tablets were evaluated for weight variation as per USP XXIV monograph using digital
electronic balance. 20 tablets weighed and average calculated. Individual weight of each
tablet compared with average weight.

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Formulation Development

D) Disintegration Test (U.S.P.)

The U.S.P. device to test disintegration consists of 6 glass tubes that are 3 inch long; open at
the top and 10 mesh screens at the bottom end. During the disintegration test, one tablet is
placed in each tube and the basket rack is positioned in a 1-L beaker of either water,
simulated gastric fluid or simulated intestinal fluid at 37 ± 2°C such that the tablet remains
2.5 cm below the surface of liquid on their upward movement and not closer than 2.5 cm
from the bottom of the beaker in their downward movement Move the basket containing the
tablets up and down through 5-6 cm at a frequency of 28 to 32 cycles per minute.

Disintegration Tester

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Formulation Development

Preparation of Aspirin Tablet by Dry Granulation Method

Theory:
In Day Granulation no solvent is required, The aggregation of particle into granules is
facilitated by the application of high stresses to the mixed powders.

The ingredients in the formulation are mixed and pre compressed on heavy duty tablet
machine. The slug which is formed is ground to uniform size and compressed I into finished
tablets.
However, when direct Compression is not possible due to the properties and those of drug
and wet granulation cannot be used because the drug is sensitive to Moisture and heat, then
dry granulation remains the only method.

There are 2 methods by which dry granules are formed:

1) Slugging
2) Roller Compaction.

Slugging:

In this technique the powders are mixed (as described previously) and then compressed into a
primordial oversized tablet using a tableting press that is capable of applying a high stress (to
ensure that aggregation of the particles and then aggregation of granules occur during
compaction). Following this the tablet is milled to produce granules of the required size.

Roller compaction:

In roller compaction the formulation ingredients are mixed and are then compressed using a
roller compactor. In this the powders are fed from a hopper on to a moving belt and then
transported to, and compressed by, the passage between the narrow gap between two
(oppositely) rotating rollers to produce a sheet/film of compressed material. The compressed
sheet is then milled to produce granules of the required size.

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Formulation Development

Stages of dry granulation:

In dry granulation, the aggregation of particles is facilitated by the application of high

compression stresses and therefore the stages/mechanisms of granule formation are different
from those described for wet granulation. In dry granulation particle-particle interactions
occur due to: (1) electrostatic forces; (2) van der Waals interactions; and (3) melting of
components within the powder mix.

Advantages of dry granulation:

1) Both roller compaction and slugging require conventional (.e. non-specialist) grades
of excipients
2) These methods are not generally associated with alterations in drug morphology
during processing
3) No heat or solvents are required.

Disadvantages of dry granulation:

1) Specialist equipment is required for granulation by roller compaction

2) Segregation of components may occur postmixing
3) There may be issues regarding powder flow.
4) The final tablets produced by dry granulation tend to be softer than those produced by
wet granulation, rendering them more difficult to process using post- tableting
techniques, eg, film coating
5) Slugging and roller compaction lead to the generation of considerable dust. Therefore,
containment measures are required. Furthermore, there may be a reduction in the yield
of tablets.

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Formulation Development

Preparation of Aspirin Tablet by Direct Compression Method

Theory:
Acetyl Salicylic acid is highly unstable and readily undergoes, hydrolysis reaction when
aspirin is available as granular material direct compression method is normally, If powdered
aspirin is available
dry granulation method (Slugging) is preferred direct compression method is economical and
quick method of production because the number of steps are involved are less compared to
wet or dry granulation method.

Flowchart for manufacture of aspirin tablet by direct compression method :

Aspirin
Weigh

Pass through
22/44-mesh sieves 5% starch

Powder passed Powder (coarse) 2%

Through 44-mesh retained on Talc
Sieve 44 mesh sieve

Fines Blend
15%

Compress

Pack

Label

Category : Analgesic, antipyretic, antirheumatic and antithrombotic

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Formulation Development

Procedure:

Depending on the number of tablets to be submitted, the working formula is calculated. A

flow sheet for the manufacture of aspirin tablets is given in Figure 3. The detailed procedure
is as follows.

Weighing:
Granular acetyl salicylic acid is weighed approximately (more than required quantity).

Screening:
Weighed aspirin is passed through 22/44-mesh sieves. The material retained on 44-mesh
sieve is collected (Hg) and is called as coarse granules. The material passed through 44-mesh
sieve is collected (I g) and is called as fines.

Fifteen per cent of fines required are weighed (J or I g). Five per cent of starch powder and
2% of talc powder are weighed.

Blending :
Coarse granules, fines, starch powder, and talc powder are blended thoroughly in mortar with
pestle in order to get a uniform distribution of ingredients. Now the granules are ready for
compression.

Compression:
Three packets of granules, each containing the practical weight of one tablet, are prepared.
These are used to adjust the pressure of the punches in order to get tablets of sufficient
hardness. The remaining granules are compressed to obtain tablets.

The production yield is calculated using the formula.

Packing:
Compressed tablets are placed in wide-mouthed, tightly- closed container in a cool, dry place.
The container is capped and cleaned.

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Formulation Development

In-process Quality Control :

1. Diameter
2. Thickness
3. Weight Variation
4. Hardness
5. Friability
6. Disintegration time: (Calcium lactate tablets hardens on storage and therefore
maximum time allowed for disintegration is 30 min).

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Formulation Development

Mechanism of Action of Aspirin :

Effect of dose – Aspirins effect and respective mechanism of action vary with dose.

A) Low Doses ( Typically 75 to 87 mg/day)

Irreversibly binds
Acetyl Serine 530 of Cyclooxygenase (COX) -1

Inhibit

Platelet aggregation of thromboxane A2

Shows

Antithrombotic effect

B) Intermediate doses (650 mg to 4g / day)

Inhibit

COX- 1 and COX-2

Block

Prostaglandin (PG)

Shows
Analgesic and Antipyretic effects

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Formulation Development

Drug interaction of Aspirin

Drug interaction may changes how medication work or increase risk for serious side effects

Some drug that may interact with Aspirin drug which causes side effect includes:

1) Mifepristone, acetazolamide
2) Blood thinners (warfarin, heparin)
3) Corticosteroids (prednisone)
4) Dichlorphenamide
5) Methotrexate
6) Valproic acid
7) Herbal medication (ginko biloba).

A) Aspirin + Warfarin Unusual Bleeding, Bruising, Vomiting, Blood in urine

or stools, headache, dizziness or weakness.

B) Aspirin + Acetazolamide ringing in your ears, rapid your breathing, Confusion,

Hallucinations, Coma.

C) Aspirin + Prednisone Inflammation in Gastrointestinal tract, bleeding,

ulceration, perforation.

D) Aspirin + Methotrexate shortness of breath, nausea, vomiting, Sore throat,

diarrhoea.

E) Aspirin + Ginkobiloba. Lightheadedness, red or black tarry stools, fresh or dried

blood that looks like coffee like coffee grounds,
Severe headache

F) Aspirin + Dichlorphenamide Confusion, hallucination, headache, nausea,

vomiting Coma.

Before using such drug with aspirin, consult your doctor if you have recently received
certain live vaccine (such as Caricella vaccine, live flu vaccine. Consult your doctor
before taking any medication along with aspirin tablet.

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Formulation Development

Uses of Aspirin

1) Aspirin is used to treat pain and reduce fever or inflammation, to relieve mild to
moderate pain from headache arthritis aches, menstrual menstrual periods, toothaches
and muscle aches.

2) It is sometimes used to treat or prevent heart attacks, strokes and chest pain (angina)

Side effects of Aspirin:

A) Severe side effects:

1) difficulty in hearing
2) Ringing in the ears
3) signs of kidney problems (change in amount of Urine).
4) Unexplained tiredness.
5) Dark urine
6) Yellowing eyes /skin.

B) Allergic reactions:
1) Swollen lymph nodes.
2) rashes
3) itching (Swelling (especially of face / tongue / throat)
4) Trouble breathing

C) Common side effects:

1) Upset stomach
2) heartburn
3) Drowsiness
4) Mild headache

Precautions:

1) Limit alcoholic beverages and stop smoking

2) Children less than 18 year old should not take aspirin if they have Chickenpox, flu or
any undiagnosed illness or if they have recently vaccine.
3) Aspirin is treat not recommended for used to treat pain or fever during pregnancy.
4) Low dose of aspirin for heart attack or stroke Prevention, may be used if directed by
your doctor.

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Formulation Development

Outcome:

After the completion of Project report on Formulation Development, I understood that ___

A) Different methods, for preparation of Aspirin tablet.

B) Evaluation parameters for aspirin tablet
C) Various instruments used in preparation of Aspirin tablet.
D) Uses, side effects, drug-drug interaction & mechanism of action of Aspirin tablet.

Conclusion:

Formulation Development of Aspirin was studied

Aspirin is in of medication called salicylates. It works by stopping the production of certain
natural substances that Swelling and blood clots. Aspirin is also available in combination
with other medications such as antacids, pain relievers and cough and cold medication.

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Formulation Development

References:

1) Asst. Professor Pawan singh, Prevesh kumar, Dr. Neelkant Prasad; Research Article;
Formulation and Evaluation of Aspirin tablet by Wet Granulation method using
different lubricant in combination Research J. Pharm and Tech 10 (9) 2017.
2) Authors Mali Kailas Krishant, Vishwajet Sampatrao; Research Article; 2017
Preparation and Evaluation of Aspirin granules (Dry Granulation)
3) Laboratory Manual of Industrial Pharmacy page 24-27; preparation of Aspirin Tablet
by Direct Compression method.
4) National Library of Medicine (.gov)
https:// www.nlm.nih.gov.in
Mechanism of action of Aspirin; Drug- Drug interaction, uses, side effects,
precautions.

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