Pharmaceutical Formulation

and Biopharmaceutics

Aniruddha Roy
Scope & Objective of the Course:

It is a course intended to give the students an insight into the

problems of making dosage forms of drugs. It brings together the
various sciences that are involved in the development of formulae
of pharmaceutical products and in evaluation of their qualities. The
laboratory component involves some fundamental exercises in the
evolution of formulae of products such as tablets, ointments,
solutions, parenteral products, sustained action medications etc. It
also imparts knowledge of newer dosage forms.

Text Book:

Mithal B.M., Text Book of Pharmaceutical Formulation, Vallabh

Prakashan, 6th edn., Delhi, 1997.
Lect. Topics to be Learning Objectives Reference
No. covered Books
Formulation – an Basic principles of formulation
1 Ch.1
introduction
The Drug Understanding different dosage
2 delivery systems forms and their characteristics Ch.2
& classification
Components of a Understanding formulation
3 Ch.2
dosage form ingredients and their effect
Design of dosage How a dosage form is formulated and
4 Ref 2 (i)
forms how to modify it for better action
Physical Understanding how physical
properties of characteristics of a drug and
5 Ch.3
drugs & formulation component affect
formulation formulation
Chemical Understanding how chemical
properties of characteristics of a drug and
6 Ch.4
drugs & formulation component affect
formulation formulation
Understanding how physicochemical
Biopharmaceutica
characteristics of a drug and
7-8 l characters of Ch.5
formulation component affect
drugs
bioactivity
 Understanding of formulation
Tablets and
9-13 aspects, manufacture of Ch.13
pellets
tablets and pellets
Formulation design and
14-16 Capsules Ch.14
manufacture capsules
Types of Parenterals and
their formulation aspects
Parenteral Understanding of design and
17-19 Ch.21
products requirements of
manufacturing facilities for
sterile dosage forms
Ocular Formulation and quality
20 dosage control of ophthalmic Ch. 22
forms products.
 How to make drug release
Sustained release
21-23 from a formulation slow and Ch.23
dosage forms
controllable.
Process of coating of a
Coating & formulation; Process for
24-26 Ch.32
Microencapsulation making microencapsulated
dosage form.
How to formulate a
Transdermal drug
27 transdermal drug delivery Ch.24
delivery systems
system
Targeted Drug Designing targeted drug
28-30 Ch. 25
Delivery Systems delivery systems
Other novel drug Designing of various novel Ch. 26
31-32
delivery systems drug delivery systems & 29
Quality control of Quality control of dosage
33 Ch.32
dosage forms forms
CGMP and Process CGMP and Process Validation
34 Ref.
Validation
Component Duration Weightage Date & Remarks
(%) Time
Surprise Tests* 10 min 15 During CB
semester
Mid-Term Test 90 minutes 30 To be CB
announced
Laboratory 20 Lab hours
Components$
Comprehensive 3 hrs 35 To be OB/CB
Exam announced

* Surprise tests will be conducted during class/tutorials on the basis

of topics covered in class
$ Lab component will consists: Day to day work 10 %; Lab viva + quiz
5%; Lab compre. 5%
Formulation – an introduction
Drug ?
• Active drug substance (active pharmaceutical ingredient - API)
•Chemical compound with pharmacological (or other direct effect )
intended for used in diagnosis, treatment or prevention of diseases
Direct clinical use of the active drug substances is
rare: Why??
•API handling and Accurate dosing can be difficult or impossible (e.g.,
potent drugs: low mg and μg doses)
•API administration can be impractical/unfeasible because of smell,
taste and low activity.
•Some API are chemically unstable in light, moisture, O2
•API can be degraded at the site of administration (e.g., low pH in
stomach).
•API may cause local irritations or injury when they are present at
high concentrations at the site of administration.
•Administration of active substance would mean to have no chance for
modification (improvement) of its PK profile.
Dosage Forms

Definition: Dosage forms are the means by

which drug molecules / APIs are delivered
to sites of action within the body to produce
optimum desired effects and minimum
adverese effect.
Need of dosage forms: overcoming the
difficulties
1. To provide for the safe and convenient delivery of
accurate dosage. Examples: Tablets, Capsules, syrups
2. Reduction is frequency of doasing (sustained and
prolonged release delivery)
3. For the protection of a drug substance from the
destructive influence of atmospheric oxygen or
moisture and gastric acid (after oral administration).
Example: enteric coated tablets
4. To conceal the bitter taste, salty obnoxious or odor
of a drug substance. Examples: Capsules, coated
tablets, flavored syrups
Need of dosage forms: overcoming the
difficulties
5. To provide liquid preparations of substances that are
either insoluble or unstable in the desired vehicle.
Example: suspension
6. To provide extended drug action through controlled
release mechanisms Examples: controlled release
tablets, capsules, suspensions
7. To provide optimal drug action from topical
administration sites Examples: ointments, creams,
ophthalmic, ear and nasal preparations
8. To improve bioavailability of drug with narrow
absorption window (gastro-retentive delivery).
Need of dosage forms: overcoming the
difficulties
9. To provide for insertion of a drug into one of the
body’s orifices Examples: rectal and vaginal
suppositories
10. To provide for the placement of drugs within body
tissues. Examples: Implants
12. In addition, many dosage forms permit ease of
drug identification through distinctiveness of color,
shape, or identifying markings
Types of Dosage Forms
TYPES OF DOSAGE FORMS: Physical
TYPES OF DOSAGE FORMS: Route of Administration
TYPES OF DOSAGE FORMS: Combined Table
 General Considerations in Dosage Form Design
Drug substances are seldom administered in their natural or pure
state, but rather as part of a formulation in combination with one or
more non-medicinal agents that serve varied and specialized
pharmaceutical functions
Through selective use of these non-medicinal agents, referred to as
excipients, pharmaceutical ingredients, or adjuncts, pharmaceutical
preparations of various types result.
It is the pharmaceutical excipients that serves to solubilize, suspend,
thicken, dilute, emulsify, stabilize, preserve, color, flavor and
fashion the many and varied medicinal agents into effective and
appealing pharmaceutical preparations.
The term “Pharmaceutics” which is the study that concerns itself with
the physical, chemical and biological factors which influence the
formulation, manufacture, stability and effectiveness of
pharmaceutical dosage forms.
General Considerations in Dosage Form Design
1. Drug Consideration in Dosage Form Design
1.1 Characteristics of Drug Substances
1.2 Drug Stability
1.3 Determining Drug Formulation Stability
1.4 Prevention Against Microbial Contamination
1.5 Appearance and Palatability
2. Therapeutic Considerations in Dosage Form Design
2.1 Nature of the disease or illness
2.2 Age of the Patient
3. Biopharmaceutics Considerations
3.1 Biopharmaceutics
3.2 Concept of Bioavailability
Oral Dosage Form
1. Should have appropriate disintegration and dissolution
time
2. Should be stable in the GI environment : Both pH and
enzyme stability
3. Should be available for absorption at the appropriate
location
4. Drugs which are susceptible for degradation should
be coated properly
5. Drug – food interaction should be taken into account.
Nature and quantity of food staffs influence gastric
emptying time and alter absorption rate
6. Oral dosage forms should have appropriate
organoleptic properties.
Systemic Dosage Form
1. Must contain only the most needed additives in the
smallest possible quantity
2. Absorption is dependent on the administration site;
however, bioavailability is normally ~100%
3. By proper selection of vehicle and administration site,
can be made sustained release formulation
4. Sterility is very important: product design should be
done accordingly.
Topical Dosage Form
1. Base must be selected based on ease of application
and removal.
2. Viscosity, absorption and transfer rate into skin
should be optimized
3. Evaporation rate should be optimal
4. Particle size should be proper so as to prevent gritty
feeling
5. Should have good spreading and covering capacity