Pharmaceutical Technology I

Assist. Prof. Dr Muqdad Alhijjaj

Department of Pharmaceutics

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 Topics: 1st semester
✓Dispersed systems: their classification; comparison between different systems.
✓Solutions and types of solutions
✓Solubility: Factors affecting solubility; expression of dissolution; dissolution
rate versus solubility; preparation of solutions containing non-volatile
materials.
✓Official solutions; classification of official solutions; preparation and uses.
✓Aqueous solutions containing aromatic principles; aromatic waters; methods
of preparations; stability.
✓Syrups: sugar based syrups; artificial and sorbitol based syrups; stability of
syrups.
✓Definition and methods of clarification; filter aids in clarification.
✓Preparation of solutions using mixed solvent systems; spirits, and elixirs.
✓Extraction; maceration and percolation.
✓Tinctures; fluid extracts; extracts of resins and oleoresins.
✓Colloidal dispersions; lyophilic; lyophobic; association colloids;
nanotechnology
✓Coarse dispersion; suspensions.

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 Topics: 2nd semester

✓Emulsions; purpose of emulsification; methods of emulsification;

emulsifying agents; HLB system; stability of emulsions
✓Lotions; liniments and collodions
✓Suppositories
✓Semisolid dosage forms (ointments, creams and gels)
✓Powdered dosage forms (powders, granules, capsules)
✓Incompatibilities in pharmaceutical dosage forms

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 Pharmaceutical Technology I

Notes:
• No. of units for this module is 4 units (3 theoretical + 1 practical).
• Assessment:
Total marks
(100) marks

Practical (20) Theory (80)

marks marks

Oral & Mid +Quizzes Final (60)

Quizzes Reports Final assay
Techniques (20) marks marks

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 References:
‘Books and research journals related to our topics’

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Why pharmaceutical
technology is
important for us as
pharmacists?

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Pharmaceutical technology teaches the
different types of dosage forms with respect
to their raw materials, composition, methods
of preparation, characterisation, evaluation
“in vitro” and “in vivo”, stability, storage,
packaging and uses.

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 Dosage and Dosage Forms

▪ Dosage (dosage regimen, dosage regime): It’s the amount of drug

prescribed by the physician to treat specific disease.

▪ Dosage form: preparation composed of the drug substance(s) in

combination, mostly, with one or more of nonmedicinal agents that have
varied and specialised functions. These nonmedicinal agents referred to
as pharmaceutical ingredients or excipients (examples?).

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 Goal Drug

In theory, a goal drug is desirable to have the following features:

• Produce the specifically desired effect.
• Be administered by the most desired route (generally orally) at minimal
dosage and dosing frequency.
• Have optimal onset and duration of activity.
• Exhibit no side effects and, following its desired effect.
• Would be eliminated from the body efficiently, completely, and without
residual effect.
• It would also be easily produced at low cost.
• Pharmaceutically elegant.
• Physically and chemically stable in various conditions of use and storage.

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Dosage Forms and Drug Delivery Systems

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 New Drug Development
Process

FIGURE : The new drug development process of a

new chemical entity from discovery through
preclinical and clinical studies, FDA review of the
N DA, and postmarketing activities. A variation of
this process is followed for the discovery and
development of new biological entities.

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 New Drug Development Process

Figure: time course for the development of a new drug. (Adapted from The Pharmaceutical
Research and Manufacturers of America (PhRMA), 2012; http://www.phrma.org/research)
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 What are the reasons
behind formulating drugs
(APIs) as dosage forms
and drug delivery
systems?

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1) Dosage forms provide
the mechanism for the
safe and convenient
delivery of accurate 2) To protect the drug substance
dosage. from the destructive influences
of the atmospheric oxygen
,humidity, or light (coated tablets,
sealed ampules).

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3) To protect the drug
substance from the destructive
influences of gastric acid after
oral administration (enteric
coated tablets).
4) To eliminate the bitter, salty, or
offensive taste or odor of drug
substance (capsules, coated
tablets, flavored syrups).

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5) To provide liquid
preparations for substances
that are either insoluble or
unstable in the desired vehicle
(suspensions).
6) To provide rate-controlled
drug action (various controlled
release tablets, capsules,
suspensions).

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7) To provide optimal drug action from topical administration
sites (ointments, creams, and ophthalmic, ear, and nasal
preparations).

8) To provide dosage forms for insertion into one of the body’s

orifices (rectal or vaginal suppositories).

9) To provide dosage forms for placement of drugs directly in the

bloodstream or body tissues (injections).

10) To provide dosage forms for optimal action through inhalation

therapy (inhalation powders and aerosols).

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The field of study that concerned with the
formulation, manufacture, stability and effectiveness
of dosage forms and drug delivery systems is
termed Pharmaceutics.

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 Pharmaceutics

✓an understanding of the basic physical chemistry necessary for

the effective design of dosage forms (physical pharmaceutics);
✓an understanding of relevant body systems and how drugs
arrive there following administration (biopharmaceutics);
✓the design and formulation of medicines (dosage form design);
✓the manufacture of these medicines on a small (compounding),
intermediate (pilot) and large (manufacturing) scale;
✓the avoidance and elimination of microorganisms in medicines
(pharmaceutical microbiology, sterilization, preservation); and
✓product performance testing (physical testing, drug release,
stability testing).

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Q:You are an industrial
pharmacist or pharmaceutical
scientist working in the R&D
department of a famous
pharmaceutical company. You
have been asked to develop a
formulation for felodipine (API)
used for treating hypertension.
What are the general
considerations that you need
keep in mind during the
formulation development
process?

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1) Physical, chemical and biological characteristics of
the drug substance(s) and pharmaceutical excipients
to be use in fabricating the product.

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 Example: Felodipine

1) Felodipine as one of the potent calcium channel antagonists normally used to treat
patients suffering from hypertension and for prevention of angina pectoris.

Chemical structure

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Example: Felodipine (API)
It is poorly water-soluble drug (practically insoluble in water) and has
high permeability through body membranes. It is classified as class II
according to Biopharmaceutical Classification System (BCS)? (homework)

Felodipine shows an extensive first pass metabolism when absorbed through

the gastrointestinal (GI) tract and approximately 84% of the administered
dose deactivated through the liver
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Example: Tween 80 ‘excipient’

Polysorbate 80 (polyoxyethylene 20 sorbitan monooleate,

molecular weight = 1310 g/mole) is a non-ionic surfactant
commonly used in the production of cosmetics, food and
pharmaceutical products.

Chemical structure

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 Example: Tween 80 ‘excipient’

❑This surface active agent has an HLB value of 15 and used for its
dispersing, emulsifying, solubilising, suspending, plasticising,
penetration enhancing and wetting activities.
❑At 25 °C, it presents as yellow oily liquid miscible with water and
ethanol and immiscible with vegetable and mineral oils.
❑Tween 80 is regarded as hygroscopic material and should be stored in
well-closed containers protected from light in a cool and dry place.
❑Tween 80 is sensitive to thermal autoxidation and hydrolysis.
❑Tween 80 is moderately toxic when administered by intravenous (IV)
route (LD50 = 4.5 g/kg) and mildly toxic after ingestion (LD50 = 25g/kg)
in mouse.

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 Homework

Q: What are the physical, chemical, and biological characteristics of the

following compounds needed to prepare an oral solid formulation?
✓Ibuprofen
✓Acetaminophen
✓PVP
✓Span 80

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 It is very important to
know your materials
before starting the
formulation development
process….

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2) Pharmaceutical materials should be compatible
with one another to produce a product that is safe,
stable, effective, easy to administer and attractive.

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3. The product should be manufactured with
appropriate measures of quality control and
packaged in containers that keep the product
stable.

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4. The product also should be labeled to promote
correct use and stored under conditions that
contribute to maximum shelf life.

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Can you classify the different
dosage forms and drug
delivery systems?

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 Classification of dosage forms

A) Based on the physical state:

1. Gaseous dosage forms: medicinal gases, inhalations.
2. Liquid dosage forms : solutions and suspensions.
3. Semisolid dosage forms : ointments, creams and gels.
4. Solid dosage forms and solid modified-release drug
delivery systems: tablets, capsules, etc.

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 Classification of dosage forms

B) Based on the route of administration:

The intended use is for systemic administration
1. Per oral (p.o.)
2. Sublingual and buccal.
3. Rectal
4. Parenteral
5. Transdermal
6. Inhalation, etc.

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 Classification of dosage forms

B) Based on the route of administration:

The intended use is for local action:
➢ Topical (on the skin or mucosa) into/onto:
- the eye, nose, ear
- the oral cavity
- the vagina, rectum
- the bronchi
- the skin
➢ Local parenterals
➢ local effect within GIT; antacids, adsorbents

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 Keynotes:

•It is important to link the different topics

related to pharmaceutics.( Pharmaceutical
calculation, physical pharmacy, pharmaceutical
technology, biopharmaceutics, and industrial
pharmacy).
•Pharmaceutics between basic knowledge and
expert level.

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 Disperse Systems
• Disperse systems are systems that consist essentially from two
components; disperse material distributed throughout a vehicle
termed dispersion medium.
• The disperse phase is also called internal phase and the
dispersion medium is named dispersing phase or external
phase or continuous phase.

Disperse phase + Dispersion medium = Disperse systems

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 Classification of Disperse Systems
• Based on the size of the disperse phase, disperse
Systems are classified into the following types:

Molecular dispersions Colloidal dispersions Coarse dispersions

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 Molecular dispersions

➢They are homogenous in character and form true

solutions
➢It is called molecular because the size of the
dispersed phase particles is small “molecules or ions”
less than 1 nm
➢They are invisible under scanning electron
microscope (SEM)
➢They pass through ultra filter and semipermeable
membranes
➢They undergo rapid diffusion
➢Examples of molecular dispersions: oxygen
molecules in air, ordinary ions of NaCl in water,
sucrose in water and molecularly dispersed solid
dispersions.

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 Colloidal dispersions
➢They have specific movement called Brownian
movement
➢They are not resolved by ordinary microscope and may
be detected under ultra microscope
➢They are visible under scanning electron microscope
➢They pass through filter paper but don’t pass through
ultra filters and semipermeable membranes
➢They diffuse very slowly
➢Their dispersed phase has a size range of 1 nm to 1 μm
➢They have low osmotic pressure
➢Examples of colloidal dispersions: nanoparticles, gels,
natural and synthetic polymers in water.

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 Colloidal dispersions

• lyophilic, solvent ‘‘loving’’ colloids, in which the

disperse phase is dissolved in the continuous phase;
• Lyophobic, solvent ‘‘hating’’ colloids, in which the
disperse phase is insoluble in the continuous phase;
• Association colloids, in which the dispersed phase
molecules are soluble in the continuous phase and
spontaneously ‘‘self-assemble’’ or ‘‘associate’’ to
form aggregates in the colloidal size range.

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 Coarse dispersions
• The size of the dispersed phase particles is greater than 1
microns
• They are visible under ordinary microscope
• They don’t pass or diffuse through any type of membranes
even ordinary filter paper
• They have negligible osmotic pressure
• Examples of such dispersions are pharmaceutical suspensions
and emulsions

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Summary & discussion

• If you have any question, please contact me on:

• Email: [email protected]

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