Design of Dosage Form

Presented by:

Ivory Diane C. Amancio, RPH CPH

Silliman University – Pharmacy Department
Dumaguete City Philippines
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Unit 2
CONSIDERATIONS IN DRUG DOSAGE FORMS DESIGN

Topics:

 Pharmaceutical and Formulation Considerations

 Biopharmaceutic Considerations

Learning Outcomes:

• Demonstrate knowledge of the different considerations in

dosage forms design
• Demonstrate understanding of the Factors affecting Drug
Delivery Systems design
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Characteristics of Drugs
Rarely administered as
pure chemicals

Given as formulated
preparations or Medicines

Excipients provide varied or

specialized pharmaceutical
functions

Excipients or Additives can increase

compactibility (Solid Dosage forms) and
improve flavor of the drug substance.
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Principal Objective of Dosage

Form Design

 Achieve a predictable
therapeutic response of a
drug.

 Can be manufactured in a
large scale batch with
reproducible product quality.

How to ensure
product Quality?
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3 Categories to ensure Product

Quality:
Biopharmaceutics
A. BIOPHARMACEUTICAL CONSIDERATIONS:
Absorption, Distribution, Metabolism and
Excretion The study of the
Factors Affecting Absorption of the Drugs
relationship between the
B. DRUG FACTORS: Physical, chemical and
Physical Properties
Chemical Properties
biological sciences
applied to Drugs,
C. THERAPEUTIC CONSIDERATIONS: Dosage forms and Drug
clinical indications Action.
patient factors
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Biopharmaceutics

The study of the

BIOPHARMACEUTICAL relationship between the
CONSIDERATIONS Physical, chemical and
biological sciences
applied to Drugs,
Dosage forms and Drug
Action.
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ADME
Physical Properties
 Particle size and Surface Area
 Polarity
 Compressibility
 Drug-Exepient Compatibility

Solution form
Chemical Properties
 Intermolecular Forces
 pH

Biological Science
Pharmacology of the drug
substance (What the Drug does
to the body)
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Routes of Drug Administration

absorption
Dosage forms are designed to
provide the drug in a suitable form
for absorption from each selected
route of administration.

Different Route
of
Administration
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Variation in Time of onset of action

for the different dosage forms

Time of Onset of Action Dosage Forms

Seconds Intravenous Injection
Minutes Intramuscular and Subcutaneous Injections, Buccal
Tablets, Aerosols, gases
Minutes to Hours Short-term depot injections, solutions,
suspensions, powders, granules, capsules, tablets,
modified-release tablets.
Several Hours Gastro-resistant coated formulations
Days to weeks Depot Injections, Implants
Varied Topical Preparations
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Routes of Drug Administration

Oral Route
Rectal
Parenteral
Topical
Respiratory
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Oral Route
Drugs intended to be absorbed in the
systemic circulation thru epithelial cells and
mucosa of the GI tract.

Buccal Route – Local Absorption;

Poorly absorbed in the GI tract
low Aqueous Solubility

ADVANTAGES:
 Most frequently used route of
Dosage Form Considerations for Oral Route to Administration
attain optimum absorption:  Simplest and most Convenient
 Safest means of drug administration

Drug Solubility
DOWN SIDE:
 Slow onset
 Irregular absorption
 Destruction of certain drugs
(insulin-containing compounds)
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Dosage Form Considerations for Oral Route Oral Route

to attain optimum absorption:

Alteration in Drug Solubility Tetracyclines (Antibiotic) + Calcium

Supplements (Calcium ions) = Complexation

Slow Gastric Emptying time

Environmental pH
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Dosage Form Considerations for Oral Route Oral Route

to attain optimum absorption:

Alteration in Drug Solubility

 Drug is inactivated by the gastric Acid
Slow Gastric Emptying time  Taken with Anticholinergic agents
(Loperamide)

Environmental pH
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Dosage Form Considerations for Oral Route Oral Route

to attain optimum absorption:

Alteration in Drug Solubility

Slow Gastric Emptying time

Environmental pH
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Rectal Route

Rectal Solution Rectal Suppository Rectal Enema

Suppositories are solid

Advantages: forms inserted into body Downside:
cavities; where they melt
 Suited for drugs inactivated by and releasing the drug.  Inconvenient
gastrointestinal fluid.  Drug absorption is irregular
 When oral route is not possible
 Drugs enter the systemic circulation
SUPPOSITORY Base  Difficult to predict
without passing the liver. -influence the degree and
rate of drug release
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3 Main Parenteral Routes

Parenteral Route
A drug is injected via a hollow
needle into the body at various
sites and to various depths.

Advantages:

 Parenteral route is essential

when rapid absorption is
essential.
 When Patient is unconscious
Characteristics:
 When drugs a poorly absorbed
 Parenteral Drugs are sterile solutions or suspension of drugs in
in oral route (destroyed by GI
water or suitable vehicle. enzymes)
 Solution – rapidly absorbed  Drug blood levels are
 Suspension – slower absorption predictable compared to oral
 Drugs suspended in oily vehicle has slower absorption route. (100% bioavailable-IV route)

 Subcutaneous solution or suspension deliver drugs at the

vicinity of the capillaries.
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Parenteral Route
Disadvantages of
Parenteral Route:

 Pain and Inconvenience

Have focused on Needle-free

injection systems and devices

• Propel the drug in aqueous

solution or powder form at
high velocity directly to the
external layers of the skin
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Topical Drug Classification according to action Topical Route

Local Action Antiseptics, Antifungal,
Anti-inflammatory agents
Systemic Action Transdermal Patches

Topical Drug Classification according to types of

formulation
-the bases paly an important role in determining
the character of drug release from the
formulation.

Severe pain Smoke Sesation Hydrophobic, oleaginous

Ointments
based dosage form.
Creams Semi-solid emulsions
(o/w emulsion)
Pastes Contains more solid than
ointments; thus STIFFER.
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Topical Drug Characteristics according to Route

Topical Route
of Administration

Eyes Type: Solution, Ointment, Cream

Characteristic – Sterile (topical)
Ears Type: Viscous Solution
- To prolong contact from affected area.
Nose Type: Solution or Suspension
Characteristics – must be delivered in by drops or fine aerosol from a spray
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Aerosol Preparation Respiratory Route

Particle smaller
than 1 um are
largely exhaled;
and greater
than 5 um are
deposited on
larger bronchial
airways

Lungs: Drug Delivery System to Lungs are through:

Alveolar – zone of rapid
 Gaseous
absorption
 Aerosol mist
 Ultrafine solid-particle form