Drug Delivery System (PHM 220)

Introduction (Week 1)

Maria Teresa S. Dela Cruz,RPh, M.S.Pharm.

August 2022
 Outline
I. Introduction
A. Definition of Terms
II. Need for Dosage form
III. General Considerations in Dosage Form Design
IV. Preformulation Studies
V. Drug Stability
VI. References
I. Introduction - Pharmaceutics
•Pharmaceutics – the general area of study
concerned with the formulation, manufacture,
stability and effectiveness of dosage forms
Definition of terms
Dosage form
• a formulation that typically contains the API(s) and
excipients in quantities and physical form designed to
all the accurate and efficient administration of the API
to the human or animal patient.
• the administration form of the completed
pharmaceutical product (e.g., tablet, capsule,
suspension, injection).
Generic Name

•the identification of a pharmaceutical

product by its scientifically and
internationally recognized active
pharmaceutical ingredient or by its
official generic name as determined by
FDA.
Definition of terms
•Drug delivery system
- Modern technology, distributed with or as a part of a drug
product that allows for the uniform release or targeting of
drugs to the body.
- a formulation or a device that enables a therapeutic
substance to selectively reach its site of action without
reaching the nontarget cells, organs, or tissues.
- engineered technologies for the targeted delivery and/or
controlled release of therapeutic agents.
Reminder
•Design and formulation of a dosage form
requires consideration of the physical, chemical,
and biologic characteristics of all drug
substances and pharmaceutical ingredients to be
used in fabricating the product.
Introduction
• The drug and pharmaceutical materials
must be compatible with one another to produce,
stable, safe & effective product.
• The product should be manufactured with
appropriate measures of quality control and packaged
in containers that keep the product stable.
II. Need for Dosage Forms
1. To protect the drug substance from the destructive
influences of atmospheric oxygen or humidity (coated
tablets, sealed ampuls)
2. To protect the drug substances from the destructive
influence of gastric acid after oral administration (enteric-
coated tablets)
3. To conceal the bitter, salty or offensive taste or odor of a
drug substance (capsules, flavored syrup, coated tablets)
Need for Dosage Forms
4. To provide liquid preparations of substances that
are either insoluble or unstable in the desired
vehicle (suspensions)
5. To provide clear liquid dosage forms of substances
(syrups, solutions)
6. To provide rate-controlled drug action
(controlled-release tablets, capsules, suspensions)
Need for Dosage Forms
7. To provide optimal drug action from topical administration sites
(ointments, creams, TDP, ophthalmic, ear and nasal
preparations)
8. To provide for insertions of a drug into one of the body’s orifices
(rectal or vaginal suppositories)
9. To provide for placement of drugs directly in the blood stream
or body tissues(injections)
10. To provide for optimal drug action through inhalation
therapy(inhalants & aerosols)
General Considerations in
Dosage Form Design
• Nature of illness
• Manner of treatment (locally or systemic action)
systemic – oral administration (tablets, capsules)
• Age of patient
children - flavored syrup
• Condition of patient
unconscious/comatose – injectable drugs
Preformulation Studies
• Deals with the physical and chemical characterization
of drug substance
• This information provides framework for the drug’s
combination with pharmaceutical ingredients in the
fabrication of a dosage form
Preformulation Studies
• Physical description of drug substance
• Microscopic examination - indication
of particle size and crystal structure
• Heat of vaporization – for aerosol drugs
• Melting Point – purity determination
• Phase rule – diagrams are constructed to provide a visual picture of
the existence and extent of the presence of solid and liquid phases in
binary and other mixtures
Preformulation Studies
• Particle size – as it affects sedimentation rate, taste,
texture and stability of the product
• Polymorphism – noncrystalline or amorphous forms
(amorphous form is more soluble than the crystal form)
• Solubility – a drug must possess aqueous solubility for
therapeutic efficacy
*For a drug to enter the systemic circulation,
it must be first a solution.
Preformulation Studies
• Solubility and particle size
• Solubility and pH
• Dissolution rate – the time it takes for the drug to
dissolve in the fluids at the absorption site
• Membrane permeability – to produce a biologic
response, the drug molecule must first cross a biologic
membrane
Drug Stability: Mechanisms of Degradation
• Hydrolysis – molecules interact with water molecules to
yield breakdown products
• Oxidation – loss of electrons from an atom or molecule
• Autoxidation – chain reaction starting with the union of
oxygen with the drug molecule and continuing with a free
radical of this oxidized molecule participating in the
destruction of other drug molecules
Drug Stability
Stability – the extent to which a product retains within specified
limits and throughout its period of storage and use the same
properties and characteristics that it possessed at the time of its
manufacture
Shelf-life – the duration/period that a product remains
stable
Example : 5 years
Expiry date (ED)= shelf life + mfg. Date
5 + 2015 = 2020 (ED)
Types of Stability Issues
1. Chemical – labeled potency within
specified limits
2. Physical – appearance, flavor, dissolution are retained
3. Microbiologic- resistance to microbial growth
4. Therapeutic – effect remains unchanged
5. Toxicologic – no significant increase
in toxicity occurs
Grouping and prayer schedule
• Group A • Group B
1. Agliday, C. 9. Iringan, J.
2. Aguinaldo, N. 10. Jacela, A.
3. Andres, G 11. Labuguen, M.
4. Arban, S. 12. Magaoay, J.
5. Bartolome, L 13. Maranan, L.
6. Buendia, A. 14. Saquing, J.
7. Dela Cruz, C 15. Villamayor, E.
8. Dela Cruz, T. 16. Zambrano, S.
Assignment
1. Watch the movie or read the
plot
Grp A The Fugitive –
Harrison Ford
Grp B Rise of the Planet of the Apes
Featuring James Franco
2. Questions will be asked
during our next class about
Scenes/information relevant to our
topic.
➢Be ready for a
quiz next week.

Thank you
very much!