PHARM 3 PRELIM

PHYSICAL PHARMACY LEC

WEEK 1: INTRODUCTION TO PHYSICAL PHARMACY This stems from the fact that :
➔ Pharmacy is an applied science, composed of
INTRODUCTION principles and methods that have been gathered
➔ Evidence-based medicine - uses the scientific from other disciplines.
method of using observations and literature
searches to form a hypothesis as a basis for The pharmacist MUST:
appropriate medical therapy. ➔ engaged in advanced studies
– This process necessitates education in basic ➔ must work at the boundaries between the
sciences and an understanding of basic various sciences and
scientific principles.” ➔ Must keep abreast of advances in the physical,
chemical, and biological fields in order to
➔ Today more than ever before, the pharmacist understand
and the pharmaceutical scientist are called upon
to demonstrate a sound knowledge of Pharmacists are also expected to:
biopharmaceutics, biochemistry, chemistry, ➔ Provide concise and practical interpretations of
pharmacology, physiology, and toxicology highly technical drug information to your patients
and an intimate understanding of the physical, and colleagues.
chemical, and biopharmaceutical properties of
medicinal products. HISTORY
➔ Physical pharmacy has been associated with
BIOPHARMACEUTICS the area of pharmacy that dealt with the
➔ Bio – life quantitative and theoretical principles of
➔ Pharmaceutics physicochemical science as they applied to the
- general area of study concerned with practice of pharmacy.
the formulation, manufacture, stability
and effectiveness of pharmaceutical More Definition
dosage forms. - The term “Physical Pharmacy” stems from the
application of physical chemistry principles to
➔ Pharmacodynamics - what the drug does to the area of pharmacy in the design of drug
the body molecules and drug products. It is also the
scientific principles applied in the preformulation
➔ Pharmacokinetics - what your body does to the & formulation process
drug
- In the past, drug delivery focused nearly
➔ LADMER SYSTEM exclusively on pharmaceutical technology (in
◆ Liberation - to free the active ingredients other words, the manufacture and testing of
from its dosage form to tablets, capsules, creams, ointments, solutions,
disintegrate/dissolve etc.). This area of study is still very important
◆ Absorption - Absorb the active today.
ingredients in the body
◆ Distribute - Circulatory system (main - Physical pharmacy attempted to integrate the
distribution channel in our body factual knowledge of pharmacy through the
◆ Metabolism - protein (albumin) development of broad principles of its own, and
- Protein (albumin) + Binding it aided the pharmacist and the pharmaceutical
(drug) = protein-bound drug & scientist in their attempt to predict the solubility,
free form (fast excretion) stability, compatibility, and biologic action of drug
◆ Excretion products.
◆ Response
PHARMACEUTICAL SCIENCE
➔ Examines the interrelationship of the - reflect the high degree of integration of the
physical/chemical properties of the drug, the biological and physical–chemical aspects of
dosage form (drug product) in which the drug is the field.
given, and the route of administration on the rate
and extent of systemic drug absorption - The advent and commercialization of
molecular, nanoscale, and microscopic drug
➔ Whether engaged in research and delivery technologies is a direct result of the
development, teaching, manufacturing, the integration of the biological and
practice of pharmacy, or any of the allied physical–chemical sciences.
branches of the profession, the pharmacist must
recognize the need to rely heavily on the basic - The integration of physical–chemical and
sciences. biological aspects is relatively new in the
pharmaceutical sciences.
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 PHARM 3 PRELIM
PHYSICAL PHARMACY LEC

- A dynamic and interdisciplinary field that aims to

integrate fundamental principles of physical and
organic chemistry, engineering, biochemistry,
and biology to understand how to optimize
delivery of drugs to the body and translate this
integrated understanding into new and improved
therapies against human disease.

- A dosage form is the entity that is administered

to patients so that they receive an effective dose
of a drug.

- If the dose is too high, a lower-dose tablet may

be prescribed. If a lower-dose tablet is not
commercially available, the patient may be ➔ As fluid from the gastrointestinal (GI) tract enters
instructed to divide the tablet. the tablet, pressure increases in the osmotic
layer and “pushes” against the drug layer,
releasing drug through the precision laser-drilled
tablet orifice in the active layer.

- However, a pharmacist who dispenses a

nifedipine (Procardia XL) extended-release
tablet or an oxybutynin (Ditropan XL)
extended-release tablet to a patient would
advise the patient not to bite, chew, or divide the
“tablet.”

- Nifedipine (Procardia XL) is a modified

release. While, oxybutynin (Ditropan XL) is an
osmotic pump drug delivery system

- This creative and elegant approach solves

numerous challenges to the delivery of
pharmaceutical care to patients. On the one
hand: ➔ Procardia XL is designed to provide nifedipine at
- it provides a sustained-release drug an approximately constant rate over 24 hr.
delivery system to patients so that they
take their medication less frequently, ➔ This controlled rate of drug delivery into the GI
- thereby enhancing patient compliance lumen is independent of pH or GI motility.
and
- positively influencing the success rate of ➔ The nifedepine release profile from Procardia
therapeutic regimens.
➔ XL depends on the existence of an osmotic
- A Procardia XL extended-release tablet is gradient between the contents of the bilayer
similar in appearance to a conventional tablet. It core and the fluid in the GI tract.
consists, however, of a semipermeable
membrane surrounding an osmotically active ➔ Medication counseling/education:
drug core. The core is divided into two layers: an - The information that the pharmacist
“active” layer containing the drug and a provides to the patient includes “Do not
“push” layer containing pharmacologically inert crush, chew, or break the
but osmotically active components. extended-release form of Procardia XL.

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 PHARM 3 PRELIM
PHYSICAL PHARMACY LEC

MODIFIED RELEASE DRUG DELIVERY

TECHNOLOGY ❖ This course should mark the turning point in the
(OROS – Osmotic controlled ­release oral delivery study pattern of the student, for in the latter part
system) of the pharmacy curriculum, emphasis is placed
upon the application of scientific principles to
practical professional problems. Although facts
must be the foundation upon which any body of
knowledge is built, the rote memorization of
disjointed “particles” of knowledge does not lead
to logical and systematic thought.

❖ CHALLENGE:
- If you are a pharmacy practitioner, you
should be able to translate a complex
OROS PUSH­-PULL scientific principle to a simple, practical,
and useful recommendation for a
patient.

WEEK 2: STATES OF MATTER

Three primary states of matter

CONFUCIUS
● “ I HEAR AND I FORGET. I SEE AND I
REMEMBER. I DO AND I UNDERSTAND.”
● The ancient Chinese proverb emphasizes the
value of active participation in the learning
process. The student is encouraged to actively
participate.

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 PHARM 3 PRELIM
PHYSICAL PHARMACY LEC

PHASE DIAGRAM - graph that gives off Temperature &

Pressure at which the substance exists as solid, liquid,
or gas.

- The triple point is at which the 3 phases exist in

equilibrium

- fixed shape
- Nearly incompressible
- Strong intermolecular force; very little kinetic
energy

SOLIDS

GAS STATE

LIQUID STATE
- Arranged in repetition 3D lattice units

GEOMETRIC FORMS:
CUBIC

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 PHARM 3 PRELIM
PHYSICAL PHARMACY LEC

WEEK 3: DENSITY & SPECIFIC GRAVITY

DENSITY (D)
➔ A measure of how matter is squeezed together
in a given amount of space. It is defined as an
objects mass per unit volume. It is one important
property of a substance.
CLEAVAGE
➔ A physical property constant at a given
temperature and density can help to identify a
substance.
➔ D=m/v
➔ The higher the density, the tighter the particles
are packed inside the substance.

➔ The density of solids is fairly constant, but for

fluids, it is more variable because fluids are
more compressible especially gases.
➔ The following may be helpful in converting from
liters to cubic meters and vice versa:
◆ 1L = 0.001 m3
◆ 1 m3 = 1000 L
◆ 1L = 1000 cm3
◆ 1 mL = 1 cm3
ARCHIMEDES’ PRINCIPLE
➔ States that the buoyant force applied to an
object is equal to the weight of the fluid the
object displaces.
◆ Bouyant force - the force applied
upward on an object by any fluid.
◆ Displacement - an object moves a fluid
so it can occupy the volume the fluid
originally occupied.

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 PHARM 3 PRELIM
PHYSICAL PHARMACY LEC

➔ Density of solid pharmaceutical materials

(e.g., excipients, blends, granules, tablets,
etc.)
◆ Useful during the design, optimization,
and scale-up of manufacturing
processes for solid pharmaceutical
dosage forms e.g., bulk densities of
excipient will clearly indicate whether a
need exists for a densifying unit
UNITS OF DENSITY operation such as dry granulation before
the manufacture of tablets.
➔ The SI units for density are kg/m3. The imperial
(U.S.) units are lb/ft3 (slugs/ft3). Other units of
➔ Density of solid pharmaceutical materials
density are the following:
◆ Densification
● Often necessary to enhance the
handling properties of the solid
materials (e.g., powder flow)
and to permit more efficient
processing operations to be
used (e.g., high-speed tablet
compression).
● Also facilitates dosing the active
ingredient to patients in
➔ Density of water (important to know) acceptably sized dosage forms.
◆ Water has a density of 1g/mL
◆ If I have 50 grams of water, I have 20
mL of water
◆ If I have 20 mL of water, I have 20
grams of water

➔ Floating and Sinking with Density

◆ If something has a greater density than
1g/mL, then it will sink.
● Example: 3g/mL > 1 g/mL
◆ If something has a smaller density than
1g/mL, then it will float.
● Example: .5 g/mL < 1g/mL
TEST YOURSELF! Will it float or sink in water?
- 5 g/ml SINK
- 2 g/ml SINK
- 0.8 g/ml FLOAT
- 1.01 g/cm3 SINK
- 0.5 g / cm3 FLOAT

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 PHARM 3 PRELIM
PHYSICAL PHARMACY LEC

➔ Specific gravity is often used by geologists to

help determine the mineral content of a rock
sample. In industry, specific gravity is used to
determine the concentrations of substances in
aqueous solutions.

SPECIFIC GRAVITY (spgr)

➔ Also known as Relative density, is the ratio of
the density of a substance to the density of a
given reference material.

➔ Specific gravity usually means relative density

with respect to water. The term "relative density"
is often preferred in modern scientific usage.
◆ Water (H2O) - standard reference in
liquid & solids
◆ Hydrogen - standard reference in gases

➔ In the United States Pharmacopeia, specific

gravities are based on data room temperatures
of 25°C, with the exception o that or alcohol that
is based on 15.56°C by government regulation.
◆ Specific gravity of Water= 1.0
◆ Substances that have a specific gravity
less than 1 are lighter than water.
◆ Substances that have a specific gravity
more than 1 are heavier than water.

Figure 5.1 = Depiction of

layering of immiscible liquids
in a test tube, mineral oil ➔ Therefore, sp gr is a factor that expresses how
being lighter than water and
much heavier or lighter a substance is – when
chloroform being heavier
compared to the standard (water)
◆ Ex. a liquid with sp gr of 1.25 is 1.25
times as heavy as water etc

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 PHARM 3 PRELIM
PHYSICAL PHARMACY LEC

III. DISPLACEMENT METHOD/PLUMMET METHOD

SPECIFIC GRAVITY OF LIQUIDS

I. KNOWN WEIGHT AND VOLUME

II. PYCNOMETER METHOD CALCULATING SPECIFIC GRAVITY OF LIQUIDS

➔ A pycnometer is a special glass bottle used to
determine specific gravity
➔ are generally available or laboratory use in
volumes ranging from 1 to 50 mL.
➔ have fitted glass stoppers with a capillary opening
to allow trapped air and excess fluid to escape

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PHARM 3 PRELIM
PHYSICAL PHARMACY LEC

USES OF SPECIFIC GRAVITY IN CALCULATIONS OF

WEIGHT AND VOLUME

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 PHARM 3 PRELIM
PHYSICAL PHARMACY LEC

COST OF GIVEN VOLUME OF LIQUID BY WEIGHT

APPLICATION
In pharmacy, it is sometimes necessary to use concepts
of density AND specific gravity to determine weights and
volumes of certain liquids
➔ Viscous liquids such as glycerin are more
accurately weighed than measured in graduated
cylinders. Density is used in the calculations
➔ Strengths of concentrated acids e.g., H2SO4, HCl
are expressed in percentage w/w. To prepare
dilute acid solutions of strength expressed in
percentage w/v it is necessary to use the specific
gravity of the concentrated acid in the calculations
➔ The specific gravity is used to find out the purity of
a drug since each of the constituents has a distinct
specific gravity.

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