Pharmaceutical Dosage Forms 3

(PT 311)- Fall 2019

Lecture (1)

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 ‫رساله الكلية‬

Mission
The Faculty of Pharmacy of October University for Modern Sciences and Arts is
nationally accredited, has British partnership, and is committed to producing
graduates who are able to compete in national and international job markets and
entrepreneurship, and to be an effective member of the medical team providing
best medical care, while heeding professional ethics, through an outstanding
academic programme and proficient academic staff. The faculty is devoted also to
provide effective community services, and exceptional applied scientific research.

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Values
Leadership spirit
Student-centeredness
‫القيم الجوهرية الحاكمة‬
‫روح الريادة‬ -
Credibility
‫محورية الطالب‬ -
Equity and non-
discrimination ‫المصداقية‬ -
Accountability ‫العدالة و عدم التمييز‬ -
Commitment to Quality ‫المساءلة‬ -
Institutional Loyalty ‫االلتزام بالجودة‬ -
Team work ‫الوالء المؤسسى‬ -
Community Orientation ‫العمل الجماعى‬ -
‫التوجه المجتمعى‬ -

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The aims of the course:
1- Introduce the students to the importance of designing, formulating, manufacturing
and evaluation of solid dosage forms.

2- Identify the role of different pharmaceutical excipients in dosage design,

preparation and stability

Course content:
- Powders.
- Granules
- Tablets
- Capsules
- Microencapsulation

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Course assessment details

Mid-Term Examination 15%

Final-term Examination 35%

Oral Examination 15%

Practical Examination 20%

Semester Work 15%

Assignment and presentation

Other types of assessment ------

Total 100 %

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 Powder and Powder Technology
Pharmaceutical powder is a
mixture of finely divided drugs
and/or chemicals (powdered
excipients ) in dry form.
The term ‘Powder’ may be used to describe:
1- The physical form of a material, that is, a dry substance composed of finely
divided particles.
Or, it may be used to describe a type of pharmaceutical preparation

• Powder may be intended for internal (oral powders)

or external (topical or dusting powder) use.

• According to BP the particle size range is 1.2 – 1.7 mm.

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 Advantages of powdered products

1- More stable than liquid preparations

Some injections present as powders are to be

reconstituted before use.

The shelf life of the dry powder is 2-3 years ,

but once it is reconstituted with water its
self life is 1-2 weeks.

* Rapid dispersion of the powder ingredients in its

solvent is due to the small particle size of all
ingredients. 9
2- Easy for shipping and handling

3- Suitable to dispense drugs with a large dose

e.g. Magnesium Trisilicate Oral Powder BP is 1-5 g
and it is more acceptable to the patient
to disperse a powder in water and swallow it as a draught.

4-Faster dissolution rate than tablets or

capsules
(as these must first disintegrate before the
drug dissolves) i.e. rapid onset time = Faster
Drug absorption

5- Convenient for small child & elderly patient

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6- More economical than other solid dosage
forms

7- No preservatives are required

8- Accurate for single doses but not accurate

if present as bulk powder
9-Less chance of incompatibility

10- Flexibility and ease of

compounding
(A.C + excipients may be added as coloring,
flavoring or sweetening agents. 11
 Disadvantages of powdered products

1- Less convenient for the patient (specially for

bulk powder) due to Patient may misunderstand the correct
dose or method of use.

2- Not suitable for dispensing:

•bitter, nauseous & unpleasant taste drugs
•hygroscopic & deliquescent drugs(tending to melt or dissolve in humi

•volatile drugs), or aromatic materials from decomposition.

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3- Not a suitable dosage form for administration of
potent drugs.
This is due to the variation in spoonful , in this case tablets
and capsules are a more common for low-dose products

4-Not suitable for the administration of drugs which

are inactivated in the stomach
In this case, it should be presented as enteric-coated form.

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 Fundamental properties of powders

1-Particle size and size distribution

2-Shape
3-Surface area
4-Specific surface: it is the surface area per unit
volume (s/v ) or per unit weight (s/w)

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 1-Powders particle size

•The USP employs descriptive terms such

as: very Coarse, Coarse, Moderately
Coarse, Fine and Very Fine.

Particle size is related to portion of powder that

is capable to pass through the openings of
standardized sieves of varying dimensions in a
specified time period under shaking ( generally in
mechanical sieve shaker).
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Sieve Shaker
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particle size distribution curve

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Description terms Approximate Particle Size

-Very Coarse - About 2.36 mm

-Coarse - About 850 µm

-Moderately Coarse - About 425 µm
-Fine -About 180 µm
-Very Fine - About120 µm

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 The main objective of the size reduction
(Why size reduction is required?)

1-To increase surface area

2-To expose more cells of the vegetable

drugs used for extraction

3- Affect the dissolution rate of the particles intended to

dissolve ( P.S = rate of dissolution)
4- Keep the suspended particles uniformly
dispersed in the liquid vehicle (p.s. 0.5-10 μm)

5- Uniform distribution of drug substance

into a powder mixture or solid dosage form
to ensure dose- to dose content uniformity
(i.e. Good mixing)
6- Penetration of particles intended to be
inhaled deeply in respiratory tract (1-5 μm)

7- Lack of grittiness of solid particles in

ointments, creams, or ophthalmic preparations
(50-100 μm)
Methods used for determination particle
size:
1-Sieving :
Particles are passed by mechanical
shaking through a series of sieves of
known and successively smaller size
2-Microscopy
3-Light energy diffraction
4-Laser diffraction

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 Powder flow
Flowability of the powder is of critical importance in the
production of pharmaceutical dosage forms.
Some reasons for producing free-flowing powders
include:
- Uniform feed from the bulk storage containers or
hoppers into the feed mechanisms of tableting or
capsule-filling equipment.

- Uniform packing and constant volume-to-mass ratio,

which in turn maintain tablet weight uniformity.

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- Uneven powder flow can result in excess entrapped air
within powders, which in some high speed tableting
conditions may promote capping, or lamination

Reason of uneven flow:

1-May be a result of presences of excess fine particles,
which increases particle-die wall friction, -- causing
lubrication problems and increase dust contamination
risks during powder transfer.

2-Cohesive and adhesive forces:

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 Adhesion & Cohesion (cont.)
Cohesion: Tendency for solid particles to stick to themselves
(occurs between like surfaces).
Adhesion: Tendency for solid particles to stick to other solid
surfaces as hopper wall (occurs between unlike surfaces).
Cohesive forces are van der Waals forces which increase as
particle size decreases and vary with changes in relative
humidity.
Cohesion provides a useful method of characterizing the
frictional forces acting within a powder bed to prevent powder
flow.

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 Factors affecting powder flowability
1-particle shape
 Spherical particles flow better
(low S.A of contact)
 Needles or flakes particles poor
flowability (very high surface of
contact to volume ratio)
Dissimilar shapes have markedly
different fowability due to inter-
particles contact areas.
2- particle size
In general: very fine
particles do not flow
freely as large particles.
(Due to the increase in S.A
and due to high cohesion
and adhesion forces).
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3-Particle density

*Normally powders flow

under the influence of
gravity.

*Dense particles are

generally less cohesive than
light particles of the same
size and shape.

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 Some Methods for improving the flow
properties of powders
1- By increasing the average particle
size:
Large particles decrease cohesive or adhesive
force than smaller particles.
A- Use granules rather than a powder (essential
in tablet manufacture).
B- The addition of a coarser fraction to a fine
powder is another possible way for improving its
flow properties.

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2- By producing the powder in
the form of spherical particles:
•Spherical powders flow easily since the
particles can “ roll over ” one another.
•Spherical powders are produced by spray
drying process e.g. spray-dried lactose,
which is a popular diluent )

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3- By the use of additives:
a- By using glidants: such as powdered talc

b-By using adsorbents: such as magnesium oxides, as the

cohesiveness of powders increases with the moisture content
due to a continuous moisture film between the particles …
-----so adsorbent is used to decrease the cohesiveness of
powders.
N.B. Angle of repose of starch, sucrose, and sodium chloride
powders increased if exposed to humid air (i.e. bad flow) .
(>40 )

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c-By treatment with silicone: It is well known that the
surface of glass containers may be rendered
hydrophobic by treatment with silicones.

It is possible to treat powders by similar means and

thus prevent formation of moisture film on the surface
of the powder.

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 Uses and packing of powders
Depending upon their intended use, powder are
packaged and dispensed by pharmacist in two main
ways:1- bulk powder and 2-divided powder.
1-Bulk Powders
1.Antacids and laxative powders: may be packaged
in bulk or as unit packages.
2.Douche powders: solutions for vaginal douche
used for cleansing of the vagina, may be packaged
in bulk or as unit packages.
3.Dentifrices or dental cleansing powders: used in
dental hygiene, generally they contain soap or
detergent and mild abrasive.
4.Brewer’s Yeast powder contain vitamin B-
complex.
 5. Dusting powders are applied to various parts of the
body as lubricants, protective, absorbent, antiseptic, and
foot powders are currently available as pressure aerosol.

e.g.1: Dusting Talc Dusting powder BP is used as

lubricant.

e.g.2 Treatment of fungal infections. As Tinaderm which

is used for Tinea infections present in athlete’s foot.

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6. Insufflations are extremely fine powders to be
introduced into body cavities (ear, nose and throat using
insufflators)
The powder is placed in the insufflator, and when the bulb
is squeezed, the air current carries the fine particles
through the nozzle to the region for which the medication
is intended. *Insufflations pd must be passed through a
100 mesh sieve..

Disadvantage of (Bulk powder)

1-Inaccurate dose due to patient measurements of varying
amounts of powder.
2-So dispensing powdered drugs in bulk amounts is
limited to non-potent drugs.
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 2-Divided powders
•They are single doses of powder individually
wrapped in cellophane, metallic foil, or paper.

•The divided powder is a more accurate dosage

form than bulk powder because the patient is not
involved in measurement of the dose.

• Cellophane and foil-enclosed powders are better

protected from the external environment until the
time of administration than paper-enclosed
powders

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Effervescent Powders:
Effervescent powders are packed in
individual dose units because of the protective
qualities of laminates (wrapped material).They
contain; sodium bicarbonate and citric acid
which react together and give out effervesce
when the patient adds the powder to water to
produce a draught.

- It is important to protect the powder from

moisture during storage i.e. prevent the
evolution of gas, which lead to the formation of
dead granules.

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Special problems in powder preparations
1- For volatile substance:
The loss of camphor, menthol, and essential oils by volatilization
when incorporated into powders
Solved by:
-The use of heat-sealed plastic bags
-or double wrapping with waxed paper inside of a bond
paper.
2- For Eutectic mixtures:
•Liquid result from combination of phenol, camphor,
menthol, thymol, antipyrine, phenacetin, aspirin, salol
and related compounds at ordinary temperatures
“Eutectic mixtures”
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Solved by:
• Using magnesium carbonate or light magnesium oxide.
• effective diluents are used for this purpose, as kaolin,
starch, bentonite or any other absorbents.
Example:
Incorporation of about 20% silicic acid (particle size, 50 um) prevent the
liquefaction of eutexia occur between aspirin and phenyl salicylate
•Generally, an amount of diluent equal to the eutectic compounds
is sufficient to prevent liquefaction for about 2 weeks.
3- For liquids:
•In small amounts, liquid may be incorporated into
divided powders.
• Solved by: Magnesium carbonate, starch, or lactose
may be added to increase the absorbability of powders
to the liquid added.
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References.
- Ansel, Pharmaceutical dosage forms and drug delivery
systems. 8th edition, 2005.
-Remington . The Science and Practice of Pharmacy,
20th edition, 2000.
http://www.scribd.com/doc/49476777/TABLETManufa
cturing-methods
Any Questions
See you
in lecture 2
(Granulation)

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