Pharmaceutical

Dosage Forms &

Drug Delivery
System
 Pharmaceutical Dosage Forms

Drugs
 an agent intended for use in the
■ diagnosis
■ mitigation
■ treatment
■ cure
■ prevention
of diseases in man or in animals
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Pharmaceutic Principles
are the underlying physicochemical
principles that allow a drug to be
incorporated into a pharmaceutical
dosage forms.
These principles apply whether the drug
is extemporaneously compounded by
the pharmacist or manufactured in
commercial distribution as a drug
product.
 Pharmaceutical Dosage Forms

Why we should be familiar with the

basic properties of dosage forms?

API handling can be difficult or impossible (e.g.

low mg and g doses)
Accurate drug dosing can be difficult
API administration can be impractical,
unfeasible
– or not according to the
therapeutically
– aims
Some API can benefit from reducing the
exposure to the environmental factors (light,
moisture…), or they need to be chemically
stabilised due to the inherent chemical
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instability
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o API can be degraded at the site of

administration (e.g., low pH in stomach)
o API may cause local irritations or injury when
they are present at high concentrations at the
site of administration
o API can have unpleasant organoleptic
qualities (taste, smell – compliance!)
o Administration of active substance would
mean to have no chance for modification
(improvement) of its PK profile

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Drug Product
finished dosage form that contains the
active ingredient, generally, but NOT
necessarily, in association with one or
more other ingredients
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DRUG PRODUCT

Drug
Product

API (Active Excipients /

Pharmaceutical Additives
Ingredients)

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Dosage Form
formulation containing a specific
quantity of active ingredient(s) in
combination with one or more
excipients
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Dosage Form
Itprovides mechanism for the safe and
convenient delivery of the drugs
Concealment of offensive taste
Protection from destructive influences
of atmospheric oxygen & humidity and
from environment
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Excipient
 Aka Additives, pharmaceutical adjuncts or
necessities
 inactive ingredient present in a dosage form
 vehicle, suspending agents, lubricants, binders
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Excipients / Additives

 Coloring agents  Thickening agents

 Sweetening agents  Suspending agents
 Flavoring agents  Binding agents
 Solubilizing agents  Solvents
 Antioxidants  Lubricants
 Preservatives  Perfumes

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Drug Delivery System

means of administering drugs as
formulated preparations
formulations which provide a therapeutic
amount of drug to the proper site in the
body promptly and maintain the desired
drug concentration
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Drug Delivery System

Provide for insertion of a drug into the
body’s orifices
Provide for optimal drug action through
inhalation therapy
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Drug Delivery System

products that allow for the uniform release
or targeting of drugs into the body
encompass the drug formulation,
interaction among drugs, formulation
matrix, the container and the patient
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THE NEED FOR

DOSAGE FORMS
1. Accurate dose.
2. Protection, e.g. coated tablets, sealed ampules
3. Protection from gastric juice.
4. Masking taste and odour.
5. Placement of drugs within body tissues
6. Sustained release medication.
7. Controlled release medication
8. Optimal drug action.
9. Insertion of drugs into body cavities (rectal, vaginal)
10. Use of desired vehicle for insoluble drugs
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Classification of dosage
forms:
They are classified according to:

Route of administration Physical form

A) Oral A) Solid
B) Topical B) Semisolid
C) Rectal C) liquid
D) Parenteral D) Gaseous
E) Vaginal E) Sterile Products
F) Inhaled F) Novel Drug Delivery System
G) Ophthalmic
H) Otic
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A) Solid Dosage Forms-

Internal External
 Powders
 Insufflations
 Tablets
 Dentifrices
 Caplets
 Snuffs
 Capsules
 Ear Powder
 Cachets
 Dusting Powder
 Pills
 Lozenges
 Pastilles
 Granules

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B) Semisolid Dosage Forms-

Internal External
 Gels  Ointments
 Jellies  Creams
 Pastes
 Gels
 Suppositories
 Pessaries
 Poultices
 Paints
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c) Liquid Dosage Forms

Internal External
 Solution  Irrigations

 Suspension  Lotions

 Emuslions  Liniments
 Mouthwashes
 Elixirs
 Nasal Drops
 Syrups
 Enemas
 Collodions
 Sprays
 Spirits
 Gargles
 Mixtures
 Drops
 Linctus
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D) Gaseous Dosage Forms-

 Aerosols
 Inhalational
 Sprays
 Insufflations
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E) Sterile Products-

 Injections
 Infusions
 Ophthalmic
 Drops
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F) Miscellaneous

 Novel Drug Delivery System

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Part II. Solid Dosage Forms

Powders and Granules

Capsules
Tablets
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A. Powders (Oral)
 mixtureof finely divided drugs or chemicals in
dry form which can be used internally or
externally
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Two Kinds of Powders Intended for
Internal Use
 Bulk Powders –  Divided Powders –
multi dose single-dose
preparations presentations of
consisting of solid, powder (for example,
loose, dry particles a small sachet) that
of varying degrees are intended to be
of fineness. issued to the patient
 Contain one or more as such, to be taken
active ingredients, in or without water.
with or without
excipients

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Powders
Advantage Disadvantages
■ Flexibility of ■ Time consuming
compounding preparations
■ Good chemical ■ Inaccuracy of dose
stability ■ Unsuitability for many
■ Rapid dispersion of unpleasant tasting
ingredients (bec. of ■ Hygroscopic and
particle size) deliquescent drugs
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Powder Preparation
I. Comminution – mechanical process of
reducing particle size
II. Blending
III. Particle size determination
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Comminution Techniques
 Trituration
■ mortar and pestle
► Types of mortar and pestle
Glass
Wedgewood
Porcelain
■ aka 1:10 dilution (10%)
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Comminution Techniques
 Pulverization by intervention
► with the use of volatile solvent
► Example: Camphor (crystalline)
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Comminution Techniques
 Levigation
► with the use of non-volatile, non-solvent
► Levigating Agents
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Comminution Techniques
 For large scale
 Milling
► with the use of rotary cutter
► Hammer
► roller mills
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Blending of Powders
 Mixing Techniques
1) Spatulation
► use of spatula to blend small
amounts of powders on a pill tile
or sheet of paper
► Not for potent powders
► For solid substances that liquefy
and form eutectic mixtures
(phenol, camphor, methol, thymol,
aspirin, phenylsalicylate and
phenacetin)
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Blending of Powders
 Sifting
■ Powders are mixed by passing
them in sifters resulting to a light,
fluffy product.
■ Not applicable for incorporating
potent drugs into a diluent base
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Blending of Powders
 Geometric dilution
► used when a potent substance is to be
mixed with a large amount of diluent
► 1:1 Ratio
 Trituration
► Used both to comminute and mix
powders
► Mortar and pestle (grinding action)
► aka 1:10 dilution (10%)
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Blending of Powders
 Tumbling
► process of mixing powders in a large
container rotated by a motor
► Widely used in industry for large volume
powder mixing
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Particle Size Reduction

 Micromeritics – the study of small
particles.
Advantages of Small Particle Size
■ increase the surface area thereby
increasing dissolution rate as well as
bioavailability, e.g. griseofulvin
■ increase extraction or leaching from animal
glands and from crude vegetable extracts
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Particle Size Reduction

 Advantages of Small Particle Size
■ Facilitates drying of wet masses
■ Improves mixing or blending of solid
ingredients
■ Permits uniform distribution of coloring agents
■ Improve the function of lubricants
■ Improves the texture, appearance and physical
stability of ointments, creams, and pastes
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Particle Size Reduction

 Disadvantages of Small Particle Size
■ Can change the polymorphic form of the active
ingredient
■ Can degrade the drug
■ Decrease the bulk density of the active
compound and excipient
■ Decrease the particle size of the raw materials
and may create problems with static charge
■ Increase the surface area which may promote
air adsorption and inhibit wettability.
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Particle Size Determination

Particle Size can be determined by:
■ Sieving – mechanical shaking through a
series of sieves
■ Microscopy – calibrated grid background or
other measuring devices
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Particle Size Determination

 Sedimentation rate – setting velocity of
particles in a liquid medium through its
gravitational / central environment.
Calculated using the Stoke’s Law.
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Particle Size Determination

 Light Energy Diffraction / Light Scattering
– reduction in light reaching the sensor as
the particle, disperse liquid/gas passes
through the sensing zone.
 Laser Holography – particles individually
imaged and sized. Pulses laser fired
through an aerosolized sp___
photographed in 3 dimensions
(Holographic camera)
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Particle Size Determination

 Cascade Impaction – particles
separated into various size ranges by
increasing the velocity of the airstream.
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USP Standards for Powders of

Animal & Vegetable Drugs
Sieve number Limit (% passed through)
Very coarse Passed through no. 8 20% through No. 60 sieve

Coarse No. 20 40% through No. 60

Moderately No. 40 40% through No. 80

coarse

Fine No. 60 40% through No. 100

Very fine All process thru No. 80 no limit

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USP Standards for Powders of

Chemicals

Sieve Limit (% passed through)

number
Coarse No. 20 60% through No. 40
Moderately No. 40 60% through No. 60
coarse
Fine No. 80 No limit
Very fine No. 120 No limit
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Types of Powders:
1. Bulk Powders
 Large quantities (non potent powders)
 Multi dose preparations consisting of solid,
loose, dry particles of varying degrees of
fineness.
 Contain one or more active ingredients,
with or without excipients
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Packaging of Powders
Bulk Powders –
■ Perforated or sifter cans is used for external
dusting powders;
■ Aerosol Containers for spraying onto the
skin
■ Wide-mouthed Jar – for easy removal of a
spoonful of powder
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Powders Commonly Dispensed in

Bulk Forms:
 non-potent  Oral powders (antacid
and laxative powders)
subtances are  Douche powders
usually  Medicated and non-
medicated powders for
dispensed in external use
bulk powder  Dentrifices or dental
cleansing powders
form.  Dusting powders
 Insufflation, etc.
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Bulk Powders
Douche
Dentrifices
Triturations
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Dentifrices
 Dentifrices are agents
used along with a
toothbrush to clean and
polish natural teeth. They
are supplied in paste,
powder, gel or liquid form.
 eg: Toothpaste, Tooth
powder, Mouthwash, tooth
soap.

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Dusting powders:
These are free flowing very fine
- powders for external use on affected
part.
- Not for use on open wounds unless
the powders are sterilized.

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Packaging of Bulk Powders

 hygroscopic, deliquescent or volatile
substances – pack in glass jar
 amber or green glass should be used if
needed (to prevent decomposition of
light sensitive compounds)
Store in tightly closed containers
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Types of Powders
2. Divided Powders
aka “chartulae”
potent substances
individualized doses paper Tabs
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Packaging of Divided Powders

 Block and Divide Method
■ individually packed in folded papers
(chartulae); metal foils or small heat-sealed
or resealable plastic bags
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Papers for Packaging Divided

Powders
1. Glassine Paper – glazed, transparent,
moisture-resistant paper; limited use
for hygroscopic and volatile powders.
2. Vegetable Parchment – thin, semi-
opaque, moisture-resistant paper;
limited use for hygroscopic and
volatile powders.
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Papers for Packaging Divided

Powders
3. Waxed paper – transparent, water-proof
paper
4. Bond Paper – no moisture resistant
property
NB:
 Hygroscopic and volatile powders are best
protected with waxed paper, double
wrapped and covered with bond paper to
improve the appearance
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Special Problems with Powders

 volatile substances (e.g., camphor,
menthol, essential oils) can be lost by
volatilization
■ Volatilization is prevented or retarded by the
use of heat-sealed plastic bags or by
double wrapping with waxed or glassine
papers inside white bond paper.
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Special Problems with Powders

Liquids are incorporated into divided
powders in small amounts.
Hygroscopic and deliquescent
substances
Eutectic Mixtures
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B. Granules
 are
prepared
agglomerates of
smaller particles of
powder

 passed through no. 4-

12 sieves

 for
flowability for
tableting
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Granules
Method of Preparation
Wet Granulation
1) moisten the powder or powder mixture. Pass
the paste through a screen of the mesh size
2) Fluid bed processing – particles in a conical
piece of equipment dispersed and
suspended. Liquid sprayed and the product
is dried to produce pellets or granules of
defined particle size.
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Granules
Method of Preparation
Dry granulation
1. Dry method – or fusion method. Use of roll
or press compactor and a granulating
machine.
2. Slugging – compression of a powder or
powder mixture under 8000 – 12000 pounds
of pressure
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Characteristics of Granules
 flow well
 more stable to
atmospheric
humidity
Less-likely to cake
or harden upon
standing
Easily wetted by
liquids

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CAPSULES
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Capsules
are solid dosage
forms in which one
or more medicinal
agents and/or inert
substances are
enclosed in a small
gelatin shell
Intended to be
swallowed whole
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Capsule
the larger the numerical size the smaller
the size
largest = 000
smallest human consumption = 5
Largest (human consumption) = 0
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Capsule Sizes Powder capacity (mg)

No. 5 60-130
No. 000 650-2000
1 in.

0.5 in.

000 00 0 1 2 3 4 5
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Hard Gelatin Capsules

 composed of two pieces in
the form of cylinders closed
at one end.
 The shorter piece, called the
“cap” fits over the open end
of the longer piece called the
“body”
 Contains 12-16% water
(which varies with storage)
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Hard Gelatin Capsules

Preparation:
■ Prepare the formulation
■ Select the appropriate
capsule
■ Filling the capsule shell
■ Cleaning
■ Polishing the filled
capsule
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 empty hard gelatin

HGC capsule shells –
manufactured from the
mixture of gelatin,
colorants and
sometimes an opacifying
agent (e.g. titanium
dioxide).
 USP permits the addition
of 0.15% sulfur dioxide
to prevent
decomposition of gelatin
during manufacture

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 Gelatin, USP –
HGC obtained by the
partial hydrolysis of
collagen (obtained
from the skin, white
connective tissues
and bones of animals.
 Type A and B are
obtained by acid and
alkali processing
respectively.
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HGC Storage
 in tightly closed  When humidity is
glass containers low, the capsules
become brittle
 Protected from
 When humidity is
dust and
high, the capsules
extreme become flaccid
humidity and and shapeless
temperature

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Hard Gelatin Capsules

Prolonged exposure to high
humidity can affect the in vitro
capsule dissolution:
■ Tetracycline
■ Chloramphenicol
■ Nitrofurantoin
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Soft Gelatin Capsules

Oblong, elliptical or
spherical.
Glycerin or
polyhydric alcohol
(sorbitol) is added
to the shells to
make them elastic
or plastic-like.
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Soft Gelatin Capsules

used to contain liquids, suspensions,

pastes, dry powders or pellets

prepared by the plate process or rotary or

reciprocating die process, accogel
capsule machine (stern machine)
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TABLETS
 Pharmaceutical Dosage Forms

Tablets
 aresolid dosage forms usually prepared with
the aid of suitable pharmaceutical excipients

 are primarily prepared by compression, with a

limited number prepared by molding

 Most commonly used

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Tablets
Advantages: Disadvantages:

1. low manufacturing 1. some drugs are

cost, easy to package incompressible
and ship
2. precision and low 2. some drugs are
content variability sensitive to
3. easy to swallow humidity and air
4. most stable of all
oral dosage forms
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Tablet Design and Formulation

 characteristics of ■ chemically and
ideal tablets physically stable
over time
■ free of defects
■ Capable of
■ strong enough to
releasing medical
withstand the
agents in a
mechanical
predictable and
stresses of
reproducible
production and
manner.
handling (friability)

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Method of Manufacture
A. dry
granulation

B. wet
granulation

C. direct
compression
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Types of Tablets
A. Compressed tablets

A.1 Multiple-Compressed
tablets
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Types of Tablets
2. Chewable tablets

meant to be chewed and

subsequently swallowed
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Types of Tablets
3. Buccal Tablets
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Types of Tablets
4. Sublingual tablets
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Types of Tablets
5. Effervescent tablets
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Other types of tablet

 RDTs ( rapidly  Rapidly dissolving if
disintegrating tablets) more than 85% of the
labeled amount of drug
substance dissolves
 immediate release within 30 minutes using
apparatus I or II in a
 delayed release volume of less than 900
mL buffer solution.
 Extended release

 sustained release

 Vaginal tablets
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B. Types of Coated tablets

1. Sugarcoated tablets
mask offensive taste
disadvantage: bulky
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Types of Coated Tablets

2. Film coated
- Less bulky, less time consuming, and more
durable

3. Enteric-coated tablets
- Designed to dissolve in alkaline pH to release
medication in the small intestine
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SOLID DOSAGE FORMS

1.) lozenges-troches or pastilles
►discoid shaped solids
2.) Hypodermic tablets
►used by doctor for extemporaneous for
parenteral solutions
►issue: None sterile environment
3.) Pellets
►formed by compression from medicated
mass intended to be implanted
subcutaneously to release the medication
over a long period time
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SOLID DOSAGE FORMS

4.) cataplasm (poultices)
► moist mass of meal, herb, etc
► applied hot in cloth
5.) Plasters-solid/semisolid adhesive masses
► spread upon a backing material (local)
6. Transdermal patch
► administers drug in prolong period of time
(systemic)
7.) Band aid
► Protective
8.) Dressing
► external
application resembling ointments used as
covering or protection
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SUPPOSITORIES
 Pharmaceutical Dosage Forms

suppositories
Solid or semi solid Dosage Forms
intended for insertion into the body
orifices (rectal, vaginal, urethral) where
they melt, soften or dissolve and exert
local or systemic effects
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Types of suppositories
Rectal
Vaginal
Urethral
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suppositories
Suppositor Wt Size Shape Age Gender
y
Rectal 2g 32 mm Bullet or Infants Both
torpedo (1/2 size
of adult)
Vaginal 5g None Oviform or Adults Female
globular
Urethral M: 4g M: 140mm Penile size Adults Both
F: 2g F: 70mm
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Suppositories
Useful in infants
debilitated or comatose patients
patients who vomit
who have nausea or gastrointestinal
disturbances
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Criteria for satisfactory

suppository bases
Should be inert, non-irritating and non-
sensitizing
Should be firm and should not melt at
room temperature
Should dissolve rapidly in the cavity
fluid (have narrow or sharp melting
range)
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Suppository Bases
Fatty / Oleaginous Bases
1.cocoa butter (theobroma cacao)
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A. Fatty / Oleaginous Bases

2. Wecobee- coconut oil

3. Witepsol

4. Hydrogenated fatty acid of

vegetable oils
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Suppository Bases
2. Water-Soluble and Water-Miscible
Bases

3. Miscellaneous Bases
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Preparation
1. Hand-rolling

2. Compression

3. Fusion method
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Part III:
Liquid Dosage Forms
 Pharmaceutical Dosage Forms

Solutions
are liquid preparations,
that contain one or more
chemical substances
dissolved in a suitable
solvent or mixture of
mutually miscible solvents
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Solubility
Descriptive Term Part of solvent required per
part of solute

Very soluble Less than 1

Freely soluble 1 to 10
Soluble 10 to 30
Sparingly soluble 30 to 100
Slightly soluble 100 to 1000
Very slightly soluble 1000 to 10000
Practically insoluble 10,000 and over
 Pharmaceutical Dosage Forms

Advantages
1. Completely homogenous doses

2. Immediate availability for absorption and

distribution

3. Flexible dosage form

► Easy to swallow
► Can be used by any route of administration
► Easy to adjust dose
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General Rules in Preparing Solutions

 know the solubility characteristics of

the drug or chemical

 choose the proper solvent

 the salt form of the drug is used

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General Rules in Preparing Solutions

 when adding salt to syrup, dissolve

salt in a few mL of water then add
syrup to volume

 if an alcoholic solution of a purely

water-soluble drug is used, add the aq.
sol’n to the alcoholic sol’n.
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A. Aqueous Solution
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Water
 Most commonly used solvent for drug
solutions
USP: seven (7) types of water for the
use and preparation of dosage forms
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Types of water
 Purified
water – obtained by distillation, ion-
exchange or reverse osmosis
■ pH 5-7
■ Used in prescription and manufactured finished
products except parenterals and other sterile solutiins
 Water for Injection – purified water that is FREE of
Pyrogens
■ Obtained by distillation or reverse osmosis
■ Used for the preparation of parenteral solutions.
 Sterile
Water for injection – WFI that is sterilized
and packaged in single-dose containers < 1L
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Types of water
 Bacteriostatic
Water for Injection – SWFI that
contains 1 or more antimicrobial agents
■ Packaged in single or multiple dose containers <
30 mL
 Sterile Water for Inhalation – water purified by
distillation or reverse osmosis and rendered
sterile
■ Not used for the preparation of parenteral solutions
or other sterile dosage forms
 Sterile Water for Irrigation
 Sterile Purified Water
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Types of water
Sterile Water for Irrigation
■ WFI that is sterilized and suitably packaged
Sterile Purified Water
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1. Aromatic Waters
aka: Medicated Waters
are clear, aqueous solutions saturated
with volatile oils or other aromatic or
volatile substances
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Aromatic Waters
uses:
■ flavored vehicle for water soluble
drugs
■ aqueous phase in some emulsions or
suspensions

■ Storage: tight, light-resistant bottles

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Aromatic Waters
preparation:
■ solution (Peppermint Water, NF)
■ distillation (Stronger Rose Water, NF)
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2. Syrups
 solutionscontaining high
concentration of sucrose
or other sugars

 examples:
■ cherry syrup (47% cherry
juice)
■ cocoa syrup
■ orange syrup
■ raspberry syrup
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Syrup, NF  aka: simple syrup

 nearlysaturated aqueous
solution of sucrose (85%
w/v)
 By Percolation
■ rapid percolation: 3-5mL/min
■ Moderate percolation: 1-
3mL/min
■ Slow percolation: not more
than 1mL/min
 Pharmaceutical Dosage Forms

Syrup, NF
low solvent capacity for water soluble
drugs

inherently stable and resistant to the

growth of microorganisms when
properly prepared and maintained
 Pharmaceutical Dosage Forms

Method of preparation
 solution with the aid of
heat
 solution by agitation w/o
heat
 percolation (USP method)
 reconstitution
 addition of sucrose to an
already prepared
flavoured/ medicated
liquid
 Pharmaceutical Dosage Forms

3. Douches
 are aqueous solutions
directed against a
part or into a cavity of
the body
 Functions as a
cleansing or
antiseptic agent
 Pharmaceutical Dosage Forms

Douches
are frequently dispensed in the form of
a powder with the directions for
dissolving in a specified quantity of
warm water
 Pharmaceutical Dosage Forms

4. Enemas
 rectal solutions
 employed to evacuate
the bowel (evacuation
enemas)
 influence the general
system by absorption
(retention enemas) or
affect locally the site of
disease
 Pharmaceutical Dosage Forms

Types of Enemas
a.) evacuation enema
►1-2 pints (473 mL)
►ex. Fleet enema- (NaHPO4 + Na2HPO4)

b.) retention enema

►<150L
►Ex. Aminophylline enema
 Pharmaceutical Dosage Forms

5. Mouthwashes
are aqueous solutions
used for its deodorant,
refreshing or antiseptic
effect or for control of
plaque
 Pharmaceutical Dosage Forms

6. Gargles
 areaqueous solutions
used for treating the
pharynx and
nasopharynx by
forcing air from the
lungs through the
gargle which is held in
the throat
 Pharmaceutical Dosage Forms

B. Non Aqueous Solution

 Pharmaceutical Dosage Forms

1. Elixirs
 areclear, pleasantly flavoured,
sweetened hydroalcoholic
solutions intended for oral use

 alcoholcontent: 5-40%, but

most of the time, varies widely

 Aromatic Elixir, NF
■ 22% alcohol
 Pharmaceutical Dosage Forms

2. Spirits or Essences
are alcoholic or hydroalcoholic solutions of
volatile substances
alcohol content: generally over 60%
uses: flavoring agents, vehicle
Storage: tight, light-resistant containers
 Pharmaceutical Dosage Forms

Methods of Preparing Spirits

1. simple solution with agitation
■ aromatic spirit of ammonia

2. solution with maceration

■ peppermint spirit
 Pharmaceutical Dosage Forms

Methods of Preparing Spirits

3. chemical reaction
■ amyl nitrite spirit

4. distillation
■ brandy (grapes)
■ whisky (cereal grains)
■ Rum ( molasses)
 Pharmaceutical Dosage Forms

3. Tinctures
 arealcoholic or
hydroalcoholic solutions
prepared from vegetable
materials or from
chemical substances

 alcohol content: 15-80%

 Pharmaceutical Dosage Forms

Tinctures
Preparation
■ Maceration
■ Percolation

examples:
■ Iodine Tincture
■ Opium Tincture
 Pharmaceutical Dosage Forms

4. Fluidextracts
are liquid preparations of vegetable
drugs containing alcohol as solvent,
preservative or both and so made that
unless otherwise specified in an
individual monograph, each mL
contains 1 g of the standard drug
 Pharmaceutical Dosage Forms

Preparation
Process A: percolation
Process D: boiling water as menstruum

Maceration
Digestion
Infusion
 Pharmaceutical Dosage Forms

Liniments
 aka: embrocations
 are nonaqueous
alcoholic or oleaginous
solutions (or emulsions)
of various medicinal
substances intended to
be rubbed on the skin
 Pharmaceutical Dosage Forms

Liniments
 rubefacient,
counterirritant or
penetrating action
 Pharmaceutical Dosage Forms

Collodions
are liquid preparations composed of
pyroxyllin dissolved in a nonaqueous
solvent mixture usually composed of
alcohol and ether, with or without
added medicinal substances
 Pharmaceutical Dosage Forms

Collodions
Preparation:
Pyroxillin
■ Soluble gun cotton
■ produced though the action of nitric acid
and sulfuric acid on purified cotton
 Pharmaceutical Dosage Forms

Flexible Collodion
prepared by the addition of
castor oil (for flexibility)
and camphor (for water-proofing) to
collodion
 Pharmaceutical Dosage Forms

C. Topical solutions
 Pharmaceutical Dosage Forms

Topical Solutions
intended for Sprays
topical Astringents
application to the Local anti-
skin or mucous infective
membranes solutions
 Pharmaceutical Dosage Forms

Astringents
 locally
applied
solutions that
constrict pores and
precipitate proteins

 aluminum acetate
 aluminum subacetate
 calcium hydroxide
topical solution
 Pharmaceutical Dosage Forms

Local Anti-Infective Solutions

 kill
microorganisms
when applied to the
skin or mucus
membranes

 povidone-iodine
 thimerosal
 hydrogen peroxide
topical solution
 Pharmaceutical Dosage Forms

Sprays
 areaqueous or oleaginous
solutions in the form of
coarse droplets or finely
divided solids to be applied
topically, most usually to the
nasopharyngeal tract or to
the skin
 Pharmaceutical Dosage Forms

Aerosol
a dosage form that is
packaged under
pressure

 activeingredient is
released upon
activation of an
appropriate valve
system
 Pharmaceutical Dosage Forms

Liquid dosage form in Air

Inhalants Vaporizers
■ Can be carried by ■ Device that reduces
an air current using liquid to vapor for
high vapor pressure inhalation
 Pharmaceutical Dosage Forms

E. Sterile Solutions
 Pharmaceutical Dosage Forms

Nasal Solutions
 are aqueous solutions
designed to be administered
to the nasal passages in
drops or sprays

 vehicle used is usually water,

but a co-solvent system may
be used

 may contain preservatives,

buffer, antioxidant, surfactant
 Pharmaceutical Dosage Forms

Nasal Drops and Sprays:

Drugs in solution may be instilled into the nose from a
dropper or from a plastic squeeze bottle.

The drug may have a local effect, e.g. antihistamine,

decongestant.

Alternatively the drug may be absorbed through the

nasal mucosa to exert a systemic effect.
The use of oily nasal drops should be avoided because
of possible damage to the cilia of the nasal mucosa.

88
 Pharmaceutical Dosage Forms

Otic Solutions
 areintended for instillation
into the ear

 vehicle:
water or glycerin, or
co-solvent

 may contain preservatives,

buffer, antioxidants,
viscosity agents and
surfactants
 Pharmaceutical Dosage Forms

Ear drops:
- Ear drops are solutions, suspensions or emulsions of
drugs that are instilled into the ear with a dropper.
- It is used to treat or prevent ear infections, especially
infections of the outer ear and ear canal.

vinay gupta

148
 Pharmaceutical Dosage Forms

Ophthalmic Solutions
 are sterile, pyrogen-free
and particle-free solutions,
suitably compounded and
packaged for instillation into
the eye
 contains water,
preservatives, buffer,
antioxidants, tonicity
adjustors, viscosity
enhancers
 pH = 7.4 or pH = 6.5 to 8.5
 Pharmaceutical Dosage Forms

Eye drops:
Eye drops are saline-containing drops used as a vehicle to
administer medication in the eye.
Depending on the condition being treated, they may contain steroids,
antihistamines or topical anesthetics.
Eye drops sometimes do not have medications in them and are only
lubricating and tear-replacing solutions.

2- Ophthalmic ointment & gel:

These are sterile semi-solid
Preparations intended for application
To the conjunctiva or eyelid margin.
 Pharmaceutical Dosage Forms

Irrigating Solutions
 sterilesolutions used to
wash or bathe surgical
incisions, wounds or body
tissues

 should be labeled “Not for

Injection” and “For
Irrigation Only”
 pH and isotonicity must
be considered
 Pharmaceutical Dosage Forms

Parenteral Solutions
 solutions injected
through the skin or
directly into the blood
vessel, muscle, organ,
or other tissues
 Pharmaceutical Dosage Forms

V) Parenteral dosage
forms:
An injection is an infusion method of putting liquid into
the body, usually with a hollow needle and a syringe
which is pierced through the skin to a sufficient depth
for the material to be forced into the body.
There are several methods of injection, including:
1-An intravenous injection:
It is a liquid administered directly into the bloodstream
via a vein.
It is advantageous when a rapid onset of action is
needed.
vinay gupta

153
 Pharmaceutical Dosage Forms

Parenteral Solutions
 must conform to strict
requirements for
microbiological
impurity, particulate
matter, and
pyrogenicity
 Pharmaceutical Dosage Forms

Parenteral Solutions
special manufacturing equipment and
facilities are needed

pH and isotonicity must be given

special consideration
 Pharmaceutical Dosage Forms

Parenteral Solutions - Uses

1. alternative when patient in unable to take
medication by mouth

2. for drugs that are inactivated by gastric acid or

first-pass effect

3. when drug action is required immediately

4. when drugs are to be delivered to an organ,

lesion, a muscle, or a nerve
 Pharmaceutical Dosage Forms

Routes of Administration
1. Intradermal (ID)
■ interface between epidermis and dermis
2. Subcutaneous (SubQ, S.C., Hypo)
■ subcutaneous fat tissue between dermis
and muscle
3. Intramuscular (IM)
■ arms, buttocks, legs
4. Intravenous (IV)
■ veins
 Pharmaceutical Dosage Forms

http://www.leer-leren.com/wp-
content/uploads/2012/07/Like-a-boss.jpg
 Pharmaceutical Dosage Forms

II. Routes of Drug Adminsitration

 Parenteral
■ intravenous
■ Intraarterial
■ intracardiac
■ intramuscular
■ subcutaneous
■ intraarticular
■ intradermal/intracutanenous
■ Intrathecal
■ intraspinal
■ epidural
 Pharmaceutical Dosage Forms

F. Disperse System
 Pharmaceutical Dosage Forms

1. Suspensions
 liquiddosage forms
containing finely
divided drug particles
distributed somewhat
uniformly throughout
a vehicle in which the
drug exhibits a
minimum degree of
solubility
 Pharmaceutical Dosage Forms

Suspensions
particleshave diameters for the most
part greater than 0.1 mcm or equal to
0.5 micrometers
 Pharmaceutical Dosage Forms

Purposes for formulating a

suspension
sustaining effect
stability
taste
 Pharmaceutical Dosage Forms

Properties of a Good Suspension

Particle size of the suspensoid should
remain fairly constant throughout long
periods of undisturbed standing
Dispensed particles of the suspension
should settle slowly and should be
readily redispersed upon gentle shaking
of the container
 Pharmaceutical Dosage Forms

Precautions:
pour suspensions in a tight container

suspensions are not filtered

label: “Shake well before use”

 Pharmaceutical Dosage Forms

Types of suspension
1. Suspended Solution
2. Gel
3. Magma or milk
 Pharmaceutical Dosage Forms

Gels
are semisolid systems
consisting of
dispersions of small or
large molecules in an
aqueous liquid vehicle
rendered jelly-like by
the addition of a
gelling-agent
 Pharmaceutical Dosage Forms

a. Glycerogelatins
are plastic masses containing
gelatin (15%),
glycerin (40%),
water (35%)
and an added medicinal substance
(10%) such as zinc oxide
 Pharmaceutical Dosage Forms

Problems
 Imbibition-
The taking up of liquid by a gel
without the significant change in its
volume

 Syneresis
– natural shrinking of gel
caused by coarsening of the matrix

 Bleeding – liberation of oil or water from

ointment base resulting from a deficient
gel structure
 Pharmaceutical Dosage Forms

Magma / Milk
a two-phase system
gel consisting of
floccules of small
distinct particles

 ex.
Milk of Magnesia /
Magnesia Magma
 Pharmaceutical Dosage Forms

2. Emulsions
 are dispersed systems
in which the dispersed
phase is composed of
small globules of a liquid
distributed throughout a
vehicle in which it is
immiscible

 particle
size 0.1 to 100
micrometers
 Pharmaceutical Dosage Forms

Cod Liver Oil Emulsion

 Pharmaceutical Dosage Forms

Phases of an emulsion
 dispersed phase / internal phase
/discontinuous phase

 dispersion
medium / external phase /
continuous phase
 Pharmaceutical Dosage Forms

Purposes of an emulsion:
increased drug stability
prolonged drug action
improved taste
improved appearance
 Pharmaceutical Dosage Forms

Types of Emulsion
1. Oil-in-Water (o/w)

■ oil is dispersed as droplets in an aqueous

medium

■ oral products and external, washable

products
 Pharmaceutical Dosage Forms

Types of Emulsion
2. Water-in-Oil (w/o)

■ water is dispersed as droplets in an oil or

oleaginous medium

■ used for external preparations when

emollient, lubricating, or protective
properties are desired
 Pharmaceutical Dosage Forms

Types of Emulsion
3. Multiple Emulsions

■ (o/w/o or w/o/w)
 Pharmaceutical Dosage Forms

Types of Emulsion
4. Microemulsions

■ appear translucent
or transparent
■ have droplet
diameter in the
nanometer size
range
 Pharmaceutical Dosage Forms

Factors that determine emulsion type

1. Emulsifier
■ some emulsifiers form either w/o or o/w emulsions,
others form only one type

2. Phase ratio (relative amounts of oil and water)

■ phase present in greater concentration tends to be
the external phase

3. Order of mixing
■ the phase that is being added by portions tends to
be the internal phase
 Pharmaceutical Dosage Forms

Emulsifying Agents
1. Natural
■ derived from animal or plant sources

Animal: gelatin, egg yolk, casein,

Plant: acacia, tragacanth, pectin, cellulose

derivatives
 Pharmaceutical Dosage Forms

Emulsifying Agents
2. Finely Divided Solids

Aka Clays
Veegum -Magnesium aluminum
silicate

Bentonite -Aluminum Silicate

 Pharmaceutical Dosage Forms

Emulsifying Agents
3. Synthetic
• Anionic
• Cationic
• Non-ionic
 Pharmaceutical Dosage Forms

Griffin Hydrophilic-Lipophilic Balance (HLB) System

HLB Value Range Surfactant Application
Antifoaming agents
W/O emulsifying agents
Wetting agents
O/W emulsifying agents
Detergents
Solubilizing agents
 Pharmaceutical Dosage Forms

Methods of Preparation
1. Wet Gum Method (English Method)
2. Dry Gum Method (Continental
Method)
3. Bottle Method
4. Nascent Soap Method
 Pharmaceutical Dosage Forms

Problems in emulsion
1.) creaming - upward
2.) sedimentation - downward
3.) aggregation – globules come together
but do not fuse
4.)coalescence – globules come together
and fuse
5.) cracking – complete separation
6.) inversion – o/w to w/o or vise versa
 Pharmaceutical Dosage Forms

Part IV:
Semi solid Dosage Forms
 Pharmaceutical Dosage Forms

1. Ointments
are semisolid preparations intended for
external application to the skin or
mucous membranes
 Pharmaceutical Dosage Forms

Uses:
1. Emollients

2. Protective barriers

3. Vehicles
 Pharmaceutical Dosage Forms

Ointment Bases
1. Oleaginous Bases
■ hydrocarbon bases
■ not water-washable, incorporation of water
with some degree of difficulty
 Pharmaceutical Dosage Forms

Ointment Bases
2. Absorption Bases
■ are not easily removed from the skin
 Pharmaceutical Dosage Forms

Absorption Bases
anhydrous type w/o emulsion
■ hydrophilic ■ hydrous lanolin
petrolatum (25 – 30% water)
■ lanolin (0.25% ■ cold cream
water) ■ Eucerin®
■ Aquaphor® ■ Hydrocream®
■ Aquabase®
■ Polysorb®
 Pharmaceutical Dosage Forms

Ointment Bases
3. Water-Removable Bases
■ are o/w emulsions resembling creams
■ easily washed from the skin, hence called
“_____________________”
 Pharmaceutical Dosage Forms

Ointment Bases
4. Water-Soluble Bases
■ do not contain oleaginous components
■ are completely water-washable, hence
called “______________________”
 Pharmaceutical Dosage Forms

Preparation:
Incorporation
Fusion Method
 Pharmaceutical Dosage Forms

2. Creams
 aresemisolid preparations
containing one or more
medicinal agents dissolved
or dispersed in either a w/o
emulsion or an o/w
emulsion or in another type
of water-washable base
 Pharmaceutical Dosage Forms

3. Lotion
a fluid suspension
or emulsion
applied to the
surface of the skin
 Pharmaceutical Dosage Forms

4. Pastes
are semisolid preparations intended for
application to the skin, and generally
contain a larger proportion of solid
material than ointments and therefore
are stiffer
 Pharmaceutical Dosage Forms

Biologics
 Pharmaceutical Dosage Forms

Types of Immunity
NaturalImmunity
Acquired Immunity

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 Pharmaceutical Dosage Forms

1. Natural Immunity

 Natural, innate
or native
immunity –
depends on
factors that are
inborn
 Pharmaceutical Dosage Forms

Natural Immunity

Further classified
into:
 Species immunity
 Racial Immunity –
human race differ
 Individual
Immunity
 Pharmaceutical Dosage Forms

2. Acquired Immunity

 Active Acquired
Immunity
 Passive
Acquired
Immunity

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 Pharmaceutical Dosage Forms

2. Acquired Immunity
 Active Acquired
Immunity –
develops in
response to
antigenic
substances in the
body.
 may occur by
natural means –
infection (termed
naturally acquired
active immunity)

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 Pharmaceutical Dosage Forms

2. Acquired Immunity
 Active Acquired  Vaccines are
Immunity
administered
 –may develop in
response to for prophylactic
administration of a action, to
specific vaccine or develop
toxoid (termed
artificially acquired acquired active
active immunity) immunity.

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 Pharmaceutical Dosage Forms

2. Acquired Immunity
 Passive Acquired  can be
Immunity classified as:
 occurs by natural acquired
introduction of the passive
immunoglobulins
produced in another immunity
individual (human or  artificial
animal) into the host, acquired passive
who is not involved
in their production. immunity

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 Pharmaceutical Dosage Forms

Biologics for Active Immunity

 Bacterial
Vaccines
Viral Vaccines
 Cancer
Vaccines

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 Pharmaceutical Dosage Forms

Biologics for Passive Immunity

 Human Immune
Sera and
Globulins
(Homologous
Sera)
 Animal Immune
Sera
(Heterologous
Sera)

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