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Pharmacy Orientation
Pharmaceutical Dosage Forms
(enhanced version)
Presented
By
Sonia S. Morales, RPh,
MSPharm
Dosage Form
also known as pharmaceuticals. It
is defined as a preparation devised
to make possible administration of
medications in measured or
prescribed amount.

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Pharmaceutics
Pharmaceutics is the science of dosage form
design.
There are many chemicals with known
pharmacological properties but a raw chemical
is of no use to a patient.
Pharmaceutics deals with the formulation of a
pure drug substance into a dosage form.
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Active Drug Substance
(Active pharmaceutical ingredient - API)
Chemical compound with pharmacological (or
other direct effect ) intended for use in
diagnosis, treatment or prophylaxis of diseases.
International non-proprietary names (INN,
generic names)

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Direct clinical use of the active drug substances as
they are is rare due to a number of good reasons:

API handling can be difficult or impossible (e.g.,
low mg and g doses)
Accurate drug dosing can be difficult or
impossible
API administration can be impractical, unfeasible
or not according to the therapeutic 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 instability

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Direct clinical use of the active drug substances as
they are is rare due to a number of good reasons:


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

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From drug substance to pharmaceutical
preparation
Besides the choice of the active drug
substance, you need to also make a
responsible decision regarding the route of
administration and the DOSAGE FORM (drug
delivery system) wrong choice can cause
failure of therapy
You should also be able to handle and
administer the drug properly or advise the
patient about it wrong use can cause failure
of therapy
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Excipients

Excipients (inactive pharmaceutical
ingredients)
Its selection depends on technological,
biopharmaceutical and/or stability reasons.
Diluents/fillers, binders, lubricants, coatings,
preservatives, colorants and flavouring
agents

Terms
Parenteral Dosage Forms are
preparation introduced into the body by
injection through the skin, the mucous, or the
serous membranes

Dosage forms for inhalation are
preparations intended to be finally dispensed
or vaporized to the mucous membranes of the
lower part of the respiratory tract.

Terms
Oral Dosage Forms - are preparations
intended to be taken orally.

Rectal Dosage Forms - are preparations
employed for systemic effect or a local
action through the rectum.


Term
Dosage Forms For Topical application
are preparations intended to be applied on
the skin or instilled into eyes, nose, or ears.


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Pharmaceutical dosage form

Pharmaceutical dosage form
Determines the physical form of the final
pharmaceutical preparation
Is a drug delivery system which is formed by
technological processing (drug formulation)
Must reflect therapeutic intentions, route of
administrations, dosing etc.

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Pharmaceutical preparation (PP)
Pharmaceutical preparation (PP)
particular pharmaceutical product containing active
and inactive pharmaceutical ingredients formulated
into the particular dosage form.
Packed and labelled appropriately
Two major types of PP according the origin:
Manufactured in large scales by pharmaceutical
industry (original and generic preparations)
Compounded individually in compounding
pharmacies


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1- Pharmaceutical preparations
manufactured by pharmaceutical industry

1.1- Original pharmaceutical preparations
undergo full and very extensive
pharmacological/ toxicological and
pharmaceutical pre-clinical and clinical
development and evaluation
particularly important is the proof of
effectiveness and safety

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- Can be released after the expiration of the patent
protection of the original preparation
The approval for clinical use is easier due to the prior
experience with the original preparation
Must be pharmaceutically equivalent: same API, dose,
pharmaceutical dosage form and the same route of
administration as in original preparation
Must be clinically bioequivalent: i.e. it must be of very
close PK profile as original preparation. PK parameters
(Cmax, tmax, AUC) are within 80-125 % range as
compared with the original preparation.



1.2- Generic pharmaceutical preparations
(authorised copies of original preparations)
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2- Pharmaceutical preparations
compounded individually
These PP are compounded individually for a particular
patient according to the physician's prescription in a
pharmacy licensed for compounding
In contrast to the past, they are used rather rarely and
mostly in specific situations
It is highly advisable that whenever the particular suitable
PP is approved and commercially available it should be
preferred over the compounding
The major disadvantage is the lack of standardization (it is
always a single-patient batch), unavailability of rigorous
QC testing and the appropriate clinical evaluation.

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The individually compounded PP
can be a justified choice when:
The drug in a particular dosage form is not
commercially available on the market
The extraordinary low or high dose is needed (young
children, elderly people, special situations e.g.,
intoxications). In this case right dosage strength need
not be readily commercially available for every patient
The patient suffers from the allergy on a specific
excipients (e.g., lactose a filler, some
colorizing/flavouring or antimicrobial agents -
parabens) or another drug appearing in the PP
Patient is unable to use a PP in its commercially
available dosage form (e.g., children, elderly)

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Classification of pharmaceutical dosage
forms according to physical properties
Gaseous dosage forms
Liquid dosage forms
Semisolid dosage forms
Solid dosage forms

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Gases
Medicinal gases, inhalation/volatile
anaesthetics (vaporised before administration
by inhalation)

Aerodispersions of solid particles (e.g.,
antiasthmatic inhalations) or liquid particles
(antiasthmatic inhalations or sprays)


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Liquids
Solutions one homogenous phase, prepared by dissolving one or
more solutes in a solvent
Emulsions
a dispersion system consisting of two immiscible liquids
o/w or w/o
cloudy appearance
Suspensions
A dispersion system where solid particles (dispersed phase) are
dispersed in liquid phase (dispersion medium)
According to the size of dispersed particles (1 nm- 0,5 mm) a
molecular, colloidal and coarse dispersions can be distinguished
May require shaking before administration
Not intended for systemic administration of drugs with high
potency






LIQUIDS

A. Solutions a homogenous mixture that
is prepared by dissolving a solid or liquid or
gas in another liquid; it represents a group of
preparations in which the molecules of the
solute or dissolved substances are dispersed
among those of the solvent

Solutions
Water used mainly as a vehicle and as a solvent
for the desired flavoring or medicinal
ingredients.
Aromatic water also known as medicated water,
clear saturated aqueous solutions of volatile
oils or aromatic or volatile substances.
Aqueous acids official inorganic acids and
certain acids although of minor significance as
therapeutic agents are great importance in
chemical and pharmaceutical manufacturing.

Solutions
Diluted acids aqueous solutions of
suitable strength usually 10% w/v except
diluted acetic acid which is 6% w/v
Douches aqueous solutions directed
against a part or into a cavity of the body
Enemas also known as evacuation
enemas. They are rectal injections
employed to evacuate bowel retention
enemas to influence the general system
by absorption, or to effect locally the seat
of disease.

Solutions
Gargles aqueous solutions used for treating
the pharynx and nasopharynx by forcing air from
the lungs through the gargle which is held in the
throat.
Mouthwashes aqueous solutions which are most
often used for their deodorant, refreshing, or antiseptic
effect.
Juices (Succi) prepared from fresh ripe fruits,
aqueous in character and used in making
syrups which are employed as vehicles; excellent
way of taking medicinal herbs.

Other Solutions
Linctuses (Lincti) liquid preparations of a
mucilaginous, syrupy, or viscous nature
containing substances which possess
demulcent, expectorant, or sedative properties.
They are usually administered in small doses
and should be directed to be sipped and
swallowed slowly without the addition of water,
so that they may form a temporary protective
or remedial film over the membranes of the
throat. Ex. Linctus Ipecacuanhae
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Other Solutions
Oxymels formulations containing acetic acid
(or vinegar), clear honey, and enough water to
give a solution with a specific gravity of 1.32,
measured with a hydrometer. Usually the
amount of water comes to 1 part. Ex. Oxymel
Marrubii (Oxymel of Horehound)
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Solutions
Nasal solutions usually aqueous solutions
which are deigned to be administered to
the nasal passages in drops or spray
form.
Otic solutions aqueous preparations
dispensed in a container which permits the
administration of drops to the ear
NON-AQUEOUS
Collodion liquid preparations containing
pyroxillin in a mixture of ethyl ether and
ethanol.
Elixirs clear, pleasantly flavored sweetened
hydro-alcoholic liquids intended for oral
use.
Glycerites solutions or mixtures of
medicinal substances in not less than 505
by weight of glycerin

NON-AQUEOUS
Inhalations are solutions of drugs
administered by the nasal or oral
respiratory route for local or systemic
effect.
Liniments solutions or mixtures of various
substances in oil, alcoholic solutions of
soap or emulsions.
Oleovitamins fish liver oils diluted with
edible vegetable oil or solutions of volatile
substances of the indicated vitamins or
vitamin concentrates (usually A and D) in
fish liver oil.
NON-AQUEOUS
Spirits known as essences; are alcoholic
hydro-alcohol solutions of volatile
substances.
Toothache drops preparations used for
temporary relief of toothache by
application of cotton saturated with the
product into tooth cavity

B. EMULSION a two phase system prepared
by combining two immiscible liquids one of
which is uniformly dispersed through the
other; they consist of globules that have
diameters equal to or greater than those of
the largest colloidal particles.

C. SUSPENSIONS a two-phase system
consisting of finely divided solid dispersed in a
solid, liquid, or gas.

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Semisolid dosage forms
1- Unshaped (without specific physical shape)

Gels -A semisolid systems in which a liquid phase is
constrained within a 3D cross-linked matrix; a semisolid
system of either suspension made up of small organic
particles or large organic molecules interpenetrated by a
liquid
Creams semisolid emulsion systems (o/w, w/o)
containing more than 10% of water.
o/w creams - more comfortable and cosmetically
acceptable as they are less greasy and more easily
water washable
w/o creams accommodate and release better
lipophilic API, moisturizing, Cold creams
lotions usually liquid suspension or
dispersions intended for external
application to the body.
magmas and milk aqueous suspensions of
insoluble inorganic drugs; they differ from
gels mainly in that the suspended particles
are layers.
tinctures alcoholic or hydroalcoholic
solutions prepared from vegetable
materials or from chemical substances

Semisolid dosage forms
1- Unshaped (without specific physical shape)
fluidextracts liquid preparation of vegetable
drugs containing alcoholic as a solvent or as
preservative or both, so made that each mL
contains the therapeutic constituents of 1 g of the
standard drug that it represents

extracts concentrated preparations of vegetable
or animal drugs obtained by removal of the active
constituents of the respective drugs with suitable
menstruum.
Semisolid dosage forms
1- Unshaped (without specific physical shape)
parenteral preparation sterile preparations
intended to be administered by injection under
or through one or more layers of skin or
mucous membranes

intravenous admixtures mixture of
intravenous fluids and drugs to be
administered by injection
Semisolid dosage forms
1- Unshaped (without specific physical shape)
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Semisolid dosage forms
1- Unshaped (without specific physical shape)
Ointments semisolid dosage forms with the
oleaginous (hydrocarbon), water-soluble or
emulsifying base
Oleaginous (hydrocabon) base: Petrolatum
(Vaseline white, yellow)
Water-soluble base: Polyethylenglycol (PEG)-
ointment syn. macrogol ointments

Pastes semisolid dispersion system, where a solid
particles (> 25%, e.g. ZnO) are dispersed in
ointments mostly oleaginous (Petrolatum)

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Semisolid dosage forms
2- Shaped
Suppositories (for rectal administration)
different shapes
Melting/dissolving at body temperature
Oleaginous (cacao butter, adeps
neutralis) or aqueous (PEGs,
glycerinated gelatine)
Pessaries (vaginal suppositories)
Similar as above, PEGs or glycerinated
gelatine are often used as base.

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Solid Dosage Forms
Unshaped (without specific shape)
- powders for external/internal use
Shaped
- Tablets
- Capsules
- Implantates (Sterile disks inserted surgically into
body tissues and designed to release drug(s) over
extended period of time)
- Transdermal patches
- Lozenges (consists of sugar and gum to medicate
the mouth and throate)
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Classification of pharmaceutical dosage forms
according to the route of administration
for systemic administration
Peroral (p.o)
Sublingual (S.L) and buccal.
Rectal
Parenteral
Transdermal
Inhalation
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Classification of pharmaceutical dosage forms
according to the route of administration
for local administration
Topical (on the skin or mucosa)
Into/onto - the eye, nose, ear
- the oral cavity
- the vagina, rectum
- the brochi
- the skin
Local parenteral (viz Parenteral above)
Oral (local effect within GIT; antacids, adsorbents)

OPHTHALMIC PREPARATIONS
sterile preparations to be used on the
eyes
Solutions intended for the eye; clear, sterile
solution to be instilled into the eyes by the use of a
dropper.
Suspensions dispersion of finely divided
relatively insoluble drug substances in an aqueous
vehicle containing suitable suspending and
dispersing agent.
Ointment intended for the eyes; they contain
medicinal agents added to the ointment base of
white petrolatum and mineral oil either as a solution
or as a micronized powder.


LENS CARE PRODUCTS sterile
preparations intended to protect the lens
1. wetting solutions
2. cleaning solutions
3. disinfection solutions
4. soaking solutions
5. artificial tears





MEDICATED



OINTMENT semi-solid preparations intended
for external applications to the skin or
mucous membranes.
CATAPLASM a soft moist mass of meals,
herb, seed usually applied hot in clothes.
PASTES concentrates of absorptive
powders dispersed in petrolatum or
hydrophilic petrolatum
POWDERS for external use are usually
described as dusting powders, usually
contain starch, talc, and zinc stearate
DRESSINGS external applications
resembling ointment usually used as a
covering or protection.
CREAMS viscous liquid or semi-solid
emulsions of either the oil in water or
water in oil type
PLASTERS substances intended for
external application; they are made of
such materials and of such consistency as
to adhere to the skin and attach to a
dressing
SUPPOSITORIES solid dosage forms of
various weights and shapes usually
medicated for insertion into the rectum,
vagina, or the urethra

POWDERS
Oral powders generally supplied as finely
divided or effervescent granules
Dentifrices may be prepared in the form of
a bulk powders generally containing soap
or detergent, mild abrasive and
anticariogenic agent
Douche powders soluble powders intended
to be dissolved in water prior to use as
antiseptic or cleaning agents for a body
cavity.

Dusting powders locally applied non-toxic
preparations that are intended to have no
systemic action.
Insufflations finely divided powders
introduced into the body cavities.
Triturations dilutions of potent powdered
drugs prepared by intimately mixing them
with a suitable diluent in 1:10 dilutions

ORAL SOLID DOSAGE FORMS
TABLET solid dosage form containing drug
substances with or without suitable
diluents and prepared either by
compression or molding methods.
CAPSULES solid dosage forms in which the
drug substance is enclosed in either a
hard or soft soluble container or of a
suitable form of gelatin
PILLS small, round, solid dosage forms
containing medicinal agents and intended
for oral administration

ORAL SOLID DOSAGE FORMS
TROCHES also known as lozenges or
pastilles; they are discoid shaped solid
containing the medicinal agent in a
suitably flavored base.
CACHETS related to capsules in as such as
they provide an edible container for oral
administration of solid drugs.
PELLETS small, sterile cylinders about 3.2
mm in diameter by 8 mm in length, formed
by compression from medicated masses
AEROSOLS both oral and topical; they
contain therapeutically active ingredients
dissolved, suspended, or emulsified in a
propellant or in a mixture of solvent and
propellant

RADIOPHARMECUTICALS radioisotopes
used in medicine for therapeutic and
diagnostic purposes


BIOLOGICAL PRODUCTS
Vaccines a suspension of attenuated (live) or
inactivated (killed) microorganisms or fraction
thereof administered to induce immunity and thus
prevent infectious disease.
Toxoid a modified antigen from an infectious
organism used as a vaccine
Immune globulin a solution containing
antibodies from the pooled plasma of not less than
1,000 normal individuals
Hyperimmune serum a special preparation
obtained from human donor polls selected for high
antibody titer against a specific disease


Examples Dosage Forms
Omega Pain Killer (Methyl salicylate, menthol,
camphor) Liniment
Cold Rub (Camphor, Menthol, Eucalyptus oil)
Ointment
Aceiti Manzanilla Solution
Acrinol Tincture
White Henna Powder
Sebo De Macho Ointment
Caladryl (Calamine) Lotion
Nizoral (Ketoconazole) Cream, Shampoo, Tablet
Examples Dosage Forms
Dermovate (Clobetasol propionate) Cream,
Ointment, Solution
Dulcolax (Bisacodyl) - Tablet, Suppository
Dimetapp (Brompeniramine maleate) - Syrup
Ponstan (Mefenamic Acid) Capsule SF 250
mg; Tablet 500 mg; Suspension
Nitro-Dur (Nitroglycerin) Transdermal Patch
Nitroglycerin Tablet; Transdermal Patch

Five reasons for the need for
dosage forms.

1. To protect the drug substance from destructive influences
of atmospheric oxygen
2. To protect the drug from the destructive influence of gastric
acid after oral administration
3. To conceal the bitter, salty, or offensive taste or odor of a
drug substance.
4. To provide liquid preparations of substance that are
insoluble in desired vehicle
5. To provide for insertion of a drug into one of the bodys
orifices
6. To provide optimal drug action from topical administration
sites, etc.




Examples of Tablets



1. Poten-Cee Ascorbic acid Pascual
2. Alaxan Ibuprofen, Paracetamol
Therapharma
3. Tylenol Paracetamol - Janssen
4. Neozep
Phenylpropanolamine,chlorphenamine
maleate, paracetamol Myra/Unilab
5. Flanax Naproxen Roche




Example of Capsules


1. Velosef Cephradine Squibb
2. Tegopen Cloxacillin Bristol
3. Omnipen Ampicillin Wyeth
4. Imodium Loperamide Janssen
5. Darvon Aspirin, caffeine, propoxyphene
Lilly


Advantages and disadvantages of
different dosage forms

1. Ease of administrations
2. Stability purposes
3. Portability/ conveniently carried
4. Elegance
5. Accurate dosage
6. Manufactured at lower cost
7. Optimal drug action and others