Pharmacy Orientation

Pharmaceutical Dosage Forms

(enhanced version)
Presented
By
Sonia S. Morales, RPh,
MSPharm

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Dosage Form

 alsoknown as pharmaceuticals. It
is defined as a preparation devised
to make possible administration of
medications in measured or
prescribed amount.
 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

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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.
 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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 1.2- Generic pharmaceutical preparations
(„authorised copies of original preparations“)

- 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.

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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

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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
25 throat. Ex. Linctus Ipecacuanhae
 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.
 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
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Semisolid dosage forms
1- Unshaped (without specific physical shape)

 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)

 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)

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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 body’s 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