Pharmaceutical Dosage Forms

Presented
By
Prof. Dr. Sanaa A. El-Gizawy

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)

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

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

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.

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

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)

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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.

2- Pharmaceutical preparations
compounded individually

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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.

The individually compounded PP

can be a justified choice when:
The

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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)

Classification of pharmaceutical dosage

forms according to physical properties

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Gaseous dosage forms

Liquid dosage forms
Semisolid dosage forms
Solid dosage forms

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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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.

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)

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

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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)

Classification of pharmaceutical dosage forms

according to the route of administration

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for systemic administration

Peroral (p.o)
Sublingual (S.L) and buccal.
Rectal
Parenteral
Transdermal
Inhalation

Classification of pharmaceutical dosage forms

according to the route of administration

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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)

Prescription Writing

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The prescription is one of the most important

therapeutic transactions between physician and
patient.
The art of prescription writing is an ancient inheritance.
The ancients started their prescription with an appeal
to the gods for its success.
The ancient symbol, Rx, signifying the appeal, was
established centuries ago and has been carried down
to the present time.

Prescription Writing
To

avoid undesirable and/or serious effects on

the patient, both physician and pharmacist
must render the highest of professional
services.
Accurate diagnosis; proper selection of
medication, dosage form and route of
administration; proper size and timing of dose;
precise dispensing; accurate labeling; and
correct packaging all must be provided.
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Parts of prescriptions

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For Arthur H. Recipe

Take thou
Potassium Acetate of.............................one drachm.
Of Solution of Acetate of Ammonium........three and a half
drachms.
Of Spirits of Nitrous Ether...........................two drachms.
Of Infusion of Buchu (a quantity sufficient) up to four
ounces.........
Signa: -Mix. Let a mixture be made.
Label: -One drachm three times a day after meals.

Parts of prescriptions

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Form of the Written Prescription

A prescription

consists of the superscription,

the inscription, the subscription, the signa, and
the name of the prescriber
1- Superscription
The date when the prescription order is written;
the name, address and age of the patient; and
the symbol Rx (an abbreviation for "recipe," the
Latin for "take")
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Form of the Written Prescription

2- Inscription
The body of the prescription, containing the
name and amount or strength of each ingredient.
3- Subscription
The directions to the pharmacist, usually
consisting of a short sentence such as: "make a
solution," "mix and place into 10 capsules," or
"dispense 10 tablets."
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Form of the Written Prescription

4- Signature

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From the Latin "signa," meaning "write," "make," or

"label," this sections contains the directions to the
patient.
These should always be written in English; however,
physicians continue to insert Latin abbreviations, e.g.
"1 cap t.i.d. pc," which the pharmacist translates into
English, "take one capsule three times daily after
meals." Since the pharmacist always writes the label in
English, the use of such abbreviations or symbols
should be discouraged.

Form of the Written Prescription

Follow: 4- Signature
The instruction, "take as directed," is not
satisfactory and should be avoided.
The directions to the patient should include a
reminder of the intended purpose of the
medication by including such phrases as "for
pain," "for relief of headache," or "to relieve
itching"
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Form of the Written Prescription

5- Labeling
When the physician wants his patient to know
the name of the drug, the box on the
prescription form marked "label" should be
checked.
6- Refills
The physician should designate the number of
refills he wishes the patient to have.
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Proprietary vs. Non-Proprietary

("Generic") Prescriptions
In

recent years, some hospitals and private

physicians are indicating on the prescription
their willingness or desire that the pharmacist
dispense a non-proprietary or "generic-named"
preparation instead of the trade name item
written on the prescription. Some have a box
on the prescription designated "N.P.P." In this
way, the pharmacist can use a form of the drug
which may be less expensive to the patient.

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Types of Drugs
Legend

Drugs: These drugs may not be

dispensed by a pharmacist without a
prescription from a physician.
Controlled Drugs: In addition to requiring a
prescription, these drugs require additional
safeguards for storage. Refills are also limited.
Over-the-Counter (OTC) Drugs: These drugs
do not require a prescription.
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Controlled Substances
Schedules of Controlled Drugs: These drugs are
divided into five schedules.
Drugs can be scheduled, unscheduled, or moved from
one schedule to another as the need arises.
Schedule I
Drugs in this schedule have a high abuse potential
(narcotic and hallucination effects). Examples are
heroin, marijuana.

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Controlled Substances
Schedule II
Drugs in this schedule have a high abuse potential with
severe psychic or physical dependence liability.
Included are certain narcotic analgesics, stimulants,
and depressant drugs. Examples are opium, morphine,
codeine, hydromorphone, methadone, meperidine,
oxycodone, anileridine, cocaine, amphetamine,
methamphetamine, phenmetrazine, methylphenidate,
amobarbital, pentobarbital, secobarbital,
methaqualone, and phencyclidine.

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Controlled Substances
Schedule III
Drugs in this schedule have an abuse potential less
than those in Schedules I and II and include
compounds containing limited quantities of certain
narcotic analgesic drugs, and other drugs such as
barbiturates, glutethimide, methyprylon, and
chlorphentemine. Any suppository dosage form
containing amobarbital, secobarbital, or pentobarbital is
in this schedule.

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Controlled Substances
Schedule IV
Drugs in this schedule have an abuse potential
less than those listed in Schedule III and
include such drugs as barbital, phenobarbital,
chloral hydrate, ethchlorvynol, meprobabmate,
chlordizepoxide, diazepam, oxazepam,
chloroazepate, flurazepam, etc.

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Controlled Substances
Schedule V
Drugs in this schedule have an abuse potential
less than those listed in Schedule IV and
consist primarily of preparations containing
limited quantities of certain narcotic analgesic
drugs used for antitussive and antidiarrheal
purposes.

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Requirements for Prescriptions

Written for Controlled Substances
Required

Information on the Prescription

Must be dated and signed on the day it is
issued. Must have the full name and address of
the patient.
Must have the name, address, and registration
number of the physician.
May be prepared by the secretary, but must be
signed by the physician.
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Refilling Prescriptions for

Controlled Substances
Refills

for Schedule II drugs are not permitted.

Refills for Schedule III, IV, and V drugs are
permitted if the number of refills is indicated on
the prescription. However, the prescription order
may be renewed only up to five times within six
months after the date of issue. After five
renewals or after six months a new prescription
order is required.
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