UNIT I – INTRODUCTION TO
PHARMACEUTICALS
Dr. M Indira
Associate Professor
Department of Biotechnology
Vignan University
SYLLABUS
• History and definition of drugs;
• Sources of drugs - plant, animals,
microbes and minerals;
• Routes of drug administration;
• Different dosage forms.
DOSAGE FORMS
TYPES OF DOSAGE FORMS:
Definition: Dosage forms are the means ( or the form ) by which
drug molecules are delivered to sites of action within the body.
The need for dosage forms:
Accurate dose.
Protection e.g. coated tablets,
sealed ampules.
Protection from gastric juice.
Masking taste and odour.
Placement of drugs within body tissues
Sustained release medication.
Controlled release medication.
Optimal drug action.
Insertion of drugs into body cavities (rectal, vaginal)
Use of desired vehicle for insoluble drugs.
They are classified according
to:
Route of Physical
administration form
Oral Solid
Topical Semisolid
Rectal liquid
Parenteral Gaseous
Vaginal
Inhaled
Ophthalmic
Otic
ORAL DOSAGE FORMS:
1-Tablet:
A tablet is a hard, compressed medication in round, oval
or square shape. Solid dosage form containing unit dose
of one or more medicament.
- Prepared by mould method or compression
method
The excipients include:
-Binders, glidants (flow aids) and lubricants to ensure
efficient tabletting.
-Disintegrants to ensure that the tablet breaks up in the
digestive tract.
-Sweeteners or flavours to mask the taste of bad-tasting
active ingredients.
-Pigments to make uncoated tablets visually attractive.
1-TABLET (CONT.)
A coating may be applied to:
1- hide the taste of the tablet's
components. 2- make the tablet
smoother and easier to
swallow .
3- make it more resistant to the
environment. 4- extending its shelf
life.
2-BUCCAL AND SUBLINGUAL TABLET:
- Sublingual and buccal medications are administered by
placing them in the mouth, either under the tongue
(sublingual) or between the gum and the cheek (buccal).
- The medications dissolve rapidly and are absorbed through the
mucous membranes of the mouth, where they enter into the
bloodstream.
- Avoid the acid and enzymatic environment of the stomach and
the drug metabolizing enzymes of the liver.
- Examples of drugs administered by this route: e.g.
vasodilators, steroidal hormones.
3-EFFERVESCENT TABLET:
Effervescent tablets are uncoated tablets that
generally contain acid substances (citric and
tartaric acids) and carbonates or bicarbonates
and which react rapidly in the presence of
water by releasing carbon dioxide.
-They are intended to be dissolved or dispersed
in water before use providing:
A- Very rapid tablet dispersion
and dissolution. B- pleasant
tasting carbonated drink.
4- CHEWABLE TABLET:
- They are tablets that chewed prior to
swallowing.
- They are designed for administration to
children e.g. vitamin products.
5- CAPSULE: Hard gelatin capsule Soft gelatin capsule
A capsule is a medication in a gelatin
container.
- € solid dosage form
- Advantage: mask the unpleasant taste of
its contents.
- The two main types of capsules are:
1 Hard-shelled capsules, which are
normally used for dry, powdered
ingredients,
6- LOZENGE:
-It is a solid preparation consisting of sugar and
gum, the latter giving strength and
cohesiveness to the lozenge and facilitating
slow release of the medicament.
- It is used to medicate the mouth and throat for
the slow administration of indigestion or
cough remedies.
7- PASTILLES
- They are solid medicated preparations
designed to dissolve slowly in the mouth.
They are softer than lozenges and their bases
are either glycerol and gelatin, or acacia and
sugar.
8- DENTAL CONES:
- A tablet form intended to be placed in the
empty socket following a tooth extraction, for
preventing the local multiplication of
pathogenic bacteria associated with tooth
extractions.
- The cones may contain an antibiotic or
antiseptic.
9-PILLS:
- Pills are oral dosage forms which consist of
spherical masses prepared from one or more
medicaments incorporated with inert
excipients.
-
10- GRANULES:
- They are consisting of solid, dry aggregates of
powder particles often supplied in single-dose
sachets. They are irregular shape particle which
are made to improve flow property of powder
- Some granules are placed on the tongue and
swallowed with water, others are intended to be
dissolved in water before taking.
- Effervescent granules evolve carbon dioxide
when added to water.
11- POWDER (ORAL):
----Solid dosage forms -- intimate mixtures of dry finely
divided drug or chemicals intended for internal or
external use.
- The mixed powders may be stored in dry form and
mixture prepared by the pharmacist when required for
dispensing , by suspending the powders in the
appropriate vehicle.
1-Bulk Powders are multidose preparations consisting of
solid, loose, dry particles of varying degrees of
fineness.--contain one or more active ingredients, with
or without excipients and, if necessary, coloring matter
and flavoring substances.
usually contain non-potent medicaments such as
antacids since the patient measures a dose by volume
using a 5ml medicine spoon. The powder is then usually
dispersed in water or, in the case of effervescent
powders, dissolved before taking.
12-LIQUID PREPARATIONS:
a.Oral solution:
Oral solutions are clear Liquid preparations for oral use
containing one or more active ingredients dissolved in a
suitable vehicle.
b.Oral emulsion:
Oral emulsions are stabilized oil-in-water
disperse
dispersions,
either or both phases of which mayd contain
i dissolved
solids either oil is n finely divided form in water or
vice versa
c.Oral suspension:
- Liquid preparations for oral use containing one or
more active ingredients suspended in a suitable
vehicle.
- may show a sediment which is readily dispersed on
shaking to give a uniform suspension which remains
sufficiently stable to enable the correct dose to be
delivered
d- Syrup:
12-LIQUID PREPARATIONS (CONT.):
e- Elixir:
-It is pleasantly flavored clear liquid oral preparation of
potent or nauseous drugs.
- The vehicle may contain a high proportion of ethanol
or sucrose together with antimicrobial preservatives
which confers the stability of the preparation.
f- Linctuses:
- --are viscous, liquid oral preparations that are
usually prescribed for the relief of cough.
- --contain a high proportion of syrup and glycerol
which have a demulcent effect on the membranes of
the throat.
- The dose volume is small (5ml) and, to prolong the
demulcent action, they should be taken undiluted.
- .
12-LIQUID PREPARATIONS (CONT.):
Oral Drops:
Oral drops are Liquid preparations for oral use
that are intended to be administered in
small volumes with the aid of a suitable measuring device.
They may be solutions, suspensions or emulsions
h- Gargles:
- They are aqueous solutions used in the prevention or
treatment of throat infections.
- Usually they are prepared in a concentrated solution with
directions for the patient to dilute with warm water before
use.
i- Mouthwashes:
These are similar to gargles but are used for oral hygiene and to
treat infections of the mouth.
13. TOPICAL DOSAGE FORMS:
1 Ointments:
- Ointments are semi-solid, greasy preparations for application to the
skin, rectum or nasal mucosa.
- The base is usually anhydrous and immiscible with skin secretions.
- Ointments may be used as emollients or to apply suspended or
dissolved medicaments to the skin.
TOPICAL DOSAGE FORMS (CONT.):
2- Creams:
- Creams are semi-solid emulsions, that is mixtures of oil and
water.
- They are divided into two types:
A- oil-in-water (O/W) creams: which are composed of small
droplets of oil dispersed in a continuous aqueous phase.
Oil-in-water creams are more comfortable and cosmetically
acceptable as they are less greasy and more easily washed off
using water.
B- water-in-oil (W/O) creams: which are composed of small
droplets of water dispersed in a continuous oily phase.
Water-in-oil creams are more difficult to handle but many drugs
which are incorporated into creams are hydrophobic and will
be released more readily from a water-in-oil cream than an oil-
in-water cream.
Water-in-oil creams are also more moisturising as they provide an
oily barrier which reduces water loss from the stratum
corneum, the outermost layer of the skin.
TOPICAL DOSAGE FORMS (CONT.):
3- Gels
(Jellies):
-Gels are semisolid system in which a liquid phase is constrained within a
3-D polymeric matrix (consisting of natural or synthetic gum) having a high
degree of physical or chemical cross-linking.
-They are used for medication, lubrication and some miscellaneous
applications like carrier for spermicidal agents to be used intra vaginally .
4- Poultice:
It is soft, viscous, pasty preparation for external use. They are applied to skin
while they are hot. Poultice must retain heat for a considerable time because
they are intended to supply warmth to inflamed parts of body.
E.g. Kaolin poultice (B.P.C.)
TOPICAL DOSAGE FORMS (CONT.):
5- Pastes :
- Pastes are basically ointments into which a high percentage of
insoluble solid has been added
-The extraordinary amount of particulate matter stiffens the system.
-Pastes are less penetrating and less macerating and less heating
than ointment.
-Pastes make particularly good protective barrier when placed on
the skin, the solid they contain can absorb and thereby neutralize
certain noxious chemicals before they ever reach the skin.
- Like ointments, paste forms an unbroken relatively water –
impermeable film unlike ointments the film is opaque and
therefore can be used as an effective sun block accordingly.
TOPICAL DOSAGE FORMS (CONT.):
There are two types of paste:
a)Fatty pastes (e.g: leaser's paste) .
b)Non greasy pastes (e g: - bassorin paste).
6- Dusting powders:
- These are free flowing very fine
powders for external use.
- Not for use on open wounds unless
the powders are sterilized.
TOPICAL
9- Liniments:
DOSAGE FORMS (CONT.):
- Liniments are fluid, semi-fluid or, occasionally,
semi-solid preparations intended for
application to the skin.
- They may be alcoholic or oily solutions or
emulsions.
- Most are massaged into the skin (e.g. counter-
irritant).
- Liniments should not be applied to broken
skin
10-Lotions:
- These are fluid preparations (aqueous) for external
application without friction--either dabbed on the
TOPICAL DOSAGE FORMS
(CONT.):
11- Collodion:
Collodion is a solution of in ether or acetone,
nitrocellulose sometimes with the
addition of alcohols.
-Its generic name is pyroxylin solution.
-It is highly flammable.
- As the solvent evaporates, it dries to a celluloid-like film.
- Compound Wart Remover consists of acetic acid and salicylic acid
in an acetone collodion base used in Treatment of warts by
keratolysis.
TOPICAL DOSAGE FORMS
(CONT.):
12- Paints:
- Paints are liquids for application to the skin or
mucous membranes.
- Skin paints contain volatile solvent that
evaporates quickly to leave a dry resinous
film of medicament.
- Throat paints are more viscous due to a high
content of glycerol, designed to prolong
contact of the medicament with the affected
TOPICAL DOSAGE FORMS
(CONT.):
•13- Pressurized dispensers (aerosol sprays): d
- Several different types of pharmaceutical in
product may be package pressurized
dispensers, known as aerosols.
- Surface sprays produce droplets of 100 um
diameter or greater.
- May be used as surface disinfectants, wound
or burn dressing, relieve irritation of bites.
-Spray-on dusting powders are also available
from pressurized containers.
RECTAL DOSAGE FORMS:
1- Suppository:
It is a small solid medicated mass,
usually cone- shaped ,that is inserted
either into the rectum (rectal
suppository), vagina (vaginal
suppository or pessaries) where it
melts at body temperature .
RECTAL DOSAGE FORMS
(CONT.):
2- Enema:
An enema is the procedure of introducing liquids into the rectum
and colon via the anus.
Types of enema:
1- Evacuant enema: used as a bowel stimulant to treat
constipation. E.g. soft soap enema & Mgso4 enema
-The volume of evacuant enemas may reach up to 2 liters.
- They should be warmed to body temperature before
administration.
RECTAL DOSAGE FORMS (CONT.):
2- Retention enema:
- Their volume does not exceed 100 ml.
- No warming needed.
- May exert:
A- Local effect: e.g. a barium
enema is used as a contrast substance
in the radiological imaging of the bowel.
B- Systemic effect:
e.g. the administration of substances into the
bloodstream. This may be done in situations where it is
impossible to deliver a medication by mouth, such as
antiemetics.
e.g. nutrient enema which contains
carbohydrates, vitamins & minerals.
VAGINAL DOSAGE FORMS:
1- Pessary:
- Pessaries are solid medicated preparations designed for
insertion into the vagina where they melt or dissolve.
- There are three types:
A- Moulded pessaries: they are cone shaped and prepared in a
similar way to moulded suppositories.
B- Compressed pessaries: made in a variety of shapes and are
prepared by compression in a similar manner to oral tablets.
C- Vaginal capsules: are similar to soft
gelatin oral Capsules differing only in
size and shape.
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.
PARENTERAL DOSAGE FORMS (CONT.):
2- Intramuscular
injection:
-It is the injection of a substance directly into a muscle.
-Many vaccines are administered intramuscularly.
-Depending on the chemical properties of the drug, the medication may
either be absorbed fairly quickly or more gradually.
-Intramuscular injections are often given in the deltoid, vastus lateralis,
ventrogluteal and dorsogluteal muscles.
- Injection fibrosis is a complication that may occur if the injections are
delivered with great frequency or with improper technique.
PARENTERAL DOSAGE FORMS (CONT.):
3- Subcutaneous
injection:
Subcutaneous injections are given by injecting a fluid into the subcutis,the
layer of skin directly below the dermis and epidermis.
Subcutaneous injections are highly effective in administering vaccines and
such medications as insulin.
INHALED DOSAGE FORMS:
1- Inhaler :
- Inhalers are solutions, suspensions or emulsion of drugs
in a mixture of inert propellants held under pressure in
an aerosol dispenser.
- Release of a dose of the medicament in the form of
droplets of 50 um diameter or less from the container
through a spring-loaded valve incorporating a metering
device. The patient then inhales the released drug
through a mouthpiece.
- In some types, the valve is actuated by finger pressure,
in other types the valve is actuated by the patient
breathing in through the mouthpiece.
- It is commonly used to treat asthma and other
respiratory problems.
INHALED DOSAGE FORMS (CONT.):
2- Nebulizer or
(atomizer):
A nebulizer is a device used to administer medication to people in forms of
a liquid mist to the airways.
-It is commonly used in treating asthma, and other respiratory diseases.
-It pumps air or oxygen through a liquid medicine to turn it into a vapor,
which is then inhaled by the patient.
-As a general rule, doctors generally prefer to prescribe inhalers for their
patients, because:
1-These are cheaper
2- more portable
3- carry less risk of
side effects.
Nebulizers, for that reason, are usually reserved only for serious cases of
respiratory disease, or severe attacks.
OPHTHALMIC DOSAGE FORMS:
1- Eye
drops:
Eye drops are saline-containing drops used as a vehicle to administer
medication in the eye.
Depending on the condition being treated, may contain
they antihistamines or topical anesthetics. steroids,
Eye drops sometimes do not have medications
lubricating and tear-replacing solutions. in them and are
only
2- Ophthalmic ointment & gel:
These are sterile semi-solid
Preparations intended for application
To the conjunctiva or eyelid margin.
OTIC DOSAGE FORMS:
1- Ear drops:
- Ear dropsare solutions, suspensionsor
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.
NASAL DOSAGE FORMS:
1- 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.
INTERMEDIATE PRODUCTS USED IN
COMPOUNDING:
Extracts: These are concentrated preparations containing the
active principals of vegetable or animal drugs which have
been extracted with suitable solvents and concentrated to
form liquid, soft or dry extract.
Glycerins: These are solutions of medicaments in glycerol
with or without the addition of water.
Infusions: These are dilute solutions containing the readily
soluble constituents of crude drugs and prepared by
diluting 1 part of concentrated infusion with 10 parts of
water. Concentrated infusions are prepared by cold
extraction of crude drugs with 25% ethanol.
INTERMEDIATE PRODUCTS USED IN COMPOUNDING (CONT.):
Oxymels: These are preparations in which
the vehicle is a mixture of acetic acid
and honey.
Spirits: They are alcoholic or aqueous
alcoholic solutions of volatile substances
used as flavouring agents.
Tinctures: These are alcoholic preparations
containing the active principals of
vegetable drugs. They are relatively
weak compared to extracts.
Aromatic waters: These are aqueous
solutions, usually saturated of volatile
oils or other volatile substances. Used as
flavoring agents.