Introduction to dosage forms and routes

of drug administration

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Outline
❑ Introduction to pharmaceutics

❑ Dosage form

➢ Definition

➢ The need for dosage forms

➢ Classification

❑ Introduction to pharmaceutical ingredients

➢ Definition

➢ Importance

❑Routes of drug administration 2

Chapter objectives

❑ Upon completion of this chapter, you should be able to:

➢ Define pharmaceutics, dosage form, excipient, route of

drug administration

➢ Describe the need for dosage forms

➢ Describe pharmaceutical ingredients used in solid,

semisolid and liquid dosage forms

➢ Describe Routes of drug administration

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Introduction: What is pharmaceutics?
❑ Pharmaceutics can be defined as :
➢ “ The general area of study concerned with the
formulation, manufacture, stability and effectiveness of
pharmaceutical dosage forms” or:
➢ “ The science that deals with the dosage form design”
❑ Pharmaceutics converts a drug (API) into a medicine.

Pharmaceutics

Ingredients Medicine 4
Pharmaceutical dosage forms
❑ Dosage form:

➢ A pharmaceutical dosage form is the entity that is administered

to patients so that they receive an effective dose of a drug.

➢ A dosage form is the form that we take our drug in

➢ Dosage form is the means by which drug molecule is delivered

➢ Designed to facilitate the administration of drug substances

➢ Contains API + inactive pharmaceutical ingredients

(excipients)
➢ Some common examples are tablets, capsules, suppositories,
transdermal patches, injections, suspensions,.
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 Pharmaceutical dosage…

DRUGS
(Active
pharmaceutical
ingredients)
+ Pharmaceutical
excipients
Preparation
processes
MEDICINES

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Why dosage forms are needed?...

❑ To produce a drug product that is stable, efficacious, attractive, easy to

administer, and safe.
➢ provide the mechanism for the safe and convenient delivery of
accurate dosage
❑ API handling, Accurate dosing and administration can be difficult or
impossible ( low mg and g doses)
eg. ethinyl estradiol, 0.05 mg
❑ API may cause local irritations or injury when they are present at high
concentrations at the site of administration
❑ To conceal the bitter, salty or offensive taste or odor of a drug
substance (capsules, coated tablets, flavored syrup)
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Why dosage forms…

❖ To protect the drug substance from the destructive influence of

✓atmospheric oxygen or humidity (coated tablets)

✓gastric acid after oral administration (eg. enteric coated

tablets)

❖ To provide liquid preparations of substances that are either

insoluble or unstable in the desired vehicle (suspensions)

❖ To provide rate-controlled drug action (various controlled

release tablets, capsules, and suspensions)

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Why dosage forms …

❑ To provide optimal drug action from topical administration

sites
▪ E.g., ointments, creams, transdermal patches, and ophthalmic, ear,
and nasal preparations)

❑ To provide for insertion of a drug into one of the body’s orifices

(rectal or vaginal suppositories)

❑ To provide for placement of drugs directly in the bloodstream or

body tissues (injections)

❑ To provide for optimal drug action through inhalation therapy

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Classification of Pharmaceutical dosage forms

They are classified according to:

Route of administration
Oral Physical form
Topical Solid
Rectal
Semisolid
Parenteral
Liquid
Vaginal
Inhaled Gas
Ophthalmic
Otic
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Solid dosage forms

❑Tablet
➢ A tablet is a hard, compressed medication in round or oval
shape
➢ The API will be compressed along with other pharmaceutical
excipients
➢ Used as oral dosage form

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Tablets ...
❖Buccal and Sublingual tablets
➢ 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.

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Tablets …
❑ Effervescent tablets
➢ 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 ↔ disintegration

➢They are intended to be dissolved or dispersed in

water before use, providing Very rapid tablet dispersion
and dissolution → rapid absorption

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Tablets…
❑Chewable Tablets
➢ Chewable Tablets are chewed within the buccal cavity prior to
swallowing

➢ Advantage:
✓Children and adults who have difficulty in swallowing
conventional tablets
– e.g. vitamin products

✓Antacid formulations in which the size of the tablet is normally

large

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Lozenges

❑ They are solid preparations consisting of sugar and gum

✓Gum gives strength and cohesiveness to the lozenge and

facilitates slow release of the medicament.

❑ It is used to medicate the mouth and throat for the slow

administration of indigestion or cough remedies.
➢ Dissolved slowly in the mouth

➢ Lubricate and sooth irritated tissues of the throat

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Capsule

❑ A capsule is a medication in a gelatin container

❑ Advantage:

➢ Mask the unpleasant taste of its contents

❑ The two main types of capsules are:

➢ Hard-shelled capsules: which are normally used for dry, powdered

ingredients

➢ Soft-shelled capsules: primarily used for oils and for active

ingredients that are dissolved or suspended in oil

✓Provide faster absorption than from other solid oral dosage

forms
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Suppositories

❑ It is a small solid medicated mass, usually cone-shaped, that is

inserted into the rectum where it melts at body temperature or
dissolve.

❑ Pessaries: are solid medicated preparations designed for insertion

into the vagina where they melt or dissolve

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Liquid dosage forms
❑ Oral solution

➢ Oral solutions are clear liquid preparations for oral use containing
one or more active ingredients dissolved in a suitable vehicle.
❑Syrup
➢ It is a concentrated aqueous solution of a sugar, usually sucrose.

➢ No need of other sweetening agents and viscosity-modifying

agents

❑ Elixir
➢ It is clear hydro-alcoholic solution for oral use
➢ The vehicle may contain a high proportion of ethanol or
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sucrose together with antimicrobial preservatives
Liquid dosage forms

Emulsion:
❑ emulsions are stabilized oil-in-water or water in oil dispersions, either or
both phases of which may contain dissolved solids.

Suspension:
❑ They are liquid preparations containing one or more active ingredients
suspended in a suitable vehicle.

❑ They 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.
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Semisolid dosage form
Ointments
❑ Ointments are semi-solid, greasy preparations for application to
the skin, rectum or nasal mucosa

❑ Ointments form a transparent unbroken relatively water

impermeable film in the skin

❑ Ointments may be used as

➢ Effective barrier against moisture loss

➢ A vehicle to apply suspended or dissolved medicaments to the skin

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Semisolid dosage forms

Pastes
❑ Pastes are basically ointments into which a high percentage of
insoluble solid has been added

❑ Stiff: The extraordinary amount of particulate matter

❑ Like ointments, pastes form

✓an unbroken relatively water impermeable opaque film

▪ Therefore can be used as an effective sun block

accordingly.

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Semisolid dosage forms

Creams
❑Creams are semi-solid emulsions, that is mixtures of oil
and water.
❑They are divided into two types:
➢ Oil-in-water (O/W) creams: small droplets of oil dispersed in a
continuous aqueous phase.
✓ O/W are more comfortable and cosmetically acceptable as

they are less greasy more easily washed off using water.

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Semisolid dosage forms

➢ Water-in-oil (W/O) creams: small droplets of water

dispersed in a continuous oily phase
✓ Advantage: More moisturizing

Gels (Jellies)
❑ Pharmaceutical gels or jellies are composed of a liquid phase
within a network structure of a solid gelling agent (consisting of
natural or synthetic gum or aluminum hydroxide).

❑ They are used for medication, lubrication, as carrier for

spermicidal agents to be used intra vaginally

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Gaseous dosage forms

Inhaler
❑ Inhalers are solutions, suspensions or emulsion of drugs in
a mixture of inert propellants held under pressure in an
aerosol dispenser.
❑ Release a dose of the medicament in the form of droplets
from the container.
❑ The patient then inhales the released drug through a
mouthpiece.
❑ It is commonly used to treat asthma and other respiratory
problems.
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Gaseous dosage forms
Pressurized dispensers (aerosol sprays)
❑ Aerosol is a two-phase system of solid particles or liquid droplets
dispersed in air or other gaseous phase, having sufficiently small
size to display considerable stability
❑ Used in the administration of drugs via the respiratory system,
mainly for local effect
➢ Can be used for
✓Systemic effect via the respiratory system,
✓Topical preparations as surface disinfectants, wound or burn
dressing, relieve irritation of bites

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❑ Drug substances are seldom administered alone
➢ They are given as part of a formulation in combination with one or more
nonmedical agents (known as pharmaceutical ingredients or excipients) that
serve varied and specialized pharmaceutical functions.

❑ For each dosage form, pharmaceutical ingredients establish the

primary features of the product and contribute to
➢ The physical form,
➢ Texture,
➢ Stability,
➢ Taste, and
➢ Overall appearance 27
Pharmaceutical excipients or additives

❑ Excipients are combined with APIs to

➢Aid their processing into dosage forms

✓ Solubilize, suspend, thicken, emulsify

✓ Modify dissolution, improve the compactability

➢Stabilize, preserve

➢Facilitate administration to patients

➢Enhance patient acceptance (Flavor, color)

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Excipients for solid dosage forms

Diluents (fillers) or bulking agent )

❑ Diluents are used to increase the bulk volume of a tablet or
capsule

➢ Increase the mass of the tablets and capsule that contain a

low concentration of therapeutic agent

✓ Eg: Starch (old), Lactose , Sucrose, mannitol, sorbitol,

micro crystalline cellulose (MCC)

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Binders
❑ Binding agents (adhesives) are added in either dry or liquid form
to promote formation of cohesive agglomerate (granule) or to
promote cohesive compacts during direct compression. →
necessary mechanical strength
➢ E.g., lactose, MCC, Acacia, Tragacanth, Gelatin,
polyvinylpyrrolidone(PVP), polyethylene glycol(PEG)

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Disintegrants
❑ Disintegrants are employed in tablet formulations to facilitate the
breakdown of the tablet into granules upon entry into the stomach
❑ Mode of action:

▪ ↑ the porosity and wettability of the compressed tablet matrix

▪ Water uptake rupturing the intra-particle cohesive forces that hold
the tablet together → disintegration

▪ Operate by swelling in the presence of aqueous fluids

Water uptake → swelling →physical rupture →widened the
channels for penetration of water → disintegration
➢ Example: sodium starch glycolate, cross povidone, cross
carmellose sodium
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Disintegrants
❑ production of gas (effervescent reaction):

➢ Tablet disintegration may also be mediated by the production

of gas whenever the tablet contacts aqueous fluids.

✓This is the mechanism of disintegration of effervescent

tablets.

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Lubricants/ anti adherents
❑ These are used to reduce friction between powders and metal
surfaces during tablet manufacture
➢ Example: Magnesium stearate, Sodium stearyl fumarate

Glidants
❑ Glidants act to enhance the flow properties of the powders within
the hopper and into the tablet die in the tablet press

❑ Reduce the friction between the powders/granules due to the ability

of the particles of the glidants to locate within the spaces between
the particles/granules

➢ E.g., Colloidal silicon dioxide, talc

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Sweetening agents
❑ Sweetening and flavoring agents are employed to control the taste
and hence the acceptability of dosage forms.

➢ If the conventional tablet contains a bitter drug

➢ If the tablet is a chewable tablet

▪ Eg. Aspartame, saccharin sodium, sucralose,

Colorants
❑ Colored tablets are generally formulated either to improve the
appearance or to identify the finished product uniquely

➢ Eg. Iron oxide red and/or yellow

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Flavouring Agents

❑ Supplement and complement to a sweetening agent

❑ Flavoring Agents mask the disagreeable odors of drugs

➢ Ensures patient compliance (especially in pediatric

formulations)

➢ Can be natural, e.g. peppermint oil, lemon oils

➢ Or artificial e.g. butterscotch

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Excipients For semisolid dosage forms
❑ One of the basic component of ointment, creams and pastes is
the base
❑ Bases have two distinct purposes:
➢ As a vehicle from which drugs may be absorbed by the skin
➢ As a protective or emollient for the skin

❑ Ointment base: The ointment base is that substance or part of an

ointment preparation which serves as carrier or vehicle for the
medicament.
➢ E.g., Lanolin, Polyethylene glycol, Petrolatum , Hydrophilic
petrolatum
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Ointment BASES

❖ An ideal topical (ointment) base should be inert, stable, smooth,

compatible with the skin, non-irritating and should release the
incorporated medicaments readily.

❖ Topical (Ointment) bases classified into four general groups:

❑ Hydrocarbon

❑ Absorption

❑ Water removable (O/W emulsion)

❑ Water-soluble bases

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Excipients For semisolid dosage forms

❑ Humectant: are a sort of hygroscopic substances that prevent

drying of preparations.

➢ Glycerol, sorbitol, propylene glycol

❑ Stiffening agent: Used to increase thickness or hardness of a

preparation, usually an ointment
➢ Cetyl alcohol ,Cetyl esters, wax, Microcrystalline, wax Paraffin, Stearyl
alcohol, White wax, Yellow wax

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Excipients For liquid dosage forms
❑Vehicles
➢ Carrying agents used in formulating a variety of liquids for oral
and parenteral administration
➢ The preferred and most commonly used vehicle in liquid dosage
forms is Purified Water USP, due to the
– Low cost and toxicity
– Physical compatibility
– Good solubilizing power

➢ Co-solvents are employed to increase the solubility of the

therapeutic agent within the formulation
▪ Glycerol and ethanol 39
Buffers
❑ Buffers are employed to control the pH of the formulated product (to
resist change in pH upon dilution or addition of acid or alkali)

❑ pH control is performed: to
maintain the solubility of the API in the formulated product

enhance the stability of products in which the chemical stability of API is

pH-dependent

❑ Examples :
Acetates (acetic acid and sodium acetate)

Citrates (citric acid and sodium citrate)

Phosphates (sodium phosphate and disodium phosphate, Potassium

metaphosphate )
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Preservatives
❑ Preservatives are used to prevent microbial growth of the formulation
❑ Example: Benzoic acid and salts (0.1–0.3%)
Sorbic acid and its salts (0.05–0.2%)
Alkyl esters of Para hydroxybenzoic acid (0.001–0.2%)

❑Antioxidants
➢ Included to enhance the stability of therapeutic agents that are
susceptible to chemical degradation by oxidation
➢ Examples:
✓ Sodium sulphite, sodium metabisulphite, sodium formaldehyde,
ascorbic acid,
✓ Butylated hydroxytoluene (BHT), Butylated hydroxyanisole (BHA )
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Viscosity-enhancing agents

❑ Suspension stabilizers: prevent settling/sedimentation

➢ usually modify viscosity, work by entrapment of solid particles

in a viscous or even gel-like structure

➢Example
– Methylcellulose,

– Hydroxyethylcellulose,

– Hydroxypropylcellulose

– Sodium carboxymethylcellulose

– Sodium alginate

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Emulsifying agent
❑ Emulsifying agent
➢ Are employed to prevent the coalescence of emulsions

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Surface-active agents

❑ Surface-active agents are amphipathic compounds used to reduce

surface tension
➢ To aid ‘wetting’ and dispersion of a hydrophobic API, preservative or
antioxidant
❑ Example
✓Oral: polysorbates (Tweens), sorbitan esters (Spans)
✓Parenteral: polysorbates, lecithin
✓External: sodium lauryl sulphate

R =CH2COOC17H33

sorbitan monooleate
polyoxyethylene 20 sorbitan (Span 80)
monooleate (Tween 80) 44
Sweetening Agents

Natural sweeteners
➢ Sucrose

➢ Sorbitol

Artificial sweeteners
➢ Much more intense sweeteners compared with sucrose

Examples:

✓Saccharin and it’s salts

✓Aspartame

✓Sucralose
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Humectants

❑ Excipients used in aqueous suspensions and emulsions for

external application.
❑ Function:
✓ To retard evaporation of aqueous vehicle of dosage form
✓ To prevent drying of the product after application to the
skin
✓ To prevent drying of product from the container after first
opening of a container
• Examples :Propylene glycol, Glycerol, Sorbitol

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Routes of drug administration

Definition : Route of drug

administration is the way
(path) through which the
dosage form is administered
into the body

Q. Which route do you prefer

more? Why?

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Oral Route (PO)

❑Drug is placed in the mouth and Swallowed

➢It is also called per oral (p.o.)

➢Commonly used dosage forms are tablets,

capsules, suspensions, and various pharmaceutical
solutions.

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Oral Route (PO)…
❑ Advantages
➢ Convenient – most natural, Can be self- administered, pain free, easy
to take
➢ Absorption - Takes place along the whole length of the gastro
intestinal tract
➢ Cheap - Compared to most other parenteral routes
❑ Disadvantages of Oral Route
➢ Sometimes inefficient - only part of the drug may be absorbed
➢ First-pass effect - drugs absorbed orally are initially transported to the
liver via the portal vein
➢ Irritation to gastric mucosa - nausea and vomiting
➢ Destruction of drugs by gastric acid and digestive juices
➢ Effect too slow for emergencies
➢ Unpleasant taste of some drugs
➢ Unable to use in unconscious patient
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Sublingual and Buccal routes

❑ Sublingual route: - drug is placed under the tongue,

disintegrates there and then absorption occurs in the mouth.

❑ The tablets used are small in size

Eg. Nitroglycerine tablets (400 μg)

Buccal Route: drug is kept in the buccal cavity where it

disintegrates and absorption occurs in the mouth

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Sublingual and Buccal routes
❖ Advantages of Sublingual and Buccal Routes
➢ Rapid absorption
➢ Drug stability: - the drug does not go to the stomach so it is not
destroyed by the enzymes and acids present in the stomach
➢ Drug bypasses the liver (and so avoid metabolism there) and
have direct access to the systemic circulation.
❖ Disadvantages
➢ Inconvenient: - In this route the drug is kept in the mouth so it
is inconvenient.
➢ Small Doses: - Small size is required to keep the drug in the
mouth.
➢ Drugs having unpleasant taste can cause problem

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Rectal and Vaginal Routes
❑ Rectal Route: - the medicament dissolves or liquefies after it is
inserted into the rectum.

➢ Suppositories are prescribed for people who cannot take a drug

orally because they have nausea, cannot swallow, or have
restrictions on eating, as is required after many surgical
operations.

❑ Vaginal Route: Some drugs may be administered vaginally to

women as a solution, tablet, cream, gel, pessaries or ring.

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Rectal and vaginal route …
Advantages of rectal and vaginal route
➢ Unconscious patients and children: If the patient is unconscious then
it is not possible to give the drug orally.
• the drug can be given through rectal/vaginal route.

➢ If patient is having nauseous or vomiting

➢ May be preferred for drugs destroyed or inactivated by the
environments of the stomach and intestines
Disadvantages:-
➢ Not easily acceptable by the patient
➢ May cause irritation
➢ Absorption may be variable
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Parenteral Routes

❑ In this route of administration, the drug does not pass through the
gastrointestinal tract.

❑ It directly reaches to the blood

❑ Drugs are administered with the use of injections

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Parenteral …

❑ Drugs may be injected into almost any area of the body, including

✓Joints (intra- articular), joint fluid area (intrasynovial),

✓Spinal column (intraspinal), spinal fluid (intrathecal),

✓Arteries (intra-arterial),

✓Skin (intradermal, ID; intracutaneous) and

✓In an emergency, even the heart (intracardiac).

❑ However, most injections go into a vein (intravenous, IV), into a

muscle (intramuscular, IM) or under the skin (subcutaneous, SC)

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Parenteral Routes …
1. Intravenous
➢ In this route of administration the drug is directly taken into the
blood(veins) with the help of injection.

➢ Absorption phase is bypassed.

Advantages:

✓ Precise, accurate dosing possible

✓ almost immediate onset of action

✓ Large quantities can be given , Can be given to unconscious patients.

✓ Drugs having unpleasant taste can be given.

Disadvantages:

✓ Invasive, pain at the site of injection

✓ Greater risk of adverse effects because high concentration attained rapidly

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✓ Risk of thrombosis and embolism
Parenteral Routes …
2. Intramuscular
❑ In this route of administration the drug is given into the muscles with the
help of injection.
➢ Drug reaches to the muscles, absorbed into the blood.
➢ Depot and slow release preparations possible
➢ Pain at injection sites for certain drugs
3. Subcutaneous
➢ In this route of administration the drug is given into the subcutaneous
layer with the help of injection.
➢ Drug once reaches to the subcutaneous layer crosses the membrane
and absorbed into the blood.
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EPICUTANEOUS ROUTE

❑ Drugs are administered topically, or applied to the skin, for their

action at the site of application or for systemic drug effects

➢ E.g., Common dosage forms: ointments, creams, lotions, gels

and patches

Transdermal patch is medicated adhesive patch that is placed on the

skin to deliver a specific dose of medication through the skin and
into the blood circulation

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EPICUTANEOUS ROUTE ….

❑ Advantages
➢ Bypass the first pass effect, and

➢ Protect the drug from gastrointestinal pH.

➢ In cases where localized action is desired, it offers remarkable

opportunity for drug action.

❑ Disadvantage
➢ skin is a poor medium to deliver drugs, because by its very
design it is supposed to prevent the entry of chemicals

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OCULAR, OTIC AND NASAL ROUTES

❑ Drugs are frequently applied topically to the eye, ear, and mucous
membranes of the nose, usually as ointments, suspensions, and
solutions.

Ocular
❑ Mainly for topical treatment of conditions and diseases of the eye

❑ common ophthalmic dosage forms include ointments, gels,

solutions, suspensions and inserts

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Nasal

❑ primarily for local effects on the mucous membranes and

underlying tissues (e.g., nasal decongestants)

❑ also used for the systemic absorption of drugs

Otic
❑ Medications are administered to the ear only for local treatment.

❑ Drops and other vehicles administered to the ear will occupy the
external auditory meatus, which is separated from the middle ear
by the tympanic membrane.

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Pulmonary route
❑ In this administration the drug is administered in the gaseous form.
e.g., Aerosols
➢ Pharmaceutical aerosols including metered-dose inhalers (MDIs) and dry
powder inhalers (DPIs) are devices that deliver a specific quantity of drug to
the lungs.
➢ The contact area of its surfaces extends to more than 30m2
➢ There are 2000 capillaries in the lungs
Advantages:
❑ large surface area, good vascularization, thin alveolar epithelium
are unique features of the lung that can facilitate systemic delivery
❑ Rapid onset of action due to rapid access to circulation.
❑ Painless

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Pulmonary route

Disadvantages
➢ Small dose
➢ Use of the devices needs training

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