INTRODUCTION TO DOSAGE FORMS:
Drugs Defined:
A drug is any substance (other than food that provides nutritional support) that, when inhaled,
injected, smoked, consumed, absorbed via a patch on the skin, or dissolved under the tongue
causes a temporary physiological (and often psychological) change in the body. Drugs are
typically distinguished from food and other substances that provide nutritional support.
Consumption of drugs can be via inhalation, injection, smoking, ingestion, absorption via a patch
on the skin, suppository, or dissolution under the tongue
Pharmaceutical drug, also called a medication or medicine, is a chemical substance used to treat,
cure, prevent, or diagnose a disease or to promote well-being. Traditionally drugs were obtained
through extraction from medicinal plants, but more recently also by organic synthesis.
Pharmaceutical drugs may be used for a limited duration, or on a regular basis for chronic
disorders.
Pharmaceutical drugs are often classified into drug classes of;
similar chemical structures,
same mechanism of action (binding to the same biological target),
a related mode of action, and
that are used to treat the same disease.
The Anatomical Therapeutic Chemical Classification System (ATC), the most widely used drug
classification system, assigns drugs a unique ATC code, which is an alphanumeric code that
assigns it to specific drug classes within the ATC system. Another major classification system is
the Biopharmaceutics Classification System. This classifies drugs according to their solubility
and permeability or absorption properties.
Medication; A medication or medicine is a drug taken to cure or ameliorate any symptoms of an
illness or medical condition. The use may also be as preventive medicine that has future benefits
but does not treat any existing or pre-existing diseases or symptoms. Dispensing of medication is
often regulated by governments into three categories;
over-the-counter medications, which are available in pharmacies and supermarkets
without special restrictions;
behind-the-counter medicines, which are dispensed by a pharmacist without needing a
doctor's prescription, and
prescription only medicines, which must be prescribed by a licensed medical
professional, usually a physician.
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The range of medicines available without a prescription varies from country to country.
Medications are typically produced by pharmaceutical companies and are often patented to give
the developer exclusive rights to produce them. Those that are not patented (or with expired
patents) are called generic drugs since they can be produced by other companies without
restrictions or licenses from the patent holder.
Dosage form
Dosage forms (also called unit doses) are pharmaceutical drug products in the form in which
they are marketed for use, with a specific mixture of active ingredients and inactive components
(excipients), in a particular configuration (such as a capsule shell, liquid form, solid form for
example), and apportioned into a particular dose. For example, two products may both be
amoxicillin, but one is in 500 mg capsules and another is in 250 mg chewable tablets. The term
unit dose refers to each drug product individually packaged. The term dosage form can also
sometimes refer only to the pharmaceutical formulation of a drug product's constituent drug
substance(s) and any blends involved, without considering matters beyond that (like how it is
ultimately configured as a consumable product such as a capsule, patch, etc.). There is a vague
boundaries and unclear overlap of these terms and certain variants and qualifiers thereof within
the pharmaceutical industry, caution is therefore often advisable when conversing with someone
who may be unfamiliar with the use of the term.
Depending on the method/route of administration, dosage forms come in several types. These
include many kinds of liquid, solid, and semisolid dosage forms. Common dosage forms include
pill, tablet, or capsule, drink or syrup, and natural or herbal form such as plant or food of sorts,
among many others. Notably, the route of administration (ROA) for drug delivery is dependent
on the dosage form of the substance in question. A liquid dosage form is the liquid form of a
dose of a chemical compound used as a drug or medication intended for administration or
consumption.
Various dosage forms may exist for a single particular drug, since different medical conditions
can warrant different routes of administration. For example, persistent nausea, especially with
vomiting, may make it difficult to use an oral dosage form, and in such a case, it may be
necessary to use an alternative route such as inhalational, buccal, sublingual, nasal, suppository
or parenteral instead. Additionally, a specific dosage form may be a requirement for certain kinds
of drugs, as there may be issues with various factors like chemical stability or pharmacokinetics.
As an example, insulin cannot be given orally because upon being administered in this manner, it
is extensively metabolized in the gastrointestinal tract (GIT) before reaching the blood stream,
and is thereby incapable of sufficiently reaching its therapeutic target destinations. The oral and
intravenous doses of a drug such as paracetamol are readily available.
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The desirable properties of a dosage form are summarized below;
1. It should be convenient to handle, use and store
2. It should be stable during storage (shelf-life) and use.
3. The dosage form should be presented in different drug strengths providing flexibility of
dose to suit different age groups (e.g, 50,100,200, 500mg tablets of the same drug)
4. It should provide the anticipated therapeutic effect. The extent and pattern of drug release
from the dosage form, onset, intensity, and duration of action should be predictable.
5. It should protect the drug substance and conceal the disagreeable taste and odour.
6. It should be economical and presentation should be elegant
7. It should permit easy identification through distinct colour, shape and identification.
TYPES OF DOSAGE FORMS:
Definition: Dosage forms are the means or form in which drug substances are presented in the
market.
CLASSIFICATION OF DOSAGE FORMS:
They are classified according to:
a .Route of administration b. Physical form
Oral Solid
Topical Semisolid
Rectal liquid
Parenteral Gaseous
Vaginal
Inhaled
Ophthalmic
Otic
SOLID 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.
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Pigments to make uncoated tablets visually attractive.
Types of tablets
i.-COATED TABLETS; A firm coating may be applied to:
- hide the taste of the tablet's components.
- make the tablet smoother and easier to swallow .
- make it more resistant to the environment.
- extending its shelf life.
ii -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.
iii-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:
- Very rapid tablet dispersion and dissolution.
- pleasant tasting carbonated drink.
IV- CHEWABLE TABLET: They are tablets that chewed prior to swallowing. They are
designed for administration to children e.g. vitamin products.
2- CAPSULE: A capsule is a medication in a gelatin container in a solid dosage for. Advantage
of capsules is to mask the unpleasant taste of its contents. There are two main types of capsules
namely;
Hard-shelled capsules, which are normally used for dry,powdered ingredients, and
Soft-shelled capsules, primarily used for oils and for active ingredients that are dissolved
or suspended in oil.
3- 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.
4- 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.
5- DENTAL CONES: A tablet form intended to be placed in the empty socket following
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a tooth extraction, for preventing the local multiplication of pathogenic bacteria associated with
tooth extractions. The cones may contain an antibiotic or antiseptic.
6-PILLS: Pills are oral dosage forms which consist of spherical masses prepared from one or
more medicaments incorporated with inert excipients. Pills are now rarely used
7- 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.
8- POWDER (ORAL): Are Solid dosage forms consists of 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. E.g include Bulk Powders which 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.
LIQUID DOSAGE FORMS:
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 dispersions, either or both phases of
which may contain dissolved solids either oil is dispersed in 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- Simple Syrup: It is a concentrated aqueous solution of a sugar, usually sucrose to which
medicaments are added. Flavored syrups are a convenient form of masking disagreeable tastes.
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.
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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.
g- 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.
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.
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.
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.)
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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. 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.
7- Liniments: 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
8-Lotions: These are fluid preparations (aqueous) for external application without friction--
either dabbed on the skin or applied on a suitable dressing and covered with a
waterproof dressing to reduce evaporation.
9- Pressurized dispensers (aerosol sprays): Several different types of pharmaceutical product
may be packaged in 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 .
2- Enema: An enema is the procedure of introducing liquids into the rectum and colon via the
anus.
Types of enema:
a- 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.
b- Retention enema: Their volume does not exceed 100 ml. No warming needed. May exert:
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- Local effect: e.g. a barium enema is used as a contrast substance in the radiological
imaging of the bowel.
- 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.
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, ventro gluteal and dorso gluteal muscles. Injection
fibrosis is a complication that may occur if the injections are delivered with great frequency or
with improper technique.
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:
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1- Inhaler : Inhalers are solutions, suspensions or emulsions 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 50um 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.
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:
- inhalers are cheaper
- more portable
- carry less risk of side effects.
Therefore, 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, they may contain steroids,
antihistamines or topical anesthetics. Eye drops sometimes do not have medications in them
and are only lubricating and tear-replacing solutions.
2- Ophthalmic ointment & gel: These are sterile semi-solid preparations intended for application
to the conjunctiva or eyelid margin.
OTIC DOSAGE FORMS:
Ear drops: Ear drops are solutions, suspensions or 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:
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
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use of oily nasal drops should be avoided because of possible damage to the cilia of the nasal
mucosa.
INTRODUCTION TO NEW DRUG DELIVERY SYSTEMS
Drug delivery is the method or process of administering a pharmaceutical compound to achieve a
therapeutic effect in humans or animals. Drug delivery is more commonly called dosage form.
Several new drug delivery systems have been formulated and are being investigated which affect
only the target organ, site or receptor, and are also called targeted drug delivery systems or
‘magic bullet’. These include;
Liposomes; They are artificial microscopic bilayer vesicles or sacs made of phospholipids and
enclosing an aqueous compartment.
Microspheres; These are small, solid particulate carriers containing dispersed drug particles
either in solution or crystalline form.
Resealed erythrocytes; These are the erythrocytes in which the pores (200-50A diameter) are
created within the cell membrane, drug is allowed to enter the cell through these pores and
finally pores are closed causing the erythrocytes to ‘reseal’.
Nanoparticles ; These are colloidal particulate systems in the submicron size range acting as
carriers of drug molecules. Their size varies from 10 to 1000 nanometers.
Monoclonal antibodies; These are artificially produced proteins, which exhibit specificity for one
single antigen. The inherent specificity of monoclonal antibodies provides the rationale for their
use in drug targeting for therapeutic applications.
Microcapsules; Microencapsulation is the process of applying relatively thin, reproducible
coatings to small particles of solids or droplets of liquids and dispersions. The process can be
adapted to a wide variety of dosage forms and product applications.
Osmotic pumps; Osmotic pumps exploit the tendency of a fluid to equalize the concentration of
substances on both sides of a semi-permeable membrane. The system can be designed to deliver
different drugs at different rates.
Ion exchange resin systems; This system involves preparation of drug charged resin and its
drying to form beads. In the GI tract the drug molecule is exchanged for an appropriately
charged ion and hence the drug is released at controlled rates.
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Transdermal drug delivery systems; These are laminated patches, which adhere to the skin and
permit absorption of drugs from the skin surface through its layers into the general blood
circulation, at controlled rates, resulting in sustained blood levels.
Implants; Implants are sterile polymeric devices of varied shapes containing one or more
medicaments for introduction into body tissues. They release the drug in a controlled manner for
prolonged time extending to several months.
Nasal drug delivery systems; Nasal administration offers an interesting alternative for achieving
systemic drug effects to the parenteral route, which can be inconvenient, or oral administration,
which can result in unacceptably low bioavailabilities. The spray pumps and the aerosol valve
orifices lend themselves to controlled delivery of nasal formulations. Both systems are simple to
use and provide multiple dosing facilities.
Intrauterine devices; Intrauterine devices (IUD) is the device inserted in the uterus and is a
popular method of contraception. The copper acts as a contraceptive agent and a single IUD is
effective for up to 4months.
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