Designing of drug to improve the site of action with in the body with respect to systemic circulation.
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DRUG FORMULATION
RAJEEV SAHAI
M.PHARM (Pharmacology)
Drug formulation
Why to use different formulation
Types of dosage forms
Composition of each dosage form
Why to use different formulation?
The physical nature of the drug
Drug size
Drug solubility
Drug taste
Drug absorption, first pass effect
Drug side effects
Drug half life
Site of disease or infection
Patient compliance
Drug
forms
Solid
dosage
forms
Liquid
dosage
forms
Semi-solid
dosage
forms
Others
Nasal
Inhalational
Solid
dosage
forms
Tablets Capsules Lozenges Powders
I-Solid dosage forms
Capsules, sustained-release capsules, tablets,
pills, are used to divide a drug or mixture of
drugs into definite doses and avoid the
inconvenience of preparing the dose from dry
powders.
Tablets are a convenient way of giving drugs
that have an unpleasant taste
Capsules
the most popular dosage forms for the oral
administration of powders, oils, and liquid
They dissolve readily in the stomach and make the
contents available for absorption only slightly less quickly
than a liquid medicament
Are usually made of gelatin and may be hard or soft
-Hard gelatin capsule : contains powder
-Soft gelatin capsule : contains Liquids
Gelatin capsules may be coated with a substance that
resists the action of gastric juice and so will not
disintegrate until they reach the alkaline secretions of the
intestine. Such capsules are said to be ‘enteric coated
Tablets
Tablets are preparations of powdered drug that are
compressed or molded into small disks.
They may be made with or without a diluent
(dextrose, lactose, starch),
And they may differ greatly in size, weight, and shape.
Compressed tablets are made with heavy machinery.
Tablets
Compressed tablets usually contain in addition to the
drug a
Diluents, are used when the amount of active
ingredient is small
A binderare substances that give adhesiveness to
the powdered drug.
A disintegrator, such a starch, helps the tablet to
dissolve readily when it is placed in water, because
the starch expands when it gets wet
and a lubricantkeep the tablet from sticking to the
machines
Tablets
Tablets are sometimes scored (marked with an
indented line across the surface) so-that they can be
broken easily if half a tablet is the dose required.
Tablets may be coated with sugar or chocolate to
enhance their palatability.
They may be covered with a colored coating to make
them more attractive to patients, easier to swallow,
or identifiable by the use of distinctive colors.
Both tablets and capsules may be enteric coated,
to protect the drug from the effect of the gastric secretions
to prevent drug irritation of the gastric mucosa
Sustained-release dosage forms
Dosage forms providing for gradual but continued
release of drug .
Sustained-release dosage forms contain small
particles of the drug coated with materials that require
a varying amount of time to dissolve.. This provides for
a long continuous period of absorption and effect.
Some particles dissolve and-are absorbed almost
immediately, others require 2 or 3 hours
Lozenges
Troches or lozenges are flat, round, or rectangular preparations
that are held in the mouth until they dissolve, liberating the drug
or drugs involved.
They usually contain water, sugar, and a mucilage in addition to
the drug and are dried in hot air.
They temporarily produce a high concentration of the drug in
the oral cavity.
They are held in the mouth until entirely dissolved.
Pills
Pills are mixtures of a drug or drugs with some
cohesive materials.
The mass is molded into globular, oval, or
flattened bodies convenient for swallowing.
They have been replaced to a great extent by
capsules and tablets.
Powders
Powders are finely divided solid drugs or
mixtures of drugs for internal or external use.
Dusting powders
Granules
Sachets
Chewable Tablets
Effervescent Tablets
Capsules
Pills
II-Liquid dosage forms
Solutions
Aqueous solutionshave one or more substances dissolved in
water. Examples are strong iodine solution (Lugol's Solution),
epinephrine nasal solution
Syrups
For their demulcent(soothing) effect on irritated membranes
of the throat e.g Promethazina hydrochloride syrup
Suspensions
Defined as preparations of finely divided drugs either intended for
suspension or already in suspension in some suitable liquid
vehicle
Liquid dosage forms
Emulsions
suspensions of fats or oils in water with the aid of an, emulsifying
agent, which lowers the interfacial tension between the two
susbtances, masking its oily feel.
These oils are more easily digested than undispersed oils.
Emulsions are stabilized by agents such as acacia and gelatin,
which coat the tiny droplets of oil and prevent them from
coming in direct contact with water.
An example is cod liver oil emulsion
Elixirs
are aromatic, sweetened, alcoholic preparations,
frequently used as flavored vehicles, such as
aromatic elixir, or as active medicinal agents if they
are medicated elixirs, such as phenobarbital elixir.
Liquid dosage forms
Liquid dosage forms
Liquid forms are composed of
Solvents
Sweeting agents
Flavouring and colouring agent
Stabilisers
Preservatives and antioxidant
Liquid dosage forms
-Ampoules and the like
1-Ampoules ( Single Dose).
2-vials ( multi -dose containers with rubber
capped stopper ).
3-Bottles.
4-Disposable syringes.
Solution
Suspension
Ampoule
Vials
Drops
III-Semi-solid dosage forms
1-Ointments and the like
-Ointments
-Creams
-Gels
-Pasts
2-Transdermal therapeutic system
3-Suppositories and the like
-Rectal supp.
-Vaginal inserts ( tablets –ovules –supp. pessary )