2 formulation administration of drugs zumiey

8/2/2019 2 Formulation Administration of Drugs Zumiey

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DRUG FORMULATIONS &

ROUTES OF DRUG ADMINISTRATION

Dr. Wan Ezumi Mohd FuadPPSK


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During Linnaeus time, there were some forms of drugsthat we seldom use today, eg:

- decoction (a plant is boiled in water)

- infusions (the same method as we use whenmaking tea)

- tinctures (extracts made with alcohol)

History


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Prepared in various forms for administration.

The physical & chemical properties of a drug -determine which form will be most effective.

The effective drugs lead to a better total outcome.

Drug Forms


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Different dosage forms affect absorption, distribution,onset times, length of action or concentration of drug in

the body.

Most drugs contain other ingredients (excipients) -facilitate the administration & absorption of the drug.

Drug preparations should be taken exactly asprescribed.

Cont


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Drug forms

Aqueous / liquid

preparations

Alcoholic

preparations

Solid & semi-solid

preparations


7/45Common drug forms and preparations


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Syrups - a solution of water & sugar to which drug

is added.

Addition of flavoring agents eliminates the bittertaste of many drugs.

Aqueous preparations


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Alcoholic preparations

Elixirs, spirits and tinctures

* Elixirs a sweetened aromatic solution of alcohol & water, to

mask an unpleasant taste.

* Spirits - an alcoholic solution of a volatile substance.

* Tinctures - an alcoholic extracts or solution of non-volatilesubstance.

Dissolved in various concentrations of alcohol.


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A number of different kinds for different purposes areavailable:-

Powders

- drug / drug extracts that are dried & ground intofine particles.

- for dermatologic use (talcum).

Solid and semisolid preparations


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Tablets

- drugs extracts that have been compressed into aconvenient form.

- most commonly used solid dosage form.

- easy to swallow.

- they usually disintegrate in the stomach morerapidly than most other solid preparations.

- low cost.

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Tablets for oral ingestion

- Compressed tablets

- Layered tablets

- Repeat-action tablets

- Delayed-action tablets (enteric-coated)

- Film-coated

- Chewable

Tablets for oral cavity

-Buccal

- Sublingual

- Lozenges

Cont


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Capsules

- drug powders or liquid, enclosed in gelatincapsules (hard / soft).

- easier to swallow than tablets.

- gelatin capsules dissolve in the stomach, therebyreleasing the drug.

Cont


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Delayed-release products

- Usually tablets / capsules that are treated withspecial coatings.

- so that various portions of the drug will dissolve atdifferent rates.

- designed to produce drug effects over an extendedtime.

- reduce the frequency of dosing.

Cont


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Enteric-coated (EC) products

- some drugs are very irritating to the stomach.

- the gastric juices of the stomach can inactive

certain drugs.

- in these cases, tablet / capsule is coated with anacid-resistant substance - will dissolve only in

the less acidic portions of intestines.

- should be taken on an empty stomach with water,either 1 hr before or 2 hrs after meals.

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Topical preparations

- Administration on or through the skin.

- Usually for dermatologic conditions.

- Conditions in which oral or parenteraladministration is impractible.

- include powder, creams, gel, paste, ointment.

Cont


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Ointments

- semi-solid preparations.

- soft oily substances (petrolatum or lanolin)containing a drug.

- applied to the skin or to the eyes (ophthalmic

ointments).

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Suppositories

- solid or semi-solid drug intended to be insertedinto a body orifice:-

* rectum

* vagina

* urethra

- drugs mixed with a substance (cacao butter) melt

at body temperature.

- for local effects (vagina, urethra) and systemeffects (rectum).

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Suppositories


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Routes of administration

The path by which a drug, fluid, poison, or othersubstance is brought into contact with the body.


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Depending on the route, the drug could beabsorbed & distributed in a matter of minutes,days, months.

How to select a particular route or dosage forms ofdrugs???

- depending on what type of effect is desired..


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Local effect - occurs when the drug activity is at

the site of administration (eye drops

etc.)

Systemic effect - occurs when the drug is introduced

into the circulatory system and

carried to the site of activity.

Local or systemic effects???


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Routes of drug administration

ROUTES OFADMINISTRATION

ENTERALADMINISTRATION

PARENTERALADMINISTRATION

TOPICALADMINISTRATION


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Enteral administration

Any form of administration that involves any part ofthe gastrointestinal tract (GIT) for systemic effect.

Oral administration (PO)

- dosage forms: solution, capsule, tablet.

- most common & convenient route.

- absorption through GIT.

Buccal & sublingual (SL) administration

- absorbed across epithelial lining of mouth.

- absorbed directly into systemic circulation.

Rectal administration

- placed in rectum and absorbed throughmucosal surface


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Advantages & disadvantages of enteraladministration

Easily self-administered.

Toxicities / overdose overcome with antidotes.

Many dosage forms

- type may affect absorption and distribution.

Affected by numerous factors

- gastric secretions pH

- gastric-emptying time

- intestinal transit time


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Parenteral administration

Any route that does not involve the GI tract.

Any route other than oral, sublingual or rectal.

For poorly absorbed drugs from the GIT & for

agents that are unstable in the GIT. Treatment of unconscious patient.

Treatment that require a rapid onset of action.

Associated with drugs administered withneedles (by injection or infusion).

Desired effects is systemic.

C


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Intravenous (IV) bolus injection (into a vein)

- acts rapidly

- many drugs, general anesthetics

Intravenous infusion

- infusion of fluids, blood

- constant input rate

- constant plasma drug concentration

Cont


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IV injection IV infusion

Cont


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Intraarterial injection (into an artery)

- When venous cannulation is impossible

- more complications compared with IV

- intraarterial injection is discouraged

- anesthetic drugs

- cancer chemotherapy

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Intraarterial injection


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Intramuscular (IM) injection (into a muscle)

- into the muscle fibers (under thesubcutaneous layer of skin)

- principle sites: gluteal (buttock), deltoid(upper arm) & vastus lateralis (thigh) muscles

- more painful than other routes

- many vaccines, antibiotics

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IM injection


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Subcutaneous (SC) (under the skin)

- used for both for short term & very longtherapies.

- sites: lower abdomen, front of thigh, upperback and back of upper arm.

- insulin.

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SC injection


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Intraperitoneal(IP) (injection into the peritoneam)

- more often applied to animals than human.

- chemotherapy drugs to treat somecancers particularly ovarian cancer.


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IP injection


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Intradermal (into the skin)

- inject into the very top layer of the skin.

- effects are generally local, not systemic.

- forms a blister-like area.

- used for diagnostic reason or immunization,eg. BCG vaccine


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Intradermal injection


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Quicker onset of action.

Difficult for self-administration, require skilledpersonnel.

Emergency situations.

Must be sterile (bacteria free).

May cause pain, fear & infections.

Advantages & disadvantages of parenteraladministration

T i l d i i t ti


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Intranasal (into the nose)

- decongestant nasal spray

Eye drops (onto the conjunctiva)

- antibiotics for conjunctivitis

Ear drops

- antibiotics / corticosteroids

Inhalation

- asthma medications

Epicutaneous (application onto the skin)

- cream for treatment of dermatologic condition

Topical administration


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Miscellaneous administration

Epidural (injection or infusion into the epidural space)

- epidural anesthesia (during labour)

Transdermal (diffusion through the intact skin)

- administered through a bandage or patchsystem.

- estrogen skin patches in HRT

Intracisternal (given between the first and secondcervical vertebrae)

- used to withdraw cerebrospinal fluid for

diagnostic purposes.


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Epidural injection /infusion

Estrogen skin patch

Onset of action


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Route Onset of action Examples

Oral (PO) 30-60 min Most medicines

Sublingual (SL) Several min Nitroglycerin

Buccal Several min Androgenic drugs

Rectal 15-30 min Analgesics, laxative

Subcutaneous (SC) Several min Insulin

Intramuscular (IM) Several min Antibiotics

Intravenous (IV) Within 1 min IV fluids, antibiotics

Intraarterial Within 1 min Cancer drugs

Inhalation Within 1 min Antiasthmatic drugs

Topical Within 1 hour Creams, oinments

Vaginal 15-30 min Suppositories

Onset of action


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2 formulation administration of drugs zumiey

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