DRUG FORMULATIONS & ROUTES OF DRUG ADMINISTRATION

Dr. Wan Ezumi Mohd Fuad PPSK

Drug Formulations
The process in which different chemical substances, including the active drug are combined to produce a final medicinal product.

History

During Linnaeus time, there were some forms of drugs that we seldom use today, eg: - decoction (a plant is boiled in water) - infusions (the same method as we use when making tea) - tinctures (extracts made with alcohol)

Drug Forms

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.

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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 as prescribed.

Drug forms

Aqueous / liquid preparations

Alcoholic preparations

Solid & semi-solid preparations

Common drug forms and preparations

Aqueous preparations

Syrups - a solution of water & sugar to which drug is added. Addition of flavoring agents eliminates the bitter taste of many drugs.

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-volatile substance.

Dissolved in various concentrations of alcohol.

Solid and semisolid preparations

A number of different kinds for different purposes are available:Powders drug / drug extracts that are dried & ground into fine particles. for dermatologic use (talcum).

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Tablets drugs extracts that have been compressed into a convenient form. most commonly used solid dosage form. easy to swallow. they usually disintegrate in the stomach more rapidly than most other solid preparations. low cost.

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

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Capsules drug powders or liquid, enclosed in gelatin capsules (hard / soft). easier to swallow than tablets. gelatin capsules dissolve in the stomach, thereby releasing the drug.

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Delayed-release products Usually tablets / capsules that are treated with special coatings. so that various portions of the drug will dissolve at different rates. designed to produce drug effects over an extended time. reduce the frequency of dosing.

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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 an acid-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 parenteral administration is impractible. include powder, creams, gel, paste, ointment.

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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 inserted into a body orifice:* rectum * vagina * urethra drugs mixed with a substance (cacao butter) melt at body temperature. for local effects (vagina, urethra) and system effects (rectum).

Suppositories

Routes of administration

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

Depending on the route, the drug could be absorbed & distributed in a matter of minutes, days, months. How to select a particular route or dosage forms of drugs??? - depending on what type of effect is desired..

Local or systemic effects???

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.

Routes of drug administration

ROUTES OF ADMINISTRATION

ENTERAL ADMINISTRATION

PARENTERAL ADMINISTRATION

TOPICAL ADMINISTRATION

Enteral administration

Any form of administration that involves any part of the 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 through mucosal surface

Advantages & disadvantages of enteral administration

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

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 with needles (by injection or infusion). Desired effects is systemic.

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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

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IV injection

IV infusion

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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

Intraarterial injection

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Intramuscular (IM) injection (into a muscle) - into the muscle fibers (under the subcutaneous layer of skin) - principle sites: gluteal (buttock), deltoid (upper arm) & vastus lateralis (thigh) muscles - more painful than other routes - many vaccines, antibiotics

IM injection

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Subcutaneous (SC) (under the skin) - used for both for short term & very long therapies. - sites: lower abdomen, front of thigh, upper back and back of upper arm. - insulin.

SC injection

Intraperitoneal (IP) (injection into the peritoneam) - more often applied to animals than human. - chemotherapy drugs to treat some cancers particularly ovarian cancer.

IP injection

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

Intradermal injection

Advantages & disadvantages of parenteral administration

Quicker onset of action. Difficult for self-administration, require skilled personnel. Emergency situations. Must be sterile (bacteria free). May cause pain, fear & infections.

Topical administration

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

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 patch system. - estrogen skin patches in HRT Intracisternal (given between the first and second cervical vertebrae) - used to withdraw cerebrospinal fluid for diagnostic purposes.

Epidural injection / infusion

Estrogen skin patch

Onset of action
Route
Oral (PO) Sublingual (SL) Buccal Rectal Subcutaneous (SC) Intramuscular (IM) Intravenous (IV) Intraarterial Inhalation Topical Vaginal

Onset of action
30-60 min Several min Several min 15-30 min Several min Several min Within 1 min Within 1 min Within 1 min Within 1 hour 15-30 min

Examples
Most medicines Nitroglycerin Androgenic drugs Analgesics, laxative Insulin Antibiotics IV fluids, antibiotics Cancer drugs Antiasthmatic drugs Creams, oinments Suppositories