Drug formulations are products designed for administering a drug to a patient.

Each active
ingredient is combined with other substances like excipients, diluents, and preservatives and
then packaged into a specific dosage form. This form gives the drug body, defines single doses,
protects active ingredients, and facilitates various administration methods.

The choice of an appropriate route of administration depends on both drug-related and

Here is a point-wise explanation of various drug formulations and administration routes:

1. Local Routes of Administration This is the simplest way to administer a drug directly to the
site where its action is required, thereby minimising systemic side effects.

● Topical Application: The drug is applied to the skin or mucous membranes for localised
action.
○ Examples:
■ Oral cavity: Nystatin suspension or clotrimazole troche for oral
candidiasis; acyclovir cream for herpes labialis; lignocaine hydrochloride
ointment or spray for topical anaesthesia.
■ Eyes: Eye drops or ointments for local infections or inflammation, such as
phenylephrine eye drops. These should be sterile and isotonic.
■ Nose: Nasal decongestants like phenylephrine in sprays or drops.
■ Ears: Ear drops for local infections or inflammation.
■ Skin: Calamine lotion for soothing or cooling effects; neomycin
ointment for skin infections; ketoconazole cream for fungal infections;
diclofenac gel for pain.
■ Vagina: Pessaries for vaginal infections; oestrogen cream.
■ Rectum: Suppositories for local effects like in anorectal lesions (e.g.,
benzocaine suppository), or methylprednisolone enema in ulcerative
colitis.
■ Urethra: Bougies for local effects.
● Administration into Deeper Tissues (Local Injection): The drug is injected directly
into a specific tissue or joint for localised effects.
○ Examples: Triamcinolone directly into a joint space for rheumatoid arthritis.
● Close Intra-Arterial Injection: Used to localise the effect of a drug, such as contrast
media in angiography, or anticancer drugs for limb malignancies.

2. Systemic Routes of Administration Drugs administered via systemic routes are absorbed
into the bloodstream and distributed throughout the body to the site of action via circulation.

2.1. Enteral Routes Drugs are administered by mouth (ingestion), sublingually, or rectally.
● Oral Route: The most common, convenient, and economical method of drug
administration.
○ Advantages:
■ Safer and cheaper.
■ Convenient for repeated and prolonged use.
■ Self-administered.
■ Toxicities or overdose can often be overcome with antidotes (e.g.,
activated charcoal).
○ Disadvantages:
■ Slower onset of action, making it unsuitable for emergencies.
■ Not suitable for unpalatable or highly irritant drugs (though capsules
can help).
■ May cause nausea and vomiting.
■ Cannot be used for uncooperative, unconscious, or vomiting patients.
■ Absorption can be variable and erratic.
■ Some drugs are not absorbed (e.g., streptomycin) or are destroyed by
digestive juices (e.g., penicillin G, insulin) or undergo extensive
first-pass metabolism in the liver (e.g., GTN, lidocaine).
○ Examples of Oral Dosage Forms:
■ Powders: Dry, finely pulverised. Often inconvenient unless large
quantities (e.g., oral rehydration salts). Effervescent powders contain
granulated sodium bicarbonate and acid, releasing CO2 in water.
■ Tablets: Compressed or moulded forms.
■ Plain, sugar-coated, or film-coated for swallowing.
■ Chewable tablets (e.g., albendazole, chewable antacid).
■ Dispersible tablets (e.g., aspirin).
■ Mouth-dissolving tablets (e.g., ondansetron).
■ Sustained-release (SR) / Extended-release (ER) /
Controlled-release preparations: Have special coatings or
membranes to control drug release, allowing slower absorption
and prolonged action, reducing dosing frequency and maintaining
stable plasma levels (e.g., SR cap. Theophylline, diclofenac
sustained release tablet, oral morphine ER tablets). These
should not be crushed.
■ Enteric-coated tablets: Protect the drug from stomach acid,
delivering it to the less acidic intestine (e.g., omeprazole,
erythromycin, aspirin, diclofenac). These should not be
crushed.
■ Pills: An archaic form where drug powder is mixed with honey/syrup and
rolled into bodies for swallowing.
■ Lozenges: Designed to dissolve slowly in the mouth for local action (e.g.,
for stomatitis, sore throat, clotrimazole for oral candidiasis).
■ Capsules: Have a soft or hard shell (e.g., omeprazole capsule). Should
not be divided.
 ■ Liquid Forms:
■ Aqueous solutions: Drug dissolved in water; often with
sweetening, flavouring, and preservatives (e.g., paracetamol
syrup).
■ Suspensions: Insoluble drugs dispersed in water with a
suspending agent; must be shaken before use (e.g., antacid
suspension, nystatin suspension).
■ Emulsions: Uniform mixtures of two immiscible liquids (e.g., oil
and water) with an emulsifying agent; must be shaken before use
(e.g., cod liver oil emulsion).
■ Mixture: Liquid containing two or more ingredients for oral use
(e.g., gripe water mixture, carminative mixture).
■ Syrup: Concentrated sugar solution with drug to mask bitter taste
(e.g., cough syrup).
■ Elixir: Clear, flavoured liquid with drug dissolved in water and
alcohol (e.g., promethazine elixir).
■ Linctus: Viscous liquid for cough relief (e.g., linctus codeine).
● Sublingual (s.l.) / Buccal Route: Tablet or pellet placed under the tongue or crushed in
the mouth and spread over the buccal mucosa.
○ Advantages:
■ Rapid absorption and quick onset of action.
■ Bypasses first-pass metabolism in the liver, as drugs are absorbed
directly into systemic circulation.
■ Action can be terminated by spitting out the drug.
■ Self-administration is possible.
■ Avoids destruction in the GI environment.
○ Disadvantages:
■ Not suitable for irritant and lipid-insoluble drugs.
■ Not suitable for drugs with a bad taste.
■ Somewhat inconvenient.
○ Examples: Glyceryl trinitrate (GTN) for angina, buprenorphine,
desamino-oxytocin.
● Rectal Route (for Systemic Effect): Drugs given as suppositories or enemas.
○ Advantages:
■ Partially bypasses first-pass metabolism (50% of drainage bypasses
portal circulation).
■ Prevents drug destruction in the GI environment.
■ Useful if the drug induces vomiting, if the patient is already vomiting, or if
the patient is unconscious.
○ Disadvantages:
■ Absorption is often erratic and incomplete.
■ Many drugs can irritate the rectal mucosa.
○ Examples: Indomethacin for rheumatoid arthritis; diazepam for status
epilepticus in children.
2.2. Parenteral Routes Involves administration by injection, taking the drug directly into tissue
fluid or blood, bypassing the enteral mucosa.

● Advantages:
○ Faster and surer drug action, valuable in emergencies.
○ Gastric irritation and vomiting are not provoked.
○ Can be used in unconscious, uncooperative, or vomiting patients.
○ No interference by food or digestive juices.
○ Liver is bypassed, avoiding first-pass metabolism.
○ Suitable for irritant drugs.
○ Suitable for drugs with high first-pass metabolism.
○ Suitable for drugs not absorbed orally.
● Disadvantages:
○ Preparations must be sterilised and are costlier.
○ Technique is invasive and painful.
○ Requires assistance (though self-injection is possible for some drugs).
○ Chances of local tissue injury (e.g., to nerves, vessels).
○ Generally more risky than oral administration.
● Intradermal (i.d.) Route: Injection into the layers of the skin (dermis).
○ Disadvantages: Painful, only small amounts can be administered.
○ Examples: BCG vaccination, drug sensitivity tests.
● Subcutaneous (s.c.) Route: Drug deposited in the loose subcutaneous tissue.
○ Advantages:
■ Self-administration is possible (e.g., insulin).
■ Depot preparations (e.g., NORPLANT for contraception, protamine zinc
insulin) can be inserted for prolonged action.
■ Provides constant, slow, and sustained effects.
■ Minimises risks of haemolysis or thrombosis associated with IV injection.
○ Disadvantages:
■ Only suitable for non-irritant drugs.
■ Absorption is slower than intramuscular, not suitable for emergencies.
■ Avoided in shock patients due to delayed absorption from
vasoconstriction.
■ Severe pain and necrosis may occur if irritant drugs are used.
○ Examples: Adrenaline, insulin.
● Intramuscular (i.m.) Route: Drug injected into large skeletal muscles (e.g., deltoid,
gluteus maximus).
○ Advantages:
■ Absorption is more rapid than oral.
■ Mild irritants, oily solutions, and aqueous suspensions (depot
preparations) can be injected.
■ Less painful than s.c. for some drugs.
○ Disadvantages:
■ Often impracticable for self-injection due to need for deep penetration.
 ■ Can produce local haematoma in anticoagulant-treated patients.
■ Aseptic conditions are needed.
■ Can be painful and may cause abscess.
■ Injury to nerves possible.
○ Examples: Paracetamol, diclofenac.
● Intravenous (i.v.) Route: Drug injected directly into the bloodstream via a superficial
vein.
○ Advantages:
■ 100% bioavailability.
■ Immediate effects, route of choice in emergencies (e.g., i.v. diazepam
for status epilepticus).
■ Maximum control over dose delivered.
■ Large volumes of fluid can be administered (e.g., i.v. fluids for severe
dehydration, dextrose normal saline).
■ Highly irritant drugs (e.g., anticancer drugs, sodium nitroprusside) can
be given as they get diluted in blood.
■ Hypertonic solutions (e.g., 20% mannitol in cerebral oedema) can be
infused.
■ Constant plasma level can be maintained via infusion (e.g., dopamine
infusion in cardiogenic shock).
■ Dose can be titrated with response for short-acting drugs (e.g., sodium
nitroprusside).
○ Disadvantages:
■ Most risky route; vital organs get exposed to high drug concentrations.
■ Irreversible; cannot be recalled.
■ Only aqueous solutions (not suspensions or oils) are suitable to avoid
embolism.
■ Can cause thrombophlebitis of injected vein and necrosis if
extravasation occurs.
■ Chances of air embolism.
■ No depot preparations for this route.
■ Requires strict aseptic conditions.
■ Usually not self-administered.
○ Examples: Administered as a bolus (e.g., i.v. ranitidine in bleeding peptic ulcer,
rocuronium); slow injection (e.g., i.v. morphine in myocardial infarction); or
infusion (e.g., dopamine infusion, mannitol infusion).
● Intrathecal / Intraventricular Route: Drug injected directly into the cerebrospinal fluid
(subarachnoid space).
○ Rationale: Bypasses the blood-brain barrier for local, rapid effects on the CNS.
○ Examples: Lignocaine for spinal anaesthesia; amphotericin B (antibiotics).

2.3. Inhalation Volatile liquids and gases are given by inhalation for systemic action, or
non-volatile liquids and fine particles are aerosolised for local or systemic effects via the
respiratory tract.
 ● Advantages:
○ Very rapid onset of action due to absorption from the vast surface of alveoli.
○ Controlled administration is possible with moment-to-moment adjustment, as
elimination is rapid in expired air.
○ Dose required is very less, minimising systemic toxicity.
○ Effective and convenient for respiratory disorders (e.g., asthma, COPD) as drug
is delivered directly to site of action, minimising systemic side effects.
● Disadvantages:
○ Irritant vapours can cause inflammation of the respiratory tract and increase
secretions.
○ Local irritation may cause bronchospasm.
○ Requires proper technique and coordination for some devices.
● Examples:
○ Gases or volatile liquids: General anaesthetics (e.g., nitrous oxide,
halothane, desflurane, sevoflurane).
○ Nonvolatile liquids and fine particle solids (Aerosols):
■ Pressurised Metered Dose Inhalers (PMDIs): Deliver a specified dose
per actuation (e.g., salbutamol PMDI). Spacer devices can improve
delivery.
■ Jet Nebulisers: Produce a mist from drug solution (e.g., salbutamol for
acute severe asthma). Preferred for severe episodes, children, and
elderly.
■ Rotahaler / Spinhaler: Portable devices for fine drug powder (e.g.,
salmeterol rotacap).
○ Inhalational steroids (e.g., fluticasone, beclomethasone, budesonide).

2.4. Nasal Route The mucous membrane of the nose can readily absorb many drugs,
bypassing digestive juices and the liver.

● Examples: GnRH agonists, calcitonin, and desmopressin applied as a spray or

2.5. Transdermal Route Achieves systemic effects by applying drugs to the skin, typically via a
transdermal patch or ointment.

● Advantages:
○ Self-administration is possible.
○ Better patient compliance.
○ Prolonged duration of action (1–3 days).
○ Provides smooth plasma concentrations without fluctuations.
○ Minimises inter-individual variations and side effects.
○ Bypasses first-pass metabolism.
● Disadvantages:
○ More expensive.
○ Local irritation and erythema (dermatitis and itching) can occur.
 ○ Patch may fall off unnoticed.
○ Rate of absorption can vary markedly.
● Examples: Transdermal patches of GTN, fentanyl, nicotine, and estradiol;
clonidine patch for hypertension.

2.6. Semisolid Dosage Forms (primarily for external application)

● Ointments: Greasy semisolid preparations for external application to skin, eye, nasal
mucosa, ear, or anal canal, with drug incorporated in an oily base (e.g., neomycin
ointment, 5% lignocaine hydrochloride ointment, nitroglycerin ointment). Not
suitable for oozing surfaces.
● Creams: Similar to ointments but with a water-in-oil emulsion base, allowing better
absorption and cosmetic acceptability (e.g., ketoconazole cream, clindamycin cream).
● Gels: Medicament in a viscous colloidal solution for external application, providing longer
contact; nongreasy and washable (e.g., diclofenac gel, lignocaine gel, povidone
iodine gel).
● Pastes: Semisolid preparations with a less greasy base, stiffer and more easily
washable than ointments (e.g., triamcinolone acetonide paste for oral inflammatory
lesions).

3. Special Drug Delivery Systems These systems are developed to prolong drug action,
achieve targeted delivery, or improve patient compliance.

● Ocusert: Placed beneath the lower eyelid, releases drug slowly for about a week (e.g.,
pilocarpine ocusert for glaucoma).
● Progestasert: An intrauterine contraceptive device that slowly releases progesterone for
a year.
● Liposomes: Minute phospholipid vesicles that encapsulate drugs for targeted delivery,
such as liposomal amphotericin B for fungal infections, reducing toxicity and achieving
targeted delivery to reticuloendothelial cells.
● Monoclonal Antibodies: Immunoglobulins produced by cell culture, selected to react
with specific antigens for targeted drug delivery (e.g., anticancer drugs using monoclonal
antibodies).
● Drug-Eluting Stents: Release drugs like paclitaxel in coronary angioplasty.
● Computerised, Miniature Pumps: For continuous subcutaneous delivery of drugs (e.g.,
insulin pump).