Lecture 5: Dosage forms 1

1-What is dosage form?

-Dosage Form: The physical form in which a drug is produced for
administration to the recipient.
-"drug delivery system" -a modern term used in place of ''conventional
dosage forms'' to describe a system for carrying a drug into the body.
Refers to both the construct of the drug, its delivery vehicle, and its
method of administration
-The physical form of the oral dosage form will influence absorption
rate and onset of action. E.g., oral solutions absorbed faster than
tablets and so act quicker.
-Range of dosage forms for the same route of administration to
optimise the delivery of the API.

What are the dosage forms available for different administration routes?

-Same drug maybe presented in several different dosage forms and strengths to
meet specific needs of user, e.g., Paracetamol available as tablets, dispersible
tablets, paediatric soluble tablet, paediatric oral solution, sugar free oral solution, oral
suspension and suppositories.
-Most acceptable formulation should be given to patient with consideration of the
clinical indication being treated and patient factors.
-Dosage form consists of active ingredients plus inert excipients (inactive
component). Can you give some examples!
2-What are the different types of oral route dosage form?

1-Tablets
-are solid preparations prepared by compression.
-Oral delivery is the most popular route of drug administration, among oral dosage
forms tablets is the most common form.
-Tablet is originated from the Latin (tabuletta) which means disc-like or cylindrical.
-The Latin name of tablet in the pharmacopeia is compressi reflect that tablet
manufacturing is dominated by powder compression.
-Tablets can also prepared by moulding and freeze drying (lyophilisation).
-European pharmacopeias define tablets as solid preparations each containing
single dose of one or more active substance.
-Each containing single dose of one or more active ingredients.
-Wide variety of shapes, sizes and surface markings

Besides the active ingredients, what are the other excipient added to ensure
the obtained tablets?

What are the different tablet presses?

1-Single-punch press:
 One pair of punches and one die.
 Die is filled with powder by gravity when hopper shoe is over the ide.
 Upper punch moves down and compress the powder
 Production of small batches, 200 tablets/minute

2-Rotary press:
 3-60 dies and set of punches
 10 000 tablets/minute

3-Hydraulic press

What are the different types of tablets?

-Immediate Release: designed to disintegrate when swallowed, dissolve and be
absorbed. No special coatings or formulation techniques to control the release of the
drug.
-Delayed Release:(m/r or sr)-designed to release the drug after a time lag, or slowly
for a prolonged drug release or sustained drug action. Must be “Swallowed whole,
not chewed.”
-Effervescent: dissolved in water before administration, solution is usually a
flavoured bubbling drink.
- Soluble/Dispersible: Dissolved in water, ease of swallowing
- Chewable: - produce pleasant tasting residue in the mouth when chewed, no bitter
or unpleasant after taste.
-Buccal or Sublingual - small and flat. Not to be swallowed whole. Counsel patient
on how to use.
-Sugar coated or film coated – coat protects tablet from environmental damage, to
mask an unpleasant drug taste, aid identification of tablet, enhance its appearance.
-Enteric coated- protects drug from the acid conditions of the stomach. Prevent
tablet from dissolving until reaches the small intestine.
Advisory labels are “Swallowed whole, not chewed.” Also “Do not take indigestion
remedies at the same time of day as this medicine.” Such as omeprazole
-Lozenges- drug incorporated in flavoured base. Dissolve or disintegrate slowly in
mouth, releasing medication generally for localized effect e.g. antiseptics for sore
throat. Also get lozenges that produce systemic effect e.g., nicotine lozenges.
-Pastilles - glycerol and gelatine base. Sweetened, flavoured and medicated.
Sucked, very popular for soothing coughs/sore throats.

What are Capsules?

 Made with hard or soft gelatine shell of various sizes.
 Drugs enclosed within gelatine container
 When swallowed gelatine shell dissolved by gastrointestinal fluids releasing
contents
What are soft gelatine capsules?
One-piece capsules containing a liquid or semi solid fill ex: cod liver oil

What are hard gelatine capsules?

Two-piece capsules shells filled with powders, pellets, semi-solids or
liquids.

There are various types of Capsules ex; Capsules delayed release pellets, inhaler.

What is the method of making capsules?

What is the difference between granules and powder?
-A powder are fine particles to which any dry substance reduced by pounding,
grinding whereas granules are tiny grain, small particles.

Oral Powders and Granules:

Powders for oral administration consist of active ingredient with excipients (diluents,
sweeteners, dispersing agents)
• Bulk powders (Undivided powders) - useful for non-potent bulky drugs with large
dose e.g. antacids Magnesium Trisilicate Powder, Compound BP
• Individually wrapped doses (Divided powders) - useful for potent drugs, accuracy of
dose is important. E.g., dioralyte sachets mixed with water before taking
• Granules/powders -for reconstitution before dispensing e.g., antibiotic
suspensions
• Effervescent granules - masks taste of salty or bitter medications

What are the advantages of Powder/Granules?

Solid preparations are more stable than liquid preparations. The shelf life of
powders for antibiotic syrups, for example is 2 to 3 years but once reconstituted with
water it is 1 to 2 weeks.
• Powders and granules are convenient forms in which to dispense drugs with a
large dose. For example if the dose of a drug is 1 to 5 g it is not feasible to
manufacture tablets to supply the drug to the patient.
• Orally administered powders and granules which are mixed with water prior to
taking are useful for patients who have difficulty swallowing tabs/caps (e.g. children)
or where rapid absorption of the drug is required (e.g. rehydration sachets)

What are the disadvantages of Powders/Granules?

Bulk powders or granules are less convenient to carry than a small container of
tabs/caps.
• Masking of unpleasant taste maybe a problem with this type of preparation.
• Bulk powders or granules are not good method of administering potent drugs with
low dose.
• Powders and granules are not a suitable method of administration of drugs that are
inactivated in the stomach. (Should be enteric coated tabs)

Solutions:
What are Solutions?
Oral solutions contain one or more ingredients dissolved in a suitable vehicle, usually
solids dissolved in liquids.

What are the different types of pharmaceutical solution used orally?

• Syrups - a concentrated, viscous solution containing one or more sugar
components, chiefly sucrose.
• Elixirs - usually contain potent or unpleasant tasting drugs. The formulation is
clear, generally contains a high proportion of sugar or sweetening agent to mask
nauseating tastes. Generally non aqueous solvents (e.g. alcohol, glycerine ) form a
significant proportion of the vehicle.
• Linctuses - viscous liquids used in treatments of cough. Should be sipped and
swallowed slowly and allowed to trickle down the throat in an undiluted form.
Contains sugar e.g., simple linctus.
• Mixtures - term used to describe pharmaceutical oral solutions and suspensions
e.g., chloral hydrate mixture

What are the advantages of solution?

• Absorption of the medicine from the GI tract is rapid
• Easy to swallow for children and some adults esp. the elderly
• Uniform distribution of medicament, no need to shake
• Flexible dosing is possible

What are the disadvantages of solutions?

• Medicaments are less stable in solution than in a dry dosage form
• Unpleasant flavours maybe difficult to mask
• Bulky to carry around
• Vulnerable to loss by breakage of container
• A means of measuring the dose is required
• Measurement depends on the accuracy and reliability of the patient

What are Suspensions?

A disperse system in which one substance (the disperse phase) is distributed in
particulate form throughout another (the continuous phase)
•In a suspension at least one of the ingredients is not dissolved in a vehicle.
• Useful way of administering large amounts of drug which would be inconvenient to
take in capsule or tablet form.

What do you need to do before administration?

The preparation will require shaking before a dose is administered

What are the advantages of suspensions?

insoluble drugs maybe more palatable, absorption will be quicker than solid dosage
forms.
What are the disadvantages of suspension?
preparation requires shaking before use, accuracy of dose likely to be less than
equivalent solution.

Emulsions:
Describe preparations intended for internal use via oral route
-Emulsions for external use are given different title that reflects their use ex: lotion

What are Emulsions?

-Emulsions are liquid preparation containing a mixture of oil and water.

What do emulsifying agents ensure?

Emulsifying agent ensures that the oil phase is finely dispersed throughout the water
as minute globules. Emulsifier arranges at the interface, anchoring its hydrophilic
part into water and its lipophilic part into oil

What do termed oil in water emulsion mean?

Oily phase (disperse phase) is dispersed through the aqueous phase (continuous
phase).

Oral doses emulsions are generally what type of emulsions?

Oral dose emulsions tend to be oil in water

-Convenient for administering oils and fats or oily solutions of unpalatable drugs of
low aqueous solubility.
-e.g., cod liver oil emulsion, liquid paraffin oral emulsion
-Must be shaken well prior to measuring a dose.

Illustration of an oil in water emulsion?

• Water is continuous phase
• Oil is disperse phase
• Emulsifying agent ensures that the oil phase is finely
distributed throughout the water as minute globules.

Which ONE of the following has the highest bioavailability?

A. Oral capsules
B. Oral tablets
C. Oral suspensions
D. Oral solutions X
E. Oral emulsions

Ear drops:
How are ear drops presented?
As a solution or suspension
What are the vehicles that may be used?
 Water
 Glycerol and propylene glycol may also be used

Why is it designed for?

-Designed to exert local effect in the ear, to soften wax (Almond oil or Olive oil)
-To treat local inflammation and infection, or to relieve pain

-Drops are inserted in the ear, using a dropper

What are the different dosage forms for the eye?

-Eye drops- Sterile solutions or suspensions of one or
more medicaments. Drops can be supplied in single or multiple dose
containers.
Eye lotions- sterile aqueous solutions used usually undiluted
for bathing the eye.
Eye ointments - sterile applied to the eyelid margin/eye.

Why do apply eye ointments in bedtime?

Eye ointments contain paraffins for dry eyes. It is best applied at nigh to relieve eye
dryness and irritation and your vision may become blurred for a short while after usin
the ointment.