Course Title: PHAR1035
Subject: Dosage Forms
Instructor: Katherine Baverstock
After completing this lecture, you should be able to:
Define what a medicine is and understand its main components.
Explain why active pharmaceutical ingredients (APIs) are rarely used alone for administration to patients.
Outline the main functions of excipients during pharmaceutical formulation.
Recognize some commonly used types of excipients.
Define what dosage forms are and describe the benefits of various dosage forms.
Describe the two main ways dosage forms are categorized.
Recognize different types of dosage forms: solid, semi-solid, and liquid.
Compare and contrast the uses, advantages, and disadvantages of different dosage forms.
A medicine consists of:
Active Ingredient: therapeutic molecule providing pharmacological effect.
Drug Delivery System: made of non-medicinal, inactive ingredients.
Roles of inactive ingredients include:
Assisting in the manufacturing process
Delivering the therapeutic molecule to the target site
Ensuring dosage accuracy, especially for small doses
Stabilizing the medicine
Improving convenience for administration
Active pharmaceutical ingredients (APIs) are rarely used alone due to:
Potency requiring very small quantities which can be unsafe from bulk material
Unpleasant smell or taste of some APIs
Chemical instability when exposed to unfavorable conditions (light, moisture, air)
Breakdown before reaching absorption site (e.g., acidic stomach environment)
Excipients are inactive ingredients that:
Have no pharmacological activity in the body
Serve as carriers for APIs
Act as manufacturing adjuvants
Regulate API release
Selection of excipients is based on:
API's chemical stability
Required manufacturing processes
Body's metabolism of the API
Fillers/Diluents: enhance size of tablets/capsules
Binders: hold ingredients together in tablets
Lubricants: prevent adherence to machinery
Glidants: improve powder flow during manufacturing
Coatings: improve appearance and protect ingredients
Disintegrants: ensure breakdown in GI tract
Preservatives: extend shelf life
Flavours/Sweeteners: mask unpleasant tastes
Colours: enhance aesthetic appeal
Definition: Physical form of a pharmaceutical product containing an API and excipients intended for patient administration.
Dosage forms are categorized to deliver APIs to specific body areas.
Area of study related to dosage forms: Pharmaceutics
Advantages include:
Accurate dosing and convenience without the need for measuring
Protection of APIs from environmental factors
Taste and odour masking
Allow targeted/localized delivery
Modify release profiles for sustained action
Tailor formulations to maximize benefits and minimize side effects
Categorized by:
Physical Form: solids, semi-solids, liquids, gases
Route of Administration: multiple dosage forms can be used per route (oral, topical, inhaled, ophthalmic, otic, rectal, vaginal, parenteral)
Solids: e.g., tablets
Semi-solids: e.g., creams
Liquids: e.g., suspensions
Gases: e.g., inhalers
Tablets:
Most common, compact, and long shelf-life
Can include excipients for lubrication, disintegration, and taste masking
Disadvantages: local irritation, first pass metabolism impacts absorption, not viable for unconscious patients
Sublingual and Buccal Tablets:
Dissolved in the mouth for rapid absorption; bypass stomach acid
Examples: angina treatments, nicotine therapy
Disadvantages: potential for oral irritation; not all drugs suitable for this route
Chewable Tablets:
Designed for easy ingestion; good for those who struggle with swallowing
Examples: vitamins, antacids
Disadvantages: taste issues; risk of mistaken use for non-chewable tablets
Capsules:
Easier to swallow, available in hard or soft shells
Excellent for taste masking or sustained release
Challenges in manufacturing
Effervescent Tablets:
Dissolve in liquid before consumption; rapid onset of action
Disadvantages: larger size; complex manufacturing processes
Lozenges:
Slow-dissolving for prolonged local effect; used for throat issues
Powders:
Dry mixtures either for internal (to dissolve) or external use (dusting)
Include bulk powders and divided doses for unique needs.
Creams:
Emulsions for skin or mucous membranes; contain both oil and water phases
Advantages: localized effects, reduced systemic side effects
Disadvantages: local irritation, limited dose accuracy, storage challenges
Ointments:
Greasy base with active ingredient for serious skin conditions
Not suitable for face; sticky texture
Gels:
Water-based for applying soluble ingredients
Suppositories:
Inserted rectally; melts at body temp for local/systemic effects
Advantages include systemic absorption without stomach inactivation
Disadvantages: inconvenient, local irritation, slow onset
Pessaries:
Similar to suppositories but for vaginal insertion; distinctive shape and larger size for treatment.
Liquid dosage forms for various administration routes; can be orally, topically, or injected
Advantages include:
Aid for swallowing difficulties, faster absorption, tailored doses
Disadvantages include:
Shorter shelf-life, requires measurement for dosing, may need special storage
Simple Solutions:
Clear mixtures of active ingredients in solvent
Linctus:
Viscous for cough relief; sweet but limited in diabetic conditions
Suspensions:
Cloudy mixtures of insoluble particles; require shaking before use.
Examples: antibiotics, analgesics
Lotions:
Thin applications for skin, either suspensions or creams.