Munson Lectures Flashcards
Routes of Administration
Ophthalmic
Otic
Nasal
Oral
Sublingual
IM
SubQ
IV
Topical
Rectal
Urethral
Vaginal
Percentages of Routes of Administration
Oral - 47%
Parenteral - 18%
Pulmonary - 16%
Transdermal - 11%
Tablets/Capsules
- stable
- accurate dose
- easy to use
- lower cost
- taste mask and controlled release
Disadvantage:
- not suitable for infants
- not suitable for non-oral medications
IV
- fast drug action
- suitable for drugs who can’t tolerate GI movement
- suitable for patients unable to swallow
Disadvantage:
- expensive
- not convenient
- painful at times
Transdermal
local treatment
Intranasal Spray
- local treatment
- systemic drug delivery
How to Choose?
dictated by disease state, convenience, and marketing
Types of Solid Dosage Forms
- tablets
- gelcaps
- loose powders
- lyophilized powder
- controlled release
Types of Tablets
- Compressed (uncoated or sugar coated)
- film coated
- enteric coated
- layered
- chewable
- tablet for solution
- effervescent
- dispensing
Advantages of Tablet to Manufacturer
- simplicity and economic for preparation
- stability
- convenience for packaging
- shipping/ dispensing was easy
- accuracy of dosing
- compactness
- portability
Advantages of Tablets for Patient
- accuracy of dosing
- compactness
- portability
- blandness of taste
- easy administration
Sugar-Coated Tablets
- formed by compression
- used for taste masking or identification
- enhance stability
Process of Sugar Coated Tablet
- sealing coat
- subcoat to interface between sealing and main coat
- apply multicoat of starch, calcium carbonate, etc
Film-Coated Tablets
- avoid use of moisture and water
- place markings on tablets
- polymeric
- add colorant
- unique properties pertaining to release
Multiple Compression Tablet
- inner core and a coating
- inner core was a sugar tablet
Multiple Layer Tablet
- lightly compress one layer
- then add another layer
- used for different types of release
Enteric-Coated Tablet
- resist dissolving in stomach pH but dissolved in higher pH
- used in drugs than can irritate stomach
- CANNOT BE CRUSHED OR CHEWED
Chewable Tablets
- help solubility
- avoid swallowing problems
- no disintegrant
- mannitol filler is common
Effervescent Tablet
- dissolve in glass of water prior to administration
- release carbon dioxide
- facilitates fast action
- must be avoided from moisture so placed in blister packs
Hard Gelatin Capsule
- used in most capsules
- made from collagen
Manufacturing
- snap together or heat sealed
Soft Gelatin Capsule
- added softening agent
- used for liquids, suspensions, pastes
- made from collagen
Manufacturing
- used two ribbons
Difference between Solid vs Solution
Solid
- slow acting
- more stable
- more convenient
- common for oral
Solution
- faster acting
- less stable
- for injections commonly
Preformulation of Dosage Form
determining the physiochemical properties necessary to formulate compound
Formulation of Dosage Form
determining the route and composition of final dosage form
Manufacturing of Dosage Form
what unit operations are necessary
Solubility
maximum amount of solute that can be dissolved in a given amount of solvent
mostly a low solubility
3 States
Completely Soluble
Supersaturated
Very supersaturated
high levels of supersaturation will cause crystallization
Physical Stability
- transformation to different crystal forms
crystalline to amorphous, hydrates, solvates, etc
Chemical Stability
- chemical reaction involved
- results in degradation product that must be characterized
Types of Chemical Reactions
Hydrolysis
Oxidation
Photolysis
Dehydration
Why can’t we administer drug substance?
- unstable
- taste masking needed
- hard to administer
How to make a stable dosage form that is easy to administer?
Add other ingredients that help stabilize the dosage form —> excipients
Types of Excipients
- Diluent
- Disintegrant
- Binder
- Lubricant
- Glidant
- Controlled Release
Diluent
- referred to ask bulking agent
- needed to make the practical weight for tablet
- helps in the composition
- enhances powder flow in manufacturing
Examples of Diluents
Microcrystalline cellulose
Lactose
Calcium Phosphate
Starch
Disintegrant
- breaks up the solid dosage form enhancing dissolution
- performed by water uptake or swelling
Examples of Disintegrants
Sodium Starch Glycolate
Croscarmellose
Crospovidone
Starch
Binders
- gives tablet the mechanical strength
- performed by water uptake or swelling
Example of Binders
Polyvinyloyrrolidone
Starch
Microcrystalline cellulose
Polymer
Lubricant
- prevents adherence of tablet to the die
- levels of 0.5-2%
- overlubrication is bad
Example of Lubricant
Magnesium Stearate
Stearin Acid
Lubritab
Talc
Glidant
- improves powder flow
- stops friction
- very fluffy
Example of Glidant
Silica
Talc
Controlled Release
- used to extend the release of the drug from matrix
- can be used to coat a tablet for specific release in body
Example of Controlled Release
Hydroxypropylmethylcellulose
Xanthan gum
Eudragits
Coloring Agent
- improve esthetics
- identification technique
- control product
MUST BE APPROVED BY FDA
What is needed to be known about the drug?
Physiochemical properties
Mechanical properties
Bio pharmaceutical properties
Physical and Chemical Properties
Aqueous Solubility
- concentration at which the solution is in equilibrium with solid phase
- depends on temperature and pressure
- key to bioavailability
Dissolution Rate
- determines how quickly drug goes into solution
- can be enhanced by fast moving agents
- important for in vivo
Ionization Constant
- protonated or unprotonated?
Polymorphism
- ability for molecule to adopt two or more conformations of molecules in crystal
- can effect bioavailability
- can have multiple crystalline forms
Amorphous
- unstable and wants to crystallize
- enhanced bioavailability
- enhanced solubility
Hydroscopicity
- amount of water taken up by solid
- can effect stability and manufacturing
Mechanical Properties
Compression and Compaction
- Elastic: reversible and deforms
- Plastic: irreversible and deforms
- Fracture: material breaks
Manufacturing Unit Operations
Weighing
Blending
Milling
Granulation
Drying
Compaction
Coating
Packaging
