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What is an excipient
Inactive ingredient
Physical Dosage Forms
Solid, semi-solid, liquid, gas
‘pessary’
a solid dosage form intended for vaginal administration
‘suppository’
dosage form intended for application within the rectum
Particle properties
physical dimensions/size, shape, surface area, and physical state
How to define spherical particles
diameter
How to define non-spherical particles
dimensions, diameter d of a sphere that occupies the same volume as irregularly shaped particle
Monodispersed particles
all particles are the exact same size→ small polydispersity index (<0.1) ex: coronavirus
Polydispersed particles
particles are different sizes→ large polydispersity index
Tyler mesh size
the number of openings per inch of mesh, the larger the mesh number, the smaller the opening
Surface are of a spherical particle
pi*d², when diameter decreases 2 times, the surface area of each particle decreases 4 times. The combined surface area for the same weight of powder increases 2 fold
True density
density without consideration of voids. ex: gold bar, density= m/v
Bulk density
have to consider interparticle and intraparticle volumes that add to the volume. ex: flour has a higher bulk density that grains or bread
Porosity
the fraction of void volume (air) in a powder material, e= 1- Pbulk/Ptrue, ex: bread has higher porosity than flour or grains
What happens when you reduce particle size
you increase the total surface area
Wettability
Ability to absorb water
What does a high or low angle of repose mean?
Higher→ wants to stay as a droplet, low wetability
Lower→ wants to spread, high wetability
What does high surface tension mean?
High surface tension→ large contact angle of repose → low wettability
What does a low surface tension mean?
Low surface tension→ small contact angle→ high wettability
What do wetting agents do? what are some common ones?
Decrease surface tension, decrease contact angle, and increase wettability. Glycerol, ethanol, surfactants
What is flowability?
Cohesive properties of power. A low AOR= more flowability, A high AOR= less flowability
How do you improve the flowability of a powder?
Increase the particle size because there’s a larger combined particle surface area. Ex: powdered sugar has a larger AD than granulated sugar
Why is blending important?
Ensures the uniformity, consistency, and efficacy of the final product. Poor blending can lead to dose variability and reduced drug potency
What is trituration?
Continuous rubbing/grinding with a mortar and pestle, useful for hard powders, tablets
What is pulverization by intervention?
Dissolve in “intervening” solvent (alocohol, acetone)
Mix in mortar or spread on an ointment slab
The solvent evaporates
Used for hard, crystalline powders that do not easily triturate and gummy substances
What is levigation?
Uses a small amount of solvent in which the particles are insoluble, then triturate, useful for ointments and suspensions
When do you use direct blending?
When the fraction x of powder A is >10%
When do you use geometrical dilution?
When fraction x of A is <10%
Capsules
Solid dosage forms in which a drug substance is enclosed in a hard/soft soluble container/shell
Advantages of Capsules
easily filled, tastless, easily administered, dose can be individualized, preferred in early-stage clinical trials, 44% of consumers prefer capsules over tabs
Diluent
(inert substance), added to increase the bulk weight of a powder in a capsule