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What are the lifestyle advantages of using a tablet or a capsule?
They are easier to dose, transport, administer, and identify
What are the pharmaceutical advantages of using a table or a capsule?
They are easier and more efficient to manufacture, cheaper to produce, and they are more stable in the solid form
How long does it take for an immediate release drug to break apart and release drug?
15-30 minutes
When do we use hard gelatin in drugs?
They’re more useful in controlled release
What are gelatin capsule shells made of?
Collagen collected from denatured animal skin
What are some advantages of using a capsule over a tablet?
They have easier release & absorption, you can open the capsule and put in food, and easier to make
What type of drug is used in clinical trials, tablets, capsules, solutions, etc.?
Capsules because they are easier to make, have less effect on the outcome, and they can easily hide the active ingredient
Not all drugs can be put in a capsule, which ones?
The ones susceptible to moisture, interact with gelatin, or the ones that break down in moisture
Sometimes capsules have a liquid in them, what are the pros and cons of this compared to a solid filled capsule?
Pros: Better absorptions and content uniformity
Cons: Risk of interaction with the shell
In the context of capsules, what is the purpose of a diluent?
To fill up the volume inside the capsule and improve cohesion with the shell
In the context of capsules, what is the purpose of a disintegrant?
This is in charge of breaking up the contents and allows the drug to release once in the stomach
In the context of capsules, what is the purpose of lubricants or glidiants?
They increase the flow of the powder mix inside the capsule
In the context of capsules, what is the purpose of surface-active agents?
They are used as wetting agents because sometimes the excipients in a capsule are water insoluble and can reduce the dissolution of said capsule
What’s a bigger capsule? 000 or 00E
000 is the biggest, 00e, 00, 0, 1, 2, 3, 4, 5 are next
What method is used when manually compounding a small number of capsules?
The punching method
What is the time frame used in the disintegration test?
15-30 minutes
In terms of content uniformity, what range is allowed?
Between 85 to 115% of what the label claims with no units being outside the range of 70-125%
What is the USP rupture test?
It is done for soft gel capsules using water and a magnetic stirrer to see if the capsule ruptures within 15 minutes
What are the two different types of tablets?
Compressed Tablet: Dry powder is tightly compressed to form the tablet we think of
Molded Tablet: Made from moist material that is then dried, they are intended to rapidly dissolve
What type of drug is used for a molded tablet?
Very potent drugs
What are some disadvantages of using a tablet?
They have the slowest dissolution rate, hard for children to take, takes a lot to manufacture, some drugs are susceptible to pressure
What is a sugar coating?
It is intended to quickly dissolve but it is very difficult to make and expensive
When do we use enteric coating?
Typically for the delayed release drugs because they break down in the higher pH of the intestine
What is an effervescent tablet?
Think of an alkaline seltzer, they do not require a disintegrant because they’ll break up in water
What is the difference between hardness and friability?
Hardness: The amount of force needed to break the tablet
Friability: How likely the tablet is to lose small portions of the surface
What are the lubricating agents used for?
To prevent the tablets from sticking to the machine
What is the purpose of a modified release dosage form?
Alter the time, rate, or location of where a drug releases
Describe extended release?
The drug is release over a time frame and this reduces the dosing frequency
Describe delayed (sustained) release?
The drug will release at certain time or place, think enteric coating
Describe repeat action?
The drug will release at some time and it will release again at some other time
Describe targeted release?
The drug will release at the intended physiologic site of action
What’s the point go an extended release drug?
To be in the therapeutic range longer
Which one has more side effects, immediate release or extended release?
Immediate release, because extended release spends less time in the toxic range and the MEC range
What are some cons that come with extended release dosage forms?
Kinda difficult to adjust a dose, there is a risk for dose dumping, and it takes longer for the onset of action to occur
What kinda dose is common for extended release dosage forms?
The dose is relatively small
What kind of health condition is extended release used for?
Typically chronic
How does a compazine spansule work?
An initial dose is released promptly and the rest of the drug is released over a prolonged period
Should you take compazine and spansule with or without food?
Without food, taking with food decreases absorptions and decreases the Cmax
How does the controlled release of coreg work?
It is a hard gelatin capsule filled with both immediate and controlled release Microparticles containing a coating
What is a multi tablet system?
A compressed tablet continued both immediate and extended release drug and it is placed in a capsule
What is the commonly used rate controlling polymer?
Cellulose polymer
How is a drug released when it is granulated with an inert plastic polymer?
Slowly released by diffusion
What dosage forms can be seen with an ion exchange resin?
Tablets, capsules, or suspensions, they’ll interact with the GI
What are some examples of an ion exchange resin dosage form?
Tusionex (basically liquid Norco) and Ionamin which is just phentermine resin
What is OROS?
Its an osmotic pump system that is rate controlled and it does this by using osmosis in its favor
How many milligrams of drug can OROS deliver?
Up to 750 mg
What are the examples of OROS delivered drugs?
Procardia XL, glucotrol XL, ditropan XL, and concerta
What is the drug release dissolution test about?
Three points of absorption are taken to see the range of drug absorbed
What are the lipophilic requirements for a drug with passive transdermal delivery?
It is highly lipophilic
What are the molecular weight requirements fir passive transdermal delivery?
Less than 500 daltons
What log K must a drug have to be passive transdermal delivery?
1-5
What water solubility must a drug have to be passive transdermal delivery?
0.05 to 1 mg/mL
Why cant morphine be used transdermally?
It has a log K of -0.1 and the skin flux is too small
What type of dosage form do we see liposomes and a percutaneous absorption enhancer?
Transdermal Formulations
What is the purpose of SonoPrep Skin permeation device?
This is a percutaneous absorption enhancer that is used with lidocaine as a way to enhance the anesthesia and shorten the onset of action
How does the sonoprep skin permeation device work?
It will transfer a low level ultrasound energy over a short period of time in order to make the outermost layer of the skin to be more permeable
What is the purpose of E-Trans?
It can be used to deliver drugs both locally and systemically using ELECTRICAL energy to transport the drug through the skin, it is good for episodic issues
What is IONSYS tm?
It is a transdermal system used for fentanyl
What kind of drugs can be used for transdermal delivery?
Very potent drugs
What are some cons of TDDS?
Can cause skin issues, susceptible to higher temperatures, there’s lag time
What are the two types of transdermal drug delivery?
Monolithic systems (matrix) and membrane-controlled transdermal systems (reservoir)
What’s the difference between the monolithic system and the membrane controlled transdermal system?
The membrane controlled transdermal system has a liquid reservoir and a semipermeable membrane whereas the monolithic system just haas a semisolid matrix
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