Mega Super DDS Study Set: IE 2

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