Dosage Forms Exam 2 - Sublingual/Buccal Drug Delivery
Sublingual drugs are typically designed for _____ drug release, while buccal drugs are designed for _____ drug release.
(Sublingual) fast (Buccal) slower (due to less permeability)
Subligual/Buccal drugs can achieve rapid ______ __ ______ and high _______ ______. e.g. SL NTG: 1-3 minutes!
(rapid) onset of action (and high) blood levels.
The sublingual/buccal route allows for avoidance of... (3 things).
- GI acid degradation - GI enzymatic degradation - First pass effect
What are some advantages of the "lollipop" format? (2)
- Unlikely to be swallowed - Can be easily removed in the event of side effects
What are the disadvantages of the sublingual/buccal route?
1) Relatively low permeability for some drugs (Because of skin-like barrier properties). 2) Drug can be washed away 3) Sometimes unpredictable bioavailability
Fentanyl "lollipops" are placed between the cheek and gum, then sucked for __ minutes.
15 (minutes).
Saliva has a pH of about _.
7
Why do you want sublingual/buccal drugs and excipients to be bland and non-irritating?
As to not stimulate saliva flow
What are some general guidelines for what to avoid when taking sublingual/buccal medications?
Avoid eating, drinking, chewing, smoking, and talking. *Basically, DO NOT DISTURB!*
Nicotine gum is formulated with a buffer to raise the pH to 8.5. What does this do?
Basic pH increases the nonionized form - which causes increased absorption!
Why is saliva critical for drug delivery?
Because it helps dissolve the drug
The epithelium is the principle barrier for drug absorption. Why is it good for systemic delivery?
Because it is highly vascularized.
Why is fentanyl a good candidate for the buccal/sublingual route?
Because it is very lipophilic, and it has a a high first pass effect.
Which membrane is thicker - the buccal or the sublingual epithelium?
Buccal epithelium is thicker (by 2-8 times!)
Drugs in the oral cavity are able to achieve systemic circulation by absorption through the...
Buccal or Sublingual epithelia
Chewing gum is an example of _________ administration.
Buccal.
Zelapar is placed on the tongue, but its adsorption is *sublingual or buccal*?
Buccal.
How are molded tablets formed?
By forcing a moistened blend of drug and excipients into a mold. It is then forced out of said mold and allowed to dry. *Like druggy dough.*
Sublingual drugs can also be delivered as sprays. How does one take NitroMist?
By spraying it on or under the tongue.
Mucoadhesive tablets are designed to stay in place and contain mucoadhesive excipients. Name a muchadhesive excipient.
Cellulose derivatives.
Striant is a buccal mucoadhesive tablet designed to do what?
Deliver Testosterone for ~ 12 hours.
What can cause the drug to be "washed away"?
Eating, drinking, saliva...
Lyophilized tablets are also known as _______-___________ tablets.
Fast-dissolving (tablets)
Keratin does what?
Helps to form a tough barrier.
The oral cavity can be a sort of "melting pot" in the sense that it has elements of the ___________ mucosa and the ________. This is because it is coated with mucous, but is also a squamous epithelium.
Intestinal mucosa (and the) epidermis.
Buprenorphine has high first pass metabolism and low oral bioavailability. This means...
It is a good candidate for the sublingual (or buccal) route.
Sublingual tablets such as Isosorbide Dinitrate, Nitrostat, Abstral, Edluar, and Zubsolv are compressed tablets intended for sublingual use. Are they highly or lightly compressed?
Lightly (to facilitate dissolution).
The Buccal area refers to the...
Lining of the cheek (typically between cheek and gum).
Zelapar is prepared by ______________.
Lyophilization.
Nicotine gum is bound to a cation exchange resin. Chewing is critical because it allows for the exchange of...
Nicotine for saliva cations.
Is the buccal and sublingual membranes keratinized?
Nope
Zelapar is a orally disintegrating tablet used for what disease?
Parkinson's
A Drug film is when a drug is mixed with a fast-dissolving __________ plus a _____________.
Polymer (plus a) stabilizer
The sublingual buccal route (particularly buccal) can also be used for ____________ _________.
Prolonged action (Can keep something in the buccal space for a while)
Fentanyl "lollipops" have rapid absorption followed by prolonged absorption. Why?
Rapid: from absorption in the mouth Prolonged: from absorption in GI
Lozenges are intended for fast or slow dissolution?
Slow
What kind of drugs are best absorbed in the sublingual/buccal route (think features).
Small lipophilic drugs.
Molded tablets tend to be harder or softer than compressed tablets?
Softer.
Muscosal variations can cause the bioavailability of a drug to be...
Sometimes unpredictable.
Which membrane has better permeability - the buccal or the sublingual?
Sublingual (because buccal is thicker)
Suboxone (buprenorphine and naloxone) is a film intended for ___________ use. Contains polyethylene oxide and hydroxypropyl methylcellulose.
Sublingual (use)
Drugs administered in the oral cavity can have both ________ and _______ effects.
Systemic (and) local (effects).
Nicotine polacrilex (Commit) is similar to Nicorette (the nicotine gum) because...
The nicotine is bound to a cation exchange resin.
Why do you want to keep NTG (Nitroglycerin) in a tightly sealed glass container?
Tightly sealed: NTG is volatile and can slowly evaporate if it's opened even slightly. Glass: NTG interacts with and passes through plastic.
True or False... Not all orally disintegrated tablets are meant for GI absorption.
True!
The Sublingual area refers to the...
Ventral surface of the tongue and floor of the mouth.
Does the nicotine in nicotine gum have a high first pass metabolism?
Yes. Systemic bioavailability thusly depends on how long the saliva is kept in the mouth.
Does the amount of saliva in the mouth vary from place to place?
Yes. There are regional differences like there being a little pool of saliva underneath the tongue.
Does testosterone have a high first pass effect?
Yiss
Are tablet molds also available for extemporaneous compounding?
Yisssssssss
