2. CONTENTS
• Definition
• Way of Administration
• Principle
• Advantage over Buccal route
• Advantage and disadvantages
• Types
• Drugs in the market
3. DEFINITION
• Sublingual (abbreviated SL), from the Latin for "under the tongue", refers to the
pharmacological route of administration by which drugs diffuse into the blood
through tissues under the tongue.
• Many drugs are designed for sublingual administration, including cardiovascular
drugs, steroids, barbiturates, opioid analgesics with poor gastrointestinal
bioavailability, enzymes and, increasingly, vitamins and minerals.
4.
5. PRINCIPLE
• When a chemical comes in contact with the mucous membrane beneath the tongue, it
diffuses through it. Because the connective tissue beneath the epithelium contains a
profusion of capillaries, the substance then diffuses into them and enters the venous
circulation. In contrast, substances absorbed in the intestines are subject to "first-pass
metabolism" in the liver before entering the general circulation.
• Sublingual administration ,it ensures that the substance will risk degradation only by salivary
enzymes before entering the bloodstream, whereas orally administered drugs must survive
passage through the hostile environment of the gastrointestinal tract, which risks degrading
them, either by stomach acid or bile, or by the many enzymes therein, such as monoamine
oxidase (MAO). Furthermore, after absorption from the gastrointestinal tract, such drugs
must pass to the liver, where they may be extensively altered;
• Video :D
9. Advantage and disadvantages
Advantages Disadvantages
• Mesenteric circulation is by passed
• No loss of drug (by first pass effect)
• Higher bioavailability and onset of action
(than oral )
• Rapid absorption due to high
vascularization
• Reduce side effects due to low dose and
high efficiency
• Fast dissolution and disintegration without
water or chewing action
• Improved drug compliance
• PH of mouth is neutral so drug will be stable
• Interferes with eating , drinking and talking
• Not for Unconscious patients
• If any is swallowed that portion must be
treated as an oral dose and subject to 1st
pass effect
• Only small doses can be accommodated
• Patient should not smoke while taking the
medication as smoking cause
vasoconstriction of BV and will decrease the
absorption of drug
10. TYPES
• Fast Disintegrating Sublingual Tablets
• Bio adhesive Sublingual Tablets
• Thin film Drug Delivery System
• Lipid Matrix Sublingual Tablets
• Sublingual Immunotherapy
• Sublingual vitamin Tablets
11. CONTINUE
• Bio adhesive Sublingual Tablets : Water soluble carrier covered with fine particles
and a bio adhesive component (applied to extended release tablets )
• Sublingual Immunotherapy : ex (allergic rhinitis ) it’s taken as drops or tablets 3 or
more times /week , containing a specific allergen which interacts with the immune
system to decrease allergic sensitivity (like sensitization)
• Sublingual Vitamin Tablets : Mainly V.B12 (we must have enough in our bodies )
14. BUPRENORPHINE
• An opioid use disorder is a medical condition that is characterized by the
compulsive use of opioids .Opioids include substances such as morphine, heroin,
codeine, oxycodone, hydrocodone, etc.
• Buprenorphine sublingual tablet is indicated for the treatment of opioid
dependence and is preferred for induction. Prescription use of this product is limited
under the Drug Addiction Treatment.
• Sublingual tablet: 2 mg buprenorphine and 8 mg buprenorphine
15. CONTENT AND THE ROLE OF EACH
• Buprenorphine sublingual tablet is an uncoated oval orange tablet, imprinted with a logo on
one side and a numeric imprint on the other side.
• The tablets contain buprenorphine HCl ( Active Constituent )
• Each tablet also contains
citric acid anhydrous(disintegrant)
crospovidone (super disintegrant)
FD&C yellow #6 HT aluminum ( Lake : colour )
lactose monohydrate ( Diluent )
magnesium stearate ( Lubricant)
mannitol ( Directly compressible Diluent )
pregelatinized starch ( binder)
sodium citrate dihydrate.(Alkalizing agent; buffering agent; emulsifier; sequestering
agent.)
16.
17. ISORDIL® SUBLINGUAL TABLETS
ISOSORBIDE DINITRATE
• WHAT ISORDIL IS USED FOR
• Isordil Sublingual tablets are for the prevention and treatment of attacks of angina.
• Angina is a pain or uncomfortable feeling in the chest, often spreading to the arms, neck and
sometimes to the shoulders and back. The pain may be caused by too little blood and
oxygen getting to the heart.
• Isordil works by opening up blood vessels which allows more blood and oxygen to reach the
heart.
• Isordil may also be helpful in the treatment of some types of heart failure.
• Isordil Sublingual tablets
• At the first signs of an anginal attack, place one or two tablets under your tongue
18. ISORDIL® SUBLINGUAL TABLETS
ISOSORBIDE DINITRATE
• Ingredients
• Active ingredient: 5 mg isosorbide dinitrate
• Inactive ingredients:
• • lactose........diluent
• • starch........ direct compressible diluet ,
may act as binder, diluent and disintegrant have
: +ve disintegration & -ve flowability
• • magnesium stearate........... act as a
lubricant
• • microcrystalline cellulose ...........act as
disintegrant
• • Erythrosine Lake............ colouring agent
• • CI 45430..................... colouring agent
19. LEVSIN®/SL TABLETS
• _Levsin®/SL is one of the principal anticholinergic/antispasmodic components of belladonna alkaloids.
• *Drug Components:
• _ 0.125mg of Hyoscyamine sulphate "active ingredient":
* treat a variety of stomach /intestinal problems such as cramps & irritable bowel syndrome.
• treat other conditions such as bladder and bowel control problems, cramping pain caused by kidney stones and gallstones .
_Inactive ingredients:
* FD&C blue #1 ... Coloring agent
* Lactose monohydrate ... Diluent
* Magnesium stearate ... Lubricant
* Mannitol ... Diluent & Sweetener
* Starch ... Disentigrant
* Stearic acid ... Lubricant
20. Levsin SL is formulated as round, blue colored tablets that are
imprinted with “AP” on one side and “113” on the other.
21. ERGOMAR® SUBLINGUAL TABLETS
• Ergomer is Prescriped for patient suffering from the migraine
• A migraine is a severe, painful headache that can be preceded or accompanied
by sensory warning signs such as flashes of light, blind spots, tingling in the
arms and legs, nausea, vomiting, and increased sensitivity to light and sound
• DESCRIPTION
• Ergotamine Tartrate Sublingual Tablets USP (Active ingredient) 2 mg
• Inactive Ingredients: Microcrystalline Cellulose (Directly compressible diluent),
Natural Peppermint (Flavor Powder), Crospovidone (super disintegrant) , Saccharin
Sodium (sweetening Powder), D&C Yellow #10 Lake(colour), Magnesium Stearate
(lubricant), FD&C Blue #1 Aluminum Lake(colour)
22.
23. SAPHRIS
Brand Name: Saphris
Composition & Role:
Asenapine Antipsychotic for the treatment
of schizophrenia and acute
mania associated with bipolar
disorder.
Gelatin Binder.
Mannitol Diluent and flavor.
24. ABSTRAL
•* What is the drug used for?
•_Abstral is used for management of breakthrough pain in adult cancer patients (+18) who are
already taking other opioid pain medicines around-the-clock for cancer pain.
•_Abstral patient must be (opioid tolerant)
• Drug Components:
• _Fentanyl Citrate "active ingredient" ... Opioid agonist (Analgesic).
• Inactive Ingredients :
* Mg stearate ... Lubricant.
* Mannitol ... Diluent & Sweetener.
* silicified microcrystalline cellulose ... Diluent & Disintegrent ... Also, improve binding capability.
* croscarmellose sodium (sodium CMC) ... Disintegrent.
26. EDLUAR
Brand name: Edluar
Zolpidem tartrate Sedative or hypnotic. used in adults
for the short-term treatment of a
sleep problem called insomnia
Mannitol Sweet diluent
Silicified microcrystalline cellulose
(mixture of microcrystalline cellulose
and silica colloidal anhydrous)
Binder
Croscarmellose sodium Super disintegrant
Saccharin sodium Sweetener
Magnesium stearate Lubricant
27.
28. ORALAIR
Sweet Vernal, Orchard, Perennial
Rye, Timothy, and Kentucky Blue
Grass Mixed Pollens Allergen Extract
Mixed allergen extract of five
pollens. Used as an immunotherapy
to treat symptoms of grass pollen
allergic rhinitis with or without
conjunctivitis.
Mannitol Sweet diluent
Microcrystalline cellulose& colloidal
anhydrous silica
Binder
Croscarmellose sodium Super disintegrant
Magnesium stearate Lubricant
Lactose monohydrate Diluent
Sweet Vernal, Orchard, Perennial Rye, Timothy,
and Kentucky Blue Grass Mixed Pollens Allergen
Extract
29.
30. ZOFRAN
ONDANSETRON Bocks the actions of chemicals in the body
that can trigger nausea and vomiting that
may be caused by surgery or by medicine
to treat cancer.
LACTOSE MONOHYDRATE Diluent
MAGNESIUM STEARATE Lubricant
CELLULOSE, MICROCRYSTALLINE Direct compressible vehicle
STARCH, CORN Glidant
POLYETHYLENE GLYCOL 6000 Polymer
POLYETHYLENE GLYCOL 400 Plasticizer
SODIUM STARCH GLYCOLATE TYPE A
POTATO
Disintegrant
TITANIUM DIOXIDE Opaque extender