Sublingual spray - spray medication under the tongue.

1. Aravindhanathan Venkatesan,
1st M Pharm in Pharmaceutics,
Dept of Pharmaceutics,
JSS College of Pharmacy,
Ooty.
SUBLINGUAL SPRAY
JSS COLLEGE OF PHARMACY, OOTY
An ISO 9001:2015 Certified Institution,
Approved by Pharmacy Council of India,
Approved by AICTE, Accredited ‘A+' Grade
by NAAC.

2. Sublingual Spray
Introduction:
Sublingual spray is an innovative
pharmaceutical administration
technology in which the drug can be
sprayed under the tongue and then
diffuses into the capillary network
and act often faster than oral
administration with more
bioavailability.
non-invasive and feasible systemic
delivery.

3. Disadvantages Advantages

4. Anatomy & Physiology
It lies beneath mucous
membrane ( sublingual fold) of
mouth floor, close to frenulum
of tongue.
It has serous and mucous acini
(Mucous Predominant).
Sublingual ducts (8 to 20) open
into mouth floor on summit of
sublingual fold.
Nerve Supply: Parasympathetic
secretomotor supply is from
facial nerve via chorda tympani,
and submandibular ganglion

5. Contin…..
Blood supply to sublingual gland
Absorption of drug by
sublingual region and effective systemic
circulation.
Sub mental and sublingual arteries.
Branches of the lingual and
facial arteries.
The venous drainage parallels the corresponding arterial supply. The
sublingual gland is mainly drained by the submandibular lymph nodes.
Diffuses in
to venous
blood
Drains to
common
trunk
internal
jugular vein
sub clavian
vein
Branchioce
phalic vein
superior
vena cava
on set of
action

6. Contin….
To brain
• The proximity with the internal carotid artery
allows fast access to this route supplying the
greater part of the cerebral hemisphere

7. Palatal
500‐600
micro meter
Gingival
250
micro meter
Buccal
200
micro meter
Sublingual
100 – 200
micro meter
ORAL MUCOSA
Drug
Unionized
form
Absorption
Due to
thin layer
of
mucosa
Penetration
will be
faster
Reaches
capillary
network
On set
of
action

8. Factors affecting
the sublingual absorption
May alter the absorption rate
in sublingual region
Thickness of
oral
epithelium &
Oil to water
partition
coefficient
Solubility &
pH and pKa –
saliva
Lipophilicity &
Binding to oral
mucosa

9. After specific
administration
drug will reaches to
the
Sublingual
Capillary network
Tablet- Ergomar-
$15 per pill
Film –suboxone -
$1.7 billion
Spray – fentanyl –
$1.7 billion
Lozenges & pills
Systemic
circulation
Comparison between other
sublingual dosage forms

10. 0
10
20
30
mins
Dosage form
Comparison between different dosage forms
on set of action
(mins)

11. Presently
• Nitroglycerin
(Nitrostat®)
• Isosorbide
dinitrate
• Fentanyl citrate
(Abstral®)
• Buprenorphine
hydrochloride
Available
• Ergoloid mesylates
• Asenapine
(Saphris®)
• Ergotamine tartrate
(Ergomar®)
Medications
• Buprenorphine
hydrochloride and
naloxone
hydrochloride
• Zolpidem tartrate
(Intermezzo®)
• Antianginal
Anti hypertensive
Analgesics
Bronchodilators.
Certain Steroids &
Peptides
For what
• No bitter taste
• Dose lowers than 20mg
• Small to moderate MW
• Good stability in water and
saliva
• Partially non ionized at the
oral cavities pH
• Undergoing first pass effect
Drug
characteristics
• open sores in
mouth,
• effect of
drinking,
• eating or
• smoking
Detrimental
factors

12. FORMULATION ASPECTS
1. Active Pharmaceutical Ingredient
2. Buffers
3. Solubilizers
4. Preservatives
5. Antioxidants
6. Propellants
7. Penetration enhancers
An ideal sublingual spray for the
drug that should possess the
following characteristics:
 Aqueous solubility should be
appropriate to provide desired
dose in a volume of formulation.
 Appropriate sublingual
absorption properties
 No sublingual irritation
 Rapid onset of action
 Low dose generally below 25-30
mg per dose.
 No toxic sublingual metabolites.
 No offensive aroma or taste
associated with drug.

13. Therapeutically active ingredients which can be dissolved or suspended in
Excipients
Actuation
unit dose as well as
multiple dose.
Dimensions and compositions
SprayThe drug needs to get into your
system quickly
have trouble swallowing medication
The medication doesn’t absorb very
well in the stomach
The effects of the drug would be
decreased by digestion
Should be BCS 1 class drug to get
more beneficial effect.
Considerations

14. In 2014,
Sublingual film
Naloxone
Sublingual
spray ( recent)
sublingual spray
- Insys
Therapeutics
$1.3 billion in the
U.S. Market, while
the total market
grew to more than
$1.7 billion
Treatment of opioid
intoxication or
overdose - Insys
Therapeutics - received
Fast tract Designation
from the FDA
Subsys® (fentanyl) was
recently approved in the
US -treatment of
breakthrough cancer
pain. (net worth $1.7
billion).
North America’s
sublingual spray
market
• increased - increasing cancer diseases –population
• healthcare facilities, reimbursement scenario and
skilled professionals to the patients
• governs the sublingual spray market over the
globe
Europe
second largest
sublingual spray
market
• The sublingual spray market in Asia Pacific and
Middle East regions are projected to grow fast
and provides increased government funds and
focus on better facilities over healthcare .

16. MARKETED
FORMULATION

17. Conclusion
• Due to rapid on set of action of drug by
these kind of sublingual spray can be
used by the patients (who needs
medication immediately) with proper
information regarding administration.

18. 1. Compounding Sublingual medications- Compounding pharmacy of America. Available from:
https://compoundingrxusa.com/blog/compounding-sublingual-medications/
2. Research and Markets: Buccal Drug Delivery Systems: Opportunities And Challenges In Buccal,
Sublingual Films, Tablets & Sprays - Detailed Analysis On Technologies And Pipeline Development –
Business Wire A Berkshire Hathaway Company. Oct 06, 2015 Available from :
https://www.businesswire.com/news/home/20151006005951/en/Research-Markets-Buccal-Drug-
Delivery-Systems-Opportunities
3. Insys Therapeutics – Market wired. Oct 29, 2015 Available from:
http://www.marketwired.com/press-release/insys-therapeutics-announces-its-naloxone-sublingual-
spray-received-fast-track-designation-nasdaq-insy-2068576.htm
4. Donald R T – Single dose fentanyl sublingual spray for breakthrough cancer pain. PMC US National
Library of medicine, National Institutes of health Jul 24, 2013. Available from:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3726301/
5. Sublingual Sprays Market: Global Industry Trend Analysis 2012 to 2017 and Forecast 2017 – 2025-
Persistence Market Research (Industry – Life science & Transformational Health) Available from:
https://www.persistencemarketresearch.com/market-research/sublingual-sprays-market.asp
6.Christopher HF , Dana TB – Anatomy, function, and Evaluation of the Salivary Glands. Pg. No- 1
Available from : chrome-extension://mhjfbmdgcfjbbpaeojofohoefgiehjai/index.html
7. Shojaie AH. Buccal mucosa as a route for systemic drug delivery: A review. J Pharm Pharm Sci
1998; 1(1):15‐30.
Reference