Sublingual drug delivery is one of the conventional drug delivery system which can be helpful in emergency condition like angina attack .

1. Makwana Saroj V,
B.k.Mody Government Pharmacy College, Rajkot.
Sublingual drug delivery

2. Sublingual drug delivery system:
They are to be placed under the tongue and produce immediate
systemic effect by enabling the drug absorbed directly through
mucosal lining of the mouth beneath the tongue.
The drug absorbed from stomach goes to mesenteric circulation which
connects to stomach via portal vein. Thus, absorption through oral
cavity avoids first-pass metabolism
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3. Factors affecting the sublingual absorption:
• Lipophilicity of drug: Drug must have slightly higher lipid solubility than tha
t required for GI absorption is necessary for passive permeation.
• Solubility in salivary secretion: Drug soluble in aqueous buccal fluid
• pH and pKa of the saliva: pH of the saliva is 6.0, this pH favors the absorption
of drugs which remain unionized.
• The absorption of the drugs through the oral mucosa occurs if the pKa is g
reater than 2 for an acid and less than 10 for a base.
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• Binding to oral mucosa: Systemic availability of drugs that bind to oral mucosa is
poor.
• Thickness of oral epithelium: thickness of sublingual epithelium-100-200 μm
which is less compared to buccal thickness.
• Absorption of drugs is faster due to thin epithelium.
• Oil to water partition coefficient:40-2000 optimal for drug absorption.

5. Rapid absorption
Dose reduction
Increase
Bioavaibility
Reduction in side
effects
Suitable in disease
like nausea,
vomiting
Not required water
Advantages:
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6. Disadvantage
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High dose can not be administered
Less area is available for absorption
Not suitable for bitter and irritating drugs
Less patient compliance
No eating, Drinking and smoking is allowed
Highly ionic drugs can not be administered

7. Bioadhesive sublingual tablet
• The new sublingual tablet concept presented is based on
interactive mixtures consisting of a water-soluble carrier covered
with fine drug particles and a bioadhesive component.
• With this approach, it is possible to obtain rapid dissolution in
combination with bioadhesive retention of the drug in the oral
cavity.
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8. Fast-disintegrating sublingual tablets
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• Tablets that disintegrate or dissolve rapidly in the patient’s mouth are convenient
for young children, the elderly and patients with swallowing difficulties, and in
situations where potable liquids are not available.
• Only the small volume of saliva is usually sufficient to result in tablet
disintegration in the oral cavity.
• Medication can then be absorbed partially or entirely into the systemic
circulation from blood vessels in the sublingual mucosa.

9. Thin film drug delivery
• Delivering drugs to the systemic circulation via a thin film that
dissolves when in contact with liquid, referred to as a dissolving
film or strip.
• Advantage:
• Potential to improve the onset of action,
• Lower the dosing,
• Enhance the efficacy
• Safety profile of the medicament.
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10. Lipid matrix sublingual tablet
• Lipid Matrix Sublingual Tablet is formulated using advances in sublingual and
liposomal technology to create a dosage form that offers a faster and more
complete absorption than traditional oral routes of administration.
• The Lipid Matrix Sublingual Tablet is a bioavailable, quick, convenient, and
consistent dosage form for many specialty neutraceuticals that are often taken
orally.
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• Examples: Glutathione MB12 (Methylcobalamin) Melatonin
• A True Sublingual Tablet + Lipid Matrix Technology:
• Not a Lozenge, Troche, or Tablet Triturate: A True Sublingual Tablet
• Rapid Dissolve Formula
• Liposomal Drug Delivery
• Bioavailable & Avoids First Pass Effect
• Convenient & Consistent Dosing Application
• Single or Combination Drug Delivery

12. Sublingual immunotherapy:
• SLIT, is a form of immunotherapy that involves putting drops of allergen
extracts under the tongue.
• SLIT is usually delivered one of two ways: drops (or tablets) of allergen extract
are placed under the tongue, then either swallowed or spat out.
• Swallowing the extract seems to work better.
• Immunotherapy by the oral route (swallowed and not kept under the tongue
for any period of time), causes too many gastrointestinal side effects (nausea,
vomiting, diarrhea), and therefore is not used.
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13. Sublingual immunotherapy:
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• Administered :
• Daily
• Multiple times per week,
• Over a period of year.
• Uses:
• Pediatric patients with allergic rhinitis and/or asthma due to grass pollen.

14. Sublingual vitamin tablet:
• The only Sublingual vitamin that all doctors recommend is vitamin B12
(Cyanocobalamin).
• Recommended to be taken once a day.
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15. Evaluation
• In vitro evaluation :
• Uniformity of weight
• Content uniformity
• Hardness
• Thickness
• Diameter
• Disintegration time
• Friability
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16. Wetting Time (WT):
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• The tablet was placed at the centre of 2 layers of absorbent
paper fitted into a rectangular plastic dish (11 cm × 7.5 cm).
• After the paper was thoroughly wetted with distilled water,
excess water was completely drained out of the dish.
• The time required for the water to diffuse from the wetted
absorbent paper throughout the entire tablet was then
recorded using a stopwatch.

17. In-vivo evaluation:
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o Pharmacokinetic data analysis
oMaximal plasma concentration (Cmax)
oTime to reach maximum plasma concentration (Tmax)
oPlasma concentration‐ curve (AUC)
o Bioavailability evaluation

18. Drugs used in the formulation of sublingual
dosage forms:
• Physostigmine salicylate -Anti‐Alzheimer’s
• Scopolamine - Opioid analgesic Spray
• Furosemide - Diuretic Tablet
• Nifedipine, Nitro-glycerine - Anti‐anginal Tablet
• Vinpocetine - Neutropic Agent Tablet
• Terbutaline sulphate -Bronchodilator Tablet
• Amlodipine besylate , Captopril - Anti hypertensive Tablet
• Ondansetron Hydrochloride - Anti emetic Film
• Salbutamol sulphate - Anti‐asthmatic agent
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19. Market preparation:
• Tenormin sublingual tablet (isoproterenol)
• Microtab sublingual tablet (nicotine)
• Nascobal sublingual tablet (vitamin B12)
• Subuter sublingual tablet (buprenorphine)
• Nitroquick sublingual tablet (nitroglycerin)
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20. References :
• An Overview On Buccal Drug Delivery System, by Surender Verma, Mahima Kaul, Aruna Rawat
and Sapna Saini, IJPSR (2011), Vol. 2, Issue 6,page no.:1-19.
• A Review on Buccal Mucoadhesive Drug Delivery Systems, by Santanu Roychowdhury, Rajesh
Gupta, Sourav Saha ,Indo-Global Journal of Pharmaceutical Sciences, 2011, Vol 1., Issue 3: Page
No. 223-233.
• A Review on Buccal Drug Delivery System Nishan N. Bobade , Sandeep C. Atram, Vikrant P.
Wankhade, Dr. S.D. Pande, Dr. K.K. Tapa, International Journal of Pharmacy and Pharmaceutical
Science Research, 2013; 3(1) page no-35-41,
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21. References :
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• An Overview on: Sublingual Route for Systemic Drug Delivery by,K. Patel Nibha1 and SS. Panchol,
International Journal of Research in Pharmaceutical and Biomedical Sciences ,Vol. 3 (2) Apr –
Jun2012,page no-913-923
• Formulation And Evaluation Of Bioadhesive Buccal Tablets Of Simvastatin B. Agaiah Goud, Kumara
Swamy. S And Praveen Kumar. V, JAPS/Vol.1/Issue 1/2011,page no-29-38.
• Buccal Drug Delivery: Past, Present and Future – A Review, by A. Puratchikody, Prasanth V.V, Sam
T. Mathew, Ashok Kumar B, International Journal of Drug Delivery 3 (2011) page no-171-184.

22. References :
• A Review on study of Buccal Drug Delivery System,by Rajesh Mujoriya, Innovative
Systems Design and Engineering ,Vol 2, No 3,page no-1-14.
• Sublingual Mucosa As A Route For Systemic Drug Delivery,by
Neha Narang1, Jyoti Sharma, International Journal of Pharmacy and Pharmaceutical
Sciences,Vol 3, Suppl 2, 2011,page no-1-5.
• Buccal Mucosa As A Route For Systemic Drug Delivery: A Review, by Amir H. Shojaei, J
Pharm Pharmaceut Sci (www.ualberta.ca/~csps) 1 (1):15-30, 1998,page no-15-31.
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23. References :
• Recent Advances In Mucoadhesive Buccal Drug Delivery Systems And Its Marketed
Scope And Opportunities ,by K.P.Sampath Kumar ,DebjitBhowmik,AmitsankarDutta
,ShravanPaswan, Issue 1 : 2012,page no:79-93.
• A review on bioadhesive buccal drug delivery systems: current status of formulation
and evaluation methods by Chinna Reddy P,Chaitanya K.S.C.,Madhusudan Rao Y, DARU
Journal of Pharmaceutical Sciences Vol. 19, No. 6 2011,page no385-405.
• Sublingual Route For Systemic Drug Delivery Amit Kumar Bind,G. Gnanarajan and
Preeti Kothiyal, Int. J. Drug Res. Tech. 2013, Vol. 3 (2), page no-31-36.
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