Ijraset Journal For Research in Applied Science and Engineering Technology
Authors: Tejal Pawar , Raj Chitte , Sanjivani Bachhav, Deepali Deore, Prajakta Bachhav
DOI Link: https://doi.org/10.22214/ijraset.2025.66524
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A sublingual tablet is a medication formulation that dissolves beneath the tongue, facilitating quick absorption of the active ingredients through the mucous membranes and into the bloodstream. Bypassing the liver metabolism and digestive tract, this technique can improve the effectiveness and speed of medication delivery. Sublingual medications are frequently used for drugs that need to start working quickly. Benefits of the sublingual route include a more consistent therapeutic impact and the avoidance of stomach upset. The salient features of the sublingual tablet include its ability to dissolve beneath the tongue, its speedy absorption and beginning of action, and its ability to prevent gastrointestinal irritation.
I. INTRODUCTION
Sublingual dose forms entail putting medicine behind the tongue, where it dissolves and enters the bloodstream through the sublingual mucosa, which is extremely vascularized. Sublingual drug delivery emerged as a response to the need for a quick pharmacological effect. All age groups are susceptible to dysphasia, or difficulty swallowing, although it is especially common in the elderly, young children, mentally retarded, unwilling, nauseous, or dehydrated patients/dieters who have trouble swallowing various dosage forms. Medications administered sublingually enter the bloodstream directly through the ventral surface of the tongue and the floor of the mouth [1].
The drug is rapidly absorbed in the reticulated vein beneath the mouth mucosa and then enters the bloodstream through the brachiocephalic, internal jugular, and facial veins. a section of the mouth that is permeable. In the oral cavity, the sublingual, buccal (cheek), and palatal areas have the lowest levels of patency. Generally, the order is determined by the relative thickness and blood flow to each component. Sublingual: situated beneath the tongue .Sublingual dosage forms are any that are positioned under the tongue, dissolve, and enable the medication to be instantly absorbed through the sublingual mucosa.The dose form is not meant to be chewed or eaten. When a medication is administered sublingually, it is inserted beneath the tongue and immediately reaches the bloodstream through the floor of the mouth and the tongue's ventral surface. The drug's dissolved active components enter the reticulated vein and are quickly absorbed [2].
Sublingual Gland:The seromucous, polystomatic gland is called the glandula sublingualis. The sublingual gland, together with the submandibular and parotid, is the smallest and most pervasive of the three primary salivary glands in the oral cavity. Located beneath the mouth diaphragm, the sublingual gland produces roughly 3–5% of the salivary volume.They are situated anteriorly and superiorly to the submandibular gland, inferiorly and laterally to the tongue, and beneath the mucous membrane of the floor of the mouth. They are bound laterally by the mandibular bone and inferolaterally by the mylohyoid muscle. The glands behind each mandibular canine are palpable. Put one index finger into the mouth and the other hand's fingertips outside to physically feel the squeezed gland between the inner and outer fingers. The sublingual gland is composed of approximately twenty minor excretory ducts, also known as ducts of Rivinus, and one major duct [1]. The largest of these, the sublingual duct (of Bartholin), joins the submandibular duct and drains through the sublingual caruncle.
Fig 1: Sublingual Gland
Mechanism of sublingual absortion:The permeability of the solution, also referred to as osmosis, the drug's molecular weight, ionization, and lipid solubility all have an impact on absorption. The medication is absorbed by the oral epithelium's cells through the mechanism of endocytosis. The stratified epithelium is unlikely to exhibit the same mechanism throughout. Nonetheless, it's thought that stimulating the salivary glands acidically and causing vasodilatation in the process helps promote absorption and uptake into the circulatory system [3]. There are mucous glands and squamous epithelium covering the mucous membrane that lines the mouth. The buccal mucosa and sublingual mucosal tissue are comparable.The salivary ducts allow saliva to be secreted into the mouth by lobules of cells that make up the salivary glands [4].
A. Advantages: [2],[5]
B. Disadvantage: [6]
C. Sublingual tablets are special because they:
D. A sublingual tablet should have the following qualities:
E. Factors:
1) Drug Solubility in Lipids:
This is the method by which the drug should be absorbed in its entirety. Its lipid solubility is slightly higher than that of other drugs needed for GI penetration, mostly for passive permeation [7].
2) pH and pKa of saliva:
because saliva has a pH of 7. Hence, pH influences how well a unionized medication is absorbed. In addition, the mucosa's pKa for absorption is greater than 2 in acidic media and less than 8 in basic media.
3) Mucosa epithelial in mouth Thickness:
The sublingual mucosal epithelium's minimum thickness is between 100 and 200 μm. Therefore, because the epithelial mucosa is thinner, medicines permeate more quickly. Therefore, it is simple for a medicine to be absorbed in little saliva.
4) Partition Coefficient:
Sublingual mucosal epithelial cells instantly absorb molecules with an appropriate oil and water partition coefficient. For the best medications, the oil and water partition coefficient can be adjusted within the range of 40 to 2000.
5) Adhesion to the Oral Mucosa:
The medication that binds to the mucosal membrane has low systemic availability.
6) Saliva Solubility:
In addition to having a high lipid solubility, the medication can be dissolved in water in oral fluids. Therefore, the drug's biphasic solubility is essential for absorption.
F. Physicochemical Criteria of drug for Sublingual Drug Delivery:
The essential physico chemical characteristics of a drug for suitable candidate. The formulation of SLTs are summarized in Table [8],[9].
Physicochemical Properties of Drug |
Accepted Range |
Dose |
< 20 mg |
Taste |
Not intensely bitter |
Stability |
Good stability in water & saliva |
Molecular Weight |
Small to moderate (163.3-342.3g/mol) |
pKa |
>2 for acidic Drug; < 10 for basic Drug |
Log p |
1.6 to 3.3 |
Lipophilicity |
Lipophilic |
Table 1: Physicochemical Criteria of drug for Sublingual Drug Delivery
Drug Name |
Brand Name |
Active Ingredient |
Dosage Form |
Manufacturer |
Description |
Market Release |
Nitroglycerin |
Nitrostat |
Nitroglycerin |
Sublingual Tablet |
Pfizer |
Used to treat angina; helps relax and widen blood vessels. |
Old (1960s) |
Lorazepam |
Ativan |
Lorazepam |
Sublingual Tablet |
Valeant Pharmaceuticals |
Used for anxiety; provides quick absorption through mucous membranes. |
Old (1980s) |
Vitamin B12 |
Nature's Bounty Sublingual B12 |
Vitamin B12 |
Sublingual Tablet |
Nature’s Bounty |
Used to treat B12 deficiency; facilitates faster absorption. |
Old (2000s) |
Midazolam |
Versed |
Midazolam |
Sublingual Tablet |
Roche |
Used for sedation; provides quick onset of action. |
Old (1990s) |
Naloxone |
Narcan |
Naloxone |
Sublingual Tablet |
Adapt Pharma |
Used to reverse opioid overdose; offers quick action to counteract effects. |
Latest (2010s) |
CBD (Cannabidiol) |
Charlotte’s Web |
Cannabidiol (CBD) |
Sublingual Tablet |
Charlotte’s Web |
Used for managing anxiety, pain, and sleep disorders; rapidly absorbed. |
Latest (2020s) |
Melatonin |
Natrol Sublingual Melatonin |
Melatonin |
Sublingual Tablet |
Natrol |
Used for sleep disorders; fast-acting to help regulate sleep-wake cycles. |
Latest (2010s) |
Buprenorphine |
Subutex, Bunavail |
Buprenorphine |
Sublingual Tablet |
Indivior |
Used in addiction treatment; provides controlled release for managing withdrawal symptoms. |
Latest (2020s) |
Fentanyl |
Sublimaze, Actiq |
Fentanyl |
Sublingual Tablet/Lozenge |
Teva Pharmaceuticals |
Used for severe pain; offers rapid relief through mucous membrane absorption. |
Latest (1990s) |
Estradiol |
Estrace |
Estradiol |
Sublingual Tablet |
Allergan |
Used in hormone replacement therapy; provides systemic estrogen. |
Latest (2000s) |
Desmopressi |
Minirin |
Desmopressin |
Sublingual Tablet |
Ferring Pharmaceuticals |
Used to treat diabetes insipidus; helps manage symptoms related to low ADH levels. |
Latest (2010s)
|
|
|
|
|
|
|
|
Table 2: summarizing different sublingual tablets [10].
II. METHODS
A.Pre-compression Studies:
The directly compressible tablet blends were evaluated for pre-compression studies to determine their flow and compressibility.
Flow Character |
Angle of Repose (degrees) |
Carr's Index (%) |
Hausner’s Ratio |
Excellent |
25 – 30 |
<10 |
1.00 – 1.11 |
Good |
31 – 35 |
11 – 15 |
1.12 – 1.18 |
Fair |
36 – 40 |
16 – 20 |
1.19 – 1.25 |
Possible |
41 – 45 |
21 – 25 |
1.26 – 1.34 |
Poor |
46 – 55 |
26 – 31 |
1.35 – 1.45 |
Very Poor |
56 – 65 |
32 – 37 |
1.46 – 1.59 |
Very Very Poor |
>66 |
>38 |
>1.60 |
Table 3: Limitations on the properties of powder flow
B. Post-compression Studies:
Average weight of the tablet |
Acceptable % deviation |
80 mg or less |
10% |
More than 80 mg but less than 250 mg |
7.5% |
250 mg or more |
5% |
Table 4.Weight variation test acceptable limits according to I.P
The results of the study showed that sublingual tablets are a more effective method of medication delivery for elderly and pediatric patients, as well as better for patient compliance. Many medications have been developed using sublingual drug delivery, particularly those that need to take effect quickly. These tablets help those who have trouble swallowing. The intended audience now includes people who prefer easy-to-use pills devoid of water. The medication in the tablets is able to enter the systemic circulation through the sublingual capillaries, which causes an immediate onset of action.
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Copyright © 2025 Tejal Pawar , Raj Chitte , Sanjivani Bachhav, Deepali Deore, Prajakta Bachhav . This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Paper Id : IJRASET66524
Publish Date : 2025-01-14
ISSN : 2321-9653
Publisher Name : IJRASET
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