Buccal and Sublingual Tablets

Principle of Sublingual administration:

  • A chemical/Substance that is absorbed when it comes into touch with the mucous membrane located below the tongue. The substance then diffuses into the capillaries, which are abundant in the connective tissue underlying the epithelium, and enters the venous circulation.] Contrarily, before entering the general circulation, substances that are absorbed through the intestines must first travel through the liver for metabolism.
  • Compared to oral delivery, sublingual administration has some benefits.
  • In contrast to orally administered drugs, which must survive passage through the hostile environment of the gastrointestinal tract (GIT) and run the risk of being degraded by either stomach acid or bile, or by enzymes such as monoamine oxidase (MAO), it safeguards that the substance will risk degradation only by salivary enzymes before entering the bloodstream.
  • Furthermore, after absorption from the gastrointestinal system, such drugs must travel to the liver, where they may be extensively altered; this is known as the first pass impact of drug metabolism.
  • For some compounds, like salvinorin A, the oral route is inappropriate due to the digestive action of the stomach and intestines.

Pharmaceuticals are produced as the following types of formulations for sublingual administration:

  1. Sublingual tablets:
    • Examples: Nitroglycerine tablets, the anti-emetic ondansetron.
  2. Sublingual strips:
    • Examples:  Suboxone.
  3. Multi-purpose tablets:
  4. Sublingual drops:
    • Example: Nicocodeine cough preparations
  5. Sublingual spray:
  6. Lozenge
  7. Effervescent buccal or sublingual tablets:
    • Example: Fentora fentanyl buccal tablet.

Definition of Sublingual

  • Both sublingually and buccal pharma drugs/medication administration are two different types  of giving drugs by mouth.
  • Sublingual administration contains placing a drug under patients tongue to dissolve and absorb into his/her blood through the tissue there.
  • Buccal administration comprises placing a drug between patient gums and cheek, where it also dissolves and is absorbed into her/his blood stream. Both buccal drugs & sublingual medication come in various form i.e tablets, films (example of sublingually film is buprenorphine and naloxone sublingual film), or sprays (Fentanyl Sublingual Spray).

When sublingual and buccal drug are given to the Patient?

Both buccal drugs & sublingual dugs are given under any or many of the following situations:

  • The medication doesn’t absorb well in the stomach or GIT;
  • Drug needs to enter your system rapidly
  • Patient have difficulty swallowing medication
  • Digestion would lessen the medication’s effects.

Numerous capillaries, or tiny blood vessels, can be found on the cheek and beneath the mouth. There, medications can enter the circulation without first passing through the digestive system.

What are the Advantages and Disadvantages of Buccal & Sublingual Drug Administration?

Buccal and Sublingual tablets are made to intended in mouth for drug administration.

Advantages of buccal and sublingual routes of drug administration Some advantages of administering drugs through the oral mucosa are:

  1. The strong blood flow in the area and absence of gastrointestinal (GI) components that slow absorption both contribute to the therapeutic effect’s rapid start (gastric emptying, presence of food, gastric disease, etc.).
  2. By avoiding portal circulation and avoiding intestine and first-pass hepatic metabolism, a drug’s oral route bioavailability can be improved.
  3. Because the active ingredient is not exposed to the hostile GI environment, some medications, such as peptides, that would otherwise be broken down by GI pH or enzymes, may be administered buccally.
  4. Those who have trouble swallowing, nausea, malabsorption syndrome, or even patients who are asleep can undergo it.
  5. Spitting out the tablet can stop the action.
  6. Self-administration is easy.

Disadvantages of buccal and sublingual drug therapy

  1. Only extremely strong medications can be efficiently administered because of the limited size of the mouth cavity. The area available for drug absorption through the buccal mucosa is roughly 200 cm2, which is about 10,000 times smaller than the duodenum.
  2. Difficulty in maintaining the medication in the site, as well as the requirement that the patient refrain from swallowing, speaking, or drinking during administration in order to prevent the medication from staying in direct contact with the mucous membrane for a longer period of time.
  3. While any of the paracellular and transcellular pathways investigated can result in drug absorption, the most common method is passive diffusion of medicines from the salivary aqueous phase through the membranes of oral mucosal cells. Since excessive lipophilicity restricts drug disintegration in the same manner that increased polarity restricts diffusion across cell membranes, medicines with intermediate polarity are therefore efficiently absorbed. Ionization level is also crucial since less ionized substances at salivary pH absorb better.
  4. Drugs with a bitter or unpleasant taste should not be administered by the buccal or sublingual routes because, in addition to irritating the patient, these formulations cause excessive salivation, which raises the risk of swallowing.
Advantages and Disadvantages of Buccal & Sublingual Drug Administration

Administration of Sublingual Medication

The administration of sublingual medication involves placing medication under the tongue, where it is absorbed directly into the bloodstream through the highly vascular sublingual mucosa. This route of administration provides rapid onset of action and avoids first-pass metabolism in the liver. Here is a general procedure for administering sublingual medication:

  1. Verify the Medication:
    • Check the medication order and ensure it is the correct medication prescribed for the patient.
    • Verify the medication’s name, strength, and expiration date.
  2. Hand Hygiene:
    • Wash your hands thoroughly with soap and water or use an alcohol-based hand sanitizer to maintain proper hygiene.
  3. Prepare the Patient:
    • Explain the procedure to the patient and obtain informed consent.
    • Assist the patient to a comfortable position, preferably in a sitting or semi-reclined position.
  4. Assess the Patient’s Mouth:
    • Inspect the patient’s mouth for any obstructions, oral lesions, or food debris.
    • Ensure the patient’s mouth is clean and free from any foreign substances.
  5. Prepare the Medication:
    • Check the medication label against the medication order for accuracy.
    • Use appropriate aseptic techniques when handling the medication.
  6. Administration Technique:
    • Place the medication tablet or film under the patient’s tongue.
    • Instruct the patient to keep the medication under the tongue without swallowing or chewing.
    • Advise the patient to avoid talking or moving the medication around the mouth to ensure optimal absorption.
  7. Monitoring and Patient Education:
    • Instruct the patient to avoid eating or drinking until the medication is completely dissolved and absorbed, typically for a specified duration (e.g., 5 minutes).
    • Advise the patient to avoid rinsing the mouth or spitting during this time.
    • Monitor the patient for any adverse reactions or side effects.
    • Document the medication administration, including the time of administration and any relevant patient responses or observations.
  8. Patient Follow-Up:
    • Assess the patient’s response to the medication and evaluate the desired therapeutic effects.
    • Provide necessary education on the medication’s purpose, potential side effects, and any specific instructions for subsequent doses.
    • Address any questions or concerns the patient may have.


Sublingual and Buccal Medication Administration 

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