The unknown advantage of sublingual drug delivery: How does it avoid the liver's "first line of defense"?!

Sublingual administration is a relatively new method of drug delivery in modern medicine. This method uses the mucous membrane at the bottom of the mouth to allow drugs to enter the bloodstream directly without passing through the digestive tract. Sublingual administration offers several advantages over traditional oral medications, including faster onset of action, less risk of drug degradation, and reduced first-pass metabolism in the liver.

When chemicals come into contact with the mucous membrane under the tongue, they can be quickly absorbed because there are a large number of microvessels there.

Substances absorbed from the intestines undergo a first metabolism in the liver, which is known as the "first line of defense." Sublingual administration is not affected by this process, allowing more of the drug to enter the systemic circulation in an unchanged form. This method is particularly suitable for certain drugs that are not acid-resistant or unstable to the intestinal environment, such as naloxone.

Compared with oral administration, sublingual administration can greatly reduce drug degradation in the gastrointestinal tract.

Sublingual dosage forms

Drugs that are administered sublingually come in a variety of forms, including:

  • Sublingual tablets: Like nitroglycerin tablets, they dissolve quickly and easily.
  • Sublingual strips: Like Suboxone, these dissolve quickly in the mouth.
  • Sublingual solution: a concentrated solution such as some cough medicines.
  • Sublingual spray: designed to allow medication to enter the blood system more quickly.

When choosing a dosage form for a drug, the solubility and stability of the drug must be considered. Basically, any substance that dissolves easily in saliva has the potential to be administered sublingually.

Certain drugs are more effective and safer when administered sublingually.

Application of sublingual administration

Sublingual administration is particularly suitable for the following situations:

  • Tranquilizers and analgesics: such as clonazepam and morphine.
  • Psychotropic drugs: Such as LSD and MDMA, these drugs are administered sublingually for rapid effects.
  • Allergy immunotherapy: Administering allergens sublingually to promote immune tolerance.
  • Vaccines: Recent studies have shown that vaccines administered sublingually may be effective in terms of immunogenicity.
Potential Challenges

Although sublingual drug delivery has many advantages, it also presents some challenges. For example, some medications may not stay in the mouth easily because of their unpleasant taste. Additionally, if certain medications are highly acidic, long-term use may cause tooth discoloration or decay.

Exceeding normal saliva secretion may affect the absorption of drugs and thus affect the therapeutic effect.

Despite these challenges, sublingual drug delivery remains a rapidly evolving technology, especially important in the treatment of certain acute conditions. As technology advances, future drug design will be more inclined to consider this option of administration. It not only facilitates rapid treatment but also has the potential to improve patient compliance.

Finally, as we look to the future, will the widespread adoption of sublingual drug delivery fundamentally change the way we think about drug administration?

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