Sublingual

The term sublingual ( see left ) comes from Latin ( sub "under" + lingua "tongue") and describes either the anatomical position (everything that lies below the tongue ) or the type of application . For example, there is a sublingual salivary gland , a sublingual fever measurement or the sublingual resorption of nitroglycerin.

Application type

In pharmacy , sublingual refers to a form of administration ( application form ) of active ingredients that are to be quickly absorbed through the oral mucous membrane under the tongue. For this purpose, special dosage forms such as orodispersible tablets , lyophilisates , chewable capsules or other fast-releasing dosage forms are used. Most of the drug is absorbed through the thin lining of the mouth under the tongue after its release . Only a small proportion of the drug is absorbed buccally ( inner surfaces of the cheeks ) or perlingually ( tongue mucosa ).

Due to the constant formation of saliva in the mouth and the small resorption area, the active substance to be resorbed must meet certain requirements. This means that only small amounts of active ingredient can be administered sublingually. In addition, the active ingredient must have a pronounced lipophilicity in order to be able to diffuse through the mucous membrane. LogP values of 1 to 5 are aimed for: Below 1, the active ingredients are usually too hydrophilic to overcome the lipophilic cell membrane, and with values ​​above 5 the active ingredient accumulates in the lipophilic membrane and does not get into the blood. Furthermore, only small active substances can get through the mucous membrane. In general, a rule of thumb of 500 Da applies .

When taken sublingually, the active ingredient enters the bloodstream more quickly because the venous blood flows from the oral mucosa directly into the superior vena cava . When ingested orally , the active ingredient must first pass through the liver in order to get into the great circulation, whereby it may be chemically changed. This is not the case with sublingual ingestion, the liver is bypassed. Another advantage over oral intake is that the drug can also be taken if swallowing is difficult.

In principle, drugs that are intended for injection by the manufacturer can also be administered in this way (e.g. there are spray bottles for sale into which ampoules can be inserted; trade name Adapplicator ). In the case of active substances that are poorly soluble in water or difficult to absorb , sublingual ingestion is not possible. In addition, the manufacturers guarantee the effectiveness of their preparations only when used in accordance with the recommendations provided. The doctor is solely responsible for the so-called off-label use (application deviating from the approval content).

Sublingual orodispersible tablets are to be distinguished from normal orodispersible tablets, which release the active substance quickly, but in which it is not absorbed sublingually and only enters the bloodstream in the gastrointestinal tract.

Drugs that are more commonly given sublingually

• Nitroglycerin for angina pectoris
• Lorazepam for anxiety and for immediate sedation , also for seizures
• Buprenorphine for severe pain
• Fentanyl citrate for severe pain
• Nicotine in smoking cessation
• Allergens in the course of sublingual immunotherapy (SLIT)

Web links

Wiktionary: sublingual  - explanations of meanings, word origins, synonyms, translations

Individual evidence

1. ^ European Pharmacopoeia Online. EDQM, accessed July 12, 2017 . 
2. ^ ^{A b} Sayeed & Ashraf: Considerations in Developing Sublingual Tablets — An Overview. PharmTech.com, accessed July 12, 2017 . 

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