-Sublingual Drug Delivery System are the dosage
form which 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.
-The tablets are
usually small and flat, compressed lightly to keep them soft. The tablet must
dissolve quickly allowing the API to be absorbed quickly. It’s designed to
dissolve in small quantity of saliva. After the tablet is placed in the mouth
below the tongue, the patient should avoid eating, drinking, smoking and
possibly talking in order to keep the tablet in place.
-Swallowing of saliva
should also be avoided since the saliva may contain dissolved drug. Bland excipient
are used to avoid salivary stimulation.
Advantages:
-First pass - The liver is by-passed thus
there is no loss of drug by first pass effect for sublingual administration,
Bioavailability is higher.
-Rapid absorption - Because of the good blood
supply to the area absorption is usually quite rapid.
-Drug stability -pH in mouth relatively
neutral so a drug may be more stable.
Disadvantages:
-Holding the dose in the mouth is
inconvenient. If any is swallowed that portion must be treated as an oral dose
and subject to first pass metabolism.
-Only small doses can be accommodated easily.
Example:
Glyceryl
Trinitrate –
A potent
coronary vasodilator which is used for the rapid symptomatic relief of angina.It
has been found impressively effective when administered sublingually;
pharmacologically active after only 1 - 2 minutes.
Some of
the drug like desoxycortisone acetate, morphine, captoprill, nifedipine and
17-B Oestradiol gives impressive absorption
when given sublingually , it has also been shown that the sublingual
administration of 17-B Oestradiol requires only 1/4 of the oral dose.
Related Post:
Types of sublingual dosage forms
Fast-disintegrating sublingual tablets
Related Post:
Types of sublingual dosage forms
Fast-disintegrating sublingual tablets
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