Guidelines for Sublingual GLP-1 Tablets
Expected Dissolution Time:
● Dissolution time may vary depending on the individual and the placement of the tablet
inside the mouth. Placing the tablet under the tongue is recommended for optimal
absorption.
● Tablets are expected to dissolve within approximately 30 seconds to 2 minutes.
● Instructions: Dissolve one tablet under the tongue once daily.
Timing Around Meals:
● For best absorption, take the tablet on an empty stomach. Avoid food or liquids for at
least 30 minutes to 1 hour post-administration. A small amount of water (less than ½
cup) is unlikely to interfere with effectiveness if necessary.
Dose Equivalence When Switching from Injection to Sublingual Tablets:
● There is currently no established dosing equivalence between injectable and sublingual
semaglutide. Injectable semaglutide has a bioavailability of around 89%, while oral is
approximately 1%, and sublingual is estimated to be similar.
● Dosing adjustments can consider the half-life of semaglutide (5-7 days) and daily
administration with sublingual tablets. Our sublingual tablets contain ingredients that
support semaglutide absorption, similar to Rybelsus, which is FDA-approved for oral
use.
○ Themaximum Rybelsus dose (14 mg daily) is considered equivalent to Ozempic
0.5 mg weekly. For patients transitioning from 1 mg injectable and aiming to
maintain rather than lose additional weight, sublingual tablets may be a viable
option.
Additional Notes on Tirzepatide:
● No oral or sublingual form of tirzepatide is currently available, and there is limited
research. However, based on peptide size and patient and prescriber feedback, dosing
assumptions have been generally well-tolerated.
Suggested Monthly Titration Dosing Schedules:
Semaglutide
● Month 1: 1mgdaily
● Month 2: 2mgdaily
● Month 3+: 3mg or 4mg daily (can use two 2 mg tablets if needed)
Tirzepatide
● Month 1: 3mgdaily
● Month 2: 4mgdaily
● Month 3+: 5mgdaily
Switching Between GLP-1 Medications:
Sublingual Tablets:
● For patients switching between GLP-1 medications in sublingual tablet form, a titration or
off-week may not be necessary unless there have been issues tolerating the original
medication. If tolerance issues occur, a waiting period of one week may be advisable to
ensure the original drug has left the system.
● Maintaining a steady level of GLP-1 in the body is crucial, as the bioavailability of
sublingual tablets is relatively low, and off-time may slow progress.
● For the first dose when switching medications, the patient should start with the lowest
available dose of the new drug. If the patient is not starting from the lowest dose, a half
tablet of the next available dose can be taken to assess tolerance. For example, when
switching from semaglutide to tirzepatide, a 3 mg tirzepatide tablet or half of a 4 mg or 5
mg tablet may be used to ensure tolerance.
● Dosage adjustments can be made as tolerated. If patients take a break from GLP-1
tablets for more than a week to a month, prescribers typically restart them at the
beginning of the titration schedule.
Injections:
● Prescribers may use several methods when transitioning patients between injectable
GLP-1 medications. Some prescribers adopt a conservative approach, gradually titrating
the patient from one medication to another, while others may introduce an off-week or
switch the patient directly to the new medication on the next scheduled dose.
● Regardless of the current semaglutide dose, starting tirzepatide at the initial 2.5 mg dose
once weekly is recommended to observe patient response.
● For patients who titrated down from semaglutide, a gradual titration up of tirzepatide (at a
rate of 4 weeks per dose increment) is advisable. However, some prescribers may
suggest increasing doses weekly, as tolerated, until reaching the corresponding dose of
the previous medication.
● Tirzepatide doses generally increase in increments of 2.5 mg, 5 mg, 7.5 mg, 10 mg, 12.5
mg, and 15 mg. The maximum dose is 15 mg, but many patients may find 10 mg
sufficient for their needs and remain at that level.
Additional Notes:
● It is common for prescribers to tailor each transition based on individual patient tolerance
and response to the medication, adjusting dosing schedules as needed to minimize side
effects and optimize therapeutic outcomes.