BRST Sublingual Nicotine Pharmacokinetics
This article examines research on a novel 2 mg sublingual nicotine tablet (BRST) that delivers nicotine 6 times faster than traditional lozenges. We analyze pharmacokinetic data showing 14-minute peak absorption, explore user experiences demonstrating 91% craving satisfaction compared to cigarettes.
Key Takeaways
The 2 mg BRST sublingual tablet reaches peak nicotine levels in just 14 minutes, compared to 82.5 minutes for regular nicotine lozenges
Initial nicotine absorption occurs at 0.4 ng/mL per minute, with 50% of maximum concentration achieved within 4 minutes.
Users rated craving reduction at 4.2 out of 7, nearly matching their cigarettes at 4.6—making BRST 91% as effective
64.7% of participants estimated they would replace their cigarettes with the 2 mg tablet, rising to 87.3% among satisfied users
All side effects were mild, including salivation, throat irritation, and hiccups—no serious adverse events occurred
Nicotine products deliver nicotine at varying rates, with most oral products providing slower delivery than cigarettes. This difference in delivery speed has limited their effectiveness as cigarette alternatives. Rose et al. (2022) published findings in Psychopharmacology examining a novel sublingual nicotine tablet technology (BRST) that delivers nicotine faster than other existing oral products.
This article analyzes both the pharmacokinetic data (how the body absorbs and processes the drug) and subjective responses from this research, focusing specifically on the 2 mg sublingual tablet formulation.
Sublingual Administration Route
The sublingual region refers to the area under the tongue. This area contains thin, permeable tissue with many blood vessels close to the surface. When medications are placed under the tongue, they can pass directly into the bloodstream through this tissue, bypassing the digestive system entirely. This route typically provides faster drug absorption than swallowing a pill, which must first travel through the stomach and liver before reaching the bloodstream.
BRST Tablet Formulation
According to Rose et al. (2022), the 2 mg BRST sublingual tablet consists of nicotine dissolved in oleic acid (a fatty acid found in olive oil) and absorbed onto silica particles compressed into tablets. When exposed to saliva, the tablet rapidly disintegrates within approximately one minute, releasing thousands of tiny nicotine-containing particles. The water in saliva then facilitates the transport of nicotine into the sublingual tissue.
How the Body Processes the 2 mg Tablet
The first study compared how quickly nicotine entered the bloodstream from a 2 mg BRST sublingual tablet versus a 2 mg nicotine lozenge (Commit®) in six healthy smokers.
Time to Peak Concentration
The key measure was "Tmax" - the time it takes for nicotine to reach its highest level in the blood. This is important because faster Tmax usually signifies quicker satisfaction from cravings.
2 mg BRST tablet: 14 minutes to peak
2 mg Nicotine lozenge: 82.5 minutes to peak
The sublingual tablet delivered peak nicotine levels nearly 6 times faster than the lozenge (p=0.01, indicating this difference was statistically significant and unlikely due to chance).
Initial Absorption Rate
Researchers measured how quickly nicotine levels rose in the first 4 minutes:
2 mg BRST tablet: 0.4 ng/mL per minute (nanograms per milliliter - a measure of concentration)
2 mg Nicotine lozenge: 0.0 ng/mL per minute
The sublingual tablet achieved 50% of its maximum concentration within just 4 minutes, while the lozenge showed no measurable nicotine absorption during this critical early period when cravings are most intense.
Peak Concentrations
"Cmax" refers to the highest nicotine level reached in the blood. Despite faster absorption on the BRST tablet, both products (BRST & lozenges) achieved similar peak levels:
2 mg BRST tablet: 4.4 ng/mL
2 mg Nicotine lozenge: 5.3 ng/mL
Total Nicotine Exposure
The "area under the curve" (AUC) measures total nicotine exposure over time. The 2 mg tablet showed lower overall exposure (949.5 ngmin/mL) compared to the lozenge *(*1189.9 ngmin/mL). Rose et al. (2022) suggest this may occur because some nicotine from the rapidly disintegrating tablet gets swallowed and broken down by the liver before reaching the bloodstream.
How Users Feel - The 2 mg BRST Tablet Experience
Rose et al. (2022) also examined how 24 smokers felt after using the 2 mg sublingual tablet following 2 hours without nicotine.
Relief from Withdrawal Symptoms
Withdrawal symptoms include irritability, anxiety, difficulty concentrating, and restlessness. Using a standardized scale (0-20, where higher scores mean worse symptoms):
Before using the 2 mg tablet: score of ~5.0
5 minutes after use: score dropped to 2.0 (p=0.0004)
This improvement shows the tablet quickly relieves the discomfort of nicotine withdrawal.
Craving Reduction
On a 0-4 scale measuring desire to smoke, participants report on average:
Before 2 mg tablet: 2.6 (moderate to strong craving)
5 minutes after: 1.0 (mild craving)
This 62% reduction in craving occurred within just 5 minutes (p<0.0001).
Comparison to Cigarettes
Participants rated how well the 2 mg tablet reduced cravings compared to their usual cigarettes (scale of 1-7):
2 mg sublingual tablet: 4.2
Their usual cigarettes: 4.6
This near-equivalent rating (91% as effective as cigarettes) represents a significant advance over traditional alternative products.
Product Acceptance
When asked about replacing cigarettes:
64.7% of participants estimated they would replace their cigarettes with the 2 mg tablet
Among those who liked the product (rating >4 out of 7), this increased to 87.3%
Physical Effects of the 2 mg BRST Tablet
Heart Rate Changes
The 2 mg tablet increased heart rate from 67.8 to 76.2 beats per minute at 30 minutes - an increase of 8.3 bpm. This mimics the cardiovascular response to cigarette smoking, providing objective evidence of rapid nicotine delivery.
Side Effects
All side effects were mild and well-tolerated:
Excessive salivation (4 participants)
Tongue or throat irritation (4 participants)
Heartburn and nausea (3 participants)
Hiccups (2 participants)
How the 2 mg BRST Tablet Compares to Other Products
To understand the significance of these findings, here's how the 2 mg BRST tablet compares to other nicotine delivery methods:
Cigarettes remain the fastest delivery method, with nicotine reaching peak levels in just 7 minutes and achieving blood concentrations averaging about 11 ng/mL. This rapid delivery drives their addictive potential.
The 2 mg BRST sublingual tablet achieves peak levels in 14 minutes with a maximum concentration of 4.4 ng/mL, positioning it as significantly faster than traditional oral products while avoiding the health risks of smoking.
Nicotine nasal sprays have been the fastest pharmaceutical alternative, with peak concentrations occurring at 10-12.5 minutes post-administration. However, many users find the nasal irritation intolerable, limiting its appeal.
Electronic cigarettes show variable absorption depending on the device and user experience. Studies report a median Tmax of 10 minutes with average peak concentrations of 8.4 ng/mL, though individual results vary widely.
Traditional nicotine gum requires much longer to reach peak levels. When used as directed with the "chew and park" method, 4 mg gum takes approximately 45 minutes to reach peak concentration. The extended chewing time and technique requirements often reduce user satisfaction.
Nicotine lozenges show similar slow absorption to gum, with peak times typically ranging from 45-90 minutes depending on the formulation and how actively the user moves the lozenge in their mouth.
Modern nicotine pouches represent the slowest oral delivery method, with studies showing peak times of 60-65 minutes and concentrations ranging from 11.9-18.4 ng/mL depending on nicotine content. While convenient, their slow onset limits effectiveness for acute cravings.
This comparison reveals that the 2 mg BRST sublingual tablet fills a gap - providing faster satisfaction than traditional oral products without the drawbacks of nasal irritation or the health risks of smoking.
Why Speed Matters
Rose et al. (2022) explain that rapid nicotine delivery is important because:
Brain receptor response: Nicotine receptors in the brain respond more strongly to quickly rising nicotine levels before they become desensitized (less responsive)
Dopamine release: Fast delivery triggers more dopamine (a "reward" chemical) in the brain
Behavioral reinforcement: The brain strongly links rapid satisfaction with the action that caused it, making fast-acting products more satisfying
Key Advantages of the 2 mg Sublingual Tablet
Based on the research findings:
Speed: Delivers nicotine in 14 minutes versus 82.5 minutes for regular lozenges
Effectiveness: Reduces cravings nearly as well as cigarettes (91% as effective)
Tolerability: Only mild side effects reported
User acceptance: Majority of users would replace most of their cigarettes with it
Study Limitations
Rose et al. (2022) acknowledge:
Small sample size in the pharmacokinetic study (only 6 participants)
No placebo control to account for psychological expectations
No direct head-to-head comparison with cigarettes in the same study
What This Means for Nicotine Users
The 2 mg BRST sublingual tablet represents a new option that delivers nicotine faster than gum or regular lozenges, but without the nasal irritation of sprays. Its 14-minute delivery time and high user satisfaction ratings suggest it could be more effective than current oral nicotine products for managing cravings.
The fact that users rated its craving relief at 91% of their cigarettes' effectiveness is particularly noteworthy, as this has been a major limitation of existing nicotine replacement products.
Conclusion
The 2 mg BRST sublingual nicotine tablet demonstrates unique absorption characteristics that set it apart from existing oral nicotine products. With nicotine reaching peak blood levels in just 14 minutes - compared to over 80 minutes for regular lozenges - it provides rapid craving relief that users rate as nearly equivalent to cigarettes.
These findings from Rose et al. (2022) suggest that sublingual delivery technology could address a gap in nicotine replacement options, providing faster relief than traditional oral products while maintaining ease of use.
Reference
Rose, J. E., Behm, F. M., Botts, T. L., Botts, D. R., Willette, P. N., Vocci, F., & McCarty, J. (2022). Novel rapid-acting sublingual nicotine tablet as a cigarette substitution strategy. Psychopharmacology. https://doi.org/10.1007/s00213-022-06171-z
