TABMELT

Why TABMELT

Why TABMELT

What is TabMelt™?

TABMELT™ is a novel patented and patent-pending sublingual drug delivery system. The patented and patent-pending TABMELT™ delivery method allows patients to simply dissolve a tablet under their tongue which may lead to more instantaneous and accurate absorption in comparison to oral drug delivery.

Why TabMelt™?

Oral drug delivery is the most common drug delivery mechanism, but over 15 million Americans have a fear of swallowing pills. Taking medications orally means that the treatment has to go through the largely acidic GI tract and through liver first-pass. In order to achieve optimum bioavailability, this suggests a larger minimum effective oral dose is required which can potentially lead to a higher risk of side effects.

Several factors influence the strategy for administering prescription drugs through specific drug delivery systems including drug safety, systemic response, permeability, absorption, potency, efficacy, bioavailability, reactogenicity, pharmacokinetics, cost-effectiveness, and dose response among other factors. Among the routes for various drug deliveries, sublingual drug delivery is emerging as a highly beneficial and advantageous drug delivery. Targeted, sublingual drug delivery may provide an alternative to oral drugs while potentially reducing the dosing needed and possibly avoiding or limiting the adverse side effects of other delivery systems. Although a novel dosing concept, sublingual drug application has been clinically studied and is one of the most effective delivery methods for cannabinoids.

TABMELT™ is a revolutionary, patented sublingual drug delivery system that will forever change the way patients take medications. The TABMELT™ delivery system is a novel, all-natural, non-toxic sublingual drug delivery system that may offer a set-dose drug delivery system that enhances bioavailability and allows patients to dose by simply dissolving a tablet underneath the tongue.  

Analysis: Sublingual vs. Oral Drug Delivery

Among the routes for various drug deliveries, oral route is the most preferred by patients and providers, but new sublingual delivery systems could be more beneficial.  Several factors influence the strategy for administrating prescription drugs through specific delivery systems.  

Among these include drug safety, systemic response, permeability, absorption, potency, efficacy, reactogenicity, cost-effectiveness, dose response, and policies surrounding production and distribution among other factors.  

Targeted, sublingual drug delivery may be more advantageous than oral delivery in providing an alternative to ineffective oral drugs while reducing the dosing needed and potentially avoiding some adverse side effects of oral delivery.

Sublingual Delivery

Sublingual Delivery

Sublingual delivery of drugs in the oral mucosal cavity is characterized by a systemic delivery of drugs through the mucosal membranes lining the floor of the mouth (under the tongue).

The skin under the tongue is part of the oral mucosa covering the entire inside of the mouth. The oral mucosa consists of two layers, the surface epithelium and the deeper lamina propria. The oral epithelium layer is very permeable to drugs. Because of that, the sublingual delivery is faster and a more effective way of delivery drugs of high molecular weight, such as B12.

Metabolism

Sublingual drug delivery avoids presystemic elimination in the GI tract, bypasses liver first pass, and depending on the drug, offers a better enzymatic flora for drug absorption.

Dosing

Because sublingual delivery is not metabolized in the digestive system, a less active dose is needed to produce the desired bloodstream dose-response.

Absorption

The maintenance of drug plasma concentration within the therapeutic index is critical for effective treatment. Sublingual delivery offers several advantages for controlled, systemic drug delivery for extended periods of time.

Because of the high permeability and the rich blood supply, the sublingual route is capable of producing a rapid onset of delivery. This makes it appropriate for drugs with short delivery period requirements, resulting in less active ingredients and a less frequent dosing regimen.

Safety

Dosing of sublingual drugs is an important consideration because of high absorption and rapid permeability. While this can be life saving in certain situations, like delivering a blood thinner to a patient in atrial fibrillation, a lower dose of the same blood thinner would be needed for long term treatment.

The advantages of targeted sublingual drug release include the reduction in dose frequency, in drug side effects and in the fluctuation in circulating drug levels.

Sublingual bioavailability is 80-100% and by circumventing the liver path it reduces toxicity and side effects caused by liver metabolites.

Cost

Disintegrating tablet delivery creates a very high concentration in the sublingual region to be systemically absorbed across the mucosa. Sublingual delivery is more permeable and provides rapid absorption and good bioavailability in comparison to oral or buccal delivery systems, meaning the cost for the active dosing is less because less is needed. Because the delivery is sustained, less of the active material is needed, reducing the cost of production.

Studies

Before a sublingual drug delivery system for each type of drug can be formulated, sublingual absorption/permeation studies must be conducted to determine the feasibility of sublingual delivery for the candidate drug. These studies involve in vitro and in vivo sublingual permeation profile and absorption kinetics of the drug as well as the need for enhancers to improve drug permeation.

As with any new drug delivery system, studies on the effect of the sublingual dosing of drugs will be needed in the future to determine the effect on the body.

Oral Delivery

Oral Delivery

Oral drug delivery is the method of swallowing a pharmaceutical drug with the intention of releasing it into the gastrointestinal (GI) tract.

Once swallowed, the drug is released in to the gastric environment in the bloodstream before it is passed through the liver where it can be chemically altered. Once the drug reaches the bloodstream, it will continue to circulate through the tissues and organs before being filtered by the liver and kidneys and excreted from the body. 

Metabolism

Oral administration of drugs has disadvantages such as pre-systemic gastric enzymatic degradation within the GI tract and further breakdown in hepatic (liver) first pass.

Dosing

Oral delivery causes significant loss of drug due to the acidic stomach environment and liver metabolism. Thus, the bioavailability of oral delivery is 5-15% of the total oral application. A higher active dose is needed to be effective in achieving the necessary bloodstream dose response.

Absorption

Absorption of oral delivery varies depending on patient metabolism and excretion, and there is little control over how much and how quickly the active dose is metabolized out of the body.

Poor solubility, stability and bioavailability of many drugs make achieving therapeutic levels via the GI tract unpredictable. The rapid secretion and shedding of the GI tract can also limit effectiveness.

Drug particles are trapped and removed by mucus, making controlled release in the GI tract difficult.

Safety

Drugs administered orally move through the digestive tract where they can interact with many tissues and organs where side effects can occur if a drug has unintended effects in the body. Drugs are also chemically altered in the body.

The liver and kidneys can be prone to damage caused by drug metabolism in the organs. The harmful effects of drug toxicity often manifest over time, and cannot be studied immediately.

Cost

A higher amount of the active ingredient in a pharmaceutical drug is needed to increase the concentration of the medication to achieve desired dose-response, meaning higher cost associated with the amount of active(s) needed in a pharmaceutical drug, resulting in a lower cost to produce.  Additionally, with sublingual delivery, there is no need to encase pharmaceuticals in hard shells to protect them from the GI tract, which increases the cost of oral delivery.

Studies

Oral drug delivery is the most widely used and most readily accepted form of drug administration and numerous studies have been done on orally administered pharmaceutical drugs.

However, additional studies are needed on new oral solutions to the poor stability in the GI tract. Additionally, many studies cannot be completed on the safety, efficacy and effectiveness of oral drugs on the body until symptoms manifest in the organs and tissues and can be correlated to a specific pharmaceutical drug.