In 2013, I consulted for a company wanting to infuse THC into coffee, which sounded simple enough.
Except it wasn't, at least not if we wanted to do it properly with regards to both solubility (the ability to be dissolved) and bioavailability (the extent to which a substance or drug is available to its intended biological destination).
A good THC product should both completely dissolve in a beverage (whether hot or cold) and be in a form that allows the consumer to metabolize the maximum amount of the available dosage (i.e., as bioavailable as possible).
Most companies utilize micro- or nano-emulsions to formulate beverages and edibles such as gummies, because it is easy and cheap. This process turns an extracted form of THC (typically a distillate) into microdroplets that are infused into a carrier fluid. This fluid is then added to whatever the product is, with the goal that the THC stays suspended in the carrier fluid and homogenizes throughout the product.
However, these emulsions have poor bioavailability and do not stay suspended in fluids indefinitely. Poorly formulated micro- or nano-emulsions rule the market today.
In a Cannabis Business Times opinion article titled “Innovating for the Benefit of Patients in Medical Cannabis,” the author cites a study noting that the “bioavailability of orally consumed cannabinoids is approximately 6% – compared to intravenous administration. In practice, this means that 94% of active compounds are not reaching the bloodstream.” The author also states that “one of the most overlooked and unresolved issues remains the low oral bioavailability of cannabinoids.”
Many of today’s emulsions produce poor oral formulations, resulting in products that are not effective in their delivery of THC. The resulting products only deliver to the bloodstream a fraction of the labeled cannabinoids.
The Need for Better Cannabis Extract Formulations
There are now superior formulations and compounds that have achieved a very high level of both bioavailability and solubility.
At this point, if cannabis is rescheduled, it could allow true scientific research to commence on the potential of cannabis compounds, and those studies will require isolates and compounds far more advanced than the micro- and nano-emulsions with poor solubility and/or bioavailability. True medical cannabis formulations and compounds will be required in the pharmaceutical industry.
Bioavailability should be of concern to a consumer because if a product contains 10 milligrams of THC, and the THC was a byproduct of micro- or nano-emulsion, the consumer will only metabolize a very small percentage of the available THC. So, consumers and manufacturers alike need to put an emphasis on products with a superior bioavailability. If the consumer consumes a given percentage of an active ingredient, they should receive it in a form they can metabolize and achieve maximum effect.
The Next Generation of Cannabinoid Formulations
Today, there are a few formulation development companies producing superior compounds than all the rest. Besides the improved quality, some offer unique qualities, such as being in a powder form that gives edible manufacturers a truly bioavailable product without variation or hot spots. These producers offer beverage manufacturers a stable powdered product that is truly soluble in liquids and has maximum bioavailability.
These powders can also be pressed into tablets that contain various formulations of specific cannabinoids and/or terpenes, or alternative cannabinoids formulated for a specific effect.
One company, Stenocare, produces a bioavailable product called Astrum oil that is formulated specifically for pharmaceutical use. It is a base formulation that can be utilized in a multitude of forms and applications. (See this April 28 CBT article for more information.) However, it remains an oil-based product, which also limits its usability: It cannot be used intravenously or intraocularly, with patients who have gastrointestinal sensitivities to oil-based products, nor in any other situation in which consuming an oil would be problematic for practical or solubility reasons.
I myself ultimately formulated a base powder formula (and continue to offer consulting and formulation services on this subject) after completing the coffee infusion product for the company that reached out to me in 2013. This company is now capable of producing a plethora of very sophisticated compound formulations using this stabilized, consistent, powder form that is bioavailable, soluble, and capable of passing the blood-brain barrier.
Terpene Isolates: The Next Frontier
There are other patented or patent-pending methods and products that yield fractionated isolated terpene compounds in an uncompromised pharmaceutical form.
There are currently granted patents in the EU, Canada, Mexico, and pending in the U.S., for methods to produce pharmaceutical-grade terpene isolates. The compounds produced from these methods are uncompromised by oxidation or thermal degradation, as happens in steam distillations.
In fact, the resulting isolates and compounds are completely organic and the truest representation of the aromatic qualities of the undried buds on the plant. The resulting terpene composition is classified as an “essence oil,” the highest classification of essential oils – true, uncompromised, pharmaceutical-grade isolates. These terpene isolates can be combined with specific cannabinoids to achieve a specific patient or consumer effect.
These terpene isolates can also be formulated with the aforementioned soluble and bioavailable powder extraction for use in edibles or vapes.
These essence oils are perfect forms to be included in the newest versions of medical nebulizers. These devices utilize vibration to create microdroplets for inhalation, making them superior to current vape offerings, as there is no heat application to compromise the essence oils. These patented nebulizers will be the preferred delivery systems by medical professionals, as the inhalation of microdroplets is much safer than inhaling heated isolates. These cannabinoid and terpene essence oil formulations will also be in a form that offers maximum bioavailability,
I believe if cannabis is ever rescheduled, or better still legalized, there will be a new horizon for cannabis research and the resulting cannabis pharmacopeia, which will require true pharmaceutical-grade isolates in a multitude of forms. While we wait for that scenario to play out, edibles and beverages still require products that are truly bioavailable and soluble to deliver superior customer and patient experiences.
