CannAquaSol

Dissolvable Cannabinoids: The Future of Cannabis Medicine

It is well-known that Cannabis oil and all Phytocannabinoids are water-insoluble and therefore poorly absorbed. To address this issue, NextHerbal Labs utilizes a technology, called CannAquaSol™, so health conscious consumers receive the maximum benefits from these phytochemicals. CannAquaSol™ is the leading delivery system innovation for dramatically improving the bioavailability of poorly absorbed phytocannabinoids. This technology is applicable to CBD isolate, CBD distillate, THC distillate and also all minor Cannabinoids.

The benefits of this technology include:

   - Controlled and measured dosing
   - Age appropriate, patient-centric dosage forms
   - Alternatives to unhealthy modes of intake such as vaping or smoking

CannAquaSol™ 1st Generation (Liquisolid Technology)
This patent-pending* 1st generation technology was developed to maximize the solubility, bioavailability and chemical stability of phytocannabinoids.

The powder/pellet can dissolve the CBD or THC in liquids over a broad range of pH.
1st generation works with common GRAS (Generally Recognized As Safe) ingredients that can be gluten-free and dairy-free.
The ingredients are FDA and Health Canada allowed for use in consumer products.
The 1st generation CannAquaSol technology offers great potential to make Cannabis-containing ingestible forms.
The 1st generation IS NOT based on:

- Micellization & Micro-emulsion - Microencapsulation
- Complexation with Cyclodextrins - Nanotechnology/Nanoparticle delivery system.
*: US patent pending: "Solid formulations with improved solubility of cannabinoids and preparation method thereof"

Slide1: Two processes for making the Liquisolid Powders.
Slide2: The Liquisolid formulation, followed by pelletization for making the Liquisolid Pellets [5].

[5]: B.R. Pezzini, et al., Liquisolid technology applied to pellets: Evaluation of the feasibility and dissolution performance using felodipine as a model drug, Chemical Engineering Research and Design, 2016, 110, pp. 62-69

CannAquaSol™ 2nd Generation (Pickering Emulsification + Spray Drying)
The characteristics of 2nd generation:

2nd generation is completely water soluble powder. As the adsorbent/carrier used in the 1st generation is an inorganic water-insoluble ingredient, after addition of this powder to water, the phytocannabinoid dissolves and the adsorbent remains at the bottom of container. Therefore, the 2nd generation of CannAquaSol™ powder could be used in many forms, including beverages.
Pickering emulsion = Particle-stabilized emulsion

Pickering emulsions have plenty of benefits over conventional emulsions (surfactant-stabilized emulsions), including a lower toxicity, preferable stability, adjustable permeability, better biocompatibility, and the diversity of available particles [6].
In the left following picture, the Pickering versus classical emulsion is depicted. Right picture shows the Spray Drying process which has been used in CannAquaSol™, 2nd generation.

[6]: J. Wu, G.H. Ma, Recent Studies of Pickering Emulsions: Particles Make the Difference, 23 June 2016, https://doi.org/10.1002/smll.201600877

Sprinkle dosage form

These formulations are drug-containing pellets or granules that can be mixed with soft food before administration. They provide almost the same dosing flexibility and ease of ingestion as liquid formulations when sprinkled on liquid or semi-solid vehicles, such as applesauce, pudding or yogurt. The food taken together with the drug can also mask the unpleasant taste and smell of the drug substance, which potentially improves patient compliance. Due to their solid state, sprinkle formulations guarantee the higher stability of loaded drugs than liquid formulations during storage [7].
As previously mentioned, the phytocannabinoid pellets formulated based on CannAquaSol technology could be used as Sprinkle dosage form.

[7]: H.S. Lee, et al., Sprinkle Formulations - A Review of Commercially Available Products, Asian Journal of Pharmaceutical Sciences (2019), doi: https://doi.org/10.1016/j.ajps.2019.05.003

General administration methods for the sprinkle drug products in various dosage forms [7].

Sublingual CBD/THC Microdosing – The New Frontier of Cannabis Administration

Sublingual Route: Fast & accurate uptake without the hazards of smoking
In addition to CannAquaSol powder and pellet, we formulated the Sublingual tablet having the CannAquaSol powder to enhance accurate dosage and immediate effects. This administration involves placing a sublingual tablet under the tongue, allowing the phytocannabinoid(s) to dissolve and enter the bloodstream through the vessel-rich tissues within the sublingual cavity.
The onset of pharmacological effects is rapid, and the duration of effects is equivalent to or exceeding other forms of administration. Since the "First Pass Metabolism" (metabolism in the liver) is by-passing with sublingual use, the bioavailability of phytocannabinoid(s) is significantly improved compared to other routes of administration.

Compressed (Tableted) Chewing Gum

At NextHerbal Labs, a number of CBD- and THC-based chewing gums have been formulated. We used a directly compressible powder which made up of a gum base and sweeteners besides CBD or THC for making the tableted chewing gums. This formulation process does not require high temperature like the traditional chewing gums made by extrusion. Therefore, the process is quick and cost-effective as it adapts to direct compression with standard tableting equipment.
Some of the advantages of a chewing gum are:

Fast absorption - many times faster than conventional oral dosage forms like tablets and hard-gelatin capsules
Consumer friendly - for the 40% of people who do not like swallowing any type of solid dosage forms
Convenient and discrete - no liquid required
High bioavailability of active ingredients – avoids first pass metabolism in liver.

Orally Disintegrating Tablet (ODT) Infused with CBD/THC

NextHerbal Labs has developed "Orally Disintegrating Tablets" of two phytocannabinoids. These tablets disintegrate rapidly in the mouth without chewing or water and are formulated for anyone who dislikes swallowing conventional tablet or capsule. Most formulations disintegrate in 30-90 seconds.
Benefits of ODT for consumers:

Allows accurate dosing - no risk of liquid spills
Improved consumer compliance - easier to take or administer than conventional tablets or liquid forms
Ideally suited for those with difficulty swallowing or chewing
More convenient than other dosage forms - easy to swallow, requires no water, and offers quicker onset of therapeutic action.

Benefits of ODT for manufacturers:

A cost-effective way to extend the product's life cycle - a new ODT formulation can create a branded, differentiated line extension
Gain entry into new markets
Better stability than liquid dosage forms
Help meet the growing demand for more consumer-friendly and compliant dosage forms.