Cannabinoids, the chemical compounds found in cannabis, have been pretty much established as lipophilic or fat-soluble. This means that. In this video Dr. Liptan explains the science of CBD, and its uses in the . The process of making a fat-soluble compound, such as CBD. It has been stated that the rationale for adding sesame oil to the formulations is to dissolve the lipid-soluble cannabinoids, THC and CBD [1,17]. Moreover, many.
Fat Soluble CBD:
These products, termed 'water-soluble' are opening a new world of possibilities and enabling CBD to be added to liquids in a stable form. Edibles are the perfect product for those who want a fun twist on taking CBD. Commonly these products come in the form of candies or baked goods. You'll find gummies, chocolate, suckers, cookies, brownies and much much more.
The main benefit of a CBD in an edible form is the ease of use. Very few people will have an issue eating a gummy bear, chocolate bar, cookie or sucker.
This means that almost anyone can give CBD a try without any hesitation. CBD edibles span a wide range of effectiveness depending on the contents. Low effectiveness is caused by a couple factors:. Dogs, cats, and other animals can too! There are a wide variety of pet-specific CBD products on the market from treats to tinctures designed to help improve your pet's life.
These products are specially designed for animal use, often carefully crafted for appropriate dosing or application methods for pets. There are a wide range of product types available specially designed for animal use. Some common examples include:. Suppositories offer a highly effective means of ingesting CBD and offer a long-lasting effect. The product itself is a bullet-shaped pill that is inserted into the anus. The contents are then absorbed directly into the bloodstream.
These suppositories are often oil-based which helps lubricate the application process. It all comes down to bioavailability - or the amount of the product and the rate that it is absorbed into the bloodstream. When inserted, the product absorbs into the body in minutes and effects last for up to 8 hours. Often referred to simply as CBD oil, a tincture is an oil or alcohol carried form of CBD that is consumed sublingually by placing it under the tongue.
This liquid product that usually comes in a small bottle with a dropper. The liquid inside is comprised of several components:. CBD tinctures are consumed via sublingual administration. These oils are placed under the tongue and held for minutes before being swallowed. The molecules carried in the oil are absorbed into the bloodstream via the mucous membranes found under the tongue making them quicker acting, with only a slightly shorter duration than capsules.
Sublingual application has an average onset time of minutes before the effects are felt. The duration of the effects lasts for up to 6 hours. The body's endocannabinoid system has receptors in the brain, throughout the nervous system, and in the skin.
Skin-based receptors mean that applying topicals directly to an inflamed, sore or irritated area can provide localized relief. CBD topicals come in a wide range of products including balms and salves. These products are designed to help in a variety of specialized ways.
These oil-based products are used to provide localized inflammation and pain relief. These patches are designed to provide slow-release, long-lasting effects for the user. These patches are effective because they hold the cannabinoid against the skin for such a long period of time when compared to a rub-on topical.
The secret to these patches is that they must provide a home, but not a great home, to CBD and other cannabis materials. What we mean by this is that when placed against the skin, the contents of the patch must prefer to leave the patch and enter the skin layers. This is accomplished by using permeation carriers and enhancers.
These additives in the patch help push the cannabinoids in the direction of the skin. Once the contents of the patch reach the skin, it is absorbed into the bloodstream and the effects take hold from there. Many users find that the slow release and easy method of use make these patches a great solution. Vaping CBD is similar to any other type of vaping - a CBD extract or isolate are vaporized via a traditional vape pen or mod and inhaled.
Of all the methods of taking CBD, inhaling has the quickest onset thanks to the high bioavailability of inhaling the molecule. There are a variety of CBD vape products available on the market including:. Next morning, animals were administered 0. Two more doses of peanut oil 0. Standard solutions with densities of 1.
Following ultracentrifugation, the top 1 mL layer containing CM was collected using a glass pipette. An exclusion criterion was the use of any medication within one week prior to the study. Three male healthy human volunteers years old were recruited for this study. After 12 hours overnight fasting, participants had a high-fat breakfast.
CM separation was performed as described above for rat CM. Following incubation, the density of the emulsion was adjusted to 1. The cannabinoid content of this layer represents the fraction of the spiked dose associated with lipid artificial particles, rat CM, or human CM. Data processing was carried out using Empower TM 2 software. Plasma samples were analysed for cannabinoids concentrations using a previously developed and validated method [ 32 ].
Samples from in vitro lipolysis fractions lipid, micellar, and sediment , artificial emulsion or CM association experiments were prepared for HPLC-UV analysis by a liquid-liquid extraction method which was a slight modification of previously reported method for synthetic lipophilic cannabinoids Table 1 [ 33 ].
Chromatographic conditions for the detection of THC and CBD in plasma, in vitro lipolysis fractions, artificial emulsion, and CM association samples are summarized in Table 1. The plasma concentration-time profiles following oral administration of THC, the main psychoactive natural cannabinoid, in lipid-free vehicle and lipid-based formulation are presented in Figure 1.
IV bolus administration was used to calculate the absolute bioavailability. The pharmacokinetic parameters derived from these concentration-time profiles are summarised in Table 2. The absolute bioavailability of THC was increased by more than 2. The plasma concentration-time profiles following the oral administration of CBD, the main non-psychoactive natural cannabinoid, in lipid-free vehicle and lipid-based formulation are presented in Figure 2.
The pharmacokinetic parameters derived from these concentration-time profiles are summarised in Table 3. The absolute bioavailability of CBD was increased by almost 3-fold following oral administration in lipid-based formulation compared to lipid-free vehicle.
The intraluminal processing of cannabinoids co-administered with dietary fats or pharmaceutical lipid excipients has been assessed in this work using an in vitro lipolysis model. The results are shown in Figure 3. Upon lipolysis of sesame oil, around one-third of THC The intestinal lymphatic transport potential of THC and CBD was assessed using incubation studies with artificial lipid emulsion and with natural rat and human CM [ 27 , 29 ].
The results of the uptake are shown in Figure 4. No significant differences were seen between the uptake of cannabinoids by artificial lipid particles, rat CM or human CM Figure 4.
Differences between data sets were statistically non-significant. Over the last few years, the medicinal use of cannabis has gained growing interest after a long period of marginalization [ 9 ]. The legalisation of medical cannabis programs has noticeably increased the access of patients to cannabis and cannabis-based medicines in many countries [ 8 ].
For many patients, orally administered cannabis and cannabis-based medicines are preferred [ 1 , 11 ]. Orally administered cannabis is often consumed with dietary fat-containing food such as cookies. Lipids are also commonly used in pharmaceutical formulations of cannabis or cannabinoids. The rationale for the use of dietary fats and lipids is to enhance the extraction of the lipid-soluble active constituents [ 1 , 12 , 13 ].
However, the impact of dietary fats or pharmaceutical lipid excipients on the systemic exposure of patients to the cannabinoids has not previously been explored. This could be of particular importance when it comes to therapeutic efficacy or potential toxicity.
In this study we aimed to assess the effect of lipids on the systemic exposure to the main constituents of cannabis, THC and CBD, following oral consumption of cannabis with dietary fats or oral administration of cannabis-based medicines.
Our results show that the co-administration of cannabinoids with lipids enhances the bioavailability of THC in rats by more than 2. Such a profound increase in systemic exposure can significantly affect the therapeutic effects or toxicity of these cannabinoids.
To the best of our knowledge there are no previously reported studies of absolute oral bioavailability of these cannabinoids in rats. To explore the mechanism s by which lipids could enhance the oral bioavailability of THC and CBD, we first assessed the effect of lipids on intraluminal intestinal solubilisation of cannabinoids using in vitro lipolysis experiments. In vitro lipolysis is a commonly used model in pharmaceutics to assess the intraluminal processing of drugs administered orally with lipid-based formulation, or following high-fat meals [ 26 ].
The results of our lipolysis experiments showed that around one-third of THC and CBD was solubilised in mixed micelles. This suggests that two-thirds of the administered dose of THC and CBD is not readily available for absorption when cannabinoids are administered orally in the presence of lipids.
Long intestinal transit times and increased bile salt and phospholipid levels due to concomitant food intake might permit more efficient solubilisation of the drugs in vivo [ 35 ]. To assess post-luminal inside the enterocytes effects of lipids on the absorption of THC and CBD, we evaluated the role of the intestinal lymphatic transport in the absorption process of cannabinoids.
The association of lipophilic compounds with CM in the enterocyte is a pre-requisite for their intestinal lymphatic transport. The affinity of compounds for CM ex vivo has previously been shown to be predictive for the intestinal lymphatic absorption of drugs [ 29 ].
In this study, the lymphatic transport potential was initially investigated by assessing the uptake of THC and CBD by artificial CM-like lipid particles. However, lipid particles lack the surface apoproteins found in natural CM which might affect the process of association [ 27 ].
Association experiments were also performed with natural CM isolated from rats and showed association values of Therefore, the data suggest that CM serve as carriers to transfer THC and CBD to the systemic circulation via the intestinal lymphatic system following oral administration with lipids. Drugs that are transported via the intestinal lymphatic system avoid hepatic first-pass metabolism and therefore achieve significantly higher bioavailability than after administration in lipid-free formulation Figure 5.
Indeed, higher bioavailabilites were reported after administration by routes that avoid first-pass metabolism such as inhalation of THC [ 37 , 42 ] and CBD [ 39 ], or rectal administration of THC [ 40 ]. In addition, it was found in that study that about two-thirds of the absolute bioavailability of PRS, was solely due to a contribution of the intestinal lymphatic transport.
These observations support our proposed mechanism of intestinal lymphatic transport as a primary mechanism underlying the enhanced exposure to THC and CBD when co-administered with LCT in rats.
In order to assess if intestinal lymphatic transport might affect bioavailability of cannabinoids in humans, the uptake of THC and CBD by CM isolated from human volunteers was also assessed in our study. Association values observed in these experiments were similar to the uptake profile seen in rat CM Figure 4.
Therefore, it is reasonable to assume that similar effects of increased systemic exposure to orally administered cannabinoids when co-administered with lipids would occur in humans. It is unclear if there is a minimal volume of lipids that is required to activate intestinal lymphatic transport mechanism. Some studies show that as little as 1 g of lipid emulsion was sufficient to activate intestinal lymphatic transport of a highly lipophilic compound in dogs [ 43 ].
In contrast, it has been demonstrated that the administration of a low dose of lipids to rats equivalent to 1 g in humans was not sufficient to enhance intestinal lymph flow.
However, a higher lipid dose equivalent to 10 g in humans significantly increased lymph flow [ 44 ]. These amounts of lipids can easily be obtained from the average meal in Western diet [ 45 ]. By encapsulating the active compound in lipid pockets, the idea is that the gut will be able to absorb the chemical components much more easily, and thus increase the availability of the CBD for the cell and tissue systems that actually need it.
Well, that does it! Hopefully this article has provided a few helpful — and practical — tips for maximizing the therapeutic effects of your CBD. That being said, keep in mind that these are only suggestions — they should not be taken as clinical advice, or as a guarantee that your CBD oil will start to work better! Leave a Reply Cancel reply.
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How to Maximize the Effects of CBD [Answered]
First, it's important to understand that CBD is a fat-soluble compound, rather than a water-soluble one. Over millions of years of evolution. There are a few water soluble CBD products out there, this is what you molecules are stored in your fats where they can reach toxic levels. There are various methods of consumption and uses of CBD oil which Because cannabinoids are fat soluble, they accumulate in the skin and.