Bioavailability vs Bioequivalence – All You Need to Know
Posted on November 18th, 2020
CBD has become quite popular over the recent years, and, for those that are aware of its therapeutic potential, it is no surprise. CBD and THC, the main psychoactive component found in cannabis, are both cannabinoids. Yet, CBD, unlike THC, is non-psychoactive. Thus, CBD will not cause you to feel ‘high’ after taking it. Because of that, you can enjoy its many possible effects without suffering any kind of impairment. Many people report that CBD gives them pain relief, aid in sleep and digestion, help with bladder issues, inflammation, or even relief from chemotherapy symptoms. There are currently many ways for you to consume CBD. Therefore, there are many different kinds of CBD products. Which one you choose to consume will impact how much of the compound actually reaches your bloodstream. So, how do you even begin to know which CBD product is best for you to choose? This is where the concepts of CBD bioavailability and bioequivalence will come in handy. What’s the difference between those two? Read on to find out more about CBD bioavailability vs bioequivalence and how knowing about it can help you when consuming CBD.
What Is CBD Bioavailability?
CBD comes in many different presentations, such as oils, tinctures, lotions, capsules, e-liquids, and many more. All of these presentations have different administration methods, and they also each come with different CBD concentration levels. Bioavailability is the degree and rate at which the bloodstream absorbs a substance. It determines how much of the substance you just took will reach your system to deliver its effects. So, if you understand bioavailability, you will be able to measure precisely the exact amount of CBD you are consuming each time. CBD and other cannabinoids enter the endocannabinoid system to interact with the cannabinoid receptors in the body. However, the process is just not that simple. This is where CBD bioavailability comes in.
Pharmacokinetics and CBD Bioavailability.
There are numerous methods to take CBD, all depending on which kind of CBD product you are consuming. Whatever process you use to administer CBD will affect just how much of it is absorbed and used by the body. That is what pharmacokinetics is, how the body processes compounds. It includes the movement of medications into, through, and out of the body. A drug’s pharmacokinetics depends on its chemical properties and other patient-related factors. Sex, age, weight, genetics, and renal function are the main factors to consider, with some other being patient-dependent. For example, a younger person will react to drugs differently than an older person would to the same amount. The same drug taken by two different people of the same will tend to have different effects depending on the factors mentioned above. This is why an evaluation of the needs of the patient takes place before administering any medicine. How is CBD absorbed, metabolized, distributed, and excreted? The bioavailability of CBD will determine just how quickly and how much of the cannabinoid will enter into your bloodstream.
The Science Behind CBD Bioavailability.
Let’s first discuss a couple of basic concepts to better understand the topics to follow. First, water solubility is the ability of a compound to dissolve in water at a specific temperature. Second, bioavailability, as said before, refers to the amount of active ingredients that make it into the bloodstream.
Cannabinoids are usually lipophilic, meaning that they are oil-based compounds that are not soluble in water. Once you put them in water, they will tend to float and will not actually dissolve in it. This is usually a problem since the human body is up to 60% water; hence CBD will have a hard time dissolving inside of it.
Once you inject an active ingredient directly into the bloodstream, its bioavailability will be 100% in one go. If ingested, it will go through a first-class metabolism, which refers to how the liver processes the stomach’s contents. This is where the active ingredients’ degradation happens as the enzymes process the liver’s digested material. Therefore, the chances of any ingested lipophilic compound getting 100% into the bloodstream if ingested will be close to zero.
Bioavailability of CBD Consumption Methods.
If you want to get the most bioavailability out of CBD, the best way to do this is intravenous, injecting it directly into the bloodstream. This delivers 100% of the CBD to your body. However, this is not actually what most people do. See, most people do not like to use needles. However, there are many other methods, each with its own bioavailability levels. These levels are:
This means to consume something through the mouth. When referring to CBD, oral consumption methods include CBD edibles, beverages, and capsules. However, oral consumption has its disadvantages. Since it will have to pass through the metabolic and digestive systems, which will filter out a lot of the CBD, thus, reducing its bioavailability. It has the lowest CBD bioavailability, with an absorption rate of around 13-19% and a half-life of about 1-2 hours. The reason for this is due to the first pass effect that happens during digestion. Also, CBD is fat-soluble, hence harder for the body to absorb.
This is one popular method that many people use when taking CBD. The sublingual gland is a vein located under the tongue. When you administer a substance to the sublingual gland, the bloodstream will directly absorb it. This practice goes by the name of sublingual consumption. Some of the products consumed this way include CBD sprays, CBD lozenges, and tinctures.
This method is very handy as it is more direct and will impact the body faster than oral consumption would. Hence, you will get high bioavailability, as only the saliva enzymes will degrade it. According to studies, the bioavailability rate of sublingual consumption will be at around 12-35%, higher than that of oral consumption.
CBD inhalation is one of the most effective ways of taking CBD as it bypasses the first-pass effect by avoiding the digestive tract. Instead, CBD will be inhaled and absorbed into the bloodstream via the alveoli, going through the lungs. When you inhale CBD, the effects will be rapid but also short-lasting when compared to other methods. You can inhale CBD in two ways; through vaping and by smoking.
When you vape CBD, the concentrate or flower heats up to a particular temperature, where the extract turns into an inhalable vapor. There is no combustion or smoke with vaping, but there are some risks involved, including that of serious lung injury. According to what research we have so far, the bioavailability of CBD when vaporized is somewhere around 56% more or less.
This was the most common way of taking cannabis before these other methods came along. According to research, smoking CBD has a bioavailability of 31%, while the half-life of smoked CBD will be 31 hours.
CBD is far more permeable through the epidermis than THC, hence the reason why many people use cannabinoid topicals. However, it is slow to work and absorb, as compared to the other methods. Research put its bioavailability at 45%.
Water Soluble CBD
As seen above, CBD is not water-soluble. Yet, through technology, some researchers broke the oil into very small particles and fused it with a surfactant. Therefore, the compound remained emulsified, and the broken-down particles did not regroup. However, the resulting compound was still not actually water-soluble. Instead, it dispersed further through a liquid, increasing the oil’s surface area and making it easier to absorb through the skin. However, this method is still new; thus, there’s little research so far about the water-soluble CBD bioavailability.
Bioequivalence Of CBD.
Bioequivalence is when you can take a substance in another consumption method but equal dosage. For example, if you have been taking CBD in one form and wonder what its equivalent dosage will be in another format. To know that, you will need to check on its bioequivalence. For example, a 10mg vape is not equal to 10mg of CBD oil administered through the tongue. This is where CBD bioavailability vs bioequivalence comes in. You will have to do some calculations to know the equivalent dose.
Basically, take the amount of CBD and the bioavailability rate of the method of delivery of the product with the highest bioavailability of the two. Multiply those to values with the percentage expressed as a decimal (i.e., 56% equals 0.56).
Then, divide the result by the bioavailability percentage (also expressed as a decimal) of the second product.
The resulting number will be the amount of milligrams the second, lower bioavailability product would need to achieve bioequivalence with the CBD product of higher bioavailability.
Bioavailability vs Bioequivalence – The Takeaway
Even though CBD has become popular, the amount of info available can overwhelm first-time users. Particularly, knowing how to determine the CBD bioavailability vs bioequivalence can be a minefield.
However, the crucial thing to do is to talk to your doctor before using CBD. They will monitor your health and see if taking CBD will have any side effects on you. This can happen, especially if you are pregnant or on some medication, as CBD does interact with a few of them. Don’t rush when choosing a CBD product. Take your time to determine its bioavailability rate and if it would be ideal for your purposes. Thus, consider several options before you narrow it down to one that suits you best.
You also better be careful with the dosage you take when determining the bioavailability of CBD. Start with the smallest dose, and see how your body reacts. Do not rush. After some time, you can increase the dosage in small bits to see how your body reacts to it. If you feel that the effects are too much, lower it next time. There’s no FDA-recommended dose of CBD; it is up to you to listen to your body.