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02-25-2017, 11:12 AM
Science vs. Experience: How Effective Are Cannabis Suppositories?
By <span><a data-ipb="nomediaparse" href="http://www.marijuana.com/blog/news/author/mknodt/" title="Posts by Michael Knodt">Michael Knodt</a> </span> on <span> </span>
<span>February 24th, 2017 </span>
There are numerous, very contradictory reports on the rectal application of cannabis online that range from <a data-ipb="nomediaparse" href="http://www.greenbridgemed.com/rectal-absorption-of-cannabis-revisited/">absolutely ineffective</a>
to <a data-ipb="nomediaparse" href="https://www.hellomd.com/health-wellness/the-butt-of-the-story-why-rectal-cannabis-is-a-great-choice-for-many-patients">best ever</a>
. The research on this type of medicine intake is almost non-predictive because there are only two relatively small studies from <a data-ipb="nomediaparse" href="https://www.ncbi.nlm.nih.gov/pubmed/2985774">1985</a>
and <a data-ipb="nomediaparse" href="https://www.researchgate.net/publication/246901979_Rectal_bioavailability_of_D-9-tetrahydrocannabinol_from_the_hemisuccinate_ester_in_monkeys">1991</a>
. Both studies conclude that the bioavailability of THC taken rectally is very poor compared to eating or inhaling.
On the other hand, there are many positive and <a data-ipb="nomediaparse" href="https://www.merryjane.com/health/what-you-need-to-know-about-using-cannabis-suppositories">credible testimonials</a>
from patients and consumers, most of them reporting a muscle-relaxing and pain-relieving effect. Further to that, people <a data-ipb="nomediaparse" href="https://sensiseeds.com/en/blog/recreational-rectal-use-cannabis-science/">report </a>
a long lasting high after having applied cannabis rectally. Individuals report that the psychoactive effect is not as distinctive as smoking or eating, but that it does last longer.
How much THC actually gets into the blood when smoking or eating?
The bioavailability of inhaled or ingested cannabis is not as significant as one may expect.
Depending on the depth of inhalation, the duration of the puff, and the length of time the inhalant stayed in the lung, only 10 to 35 percent of the available THC in a joint will reach the smokers bloodstream; 65 to 90 percent of lost THC is a result of side streams and incomplete uptake of THC via the mucosa of the respiratory tract; 30 percent is lost through combustion before inhalation. Vaporizing cannabis, however, is more effective. In a vaporizer test that did not include blood testing, it was found that an average of only about 35 percent of the available THC was exhaled by the subjects.
For oral intake (food and/or drink) the maximum THC blood concentration is determined after 60 to 120 minutes. Some of the THC is digested by gastric acid, but most of it is absorbed in the upper gastric region and reaches the liver via the portal vein. At this stage, most of the THC is metabolized; only 4 to 12 percent of the ingested THC gets into the consumers blood circulation. However, some metabolites of THC, especially the metabolic product 11-hydroxy-THC (11-OH-THC), act similarly psychoactive to THC after passing through the liver.
The Efficiency of Cannabis Suppositories
In the studies to which all medical claims have been based so far, it has been found that the bioavailability of rectally applied THC is significantly increased if the THC molecule is <a data-ipb="nomediaparse" href="https://en.wikipedia.org/wiki/Transesterification">transesterified
</a> beforehand. The THC-Ester THC-hemisuccinate (THC-HS) is absorbed better in the rectum, it then passes directly into the bloodstream to reach the liver where it is finally metabolized. The first <a data-ipb="nomediaparse" href="https://www.google.com/patents/DE69432527T2?ei=Vo7qTeXoF4SesQPyrdnwDQ">patent</a>
for such THC suppositories was filed in 1994. In relevant forums, you will also find detailed <a data-ipb="nomediaparse" href="https://forum.grasscity.com/threads/prep-of-delta-9-thc-hemisuccinate-thc-hs.992687/">instructions</a>
how to transesterify THC into THC-HS. In addition, the medical experts in the mid-90s found that plant fats such as coconut fat are poorly suited as THC carriers. Any active substances in a suppository must first <a data-ipb="nomediaparse" href="https://books.google.nl/books?id=s_FrCgAAQBAJ&pg=PA340&lpg=PA340&dq=rectal+absorption+of+fat&source=bl&ots=kGJcr-Sjwt&sig=Ab7IgcLPXGOcCLrXELtKf4tFcpQ&hl=en&sa=X&ved=0ahUKEwiX9oSTkrfPAhVImBoKHajUC9QQ6AEIPzAG#v=onepage&q=rectal%20absorption%20of%20fat&f=false">dissolve</a>
in the aqueous mucus of the rectum before entering the bloodstream. Without the transition through the aqueous mucus layer, the THC can not be absorbed directly. Greasy or oily carriers like the cocnut fat mentioned above reduce absorption, active substances such as cannabinoids should not be combined with them for the preparation of suppositories. The best bioavailability was achieved when THC was linked to THC-hemisuccinate and a pharmaceutical glycerol (Witespot 15, a substance often used in suppositories, as carrier material). The bioavailability strongly differed depending on suppository formulations. Comparing THC-HS to other polar esters of THC, Witepsol H15 mixed with THC-HS showed the highest bioavailability when evaluated in monkeys. The carrier substance is offered as an emulsifying wax for suppository-production by pharmaceutical wholesalers and has similar properties as the less effective greasy or oily carriers. With the transesterified active substance, an average THC content of 13.5 percent was found in the monkeys under evaluation. The rectal bioavailability of this formulation was calculated to be about as twice as high as oral bioavailability of THC.....
<a data-ipb="nomediaparse" href="http://www.marijuana.com/blog/news/2017/02/science-vs-experience-how-effective-are-cannabis-suppositories/">http://www.marijuana.com/blog/news/2017/02/science-vs-experience-how-effective-are-cannabis-suppositories/</a>
By <span><a data-ipb="nomediaparse" href="http://www.marijuana.com/blog/news/author/mknodt/" title="Posts by Michael Knodt">Michael Knodt</a> </span> on <span> </span>
<span>February 24th, 2017 </span>
There are numerous, very contradictory reports on the rectal application of cannabis online that range from <a data-ipb="nomediaparse" href="http://www.greenbridgemed.com/rectal-absorption-of-cannabis-revisited/">absolutely ineffective</a>
to <a data-ipb="nomediaparse" href="https://www.hellomd.com/health-wellness/the-butt-of-the-story-why-rectal-cannabis-is-a-great-choice-for-many-patients">best ever</a>
. The research on this type of medicine intake is almost non-predictive because there are only two relatively small studies from <a data-ipb="nomediaparse" href="https://www.ncbi.nlm.nih.gov/pubmed/2985774">1985</a>
and <a data-ipb="nomediaparse" href="https://www.researchgate.net/publication/246901979_Rectal_bioavailability_of_D-9-tetrahydrocannabinol_from_the_hemisuccinate_ester_in_monkeys">1991</a>
. Both studies conclude that the bioavailability of THC taken rectally is very poor compared to eating or inhaling.
On the other hand, there are many positive and <a data-ipb="nomediaparse" href="https://www.merryjane.com/health/what-you-need-to-know-about-using-cannabis-suppositories">credible testimonials</a>
from patients and consumers, most of them reporting a muscle-relaxing and pain-relieving effect. Further to that, people <a data-ipb="nomediaparse" href="https://sensiseeds.com/en/blog/recreational-rectal-use-cannabis-science/">report </a>
a long lasting high after having applied cannabis rectally. Individuals report that the psychoactive effect is not as distinctive as smoking or eating, but that it does last longer.
How much THC actually gets into the blood when smoking or eating?
The bioavailability of inhaled or ingested cannabis is not as significant as one may expect.
Depending on the depth of inhalation, the duration of the puff, and the length of time the inhalant stayed in the lung, only 10 to 35 percent of the available THC in a joint will reach the smokers bloodstream; 65 to 90 percent of lost THC is a result of side streams and incomplete uptake of THC via the mucosa of the respiratory tract; 30 percent is lost through combustion before inhalation. Vaporizing cannabis, however, is more effective. In a vaporizer test that did not include blood testing, it was found that an average of only about 35 percent of the available THC was exhaled by the subjects.
For oral intake (food and/or drink) the maximum THC blood concentration is determined after 60 to 120 minutes. Some of the THC is digested by gastric acid, but most of it is absorbed in the upper gastric region and reaches the liver via the portal vein. At this stage, most of the THC is metabolized; only 4 to 12 percent of the ingested THC gets into the consumers blood circulation. However, some metabolites of THC, especially the metabolic product 11-hydroxy-THC (11-OH-THC), act similarly psychoactive to THC after passing through the liver.
The Efficiency of Cannabis Suppositories
In the studies to which all medical claims have been based so far, it has been found that the bioavailability of rectally applied THC is significantly increased if the THC molecule is <a data-ipb="nomediaparse" href="https://en.wikipedia.org/wiki/Transesterification">transesterified
</a> beforehand. The THC-Ester THC-hemisuccinate (THC-HS) is absorbed better in the rectum, it then passes directly into the bloodstream to reach the liver where it is finally metabolized. The first <a data-ipb="nomediaparse" href="https://www.google.com/patents/DE69432527T2?ei=Vo7qTeXoF4SesQPyrdnwDQ">patent</a>
for such THC suppositories was filed in 1994. In relevant forums, you will also find detailed <a data-ipb="nomediaparse" href="https://forum.grasscity.com/threads/prep-of-delta-9-thc-hemisuccinate-thc-hs.992687/">instructions</a>
how to transesterify THC into THC-HS. In addition, the medical experts in the mid-90s found that plant fats such as coconut fat are poorly suited as THC carriers. Any active substances in a suppository must first <a data-ipb="nomediaparse" href="https://books.google.nl/books?id=s_FrCgAAQBAJ&pg=PA340&lpg=PA340&dq=rectal+absorption+of+fat&source=bl&ots=kGJcr-Sjwt&sig=Ab7IgcLPXGOcCLrXELtKf4tFcpQ&hl=en&sa=X&ved=0ahUKEwiX9oSTkrfPAhVImBoKHajUC9QQ6AEIPzAG#v=onepage&q=rectal%20absorption%20of%20fat&f=false">dissolve</a>
in the aqueous mucus of the rectum before entering the bloodstream. Without the transition through the aqueous mucus layer, the THC can not be absorbed directly. Greasy or oily carriers like the cocnut fat mentioned above reduce absorption, active substances such as cannabinoids should not be combined with them for the preparation of suppositories. The best bioavailability was achieved when THC was linked to THC-hemisuccinate and a pharmaceutical glycerol (Witespot 15, a substance often used in suppositories, as carrier material). The bioavailability strongly differed depending on suppository formulations. Comparing THC-HS to other polar esters of THC, Witepsol H15 mixed with THC-HS showed the highest bioavailability when evaluated in monkeys. The carrier substance is offered as an emulsifying wax for suppository-production by pharmaceutical wholesalers and has similar properties as the less effective greasy or oily carriers. With the transesterified active substance, an average THC content of 13.5 percent was found in the monkeys under evaluation. The rectal bioavailability of this formulation was calculated to be about as twice as high as oral bioavailability of THC.....
<a data-ipb="nomediaparse" href="http://www.marijuana.com/blog/news/2017/02/science-vs-experience-how-effective-are-cannabis-suppositories/">http://www.marijuana.com/blog/news/2017/02/science-vs-experience-how-effective-are-cannabis-suppositories/</a>
