Oral intake of a cannabinoid together with a meal

Oral intake of a cannabinoid together with a meal improved bioavailability by avoiding first-pass metabolism


Researchers of Monash University in Victoria, Australia, investigated the reason why the oral bioavailability of a synthetic cannabinoid receptor agonist (CRA13) was significantly improved if taken together with a meal rich in fat. Oral bioavailability was assessed in human volunteers and in dogs with and without a meal. Food had a substantial positive effect on the oral
bioavailability of CRA13 in human volunteers and in dogs. This cannabinoid is highly lipophilic (soluble in fat) as other cannabinoids including THC.

The absolute bioavailability of the cannabinoid was low in fasted dogs (8-20 per cent), in spite of good absorption (72-75 per cent of radio-labelled CRA13 recovered in the systemic circulation). In fed dogs, bioavailability increased to 47.5 per cent and the majority (43.7 per cent) of the dose was absorbed via the lymphatic system of the intestine. Researchers concluded that the positive food effect for CRA13 does not appear to result from
increased absorption. Rather the increase in bioavailability was stimulated via almost complete transport into the lymph, in turn resulting in a reduction in first-pass metabolism. In fasted dogs most of the cannabinoid was metabolised, i.e. changed to inactive compounds, at once in the liver before reaching the whole body, while the liver was bypassed in fed animals.

(Source: Trevaskis NL, Shackleford DM, Charman WN, Edwards GA, Gardin A, Appel-Dingemanse S, Kretz O, Galli B, Porter CJ.
Intestinal Lymphatic Transport Enhances the Post-Prandial Oral
Bioavailability of a Novel Cannabinoid Receptor Agonist Via
Avoidance of First-Pass Metabolism. Pharm Res. 2009 Mar 12.

Full report is attached below.

Thanks for posting this mate! Interesting stuff.

However I wonder if CRA13 (a synthetic not found in natural cannabis) behaves like 11-hydroxy when eaten? It's a different molecule, albeit an analogue.
This is part of Norvartis Pharmaceuticals' research into making Rx products that block the effects of natural cannabinoids and endocannabinoids.

Sorry I don't understand exactly what this is about.

Is it some scientist that learned that THC binds with fat/alcohol?


Maybe I just smoked a bit to much Ill try to read it again later

For those of you who don't speak "Sci"

For those of you who don't speak "Sci"

At Monash University in Australia, scientists wondered why you get higher when you eat your "edibles" with a high fat meal. They used both humans and dogs to see how this worked with a synthetic cannabinoid- CRA 13 which, like THC, mixes easily with fats.

The hungry dogs' bodies absorbed the CRA13, but only 8 to 20% could be used. Fed dogs were able to use 47.5% of the CRA13 and absorbed most of it through their guts. It doesn't look like the fed dogs absorbed more. Instead, they think the dogs' bodies were too busy digesting everything and missed absorbing most of the CRA13 until it was in their guts. The dogs' guts sent it right into the lymphatic system where the active CRA13 spreads through their bodies and got them high. In hungry dogs bodies, most of the CRA13 was absorbed right off the bat in the stomach and then was sent directly to the liver where it was changed into inactive byproducts, resulting in less of a high.


So eat your "edibles" with a high fat meal. It may take a bit longer, but the high will be better. If you eat it while hungry, much of the THC will go through your liver and it get changed to something else. If your stomach is "busy" with other foods, the THC will get absorbed in your guts and bypass the liver, going into the lymph system and through your body.

Granny

It's a very interesting finding for therapeutic administration of some pharmaceutical cannabinoids, but may have limited bearing on administration of therapeutic cannabis or even Marinol for that matter as delta-*-THCs available form the plant and from synthetic Marinol are prodrugs from 11-HO-THC (i.e., delta-9,1,8-THC's are metabolized into the more potent and longer lasting 11-HO-THC through first pass metabolism). Now if it is found that delta-9-THC and the like are absorbed in the same fashion following co-administration of oral doses with food that would be very worth knowing for the therapeutic cannabis using community. Indeed this might explain why the same dose of cannabutter baked into something like bannana bread can appear to have greater faster impact than the same dose of cannabutter taken in gel caps.

huh huh, huh, huhuhu huh, you said ORAL, huh huh....

^In your case idiot, I might make it a fucking big suppository!

So is it because the cannabis is absorbed slower due to energy being used to absorb the meal that was fed first? How does conversion change from the gut to the liver? Guess Im the only one who liked beavis and butthead, heh heh, heh....

Moose thanks for posting and also for simplifying for us non-sci peeps...DD

Thanks for this information.

It shows the reason why avocado and nuts and seeds eaten with cannabis is more effective than just eating the cannabis with sugars becuse most of the oils in them are long chained which takes longer to break down than sugars and short/medium chained fats such as coconut oil.

Also, to increase the effect taking grapefruit juice and other citrus fruits as well as fruits in general will increase the effects because they inhibit the p450 enzymes which convert a lot of the thc into inactive metabolites. If you eat different fruit daily it will help prevent you from getting used to the bud and will always get a good high from the same herb if smoked daily.

If you eat some ghee(clarified butter, the more yellow the better) and coconut oil with your food as well as nuts, seeds, avocado and eat different fruit daily you will get the benefit of having a potent high because some of the cannabinoids mixed with the ghee and coconut oil will get turned into a more potent form during the first pass into the liver and the rest will go to the lymphatic system to be slowly released into the bloodstream.

Smoking Moose said:

^In your case idiot, I might make it a fucking big suppository!

Click to expand...

Obviously not a Beavis and Butthead fan?

No mate, it's not that. It's just that I do not find anything funny about medicinal cannabis. It is a serious business and it should be treated seriously. I have a box full of suppositories put aside for idiots who mock serious issues, including one suppository with Habanero paste included, for that extra kick in the ass lol.