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Researchers inject mice with CRUDE CANNABIS (?)

red22

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Back when I was asking if the microemulsion process used for IVing poorly water soluble drugs could be used for hash I was given a lot of grief, so I find this to be a little ironic.


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Gill ER, Jones G. Brain levels of Δ1-tetrahydrocannabinol and its metabolites in mice-correlation with behavior, and the effect of the metabolic inhibitors SKF 525A and piperonyl butoxide. Biochem Pharmacol 1972; 21:2237-2248.

Bottom of page 2245.

You can get a full copy on http://libgen.org
 
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It's from 1972... Can't help but feel that it's going to be some bullshit study supporting the 'war on drugs' which was heavily emerging.
 
Just because you can inject crude cannabis doesn't mean you should.
 
So what's the differential on people injecting cleaned up (crudely purified - sorry for the oxymoron - i.e. enough to let it pass a wheel filter) extract of cannabis vs. extract of opium vs. extract of DMT-containing plant material?
Not sure what they mean in the quote in the OP, but if they mean crude and unseparated mix of actives though filtered... it would make sense. (Other good luck with the -4 gauge needle.)

THC-like cannabinoids not being water soluble is one issue of course, but in clinical settings they should be able to handle that. I've been experimented on with IV delta-9 and I still don't know how they dissolve and IV hydrophobics like that and likewise for IV benzos. I've been meaning to ask.
 
Just because some scientists injected MICE with poorly filtered drugs 42 years ago doesn't mean you should experiment with this yourself....or you can try, and get very sick. This is no justification.
 
THC-like cannabinoids not being water soluble is one issue of course, but in clinical settings they should be able to handle that. I've been experimented on with IV delta-9 and I still don't know how they dissolve and IV hydrophobics like that and likewise for IV benzos. I've been meaning to ask.

People ether use non-water solvents to dissolve the drug (like injectable diazepam) or form a milk-like emulsion of oil in water (like propofol). Usually it needs high-shear mixing and some biologically inert surfactants to make it stable.

Technically you could emulsify hash oil or any oil fraction of cannabis with Cremophor and sterile water and have a bag of injectble THC. The problem is it would be hard to make, standardise, and of course messy and a hassle to administer rather than just baking a tray of brownies or smoking a bowl. It would also be way more likely to cause allergic reactions.
 
Wouldn't THC dissolve in oil just like injectable steroids?
 
Apparently glycerine is used as a non polar IV solvent.

Thanks for bumping this thread. I have way more info than that, but I forgot to post it. I was going to post it in response to Solipsis's post. Here are several studies in which THC, et al, were administered to humans intravenously, all of which detail the formulas used. One study is about water-soluble chemical modifications to cannabinoids.

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Contents:

Intravenous injection in man of 9 -tetrahydrocannabinol and 11-OH- 9 -tetrahydrocannabinol. Perez-Reyes M, Timmons MC, Lipton MA, Davis KH, Wall ME. Science. 1972 Aug 18;177(4049):633-5.

A comparison of the pharmacological activity in man of intravenously administered delta9-tetrahydrocannabinol, cannabinol, and cannabidiol. Perez-Reyes M, Timmons MC, Davis KH, Wall EM. Experientia. 1973 Nov 15;29(11):1368-9

Oral and parenteral formulations of marijuana constituents. Rosenkrantz H, Thompson GR, Braude MC. J Pharm Sci. 1972 Jul;61(7):1106-12

Development and pharmacokinetic characterization of pulmonal and intravenous delta-9-tetrahydrocannabinol (THC) in humans. Naef M, Russmann S, Petersen-Felix S, Brenneisen R. J Pharm Sci. 2004 May;93(5):1176-84

Pharmacological characterization of novel water-soluble cannabinoids. Martin BR, Wiley JL, Beletskaya I, Sim-Selley LJ, Smith FL, Dewey WL, Cottney J, Adams J, Baker J, Hill D, Saha B, Zerkowski J, Mahadevan A, Razdan RK. J Pharmacol Exp Ther. 2006 Sep;318(3):1230-9. Epub 2006 Jun 6.


And here are books on the preparation of water-insoluble drugs. I had originally come across a preview of the first one when I was Googling to understand more about the preparation of water-insoluble drugs; wasn't able to download it, but came across a full copy of another one listed; and eventually was able to download the first one on bookfi.org and came across even more books on the topic via their search and eventually downloaded all the ones listed below. I recommend http://libgen.org because it searches BookFi and it's a bigger operation (the highlight is the scientific articles search engine). Best source for ebooks I've come across is the invite-only http://ebook.farm btw (includes academic books).


Formulating Poorly Water Soluble Drugs (AAPS Advances in the Pharmaceutical Sciences Series). Robert O. Williams III, Alan B. Watts and Dave A. Miller (2011)

Water-Insoluble Drug Formulation. Rong Liu (2008)

Microemulsions: Properties and Applications. Monzer Fanun (2008)

Handbook of Microemulsion Science and Technology. Promod Kumar & K.L. Mittal (1999)

Microemulsions: Background, New Concepts, Applications, Perspectives. Cosima Stubenrauch (2008)


Good definition of emulsion, the type of formula used for IV cannabinoids.


Source: http://pharmlabs.unc.edu/labs/emulsions/intro.htm


Introduction


An emulsion is a thermodynamically unstable two-phase system consisting of at least two immiscible liquids, one of which is dispersed in the form of small droplets throughout the other, and an emulsifying agent. The dispersed liquid is known as the internal or discontinuous phase, whereas the dispersion medium is known as the external or continuous phase. Where oils, petroleum hydrocarbons, and/or waxes are the dispersed phase, and water or an aqueous solution is the continuous phase, the system is called an oil-in-water (o/w) emulsion. An o/w emulsion is generally formed if the aqueous phase constitutes > 45% of the total weight, and a hydrophilic emulsifier is used. Conversely, where water or aqueous solutions are dispersed in an oleaginous medium, the system is known as a water-in-oil (w/o) emulsion. W/O emulsions are generally formed if the aqueous phase constitutes < 45% of the total weight and an lipophilic emulsifier is used.

Emulsions are used in many routes of administration. Oral administration can be used, but patients generally object to the oily feel of emulsions in the mouth. But some times, emulsions are the formulation of choice to mask the taste of a very bitter drug or when the oral solubility or bioavailability of a drug is to be dramatically increased.

More typically, emulsions are used for topical administration. Topical emulsions are creams which have emollient properties. They can be either o/w or w/o and are generally opaque, thick liquids or soft solids. Emulsions are also the bases used in lotions, as are suspensions. The term "lotion" is not an official term, but is most often used to describe fluid liquids intended for topical use. Lotions have a lubricating effect. They are intended to be used in areas where the skin rubs against itself such as between the fingers, thighs, and under the arms.

Emulsions are also used a ointment bases and intravenously administered as part of parenteral nutrition therapy. Their formulation and uses in these roles will be covered in the appropriate chapters.

The consistency of emulsions varies from easily pourable liquids to semisolid creams. Their consistency will depend upon:
the internal phase volume to external phase volume ratio [*]in which phase ingredients solidify [*]what ingredients are solidifying


Stearic acid creams (sometimes called vanishing creams) are o/w emulsions and have a semisolid consistency but are only 15% internal phase volume. Many emulsions have internal phases that account for 40% - 50% of the total volume of the formulation. Any semisolid character with w/o emulsions generally is attributable to a semisolid external phase.


W/O emulsions tend to be immiscible in water, not water washable, will not absorb water, are occlusive, and may be "greasy." This is primarily because oil is the external phase, and oil will repel any of the actions of water. The occlusiveness is because the oil will not allow water to evaporate from the surface of the skin. Conversely, o/w emulsions are miscible with water, are water washable, will absorb water, are nonocclusive, and are nongreasy. Here water is the external phase and will readily associate with any of the actions of water.

Emulsions are, by nature, physically unstable; that is, they tend to separate into two distinct phases or layers over time. Several levels of instability are described in the literature. Creaming occurs when dispersed oil droplets merge and rise to the top of an o/w emulsion or settle to the bottom in w/o emulsions. In both cases, the emulsion can be easily redispersed by shaking. Coalescence (breaking or cracking) is the complete and irreversible separation and fusion of the dispersed phase. Finally, a phenomenon known as phase inversion or a change from w/o to o/w (or vice versa) may occur. This is considered a type of instability by some.
 
Your welcome, Solipsis.

So what exactly happens to the oil that is a part of black tar heroin when black tar heroin is injected? Does it just get rebounded by the BBB and get excreted?
 
By the way, Solipsis, can you tell about your intravenous THC experience?
 
Yeah, well the setting was only so-so since I was walking around with a cannula in my arm and it was a private research center: some of it was made comfortably, but other parts were reminding of a hospital. Each study lasted a week. And each day they randomly administered either a certain dosage of cannabinoid, or a set dose of midazolam or placebo via bolus IV, double blind.
Obviously I didn't really feel like doing the tests, like a sway test that checked how well I could stand up without swerving all over the place, or memory tests etc. There were just guys and gals looking at me seriously while I was either kinda sedated, or (obviously) sober, or moderately to strongly stoned / high. I didn't truly mind the tests, but of course it is not what I would prefer to do when high. Still, compared to odd jobs it is pretty cool IMO.

By the way I participated in such studies twice, both times with cannabinoids, and I am not really sure actually if it was THC or if there were other new water-soluble synthetics. I really have to contact them sometime... IIRC what they injected me with was all clear, no emulsion or anything. So maybe water soluble stuff after all?
One of those times a friend participated in the trial with me.

I remember once getting a lunch-break and not being able to stop laughing :D that was definitely not a placebo day. I think it is kind extraordinary to have such a clean feeling of being high, without having smoked anything, and it being a single substance in a single 'hit'. Home-made hash oil is also very "neat" stuff and vaped cannabis might also be an interesting comparison, but still hardly anything could be as pure and potent as that stuff they had there. From what I can tell it felt natural like a THC or THC-like compound, not like a JWH-xxx or anything. But of course who can be sure.

Some other time, there was a dude who totally lost it... apparently he had never been stoned before, and he was running up and down the corridor screaming and mowing his arms. He had to be brought to the (very nearby) medical care unit where he apparently peed a record amount of piss. We were informed later that he was fine and there were no physical issues involved... but they still had to shut down the study and we got our money anyway...
 
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Can one simply intramuscularly inject THC, by the way? Cuz aren't steroids oils (which are IMed all the time)?


THC is a light yellow resinous oil, sticky at room temperature which hardens upon refrigeration. THC is highly lipophilic, practically insoluble in water, having an octanol:water partition coefficient of 6,000:1 (at pH 7).87

87. Gill ER, Jones G. Brain levels of Δ1-tetrahydrocannabinol and its metabolites in mice-correlation with behavior, and the effect of the metabolic inhibitors SKF 525A and piperonyl butoxide. Biochem Pharmacol 1972; 21:2237-2248.
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Cannabinoids. Vincenzo Di Marzo (2004), p. 16.
 
I don't understand your post. Like I said, aren't steroids of the same makeup as THC?
 
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