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HPBCD DMT very bioavailable sublingually under tongue, combo with tetrahydroharmine, Ayahuasca Options
 
murklan
#21 Posted : 5/12/2021 7:47:59 AM

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Thanks for the posts and findings ava69, really interesting. I find it hard to get hold of HPBCD (I'm in europe) but if I can I will experiment with it for sure.
 

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ava69
#22 Posted : 5/12/2021 12:23:22 PM

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Murklan said:
Quote:
Thanks for the posts and findings ava69, really interesting. I find it hard to get hold of HPBCD (I'm in europe) but if I can I will experiment with it for sure.
Appreciate the kind words Murklan. I have seen it for sale in Europe at couple places, just google "add to cart hydroxy propyl beta cyclodextrin euro" Auction sites and elsewhere carry it.

I bought my 1kg tub from a supplier of sports supplements 12 years ago, as it was sold right along side pro-hormones which converted to testosterone in the body at a rate of 95% compared to testosterone alone, as you guessed, all pro-hormones like 4-androstenediol were all later banned.

I've been a weight lifter/bodybuilder since my early 20's when I was a full time lifeguard on the beach (love the water, water spirit)...currently my bodyweight is 220lbs at 12 percent bodyfat, follow a strict Palumbo high-protein keto-diet daily for years, 1.2 grams protein per lb of bodyweight per day. I get all my meals and 65 gram protein shake within an 8 hour window everyday (6am till 3pm), and fast after 3pm till I wake up the next day. This keeps my bodyfat low yet retains all the muscle. I run on the treadmill during the fasting period once I get home for 20 to 30 minutes at least 3 times a week. I take bcaa's before I hop on treadmill to keep any muscle from breaking down.

Even at this weight, I still find that 200mg of harmine completely inhibits the monoamine oxidase in my body...in all of my 70 Ayahuasca experiences using 200mg harmine + 220 to 250mg tetrahydroharmine over many years, I find the alkaloid amounts to completely activate 30 to 35 grams of Hawaiian psychotria to the full extent.

Later tonight I will take 200mg harmine + 250mg tetrahydroharmine + 70mg HPBCD DMT (490mg HPBCD powder kneaded, crushed & stirred for 30 seconds into 70mg DMT on a spoon with many drops of water forming a sticky complex for the oral use)...I will report back. Several papers I have read indicate that HPBCD complexed pharmaceuticals even when delivered orally out-performed normal oral versions of themselves by many factors.

I always mix everything together into a 2oz hot water tea with a dash of crushed vitamin C to dissolve the freebase harmine and THH, along with the HPBCD DMT, stir all together well in the hot water tea, just as the Shaman's do, take all together at exact same time, works incredibly well, far better than spacing out the DMT from the harmalas, I should know, I ran several experiments years ago, and the tea where ALL was mixed together outperformed all the other trials consistently.
 
ava69
#23 Posted : 5/12/2021 3:53:21 PM

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Here is the HPBCD DMT solution ready to go for tonight

1. Materials: 70mg DMT for oral use, 490mg HPBCD, 1ml pipette, 0.25 to 0.50ml VERY HOT water from a nearby microwaved coffee cup of hot water.

2. Made a 1:1 molar ratio (1:7 mg ratio) of host drug DMT to HPBCD by adding 70mg of DMT onto spoon, added 490mg of HPBCD on top DMT, add 0.500 ml of VERY HOT near boiling water (10 drops) drawn up with pipette from microwaved water in coffee cup. For sublingual use don't overdo the drops, 0.250ml of water (5 drops) is plenty...if you accidentally add too much water then run a fan over spoon to evaporate some of it off.

Knead, mash and stir it all together for 2 minutes using the end of a spoon, notice the two separate powders turn into a homogenous transparent solution when done mashing.

3. For oral use, add the spoon of HPBCD DMT water to 2oz of hot water (120 degree F), it will all dissolve instantly into a totally clear homogenous solution (bottom left photo), take PH of water, it is safe to drink, reads ph = 8 to 9.

4. Store in fridge till later, when ready heat water back up in a pyrex dish on stove to 110 degree F or so, add 200mg harmine + 150 to 250mg tetrahydroharmine, add 150mg pure ascorbic acid (vit C) to help dissolve harmine & THH if they are in freebase form.

Stir all together and consume in dreams, just the way the Shaman's do it, take it ALL mixed together at the exact same time, works incredibly well this way, have over 70 experiences with Ayahuasca over many years.

5. Several papers I have read indicated that HPBCD complexed pharmaceuticals even when delivered orally out-performed normal oral versions of themselves by many factors.

490mg of HPBCD powder may look like alot when laid out, but when even just a few drops of hot water is added to it, it shrinks into a small sticky clear liquid mass as it is derived from a sugar molecule.

With the Ayahuasca journey, she guides you to the existence of a higher spiritual plane...recognized to which insight can and must be gained, yet it does not reject the mundane reality as inferior or empty. This joyous embracement of the world of form leads to words like profound pleasure, beauty and joy. This loving reappraisal of the worldly forms leads the way to higher divine planes.

Last pic: beautiful Shaman woman
ava69 attached the following image(s):
57.JPG (71kb) downloaded 541 time(s).
 
Brennendes Wasser
#24 Posted : 5/12/2021 5:28:27 PM

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Interestingly I found out that a colleague at work also has HPBCD and ACD. I thought of trying the Salvia-complexation-thing.

But I did not find any real procedure for this on the nexus. I thought I will need to make sure that both ingredients will be soluble in the same solvent, for maximized contact. This can only be achieved for pure mixtures in DMSO and this is not a solvent to be removed again.

But I figured out some mixtures of Acetone to use for Salvinorin AND HPBCD.

Dissolve Salvinorin in minimal amount of Acetone, add 4x volume of water afterwards. 20 % Acetone in Water still keeps Salvinorin dissolved. Then you can dissolve any HPBCD.

ACD has a much worse solubility (HPBCD seems to be just made for improved solubility in general) and will not do the trick. Then you could stirr and cause complexation.




Now while you have DMT and not Salvinorin this is not directly comparable, but I am still quite wondering why only plain water can be used. I mean yes the dissolved HPBCD may take up the DMT. But if the DMT will NEVER get dissolved in the first place, then there is no contact between guest and host. So I really wonder if this would really do the trick, if you just have a suspension of DMT?

Normally I would assume this leads to a HPBCD-solution with suspended DMT Confused

Maybe I should try with Salvia and my solvent mix and then try pure water ...
Check the

BIG Analysis on DMT !

Lots of interesting and possibly new stuff unraveled ;o
 
ava69
#25 Posted : 5/12/2021 11:12:01 PM

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Brennedes Wasser said:
Quote:
Interestingly I found out that a colleague at work also has HPBCD and ACD. I thought of trying the Salvia-complexation-thing.

But I did not find any real procedure for this on the nexus. I thought I will need to make sure that both ingredients will be soluble in the same solvent, for maximized contact. This can only be achieved for pure mixtures in DMSO and this is not a solvent to be removed again.

But I figured out some mixtures of Acetone to use for Salvinorin AND HPBCD.

Dissolve Salvinorin in minimal amount of Acetone, add 4x volume of water afterwards. 20 % Acetone in Water still keeps Salvinorin dissolved. Then you can dissolve any HPBCD.

ACD has a much worse solubility (HPBCD seems to be just made for improved solubility in general) and will not do the trick. Then you could stirr and cause complexation.

Now while you have DMT and not Salvinorin this is not directly comparable, but I am still quite wondering why only plain water can be used. I mean yes the dissolved HPBCD may take up the DMT. But if the DMT will NEVER get dissolved in the first place, then there is no contact between guest and host. So I really wonder if this would really do the trick, if you just have a suspension of DMT?

Normally I would assume this leads to a HPBCD-solution with suspended DMT Confused

Maybe I should try with Salvia and my solvent mix and then try pure water ...
Very interesting Brennendes Wasser, thanks for sharing!


Part 12: 70mg DMT complexed to 490mg HPBCD oral Ayahuasca report, +5 Shulgin scale


Well, maybe I can end the confusion a little bit on the HPBCD DMT. The experiment was a success...I took the 70mg DMT complexed to 490mg of HPBCD all kneaded/crushed using end of another spoon...and mixed on a spoon for 2 minutes with 0.500 milliliter of VERY HOT near boiling water (around 10 drops of water). What I do is heat up a bit of water in a coffee cup in microwave & draw up drops of it using pipette. I read using hot water speeds & aids the mixing of the HPBCD to host drug.

I added the 0.5ml spoon full HPBCD DMT solution to 2oz of 120 degree hot water...this then immediately turned into 100% transparent water when it hit the hot liquid in the pyrex cup...This was stored in fridge until use...then when I was ready, the 2oz clear transparent liquid HPBCD DMT water solution, once re-heated up in pyrex pot on stove, to this was then added 200mg harmine + 250mg THH and also 150mg of pure ascorbic acid (vit C) to help dissolve the freebase harmine + thh.

I gulped it down in one shot...there was virtually no taste! I think the HPBCD completely masked the taste of the nasty DMT...I was shocked...took it all together at same time at 3:30, I'm writing this 3 hours later.

It came on exactly like 30 grams of hawaiian psychotria! there was no difference between this and the leaf brew, again I was shocked...it gripped me powerfully, heavy tryptamine buzz and high frequency. The THH already imparts a body frequency buzz + DMT tryptamine buzz = amazing amplified body frequency.

A vibrating neon colored fortress like a magnetic field surrounded me in the room, it shined off of every object similar to a UV blacklight glow...this neon visual vibration appeared all around me, given off by everything around me. The vibrational frequency field reminded me of the tractor beam in Star Trek when they would transport. I've experienced this same phenomena with past journeys involving 30 to 35 grams of potent Hawaiian psychotria...but never with plain freebase DMT or DMT salts before, only again with this HPBCD DMT.

I had to remain in one spot sitting as it was so strong for 1 hour straight, the walls in the room filled with 3-D ish like honeycomb orange & brown geometrics that appeared to bulge slightly off the surface, like the inside of a bee hive, neon colors were abundant, heavy tracers...the beauty all around me was infinite, beautiful CEV's (spinning and dancing or constantly morphing geometrics) and OEV...I was amazed to say the least.

In conclusion, I am impressed with this route of administration via sublingual or oral.

During the oral Ayahuasca journey (200mg harmine + 250mg THH + 70mg DMT complexed to 490mg HPBCD) for the first hour, all objects glowed or shined as if in caught in a neon colored magnetic transporter beam.
ava69 attached the following image(s):
For the first hour, all objects shown as if in caught in a neon colored magnetic transporter beam.JPG (77kb) downloaded 640 time(s).
 
ava69
#26 Posted : 5/14/2021 12:56:39 PM

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Update at 8pm 5/12/21 around 5 hours later same night, the 250mg 10.5 hour half-life tetrahydroharmine (THH) was still active in my body.

Took sublingual 35mg DMT complexed to 245mg HPBCD on a spoon with less than 0.25ml (only 5 drops) of VERY HOT near boiling water, this was using water that was pre-heated up in microwave in coffee cup, then taken up with end of pipette, and dropped onto spoon with the HPBCD powder/DMT crystals. I kneaded, mashed & mixed it all together using end of a spoon for 2 minutes.

It ALL dissolved into a clear sticky solution after mashing it with end of spoon for 2 minutes--I drew it up from spoon using pipette and placed drops under tongue. It felt like all the DMT dissolved into bloodstream, experienced great effects held under tongue for 15 minutes--sweet taste, as the outer shell of HPBCD is formed from a sugar molecule--no burn! It helped mask the taste of the nasty DMT.

5 minutes after the 15 minute sublingual period, my heart rate & pulse greatly increased, pupils dilated when I looked in mirror, had colored CEV visuals and long CEV lingering after images, open eyed beauty was profound, music sounded incredible once again, felt euphoria and elation. Zero nausea.

Highly recommend complexing DMT to HPBCD for oral use, which simulates actual very strong (+5 Shulgin scale) hawaiian psychotria leaf brew imho, as I've had over 70 hawaiian psychotria + Caapi journeys in the past over many years, or for sublingual use. The HPBCD complexed DMT imho absorbs many factors better than plain DMT freebase or DMT salts in the body, as I have over a dozen experiences with the oral freebase and DMT formed salts in the past for oral use (all only +3 on Shulgin scale). I was blown away by the oral & sublingual HPBCD DMT.

Oral use: 1:1 molar ratio of host drug DMT to HPBCD powder = 1:7 DMT to HPBCD mg weight ratio (70mg DMT to 490mg HPBCD)

SublinguaL: 1:1 molar ratio of host drug DMT to HPBCD powder = 1:7 DMT to HPBCD mg weight ratio (35mg DMT to 245mg HPBCD)

245mg of HPBCD powder may look like alot when laid out, but when even just a few drops of hot water is added to it, it shrinks into a small sticky clear liquid mass as it is derived from a sugar molecule, perfect for "under the tongue" use.

Highly recommend HPBCD complexed DMT. Smile
 
Loveall
#27 Posted : 5/14/2021 1:50:25 PM

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Brennendes Wasser wrote:
Interestingly I found out that a colleague at work also has HPBCD and ACD. I thought of trying the Salvia-complexation-thing.

But I did not find any real procedure for this on the nexus. I thought I will need to make sure that both ingredients will be soluble in the same solvent, for maximized contact. This can only be achieved for pure mixtures in DMSO and this is not a solvent to be removed again.

But I figured out some mixtures of Acetone to use for Salvinorin AND HPBCD.

Dissolve Salvinorin in minimal amount of Acetone, add 4x volume of water afterwards. 20 % Acetone in Water still keeps Salvinorin dissolved. Then you can dissolve any HPBCD.

ACD has a much worse solubility (HPBCD seems to be just made for improved solubility in general) and will not do the trick. Then you could stirr and cause complexation.




Now while you have DMT and not Salvinorin this is not directly comparable, but I am still quite wondering why only plain water can be used. I mean yes the dissolved HPBCD may take up the DMT. But if the DMT will NEVER get dissolved in the first place, then there is no contact between guest and host. So I really wonder if this would really do the trick, if you just have a suspension of DMT?

Normally I would assume this leads to a HPBCD-solution with suspended DMT Confused

Maybe I should try with Salvia and my solvent mix and then try pure water ...


See attached for a thesis that looked at salvinorin A solubility in water in the presence of an BCD (they used captisol which is similar to HPBCD and has the same inner ring). Solubility increased linearly with the BCD.

I believe there is a finite solubility of DMT FB in water and HPBCD would increases it several fold and linearly with HPBCD concentration.

In the salvinorin complexation thread aqueous ethanol dissolved both salvinorin and HPBCD for complexation - just FYI in case you hadn't seen that already.
💚🌵💚 Mescaline CIELO TEK 💚🌵💚
💚🍃💚 Salvinorin Chilled Acetone with IPA and Naphtha re-X💚🍃💚
 
Loveall
#28 Posted : 5/14/2021 2:15:19 PM

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Note that (as I understand things) linear drug solubility increase with HPBCD concentration is a sign of complexation. The slope when moles are used represents the complexation efficiency (can be > 1 if two molecules fit in one HPBCD site). There are papers with explicit formulas.

As long as there is enough water to dissolve the HPBCD and room for the complex (linear regime), the total amount of complexed drug is a function of the HPBCD and drug ratio, independent of the water volume. Adding more water does nothing other than increase the volume, not the complexation %.

So in practice, choose a drug/HPBCD molar ratio (1 is a good start). Slowly add water till it all dissolves. If drug won't dissolve well try a higher molar ratio. Something along those lines makes sense to me.

ava69, have you tried harmala FB/DMT FB/HPBCD/water paste sublingually. Maybe it would be interesting to try to make an Pharmahuasca/HPBCD paste.
💚🌵💚 Mescaline CIELO TEK 💚🌵💚
💚🍃💚 Salvinorin Chilled Acetone with IPA and Naphtha re-X💚🍃💚
 
ava69
#29 Posted : 5/14/2021 2:41:42 PM

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Loveall said:
Quote:
ava69, have you tried harmala FB/DMT FB/HPBCD/water paste sublingually. Maybe it would be interesting to try to make an Pharmahuasca/HPBCD paste.
Thanks for your reply to Brennendes Wasser above and additional knowledge...very interesting!

Also, you read my mind Loveall, that is my next project. With the oral Ayahuasca, even though it is a mind-blowing powerful experience for 90 minutes, and the next day there is no hangover, the 200mg of harmine always gives me a bit of slight dizziness during the journey, everything else is over the top phenomenal, no nausea, etc. The dizziness turns me off a bit.

Dr. Narang in the 5 page sublingual paper said "under the tongue" pharmaceuticals are at least 3 to 10 times stronger than oral pharmaceutical, so since 200mg of harmine is potent orally, I will use 1/3rd the amount sublingually or 65mg of harmine.

So then complexing 65mg of freebase harmine (1/3rd of an oral dose should work well) to 390mg of HPBCD powder with 5 drops (0.250ml) of VERY HOT water all mashed and mixed on a spoon again for 2 minutes to form a 1:1 molar ratio of harmine to HPBCD for sublingual use under tongue for 15 minutes along with the...sublingual 40mg DMT complexed to 280mg HPBCD using 5 drops of VERY HOT water again should create a powerful experience identical to oral prep...will find out next week.

I will do this all on one spoon next week using less than 10 drops (less than 0.500ml) of very hot water to complex the 65mg harmine + 40mg DMT to 670mg of HPBCD powder, this should again form a transparent clear sticky solution after kneading, mashing and mixing it for 2 minutes or so.

Of course, I always take 250mg of tetrahydroharmine (THH) orally one hour beforehand, as I get no nausea or dizziness from it, and it combines EXTREMELY well with the DMT for an experience nearly identical to true Ayahuasca, but no nausea.

Molecular weight of harmine = 212, molecular weight of HPBCD = 1300. Thus a 1:1 molar ratio = 1:6 host drug to HPBCD mg weight ratio.

670mg of HPBCD powder may look like alot when laid out, but when even just several drops of hot water is added to it, it shrinks into a small sticky clear liquid mass as it is derived from a sugar molecule, perfect for "under the tongue" use.
 
Loveall
#30 Posted : 5/14/2021 2:49:59 PM

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Sublingual harmala FB is pretty strong (but shorter lasting). I would start with a lot less harmalas for sublingual route, maybe, 10mg of harmala FB (harmine/THH mix), 20mg DMT, 200mg HPBCD.

I'm thinking of trying this with the dense paste/knead method.
💚🌵💚 Mescaline CIELO TEK 💚🌵💚
💚🍃💚 Salvinorin Chilled Acetone with IPA and Naphtha re-X💚🍃💚
 
ava69
#31 Posted : 5/14/2021 2:56:59 PM

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Amazing orally see post #25, or sublingual, see post #26.

HPBCD is itself very soluble in water (greater than 1000 mg/ml at room temperature). This increases with VERY HOT near boiling water. So now you see how I used 70mg DMT to 490mg HPBCD in 10 drops for oral use...or the 35mg DMT to 245mg HPBCD in 5 drops very hot water I used for sublingual use.

For example, if one were do an experiment to simulate oral Ayahuasca by complexing 670mg of HPBCD powder to 65mg harmine (1/3rd of an oral dose should work fine) + 40mg DMT all together on a single spoon for "under the tongue" sublingual use in order to avoid the dizziness of using say 200mg oral harmine, (but I always take 150 to 250mg THH orally 1 hour earlier which causes me no nausea or dizziness)...

...this may look like alot when laid out on spoon, but once you add between 5 and 10 drops of very hot near boiling water from a pipette taken up from a nearby coffee mug, the HPBCD shrinks into a small sticky clear liquid mass as it is derived from a sugar molecule, perfect for "under the tongue" use. After 2 minutes or so of kneading and mashing all on the spoon using the end of another spoon with the drops of hot water, it forms a TRANSPARENT CLEAR solution.

P.S. I feel great next 2 days. No hangover, cactus trips are great but usually I feel a bit tired the next day, I feel no tiredness from the oral 200mg harmine + 250mg THH + 70mg dmt complexed to 490mg HPBCD oral journey...the trip is strong for 90 minutes, 3 hours total or so...THH leaves a great afterglow next day.
ava69 attached the following image(s):
HPBCD solubility.JPG (24kb) downloaded 665 time(s).
 
ava69
#32 Posted : 5/14/2021 11:59:19 PM

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Part 14: 300mg Tetrahydroharmine (THH) teaching visions all by itself


At 9pm that same night, took another 100mg of THH, for a total of 350mg of THH for afternoon & night, before I fell asleep, I watched dream-like monochrome imagery (usually always in green or blue for me) as the THH was still working...for around 45 minutes I viewed mind-blowing vistas--grand architecture and cities, a bookshelf full of ancient books, a view of the gardens in front of what looked like Versailles, France.

I traveled down a street in Midieval period where I saw beautiful women walking along the street, I could make out the houses & markets along the street. Many of these visions are like slow speed movies being played, way beyond 4k, highly detailed...true Ayahuasca visions...this always happens when I take at least 300mg or more of tetrahydroharmine during the late afternoon/early night. This is one of the best parts of the journey imho.

I've taken 300mg of THH on it's own many times and for hours with eyes closed I view endless dream-like visions, like slow and high speed movies being played for 2 hours...totally unlike normal dreams, she seems to tap into the "Akashic record" of the universe, the ether where all events, past, present, and future are stored...she shows you artwork, architecture, nature, culture, fantasy, history, the future, spiritual, supernatural. The visions are also characterized by the extraordinary beauty that they manifest.

Tetrahydroharmine was called by one researcher "the tryptamine of the beta-carboline world" to give an example of her remarkable visionary properties. She is an isomer of a hormonal-like compound found in the brain naturally, she is what gives Ayahuasca her telapathine or telethapy properties and CEV dream-like visionary power.

I agree that 300mg THH in Caapi is just as visual as 100mg harmaline (as reported in TIHKAL), but without the nausea and dizziness, but it's not especially visual until say 250 to 300mg, then it gives one 1.5 to 2 hours of incredible closed eye realistic visions, this places it very high on the "psychedelic periodic table" for visions compared to just about any other entheogen.

It's like entering a university, she teaches you for hours with not only sequential visions one after another, but visions seen in continuous slow and high speed movies. She tells you a story for a long period. There is a theme to it all each time, the beautiful visions never repeat session to session. I only rarely go beyond 300mg THH, as a little dizziness sets in above 300mg for sure. No dizziness at 250mg, only a tiny bit at 300mg.

Several weeks ago, after drinking 300mg tetrahydroharmine, I saw the interior decorations of palaces, the checkered floors, the beautiful windows and furniture, the winding stair cases, I was blown away.

I've seen sacred temples for religious worship, beautiful animals and super fine women, birds of all kinds, even the lost city of Atlantis, I was taken in for a bird's eye view, zooming in from way above to all the way down into the city center.

Caapi tells a story when you drink it with eyes closed, she teaches you things, the most beautiful "realistic visions" that no other entheogen comes close to showing you, these realistic visions go on forever with Caapi, I can recline and watch for 2 hours or more the visions, the visions are quite powerful for the first 45 minutes. You can take additional THH hours later to bring back the visions again for another 45 minutes, the doses are additive.

300mg plus of THH showed me closed eye vision of gardens at Versailles, France
ava69 attached the following image(s):
300mg plus of THH showed me CEV of gardens at Versailles, France.JPG (83kb) downloaded 551 time(s).
 
Loveall
#33 Posted : 5/15/2021 1:33:19 PM

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Brennendes Wasser wrote:
Interestingly I found out that a colleague at work also has HPBCD and ACD. I thought of trying the Salvia-complexation-thing.

But I did not find any real procedure for this on the nexus. I thought I will need to make sure that both ingredients will be soluble in the same solvent, for maximized contact. This can only be achieved for pure mixtures in DMSO and this is not a solvent to be removed again.

But I figured out some mixtures of Acetone to use for Salvinorin AND HPBCD.

Dissolve Salvinorin in minimal amount of Acetone, add 4x volume of water afterwards. 20 % Acetone in Water still keeps Salvinorin dissolved. Then you can dissolve any HPBCD.

ACD has a much worse solubility (HPBCD seems to be just made for improved solubility in general) and will not do the trick. Then you could stirr and cause complexation.




Now while you have DMT and not Salvinorin this is not directly comparable, but I am still quite wondering why only plain water can be used. I mean yes the dissolved HPBCD may take up the DMT. But if the DMT will NEVER get dissolved in the first place, then there is no contact between guest and host. So I really wonder if this would really do the trick, if you just have a suspension of DMT?

Normally I would assume this leads to a HPBCD-solution with suspended DMT Confused

Maybe I should try with Salvia and my solvent mix and then try pure water ...


In one salvinorin complexation thread we used aqueous ethanol (75.5% everclear) and that dissolved everything. Got some good results, but ran into issues with repeats. Maybe heat/light were causing issues in the process.

I think there is merit to using only water. Why? Because how the low solubility drug dissolves in water when HPBCD is present informs us of the complexation.

Looking at the details behind this statement. Let's call,

[So], drug solubility in pure water (can be low)
[Ht], total HPBCD concentration

For a 1 to 1 drug (S) and HPBCD (H) complex (SH),

S + H <-> SH

The total amount of cyclodextrin concentration is [Ht] = [H] + [SH]

The complexation is in dynamic equilibrium:

Kc = [SH]/([S][H])

Combining the last two equitons we can get [SH]:

Kc = [SH]/([S]([Ht]-[SH])) ==> [SH] = Kc[Ht][S]/(1+Kc[S])

The total drug solubility is:

e = [S] + [SH] = [S] + Kc[S]/(1+Kc[S]) * [Ht]

When [Ht] = 0, e = [S], which can be interpreted as the plain water solubility ([So]). As long as there is enough starting drug trying to be dissolved, [S] = [So].

e = [So] + Kc[So]/(1+Kc[So]) * [Ht]


Which is a very nice linear equation and explains the plot in the previous post for salvinorin and captisol.

Essentially, as Ht is added, more drug goes into solution at a certain rate. That rate is the slope of the equation above and we can see the explicit forms depends on the drug solubility in plain water and the complexation equilibrium constant. For large Kc[So] (good complexation and decent water solubility), the slope tends to ~1. So a 1 to 1 molar ratio make perfect sense. Otherwise, more HPBCD will be needed to dissolve all the drug and in practice the ideal molar ratio is 1+1/(Kc[So]) > 1.

Anyway, start with a high [Ht] solution. Then add drug, it will go into solution as So and also as it complexes (which should be most of it for poorly soluble FB). Eventually, it will stop going into solution once e is reached.

Attaching a file that also explains this as I understand it.
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ava69
#34 Posted : 5/15/2021 6:08:18 PM

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Thanks Loveall for the paper "Cyclodextrins in pharmaceutical formulations II: solubilization, binding constant, and complexation efficiency" by Jambhekar and Breen, downloaded and read the paper, thanks for the brief summary you gave above.

Latest experimental findings:

part 10: update 5-12-21 see post #25, ORAL AYAHUASCA REPORT: 70mg DMT complexed to 490mg HPBCD in 10 drops very hot water formed clear 0.500ml solution after 2 minutes of kneading/mashing on a spoon: clear solution mixed into 2oz hot water solution of 200mg harmine + 250mg THH resulted in +5 Shulgin scale experience IDENTICAL to 30 grams potent Hawaiian psychotria brew (Having taken 30 to 40 grams of Hawaiian psychotria with Caapi over 70 times over a period of many years).

70mg HPBCD DMT absorbed several factors better than oral freebase DMT or DMT salts (all were mild +3 experiences in a dozen trials, due to poor oral body absorption). The HPBCD DMT out performed and absorbed better than the dozen DMT salt experiments (70 to 120mg) I performed years ago. The results are similar to several papers I have read in which HPBCD was used to enhance the absorption of oral pharmaceuticals over their normal oral absorption by many factors.

Example shown below: HPBCD improves oral absorption profile for Ofloxacin, a second generation fluroquinolones by 54 to 89 percent.

part 11: update 5-12-21 see post #26, additional 35mg DMT complexed to 245mg HPBCD in 5 drops (0.250ml) very hot water formed clear 0.250ml solution after 2 minutes of keading/mashing on a spoon: held "under tongue for 15 minutes" resulted in another strong sublingual experience.
ava69 attached the following image(s):
Example, HPBCD improves oral absorption profile for Ofloxacin, a second generation fluroquinolones by 54 to 89 percent..JPG (26kb) downloaded 528 time(s).
 
ava69
#35 Posted : 5/16/2021 2:39:21 PM

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Loveall came up with a GREAT IDEA Smile which I would never of thought of on my own. He suggested taking a sublingual harmala + DMT all in HPBCD complexed form to simulate Ayahuasca. I find this a great idea as I would like to avoid the slight dizziness that harmine at 200mg gives me for a couple hours. So this is what I will do tomorrow, and show 4 pics.

That's the great thing about Ayahuasca, you can take her at least once a week, and there is no tolerance, it's been a week since last experiment, so I will give it a go.

Dr. Narang saids "under the tongue" pharmaceuticals are at least 3 to 10 times stronger than oral pharmaceuticals, so since 200mg of harmine is potent orally, I will use 1/6th the amount sublingually or 35mg of harmine.

"Sublingual mucosa as a route for systemic drug delivery" by Narang & Sharma 2010:
https://innovareacademic...pps/Vol3Suppl2/1092.pdf

The 75mg combined 35mg harmine + 40mg DMT should absorb just fine: even 100mg doses of viagra can be administered under the tongue, the scientist noting that much less of the drug was required, and that it began working in only one half the normal time of an oral dose:

"The start of pharmacological activity after sublingual administration of sildenafil citrate in 30 patients affected by erectile dysfunction." by Siati & Franzolin 2003: https://pubmed.ncbi.nlm.nih.gov/12741340/

Also, 70 DMT complexed to 490mg HPBCD in 0.5ml very hot water formed a clear solution after 2 minutes of mashing together, which when I used orally with 200mg harmine + 250mg THH all mixed together in 2oz hot water...was indeed many factors more potent and "all encompassing" (+5 Shulgin scaleShocked ) just like 30g hawaiian psychotria leaf brew as compared to free base or DMT salts used orally in a brew (all were mild +3 experiencesSad ), similar to many pharmacology studies, for example:

HPBCD improves oral absorption profile for Ofloxacin, a second generation fluroquinolones from 54 to a whopping 89 percent.Thumbs up

I will as usual take 250mg tetrahydroharmine orally 1 hour before, it never gives me any nausea or dizziness at this dosage or less, 150mg to 250mg is recommended, as it's the 2nd highest ingredient in Caapi based true Ayahuasca.

1st pic will show = 35mg harmine freebase + 40mg DMT all next to the HPBCD powder.

210mg HPBCD to complex the harmine + 280 HPBCD to complex the DMT = 490mg HPBCD total.

So the pic will show a pile of harmine, a pile of DMT, and a pile of 490mg HPBCD powder.

* Molecular weight of harmine = 212, molecular weight of HPBCD = 1300. Thus a 1:1 molar ratio = 1:6 host drug to HPBCD mg weight ratio.

* Molecular weight of DMT = 188, molecular weight of HPBCD = 1300. Thus a 1:1 molar ratio = 1:7 host drug to HPBCD mg weight ratio.

490mg HPBCD may look like a lot when laid out on spoon, but once you several drops of very hot near boiling water from a pipette taken up from a nearby coffee mug, the HPBCD shrinks into a small sticky clear liquid mass as it is derived from a sugar molecule, perfect for "under the tongue" use. 1000mg of HPBCD dissolves into 1ml (20 drops) water at room temp, the solubility even goes way beyond this when using very hot water. On a glass dropper: 0.250ml = 5 drops, 0.500ml = 10 drops.

2nd pic will show the 35mg harmine + 40mg dmt + 490mg HPBCD powders all on a spoon with the very hot near boiling drops of water added that I will be using.

3rd pic will show the (hopefully) transparent clear homogenous solution on the spoon after kneading and mashing it all together for 2 minutes or so.

4rth pic will as usual show a woman with tongue exposed (a la ava69 believes that women, like Mother Earth, are caretakers of this planet, a feminist ethic that binds us to mother earth), showing how the drops are then put under tongue and held for 15 minutes, strong effects commencing 5 minutes after the 15 minute sublingual period.
ava69 attached the following image(s):
sublingual.JPG (33kb) downloaded 290 time(s).
 
Loveall
#36 Posted : 5/16/2021 5:00:29 PM

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A few more thoughts on HPBCD for optimal buccal delivery. We don't want excess HPBCD since it will get in the way and "hold on" to the drug. On the other hand, we want enough HPBCD to dissolve the drug so it can diffuse into the body.

So there is an optimal molar ratio. 1:1 is a great starting point, but there may be a higher or lower ratio that is better if the complexation slope is larger than 1 or if So is large.

The attached paper has a great explanation, and some data for hydrocortisone (see image). Absorption of a 1.6% hydrocortisone peaks at 8% cyclodextrin (which is the point when all the drug dissolves), that is a 1:1.25 Drug:HPBCD ratio.

So in experiments, 1:1 molar is a great starting point, but tests at slightly higher HPBCD would be interesting. We could see effects getting stronger and then decreasing as HPBCD is increased.

This may be important in the salvinorin work also. From the solubility curve in the previous post, saturation for salvinorin happens at ~ 1:200 drug:HPBCD molar ratio, which is much higher than anything we tested on the salvinorin complexation thread.

In principle, one can start with undissolved drug and water. Then add 1:1 HPBCD, does all the drug dissolve? If yes, it's likely we are close to optimal already, perhaps less HPBCD could improve things. If no, add HPBCD slowly and stop when all the drug is dissolved. The HPBCD/Drug ratio saturation point should be optimal for buccal administration.

Finally, in practice as the drug is absorbed the remaining drug:HPBCD ratio decreases, pushing the system towards the unsaturated direction. Maybe starting at a lower HPBCD delivers the maximum amount of drug since both sides of the diffusion peak are utilized (going from the saturated to unsaturated region as drug is absorbed.
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💚🍃💚 Salvinorin Chilled Acetone with IPA and Naphtha re-X💚🍃💚
 
ava69
#37 Posted : 5/16/2021 9:33:36 PM

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Thanks Loveall, that's a very good paper you attached. I like the idea you gave of adding the HPBCD last to the host drug and very hot water to see "just how much you really need to absorb it all during the 2 minute mashing" and even experimenting with the slightly higher molar ratios.

If this [35mg harmine freebase complexed to 210mg HPBCD] + [40mg DMT complexed to 280 HPBCD], total = 75mg alkaloids complexed to 490mg HPBCD works tomorrow, this sublingual "under the tongue" administration of it all could very well be my favorite way of using this, as I would like to mimimize the normal way I do this of using 200mg oral harmine which always gives me slight dizziness and heaviness for couple hours.

From 2015 Nexus thread "My sublingual Harmala freebase experience":
Quote:
Steppa:
When I use harmalas sublingual I use them in a range between 25mg and 40mg and get good effects.

Goneandback:
I never exceed 35mg sublingual and have strong effects from just that. You can activate dmt sublingualy if you take the harmalas that way as well, but sublingual harmalas will not inhibit the enzymes that are present in your gut which are responsible for the break down of dmt. If you take the harmalas sublingually, you will need to take the dmt sublingually as well. I am not sure on the dosage for this though.

jamie:
30mg sublingual sounds about right for sufficient mao inhibition..and for me at least some visionary or entheogenic effects. 50mg sublingual can be a large dose. It is very active sublingual. Oral doses are naturally much higher at 200mg.

Last week, using 10 drops of very hot water to complex 70mg of DMT to 490mg HPBCD for oral use, it was an excess of water...so I'm certain I will be able to use around same amount of less of very hot water drops to complex the above for tomorrow for sublingual use.

Of course, I always take 250mg of tetrahydroharmine (THH) orally around 1 hour before the sublingual harmine + DMT for a "true Ayahuasca journey experience."

Just like Professor8 said back in 2010, she (THH) has the ability to raise your vibration or whole-body frequency (this is really felt strongly) in a most powerful way. She brings a diamond-like crystalline prismy texture & super clear watery dimension to Ayahuasca, like looking down through 10 meters of shimmering Caribbean Sea on clear blue day. She brings a dimension of pure light to the entheogenic experience and encourages entities & intelligences of only the Highest Order.
 
fog
#38 Posted : 5/17/2021 11:03:11 AM
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Really interesting findings! Do you know if the complex would be stable in solution? If one were to make a tincture for example?
 
ava69
#39 Posted : 5/17/2021 2:36:54 PM

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Fog said:
Quote:
Really interesting findings! Do you know if the complex would be stable in solution? If one were to make a tincture for example?
Thanks Fog. Yes, the formed complex liquid will remain stable indefinitely in a tincture, it can be frozen. Don't leave in fridge for more than a few days or bacteria could grow.

I'm taking 250mg THH orally one hour beforehand, then will take the 35mg harmine + 40mg dmt (75mg total alkaloids) all complexed to 490mg HPBCD powder (forms a 0.500ml or 10 drop solution after 2 minutes of kneading or mashing the mix on a spoon using very hot water drops using end of spoon) held under tongue for 15 minutes, and report results tonight, along with pics of the process.

This being done to simulate "true Ayahuasca" but hopefully without experiencing "the slight dizziness and heaviness" I experience from using 200mg oral harmine. THH causes me no nausea or dizziness whatsoever at 250mg, so I love to use it in combination all the time, imho 250mg THH is very similar to 250mg of mescaline, very beautiful compound. It combines extremely well with DMT.

Have over several weeks experienced 30mg, 35mg and 50mg sublingually and 70mg orally, trip reports above in this thread. The HPBCD DMT absorbs very well under tongue, but I am trying the above to see if the harmine will MAX OUT the activation of the sublingual DMT, hopefully resulting in maximum powerful Ayahuasca, identical to oral potent Hawaiian psychotria effects, which I have over 70 experiences. The harmine also has nice effects (like being in a relaxing hot tub) on it's own which I wish to include.

This will be my last post, as I need to head back to the gym & water park over the summer.

I will leave it up to the rest of you to experiment should you wish to. I love the HPBCD DMT so much, that I will continue to use it the rest of my life. I'm a very visual person, and love good music, that's why I like to show lots of pics. Ayahuasca is a great way to stay Psychedelic for the rest of your life.

Stay true to yourself. Love, peace and music
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Ready for tonight:

1) 35mg harmine + 40mg DMT + 490mg HPBCD laid out

2) 75mg alkaloids + 490mg HPBCD put in spoon

3) 10 drops (0.500ml) near boiling water added from a nearby coffee cup, used the end of a spoon to knead, mash & stir it all together for 2 minutes, light brownish liquid formed, stored in fridge till ready. Alternately, a mortar & pestal can be used to knead & crush/stir the alkaloids into the HPBCD.

4) Tonight: take 250mg tetrahydroharmine 1 hour before, then place 0.5ml solution under tongue, hold for 15 minutes, 5 minutes later harmine + fully activated 40mg DMT should be felt strongly, for 60 to 90 minutes of strong effects. Re-dose again later if want to.
 
ava69
#40 Posted : 5/17/2021 11:49:27 PM

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Results:

1) The HPBCD harmine + DMT sucked really bad, I think the harmine interfered not only with the complexing of the DMT but also the absorption of the DMT under tongue, will never repeat again, effects were very mild.

2) So then, 1 hour later I complexed 60mg of DMT to 420mg of HPBCD, shown in pics, held under tongue for 15 minutes, and it began to come on in only 10 minutes, beautiful strong effects! Now that's more like it, long duration about 90 minutes total. As usual, took 250mg THH 1 hour before. Bad ass!

Experienced PHENOMENAL strength, active for 90 minutes, profound open eyed beauty, maxed out dilated pupils, heavy CEV imagery, music incredible, very euphoric.

3) So my favorites are:

* For oral use: 70mg DMT complexed to 490mg HPBCD using 10 very hot water drops, mashed all together on spoon for 2 minutes, then add this to 2oz of hot water containing 200mg harmine + 250mg tetrahydroharmine + 150mg pure ascorbic acid (vit c) to help dissolve freebase harmalas = 10 out of 10, this gives an experience identical to using 30 grams of potent Hawaiian psychotria, I've had over 70 Ayahuasca journeys using Caapi + hawaiian psychotria, and this was no different! zero nausea and went down in one gulp--taste was pretty much non-existent. All of my dozen 70 to 120mg freebase or DMT salt used orally with Caapi were all only +3 on shulgin scale, all very mild. This on the other hand was a +5 on Shulgin scale, just as strong as the leaf and all encompassing like the leaf. See trip report on post #25.Thumbs up

I'm glad to discover this, as for years all the dried Hawaiian psychotria has been extinct, I think it has all been diverted to the numerous Ayahuasca centers in South America.

* For sublingual use: 60mg DMT complexed to 420mg HPBCD using 10 very hot water drops, mashed all together on spoon for 2 minutes, then pour this under tongue and hold for 15 minutes = 9 out of 10, very awesome strength and zero nausea, it stings a little, but the results are worth it, at the end of the 15 minutes, I spit out all the saliva that's collected in mouth into a cup instead of swallowing...nice long 90 minutes duration. Thumbs up


 
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