Ethnobotanicals Salvinorin HPBCD Cyclodextrin Complexation for Sublingual Administration

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Salvinorin HPBCD Cyclodextrin Complexation for Sublingual Administration

I am in a great mood (strong afterglow) this morning after having a +5 Shulgin level experience last night with a tea I made from 750 grams of home grown very potent bridgesii chunks from around the core boiled into a tea. Drank the tea first, then 1 hour later took 5 hits of LSD, also drank a morning glory seed solution in sherry wine made from 25g (875) seeds. I took the MG seed wine at same time as LSD. The MG seed wine adds divine spirituality, infinite beauty & euphoria, incredible dimensions, extreme saturated color & music enhancement to the experience along with the mescaline. Absolutely amazing experience all night long. Highly recommend. I do this at least once a month.

How to make the zero nausea morning glory wine: https://www.shroomery.org/forums/showflat.php/Number/27850299

Concerning thread "Salvinorin Cyclodextrin Complexation for Sublingual Administration" by Brennendes Wasser

Brennendes Wasser said:

So I was thinking about making a Salvia Nosespray the first time I had some, but then tossed it as my stuff still had some grey impurity. My only experience with smoked Salvia in Holland was way too harsh to give it another BIG go Shocked . Therefore I thought I would toss this molecule completely.

But now I might tackle it again as I may pre-weigh the Salvinorin much better with some crystals.

So Loveall you found that you should stirr the Salvinorin in excess Ethanol while evaporating, to ensure close contact with HPBCD and then re-dissolve in any suitable liquid?

My plan would be as following:

10 mg Salvinorin A
3x EQ of HPBCD
in 0,5 ml Ethanol

stirred for 2 h and then evaporated overnight.

This is dissolved in 0,5 ml water and put into a Nosespray.

I guess a super easy proof of Complexation is even if everything dissolves later in water or not Confused

As I know that 1 push Nosespray = 0,... mg of Salvinorin A (in theory), I could sit there and start ramping up that Nosespray to record whenever I get some effects.

So I guess 10 mg totaly would be enough to at least get a threshold effect IF all the Salvinorin was complexed? If absolutely nothing happens after incorporating that 10 mg I guess it is more likely that the complexation did not work (or did not enhance bioavailability) than the dose was too small?

May I make a kind suggestion. I'm a lifetime chemist and have used cyclodextrins for over 2 decades. I used to complex HPBCD to pro-hormones and testosterone to make them absorb under tongue with incredible penetration. 20 years ago I used to converse with chemist Patrick Arnold on how to complex pro-hormones when they were legal until the Gov't banned them, as they worked as well as regular testosteone. Then used with DMT at least 50 times over a 2 year period.

--> Drop the ethanol as ethanol is not used when complexing freebase alkaloids to HPBCD, as the ethanol is polar and competes for entry into the hydrophobic (water repelling) inner HPBCD cone. The outside of the HPBCD cone is hydrophilic (mixes with water).

This means your salvinorin A has much less chance of entering the tornado trap cone of the HPBCD in appreciable quantitites as the ethanol will also be entering.

From "Thermodynamic properties of hydroxypropyl Beta cyclodextrin and guest interaction, a survey of recent studies, 2021.pdf" page 4 top:

Calorimetric titration showed that at ethanol molar fraction higher than 0.2 at neutral and alkaline pH, and higher than 0.1 at acidic pH, the complex does not form. These results indicate that ethanol competes with water for the cavity of HP-β-CD. DSC data of dried HP-β-CD, coming from hydroalcoholic solutions, confrm this hypothesis. In summary, the solubility enhancement of quercetin in higher concentrations of ethanol is counterbalanced by a lower propensity for the complex formation.

Dr. Narang:

The absorption of drugs through the sublingual route is 3 to 10 times greater than oral route and is surpassed by hypodermic injection. Sublingual mucosa under tongue is only 100 to 200 microns thick.

MESO-Rx, "Ask Patrick Arnold #10", April 15, 1999 By Chemist & bodybuilder Patrick Arnold:

Sublingual hydroxypropylbetacyclodextrin (HPBCD) complexed testosterone has a very high bioavailabilty however as the peak blood levels are seen rather quickly (20 to 40 minutes). These peaks are quite high however and the drop off is substantially gradual as in the EMU study testosterone levels of greater than 60% over baseline were still measured after 2 hours.

Straight testosterone or prohormones do not have very good absorption under the tongue. When complexed with cyclodextrin the properties change to enable it to absorb extremely well. It would be a long and detailed explanation but that is the jist of it.

DMT is very similar to pro-hormones, poor absorption under tongue, but when complexed to HPBCD, it absorb's extremely well, studies show up to 400% increased penetration. Chemist Patrick Arnold taught me how to complex pro-hormones in my 20's: Ask Patrick Arnold #11 - MESO-Rx (thinksteroids.com)

Patrick Arnold's latest project: Once part of sports' dark era, Patrick Arnold is on new quest | News | news-gazette.com

Instructions for complexing Salvinorin A to HPBCD or Hydroxy Propyl Beta Cyclodextrin. You can use the more common Beta-hydroxy propyl beta cyclodextrin, works just as well as the plain HPBCD. I bought a 1 kilogram tub from china for only sixty dollars many years ago.

1. Add 10mg salivonrin A to a spoon.

2. Molar mass of salvinorin A is 432.469 g·mol−1, add 1:1 molar ratio of host drug DMT (432g/mol) to HPBCD (1300g/mol) powder, this means 1:3 mg ratio host drug to HPBCD. The HPBCD is only able to complex freebase drugs, not the salt or hcl.

3. So then add x 3 or 30mg HPBCD to the spoon on top the salvinorin A.

4. Add 3 to 4 drops of very hot near boiling water from a nearby microwaved coffee cup to the mix and crush the ingredients together for 2 minutes. Since the HPBCD is like a glucose sugar it shrinks down to nothing and complexes with the host drug.

5. Place complex under tongue and hold for 5 minutes, it will all dissolve. Simply place underside of tongue onto spoon, the complex will all adhere as it is sticky.

6. HPBCD has been shown in studies to increase penetration of the freebase host drug by up to 400% into the sublingual mucosa under the tongue. The bulky HPBCD is not dissolved but it opens tight juctions under the tongue so that the host drug can enter with greatly increased efficiency. Most of the bulky HPBCD ends up in your saliva that you spit out into a cup after 10 minutes.

7. I have used this same HPBCD formula to complex DMT and it achieves even greater absorption into bloodstream then even oral dmt taken with 200mg harmine, 60mg easily a +3 Strength level, 100mg is a +5 level.

Full instructions for sublingual or the one-shot HPBCD DMT Ayahuasca (your choice):
1) place 60mg of DMT onto a spoon (60mg for beginners)
2) add 1:1 molar ratio of host drug DMT (188g/mol) to HPBCD (1300g/mol) powder, this means 1:7 mg ratio DMT freebase to HPBCD, use a 1:8 mg ratio DMT to HPBCD if you are using the 2-Hydroxypropyl-β-cyclodextrin. For harmine freebase, 212g/mol or 1:6mg ratio harmine to HPBCD. The HPBCD is only able to complex freebase drugs, not the salt or hcl.
3) this means 60mg dmt placed on spoon, then add 420mg of HPBCD on top DMT, use 480mg HPBCD if you are using the 2-Hydroxypropyl-β-cyclodextrin.
4) add 8 drops of very hot near boiling water to the mix from a nearby microwaved coffee mug for DMT doses of 90mg, use 10 drops of boiling hot water to mix DMT doses of 120mg. Use 10 to 12 drops of hot water for 150mg DMT. 10 drops usually still works well for 150mg DMT. Just experiment a bit. You will want to use less drops of hot water (1 drop per 12mg DMT) for higher doses of DMT so it will fit comfortably below the tongue. 60mg DMT = +3 Shulgin level strength, 90mg DMT = +4 Shulgin level life strength. 120 to 150mg DMT = +5 Shulgin level life changing experience.
5) Knead or crush the HPBCD powder into the dmt using the end of another spoon for 2 minutes, scrape & mix everything back and forth hard using your muscles. This is how scientist pre-pare these complexes by kneading.

Note: DRY THE BOTTOM of tongue/sublingual mucosa with a tissue before applying.

What I do now is take 200mg of harmine and 200mg of pure THH orally, then 1 hour later once I feel the harmine and THH, I take sublingual HPBCD DMT (around 100mg) hold under tongue for 15 minutes, all dissolves, gives a 1.5 hour very strong extremely euphoric and visual experience, then I re-dose more sublingual DMT at the 1.5 hour point again, holding under tongue, continues to work at full strength, as the oral harmine has a half life of from 1 to 3 hours, continues to work for 3 hours to 5 hours. Please start with only 60mg DMT if you duplicate this, 60mg = +3, 100mg = +5 in strength.

I way prefer taking DMT under tongue instead of orally, as zero nausea, goes straight to brain, no dizziness, the only way I use it, very bad ass this way. None of the negatives of oral Ayahausca. There is something about DMT moving thru the stomach that makes it nausea prone, dizzy, and weird and strange, this is all avoided by using it under tongue. The harmine lowers MAO in the brain for 3 to 5 hours, so you can use the dmt under tongue with many re-doses, as it prevents the DMT from being zapped by mitochondria in the brain.

One-shot hpbcd dmt ayahuasca and sublingual hpbcd dmt ayahuasca, absorbs 2 to 3 times better than DMT salts, masks taste - Botanicals - Mycotopia

HPBCD DMT sublingually active under tongue - Botanicals - Mycotopia

I don't have access to Salvinorin A, but can assure you, this HPBCD complexing of host freebase drugs with plain hot water, and formed on a spoon in only 2 minutes will astound you. HPBCD is one of the greatest modern discoveries in the field of pharmacology and chemistry.

 

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Yes, the 1:1 molar guest:host ratio is the most commonly used in scientific work. I've encountered very few examples outside this ratio. Most scientist say the 1:1 molar ratio works the best, and there is no need for any other in most of the papers I have read.

HPBCD = 1300g/mol
B-HPBCD = 1400 g/mol (these molar mass ratios are approximate and not exact, you can encounter different)

The complex of salvinorin A with HPBCD or DMT with HPBCD in drops of water and crushed together for 2 minutes using the end of another spoon using your muscles to mix and grind it all together on the spoon should remain in liquid form at all times when ground together for 2 minutes with the drops of hot water. This liquid is flowable and you can even pour it from off the spoon into a syringe for storage to use later.

Hydroxypropyl beta cyclodextrin is a white to off-white crystalline powder. It is freely soluble in water and propylene glycol. It's solubility in water is more than 100g per 100ml under 25 degrees celsius.

With hot water, the solubility in water basically doubles. This is why I use near boiling hot water drops from a nearby coffee mug, using a pipette to draw up the water.

It cannot unfortunately be evaporated down, as the complex is already sticky (like how a sugar is sticky) and if you try to evaporate it down it will become a super sticky glob that will not even come off the spoon, it is like plaster.

It is best to use it right away, by placing the bottomside of your tongue onto the spoon, it will all adhere as it is sticky, and absorbs very fast under tongue.

What I do when I complex DMT with HPBCD and the drops of hot water, is store the resulting liquid by removing the plunger from a 3ml syringe (100 of these for less than ten dollars on-line with storage caps), and allowing the liquid to flow from off the spoon into the syringe, then replace the syringe plunger, and store the syringe in the freezer, it will keep forever this way.

When ready to use, simply drop syringe into a cup of warm water (cap on bottom of syringe will keep liquid from coming out) and it will defrost and become flowable again, then you can shoot the liquid under your tongue.

When I am tripping and need a 2nd dose around 1.5 hour later, I simply pull out another syringe from the freezer, defrosts in less than 30 seconds, and shoot contents under my tongue and hold in the sublingual mucosa.

A 60mg DMT HPBCD dose absorbs in 10 minutes, and a dose of 100mg dissolves in 15 minutes. Of course, I take 200mg of harmine freebase and 200mg of tetrahydroharmine freebase 1 hour before (2 highest ingredients in caapi).

When I feel the harmalas working, I shoot the HPBCD DMT liquid from the syringe under my tongue, hold it for 10 to 15 minutes, I spit out any collected saliva into a cup at the end of the 10 to 15 minute point...and it works powerfully around 20 minutes after you begin all this (works in 1/2 the time of an oral dose of 45 minutes), lasts strongly for 90 minutes, then I can easily re-dose again at that time, and even a 3rd time if I choose, as the harmine lowers mao in the brain for several hours, keeping the DMT from being zapped by mao mitochondria in the cells of the brain.

I've taken oral Ayahuasca over 80 times, and this sublingual HPBCD DMT is just as powerful as the oral form, no difference in strength except if feels stronger sublingually imho, but I prefer the sublingual as there is no nausea, no dizziness, no weird symptoms, only way I use it. It's more euphoric for me this way too. I love music and can listen to music for hours when using this sublingual Ayahuasca, as good as listening to music on mescaline, no difference, just heavenly.

HPBCD is very safe and effective used this way, as the 1300g/mol bulky HPBD cannot readily penetrate the sublingual mucosa as it is just too thick, (only very little gets thru according to studies on the sublingual, not even worth mentioning) but it does facilitate the transfer of the very low molecular weight DMT 188g/mol or salvinorin A (432 g/mol) into the bloodstream. Think of how aloe vera also achives similar kind of results.

What's even more impressive, is that the HPBCD allows the DMT or salvinorin A to penetrate into the bloodstream from the sublingual mucosa under tongue as the POTENT FREEBASE, reaching the brain quickly. DMT salts have been shown to not work via absorption under the tongue, but DMT freebase reaches the brain fast this way but also up to 400% increased penetration via the use of HPBCD which opens up tight junctions in the only 100 to 200 micron thick sublingual mucosa.

Chemist Patrick Arnold can be considered the "grandfather of pro-hormones and HPBCD" as he created and patented sublingually absorbed pro-hormones with his company Ergopharm that made millions of dollars selling these HPBCD complexed pro-hormones to use under tongue for 10 years, until the Gov't made pro-hormones illegal as they worked as well as tesoterone.

I made and used them over 20 years ago, had my testosterone level tested 1 hour after I took and held a 10mg HPBCD complexed 4-androstenidiol dose under my tongue for only 5 minutes, my test levels rose from my normal 300 ng/dl (low end) to an impressive 3500 ng/dl...way above the range of 1200 ng/dl tested in natural athletes at the high natural end. 3500 ng/dl is in the steroid level. Pro-hormones and testosterone both absorb very poorly under tongue, just as DMT in it's natural form is poorly absorbed. But when complexed with HPBCD, they achieve extraordinary penetration into the bloodstream.

I have a picture of the Ergopharm HPBCD pro-hormone complex which was sold for 10 years on the link #3 above from the table of contents. They also made a nasal spray HPBCD complex which worked just as well, but I preferred the sublingual. I used to communicate with Patrick Arnold via deja news groups which is how I learned how to do this. Once he left deja news groups (bought out by google groups) he started his company, Ergopharm, 2 pics of him in top links in post #1.

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Brennendes Wasser said:

My ultimate goal would be creating nose sprays from this, with a very precise dosing possible. 1x Spray of what I have here is 73 mg water so it would be super easy to make some precise concentrations. Furthermore in pure water I guess that carbohydrate solubility is super high so no need to spray like 1 ml into the nose. I just did it once with a DMT Fumarate solution and it was terrible. Effect was really weak, but nose burned for 20 min, while whole experience lasted only 30 min. I guess if HPBCD masks the taste it would do the same in your nose.

Yes, you could easily make a HPBCD complexed salvinorin A water liquid to spray into nose, once you make your 3 to 4 drop complex on the spoon in less than 2 minutes of mixing and crushing, then pour it into your nasal bottle that already has some liquid water in it with perhaps some drops of something to keep it sterile, and store in fridge when not in use. Then just spray it into nose, it should work wonderfully.

Yes, the HPBCD will mask any taste of DMT when used orally, and you will notice just like my pics, when you add the HPBCD DMT complex to some hot water, it is 100% totally clear or transparent.

But there is still a menthol like sting when using HPBCD complexed DMT sublingually, as the HPBCD is only acting to facilitate the transfer of the nasty tasting DMT into the sublingual mucosa. Most of the HPBCD ends up in the saliva you spit out after 10 minutes, it's just too bulky to enter to the mucosa, but the low molecular weight DMT passes thru easily once the HPBCD opens up the tight junctions in the sublingual tissue.

Ergopharm made a 4-androstenidiol HPBCD complex nasal spray that was called "cyclo-diol spray". I did use it and it worked great, you could feel the rise in testosterone within a minute of using it, very powerful.

Like I said, this same sublingual complex sent my tesosterone level (300ng/dl) quite low for a male into the stratosphere, after using it, my testosterone levels read 3500 ng/dl one hour after use when I paid eighty dollars to have my bloodwork lab pulled for this at the local labcore with doctor required and submitted paperwork to have done. 1200 ng/dl is the high natural level for athletes every tested, 3500 ng/dl is in the high steroid level.

One thing the Gov't hates are pschoactive drugs, psychedelics, and anyone with muscles...so they banned all the pro-hormones just like they did all the psychedelics.

Lack of effect of sublingual salvinorin A, a naturally occurring kappa opioid, in humans: a placebo-controlled trial:
https://www.ncbi.nlm.nih...mc/articles/PMC3063546/

Sublingual Ayahuasca, my psychedelic of choice: https://www.shroomery.org/forums/showflat.php/Number/28189371