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Alchemica

Designing CNS therapeutic essential oil blends

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Basically, I've decided for a bit I'll put my autistic focus into blending therapeutic essential oils. I'll be aiming to base the oils on their pharmacology rather than blending for an olfactorily nice blend (be nice if I could do both, I'll try).

 

So far, I've come up with...

I'll probably do a calming/memory one [rosemary, lavender (active at 80mg+) , lemon balm, incensole acetate rich frankincense, lemon myrtle if it's not too sensitising] and a neuroprotective/restorative one with mainly copaiba oil, incensole acetate rich frankincence and rosemary oleoresin. CB2 agonists are really promising for schizophrenia, pain, inflammation and neurodegenerative things like Parkinson's disease, Huntington's chorea, cerebellar ataxia, MS etc [1]. These oils seem to be relatively safe for ingestion if needed...
 

  • Copaiba oil (high in β-caryophyllene, CB2 agonist)
  • Rosemary oil (high in α-pinene, anti-inflammatory via PGE1, acetylcholinesterase inhibitor - aiding memory, positive modulator of GABAA receptors at BZD sites) The essential oil from rosemary has been shown to affect cognition and mood and these effects have been attributed to the presence of cineole and α‑pinene
  • Rosemary oleoresin, rich in carnosic acid and rosmarinic acid: Carnosic acid and rosmarinic acid also exhibited neurotrophic effects and improved cholinergic functions (AChE and BChE), they both upregulate genes involved in dopaminergic, serotonergic and GABAergic pathways (GABA transaminase), too
  • Lavender for the linalool and acetate (VDCC blocker)
  • Melissa officinalis oil. Lemon balm and preparations thereof also have been shown to improve mood and mental performance. These effects are believed to involve muscarinic and nicotinic acetylcholine receptors. Positive results have been achieved in a small clinical trial involving Alzheimer patients with mild to moderate symptoms. Essential oils obtained from Melissa officinalis leaf showed high acetylcholinesterase and butyrylcholinesterase co-inhibitory activities.
  • Incensole acetate: neuroprotective, anti-inflammatory, anxiolytic, antidepressive, 'spiritual' TRPV3 agonist

 

For pain, one day I'd like to make a curcumin, boswellic acids and tetrahydropalmatine blend, or something like that. Copaiba oil is promising for inflammation and pain, as are citronellal-rich oils [2]


Anyone ever done anything like this and have words of wisdom?

Once I get a decent blend, I'd like to be able to give samples to people with chronic conditions who might be able to benefit

 

Edited by Alchemica
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Also thinking of a version for autism if I get the time and have the cash to get some flavonoids.

That would be something aiming for a blend of luteolin (100 mg/dose, from chamomile) and quercetin (70 mg/dose), and the quercetin glycoside rutin (30 mg/dose) [1] in a blend of essential oils [thinking mostly copaiba] and probably some omega-3 concentrate. Ideas for this are also welcomed. Won't put too much on my plate though at the moment.

For more information on polyphenols for CNS conditions: [2]: 

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I'd be a little worried about the lavender, being estrogenic and all.

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Hmm it seems the Lavandula angustifolia essential oil which is the one I'd use isn't too problematic estrogen activity wise. All the lavender being estrogenic research is questionable. "The new research findings represent a major development in our knowledge of lavender oil safety, since the possibility of estrogenic action now looks remote. While no single test should be taken as absolutely conclusive, we can expect the volume of noise about lavender being estrogenic to diminish considerably.".[1]  Silexan, a commercial lavender oil product for anxiety with efficacy comparable to paroxetine and lorazepam for GAD has been marketed. Still I'll do more research.

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Nice work alchemica :) I would love to try some or even borrow your recipes if you think it is worthwhile once your completed.

 

i experimented with essential oils a few years back, namely oilhuasca style combinations. I never saw rainbows but some of the combinations were defiantly psychedelic. I think I was following a lot of what "69ron" was writing at the nexus, I think I copied the posts onto here somewhere too if you want me to find them.

 

thanks man

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Do you use the oil blends orally alchemist?

Dood I read all the oilahuasca threads around and there was a lot of theory flying around but not much solid evidence at the time. I remember experimenting with 'meggsy back when I was a teen and it's pretty intense! Lasts waaay too long for my liking!

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I've used lavender and copaiba before orally - the lavender is definitely helpful for anxiety (but tastes bad so needs to be capped). The copaiba was when i was really ill so it was hard to tell how well it works but I'd say it's going to be a good non-psychoactive therapeutic that tastes OK. Lately I've been sipping on a homemade tincture of Boswellia papyrifera. Nice and spiritually uplifting, positive mood, clear mind. I'm planning on making some ethanol and vegetable oil tinctures with added myrrh and benzoin for friends.   Haven't had the chance to sample the other oils yet. I have a friend that is really into his lemon oil, the limonene has some interesting CNS effects.

Haven't played around much with pronounced psychoactive aims in mind - more interested in therapeutics these days.

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Quote

I remember experimenting with 'meggsy back when I was a teen and it's pretty intense! Lasts waaay too long for my liking!

ROFL....been there:wink: 3 days in delerium after eating way too much tinned, chopped whole nutmeg.

 

Never, ever again....first and only go at that.

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Why am I so excited by copaiba oil? β-caryophyllene. The other side of phytocannabinoids, the less 'fun' but equally therapeutic side! This link is a simple guide on using copaiba.
 

http://oilhealthbenefits.com/copaiba-essential-oil/


CB2 agonism is really neat and not 'psychoactive' in a dramatic way. Endocannabinoids drive the acquisition of an alternative phenotype in microglia. Microglial CB2 cannabinoid receptors are neuroprotective, suppress microglial activation and trigger anti-inflammatory pathways. CB2-induced inhibition of Th17 differentiation is highly relevant for autoimmune conditions.CB2 agonism is promising for multiple CNS conditions, including neurodegenerative conditions [1].


β-caryophyllene is a promising therapeutic candidate to treat CNS disorders involving brain damage [2]


CB2Rs modulate dopamine and are likely useful targets for schizophrenia. [3]


β-caryophyllene has significant anticancer activities, affecting growth and proliferation of numerous cancer cells. [4]


The selective activation of CB2 may be considered a novel strategy in pain treatment, devoid of psychoactive side effects associated with CB1 stimulation. Thus, β-caryophyllene as selective CB2 activator may be taken into account as potential natural analgesic drug. [4]

CB2 receptors modulate energy homeostasis and obesity associated metabolic pathologies in the absence of any adverse impact on mood [5]


[1] https://www.ncbi.nlm.nih.gov/pubmed/27679556
[2] https://www.ncbi.nlm.nih.gov/pubmed/27565895
[3] https://www.ncbi.nlm.nih.gov/pubmed/27618677
[4] https://www.ncbi.nlm.nih.gov/pubmed/27696789
[5] https://www.ncbi.nlm.nih.gov/pubmed/26588700

 

What I've been up to and what's happening:
 

This week I've been getting to know Boswellia better. Quite a nice plant to work with. Happy with knowing the space now and the therapeutic potentials. Hopefully late next week I'll start on my new tinctures. Also enjoyed rosemary and honey tea.
 

While I know lavender's space really well, my priority later next week is to get to know rosemary EOs. I've got two varieties to get to know, verbenone and the cineole chemotypes. Hoping the supplier can get me the CoAs so I can get to working more intimately and in a scientifically informed way with them. Also have to compare that to the α and β-pinene rich pine oils. Really wish I had all my stuff to test out some fractions so I could get to know α-pinene itself but I gave up those days.

 

Another priority will be getting back on copaiba. Really keen to get on a neuroprotective regime myself. I only got to know this spirit when I was really ill so I have some more experience to gain. I'm also hoping to do a blend for pain/fibromyalgia etc that is based on the latest science: copaiba and citronellal rich oils. Also want to prepare some isolated boswellic acids and find a good source of cheap curcumin.

 

After I know those spaces better, I'll start to get to know lemon, lemon myrtle and lemon balm. Then I'll get around to doing some blends. Then time for more testing.

Edited by Alchemica
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With my Boswellia trials:
 

I've been doing some comparisons of Boswellia papyrifera and carterii (both ethically harvested). The nicer olfactory (and taste for the adventurous!) notes come from the carterii (ethereal, sweeter, mentholic) compared to the papyrifera (earthy, camphorous, octanolic) and the effects seem to be different from the concentrated ethanol tinctures, papyrifera personally being a nicer experience. Warming, anxiolytic, antidepressive, mentally clearing, provides clear spiritual direction and an empathetic feeling while carterii seems to be more a cerebral, ethereal ungrounded feeling. I've been trying to base the tinctures on the variety high in incensole acetate going by [1.2] but [3] uses carterii. I'm feeling a blend of the two might be the best combination for olfactory and spiritual delight.

 

Snu gives the following for carerii: "oleo-resins have yielded 5-10% essential oil, containing pinene, dipentene, limonene, thujone, phellandrene, cadinene, cymene, p-cymol, myrcene, terpinene, camphene, olibanol, verbenol, verbenone, bornyl acetate, octyl acetate, incensyl acetate, octanol, linalool and incensole as well as 60-65% resins ( α- and β-boswellic acid), 20% gum, and 5-8% bassorine."
 

The tinctures should retain anti-inflammatory boswellic acids so that's a nice addition.
 

[1] http://scidok.sulb.uni-saarland.de/…/Dissertation_Fertig_21…
[2] https://www.ncbi.nlm.nih.gov/pubmed/22545396
[3] https://dx.doi.org/10.1096%2Ffj.07-101865

 

If anyone who is more experienced in perfumery can better describe the differences of taste and smell of fresh resins, that would be sweet. Who's had the chance to sample both themselves?

 

As for the content of incensole acetate from one source.

B. papyrifera CO2 17% incensol and 7.5% incensole acetate

B. serrata CO2 - 12% Incensole acetate
B. carterii CO2 - 7.4% Incensole acetate [pers. comms]

The EOs contain little IA.

 

Edited by Alchemica
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The other constituent I want to get to know is thymoquinone. I can get commercial 10% thymoquinone from Nigella sativa extract reasonably cheap, otherwise its rather pricey.

I've tried Black Seed Oil and have to say it's nice tasting but is mainly fatty acids.

Essential Oil Composition (1.4%) Black Seed Oil
Carvone 21.1%
α--Pinene 7.4%
Sabinene 5.5%
β-Pinene 7.7%
P-cymene 46.8%
Others 11.5%
Fatty Acids Black Seed Oil.
Myristic Acid (C14:0) 0.5%
Palmitic Acid (C16:0) 13.7%
Palmitoleic Acid (C16:1) 0.1%
Stearic Acid (C18:0) 2.6%
Oleic Acid (C18:1) 23.7%
Linoleic Acid (C18:2)(Omega-6) 57.9%
Linolenic Acid (18:3n-3) (Omega-3) 0.2%
Arachidic Acid (C20:0) 1.3%
Saturated & Unsaturated Fatty Acids Black Seed Oil
Saturated Acid 18.1%
Monounsaturated Acids 23.8%
Polyunsaturated Acids 58.1%

Extraction of pharmacologically active thymoquinone in nigella sativa L.
 

I might try an alcohol extract on Nigella sativa seeds (this protocol uses microwave assisted extraction [1])

Anyone played around with it?

 

Edited by Alchemica
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Why is a rosemary extract so great for brain healing? It's high in rosmarinic and carnosic acids. Here's a brief review of recent literature.
 

Rosmarinic acid exhibited antioxidant, neuroprotective, and antidepressant-like effects. Rosmarinic acid can enhance neural plasticity by modulating glutamatergic signaling pathways, as well as providing neuroprotection with reduced cholinergic activity. Acute rosmarinic acid treatment enhances long-term potentiation, BDNF and GluR-2 protein expression [1].
 

It enhances learning and memory and reduces brain tissue markers of oxidation that occur with age [2].
 

Oral rosmarinic acid increased the protein expression of glutamic acid decarboxylase (GAD65/67) and GABAA receptors subunits except β1 subunit, exerting anxiolytic effects [3].
 

Rosmarinic acid may be able to improve cognition by inhibiting prolyl oligopeptidase (POP). POP is a protease that cleaves arginine-vasopressin (AVP), substance P (SP), oxytocin, and angiotensin IV, which have all been shown to have neurological function in addition to their physiological functions. It dose-dependently inhibited the formation of Aβ as well as destabilizing preformed Aβs. It has inhibitory effects on acetylcholinesterase. The anti-inflammatory effects of rosmarinic acid along with its immunomodulatory effects may also make it a novel agent for the treatment of auto-immune disorders. [4].
 

Rosmarinic acid displayed acute anticonvulsant-like activity against induced seizures [5].


Carnosic acid and rosmarinic acid also exhibited neurotrophic effects and improved cholinergic functions (AChE and BChE), they both upregulate genes involved in dopaminergic, serotonergic and GABAergic pathways (GABA transaminase) [6]


It seems to be useful in various animal models of neurodegenerative diseases.

 

[1] https://www.ncbi.nlm.nih.gov/pubmed/27163641
[2] https://www.ncbi.nlm.nih.gov/pubmed/27527000
[3] https://www.ncbi.nlm.nih.gov/pubmed/27469144
[4] https://restorativemedicine.org/…/the-effect-of-rosmarinic…/
[5] https://www.ncbi.nlm.nih.gov/pubmed/27448240
[6] https://www.ncbi.nlm.nih.gov/pubmed/23085339

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Much to my disappointment, the rosemary essential oils are looking too risky to be used orally in something I'd prepare for others, simply too much camphor/cineole in both chemotypes I have and not enough pinenes to be content with safety. Have to chase down some pure α-pinene one day. I'll stick with a standardised rosemary extract (20% rosmarinic acid) and use the rosemary oil externally. I can get a nice anxiety blend starting with with lavender and lemon balm, both OK at sensible doses orally. A 5:2 Lavandula angustifola:Melissa officinalis is my starting point and smells pleasant. I'll do some testing.

 

0.5mL of the 5:2 is actually rather potent, much more so than the equivalent of pure lavender oil. Quite a nice feeling. Interesting to see there has been reported "patients should be made aware that it may have a risk of dependency and can lead to withdrawal symptoms." I'm going to be cautious of this one. Never noticed abuse potential or withdrawal with lavender alone but this is a much nicer feel. Not sure I'd want to give people something quite this strong but I can see it would be effective for anxiety.

 

Back on the copaiba @ 500mg/day. We'll see if I can keep mental health good with that.

To prepare my 'Frankincense +' tinctures and oleoresins (these could be bettered, but it's a starting point)
 

Boswellia papyrifera/carterii, myrrh and benzoin were finely powdered individually in an electric blender. Smell is divine.

Preparation of tincture: B. papyrifera (50g), carterii (10g) and myrrh (15g) were suspended in pure ethanol benzoin tincture (150mL) and ultrasonicated at 50°C for 1hr and will be left to stand for ~1 week. Solids will be removed, washed with a small quantity of hot ethanol to give the tincture.

 

Preparation of oleoresin*: B. papyrifera (30g), carterii (10g), myrrh (15g) and benzoin (5g) were suspended in copaiba oil (120mL) and ultrasonicated at 70°C for 1hr then warmed on a hot water bath at 100°C for 2 hrs. The mixture will be filtered while hot to give the oleoresin for topical/oral application. (Remaining solids will be washed with a small quantity of ethanol to give a small quantity of second tincture I'll try out.)

 

*modified from https://apothecarysgarden.com/…/how-to-make-a-whole-extrac…/

 

The tincture is quite nice and uplifting at a couple - several mL. I add it to water and the oils and solids drop out which I to give a milky suspension which I gulp down, I'd imagine it to get better with higher doses but I'm not looking for strong effects (and the alcohol would add to the effect, I'm not looking for intoxication).

Edited by Alchemica
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I'd be interested in trialing a rosemary/memory related admixture if you are willing or curious.  Would be fascinating to see if it helped with my study.

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Sounds great @Mapacho I'll send you some complimentary rosemary extract (20% rosmarinic acid) in the near future when I get my bulk pack if you are up for testing it for me (I'll also be giving it a whirl) and report back with any results. Otherwise PM me if you want to buy it and I'll give you a supplier.

Edited by Alchemica
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I jumped the gun and decided that I'd take half the frankincense ethanol tincture out, add ~15mL of hemp seed oil and evaporate at room temp. Best method of delivery yet IMO. Potent, interesting in taste... I'll get @Mapacho to do a bioassay and report back soon.

Decided to make some flavoured chocolates with essential oils. I used the following recipe:

 

Quote

80gm Cacao Butter, 1 tablespoon coconut oil, 3 tablespoons Agave nectar and 55 g Cacao Powder. Melt the cacao butter, coconut oil over a pot of boiling water, stirring all the time, add agave and stir in to combine, add essential oil of your choice and then add cacao powder stirring till lovely and smooth and shiny. I usually get between 23-30 chocolates.


For frankincense I added 3 drops EO. Could have added more ;)
For lemon balm I added 6 drops EO. Decent taste.

For lemon myrtle I added 6 drops EO. Good taste.

I can see a higher dose of EO could give some interesting therapeutic benefits...

Edited by Alchemica
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Settled on trying 0.5mL of Boswellia carterii EO to get a 'safe' but rough feel for what α-pinene might be like (contains ~30-60% α-pinene). I can see the therapeutic potential - anxiolytic, antidepressive with a nice 'cloudy' warmth. Just want a cheaper source. At least this is a nice functional state, without the heavy sedation of the Lavender/ Melissa officinalis mix. Not something I'd use regularly as it does act at GABAA receptor BZD sites but worth knowing. This with a bit of incensole acetate could be neat.

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I'm going to make a preparation of 70% boswellic acids in copaiba oil as my starting point for pain relief. Curcumin would be a nice addition but I want to see what the combination of 5-lipoxygenase inhibition with CB2 agonism is like. If you have inflammation/pain and want a natural option, do get in touch to be a free sample tester in the near future. Probably be able to do two samples of this mix, free if you report any results.

*for topical application.ONLY.

 

Copaiba alone seems to be OK orally at <0.5mL but if you go quite a bit above that you can get nauseous. Not sure how it is metabolised so drug-interactions could be present.

Edited by Alchemica
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Trying to work on my chocolate recipe. Ideas welcomed. Looking for therapeutic things to replace cacao butter and to cram in as many polyphenols while leaving room for me to add therapeutics. Thinking a blend of ethanolamide lipids with hemp oil might get the melting point down OK? Throw some ideas at me.

 

My recipe at the moment:

20g cacao butter, 20g hemp seed oil, one tablespoon agave syrup and 60g cacao powder is where I'm at. Chucked a whole bunch of frankincense EO in this lot. Tastes quite good just need to work on the melting point and mouth feel possibly. I'm going to replace the agave with  maple syrup or coconut syrup

At 0.7mL Boswellia carterii EO, the sedation gets stronger and interestingly, gives THE most amazing, vivid dreams. I have not been able to recall dreams since my childhood (except in EtOH withdrawals and stuff where they've just been frightening ones) and to have this was quite surprising. Guess it could be the AChE inhibition. I have to do more research into how this is likely metabolised, potential for drug interactions and half-life. Also need to give my GABAA receptors a break, No notable side effects other than improved GI peristalsis which is for me helpful.

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I can't help you mate but I do know you are onto something.  Anxiety chocolate.  What's not to love?

 

giphy.gif

 

 

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Managed to tweak the chocolate recipe and come up with something I deem highly therapeutic.

5g oleamide
1 tsp hemp seed oil
1. Melt on a hot water bath until combined into a solution. Add:
15g cacao butter (dark cooking chocolate can be substituted)
1 tsp agave syrup. Combine until melted.
2. Slowly stir in:
15g cacao powder

Weigh and work out the percentage oleamide. Yield should be ~ 40g 12.5% oleamide chocolate. 4g of this delivers 500mg of oleamide which I deem efficacious and therapeutic.

 
@ 300mg there is some peripheral 'niceness' in the legs, I could see it being good for pain without feeling stoned. Maybe slight anxiolysis and mood improvement but nothing extreme. Added supplemental 200mg.
 
With the supplemental 200mg, effects are still mild. Maybe more relaxed. Could be a good way to safely unwind (assuming people won't drive on anything that could possibly impair them). I'm quite content with the safety profile and lack of abuse potential of oleamide.

With 4g chocolate:


The final verdict on 4g of healthy flavonol rich 12.5% oleamide chocolate (500mg active oleamide) is that is does have subtle therapeutic properties. My mood hasn't been the greatest lately and I've been struggling getting sleep and breaking out of repetitive behaviours and this seems to have mild calming, anti-obsessive and mood improving benefits. It also is devoid of overt psychoactivity, inducing more therapeutic benefits than anything recreational.
 

Interestingly this still has affinity for both PPAR-γ and some for PPAR-α, analgesic, neuroprotective, antidepressant, GABAA and anxiolytic activity, sleep improving qualities etc.

I've pushed oleamide
into the grams and it seems to be devoid of cannabinoid-ike psychotomimetic properties (of which I am vulnerable to). Anxiolysis and improved sleep quality are notable but I suggest caution with doses. Don't do grams, I was screening for anything dangerous. I hear some find 80mg therapeutic. 

 

There may be withdrawal symptoms, so do not use frequently.

I would suggest caution using this as a frequent therapeutic and suggest you look into palmitoylethanolamide if you require daily healing. Looking at getting palmitoylethanolamide in bulk, maybe we should do a group buy?

 

To compare to palmitoylethanolamide at 1200mg (therapeutic dose) pushing to 1800mg (there could be some synergy between earlier oleamide, so I have to do proper trials with a washout period, just keen to know both as early as possible): quite a pleasant slowly building relaxation, strong peripheral 'niceness', prominent anxiolysis, clear focus. Enjoyable, mood is good but not an addictively rewarding experience. Seems to combat nicotine and alcohol cravings quite well (both have been challenging recently, PPAR agonists are promising for relapse prevention). A useful therapeutic it seems. I wouldn't want to drive with the peripheral feelings present even though cognition is clear
 
This seems to have a ceiling effect too. Supplementing the dose further (+ 600 mg x 2) doesn't seem to go further which is encouraging. I am a lightweight when it comes to anything related to direct cannabinoids, I don't use them for that reason so I might not be the best test subject (I'm actually looking for the other activities as personally being more therapeutic) but I can see the therapeutic usefulness of these substances in my case. I don't think it's something I'd want at high doses for daily use which is also a plus. More something to scratch that persistent itch every now and then, although the neuroprotective benefits, mood improvement and anxiolysis are something that I could often benefit from.

 

 Confident that palmitoylethanolamide lacks drastic abuse potential but displays good therapeutic efficacy. I'm giving this one a break for a bit but it's definitely worth looking into for anyone struggling with pain, anxiety, depression.

 
 
 
Edited by Alchemica
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 _

Edited by coin

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Awesome post, awesome ideas! Immediately I was attracted to the combination of the rosemary with lemon balm. Any of the other additions sound very interesting also! Intrigued by the chocolate. Maca powder instead of or partially replacing cocoa powder might add some general dietary health benefits? 

 

Happy to be a guinea pig lol. 

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 The package arrived in the mail this morning.  I`m fairly confident that a good sniffer dog could follow its path across australia. Does it smell good or what! Thankyou alchemica! I am wondering how to imbibe this.  Will it work effectively as a tea or should I consume it directly in a smoothie?

 

Also, I have been microdosing for a few days so I will let that settle down before I start any reporting of effects.

 

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