Methylcobalamin Inhalation Therapy

[Hip]

Oxford Biosciences said:

Methylcobalamin is an extremely large molecule with a molar mass of 1344.40 g/mol so it would be very unwise to introduce this into delicate lung tissue.

I think this is just the company covering their ass.

I suspect so too. Although B12 methylcobalamin is a large molecule at1344 daltons, insulin is much larger still at 5808 daltons, and yet pulmonary delivery of insulin has been FDA approved (as a replacement for insulin injections in diabetes — see the Afrezza and Exubera insulin lung inhalation systems).

 

[skwag]

B12 methylcobalamin is reasonably stable under heating: this article mentions that: "In neutral media and in the absence of light, the carbon—cobalt bond in methylcobalamin is very stable to thermal breakdown, and the molecule can even stand heating to 100°C for 20 minutes."

Unfortunately, the linked article has disappeared, but Hips quote is accurate. A recent paper has more information on the heat stability of methycobalamin in solution. Their conclusion is different.

In degradation studies for thermal Stress at 100º, 110º and 121ºC, the percent recovery was found to be 88.25, 70.47 and 54.38%.This proved that there was degradation of Methylcobalamin under heat conditions. The proposed method possessed good reproducibility, accuracy and revealed that the commonly used excipients and additives in formulation were not interfering. The method can be adopted for routine quality control.

Note that b12 samples were heated (autoclaved) for 30 minutes in this study.

 

[skwag]

A recent paper has more information on the heat stability of methycobalamin in solution. Their conclusion is different.

I have spent some more time going through this paper. I now believe their analysis is flawed, and that methylcobalamin is not as heat sensitive as they claim. (This is in line with the paper, Stability of high-dose methylcobalamin injection,
which Hip also referenced, showing that less than 2% of the methycobalamin is degraded after autoclaving for 30 minutes at 115 degrees Celsius.)

The main problem is that their methylcobalamin samples appear to be contaminated with hydroxocobalamin. This probably occurred as a result of light exposure, since the paper does not indicate that they took any such precautions when preparing samples.

The uv absorption profiles of their "methylcobalamin" samples contain a peak at 350nm. If we look at other sources, such as Fig 2A from here for example, we see that methylcobalamin does not have a peak 350nm, but hydroxycobalamin does.

It seems this paper may have actually shown that hydroxocobalamin is unstable under heat stress.

 

[Matt_C]

I bought a vape and some juice and some of the b12 from Bio Alternatives pure water linked in this thread. It's 1mg per ml or thereabouts. I'm not convinced from my first attempt. @AlmostEasy noted too that this brand of liquid mb12 isn't strong enough to get much of an effect. I noticed an effect but I also noticed some extra brain fog that I don't often deal with these days, also experienced by @aturtles. I looked around in some forums to see if others who vape get similar feelings and I came across this:

https://www.e-cigarette-forum.com/forum/threads/the-foggy-head-feeling.184466/

It seems some experience brain fog from PG, which is a liquid alcohol. I'm going to get some pure VG and give that a go with some stronger MB12 soon.

 

[ahmo]

@Matt_C Are you aware of this thread re nasal spray? My next method to try.
http://forums.phoenixrising.me/index.php?posts/697712/

 

[Matt_C]

Hi @ahmo, yes I'm aware and i'm part of the group buy. Looking forward to getting the gear! Have you tried vaping? From your posts it looks like you weren't able to go ahead with it.

I'm not sure if a nasal spray will be much more effective than sublingual though, it's all mucosa right? I guess it will be an alternative for when I don't want the tablets lining my mouth.

 

[garyfritz]

I suspect oral/nasal will work similarly. There are sprays (such as Readisorb) that are used orally.

But I've heard people refer to something in the nasal cavity (olafactory bulb maybe?) that supposedly gives a more direct route to the CNS ?

 

[Matt_C]

I suspect oral/nasal will work similarly. There are sprays (such as Readisorb) that are used orally.

But I've heard people refer to something in the nasal cavity (olafactory bulb maybe?) that supposedly gives a more direct route to the CNS ?

Oh yeah, the olfactory nerve. I read that as well.

 

[ahmo]

Hi @ahmo, yes I'm aware and i'm part of the group buy. Looking forward to getting the gear! Have you tried vaping? From your posts it looks like you weren't able to go ahead with it.

I'm not sure if a nasal spray will be much more effective than sublingual though, it's all mucosa right? I guess it will be an alternative for when I don't want the tablets lining my mouth.

I didn't try vaping because I didn't want to buy a piece of equipment I might not need. Same with my thoughts about trying a nebulizer. Once I switched to transdermal, I was happy to let the others go.

For me, sublingual was undesirable because of spending 4 hours a day with this stuff sitting in my gums. Not about efficacy. If I find the nasal spray problematic, I'm happy to keep using the crystals for DIY transdermal.

I've only just increased the 2.5mg dose I've been using for about a year, resuming 5mg. I can't notice a distinct difference, because it's hot and that makes everything hard. But my body wants me to stay with it. So I'm currently on Mb12 5mg, folate 3mg, AdenoB12 40mg once weekly.

 

[Matt_C]

I didn't try vaping because I didn't want to buy a piece of equipment I might not need. Same with my thoughts about trying a nebulizer. Once I switched to transdermal, I was happy to let the others go.

For me, sublingual was undesirable because of spending 4 hours a day with this stuff sitting in my gums. Not about efficacy. If I find the nasal spray problematic, I'm happy to keep using the crystals for DIY transdermal.

Yeah I kind-of impulse bought my vape and now I'm hoping I'll use it! I think i will but need to experiment. Otherwise I'll sell it on eBay or something.

Did you know you can hire nebulisers from pharmacies for a small fee? Google it or ring some pharmacies near you.

 

[ahmo]

Thanks Matt. I feel nasal spray might be a tad safer than creatng a sterile solution for my lungs. Also simpler.

 

[Matt_C]

Is anyone still inhaling B12? Just wondering about results, experiences etc. I realized recently that B12 might be damaged by the heat produced by the vape. B12 can break down at high enough temperatures although B12 is said to be stable when exposed to heat but there is a point at which it breaks down. Common vape temps, from what I've read, are around 200-250 degrees celcius and I've read B12 shouldn't be exposed to heat higher than 105c for prolonged periods.

 

[ahmo]

I'm just about to mix my first batch of nasal spray. There's a thread somewhere, I think it's entitled B12 group buy. Inhaling seemed to me to need extra equipment, and had the hazard of keeping things sterile to go into lungs. I've been using DIY transdermal, and am hoping the nasal spray is even more efficient.

 

[Sellotape]

I see this thread has gone on for a while but I found it interesting and wondered whether any of the original "experimenters" (@bluewhistled, @skwag, @aturtles) - now that more time has elapsed, are still vaping B12.

Either way, as technology is still moving on, I wanted to suggest 2 additional options that might help partially or perhaps totally get around the primary concerns, particularly a) inhaling additional compounds that were not necessary or desirable, and b) the possibility of damaging the B12 at conventional vaping temperatures.

The first is of course temperature-control, which is fairly commonplace now. It's still maturing, but after a bit of a learning curve you can essentially limit the upper temperature of the coil - and hence the vapourized B12 - to anywhere from say 100C to 250C. Actual ranges are probably larger but I'm guessing where B12 is concerned anything outside those ranges is meaningless. Now... vaping at only 100C is not particularly satisfying, but heading towards 150C starts to work. Someone who knows more about the temperature at which B12 begins to meaningfully degrade (in only a few seconds) could suggest a useable maximum?

The second is the style of vaporiser that has become popular for "herbs", and by herbs I of course mean cannabis. This is essentially a very small oven, so the contents are vapourized without the need for mixing them with a liquid such as PG or VG. Temperature can again be set fairly accurately over a wide range, so if anyone knows the temperature at which B12 crystals vaporise, you could set the temperature just above that and get B12-only vapour. There is the volcano-style desktop thing, but handheld portable ones are now commonplace too.

 

[ahmo]

skwag and atrutles, and I, have gone on to making saline solution from B12 crystals, using it as nasal spray. Simpler than inhaling, likely safer. There was a group buy of crystals, presumably there will be another in time.

 

[skwag]

Hi Sellotape,

I never got fantastic results with the vaping and I didn't continue vaping much longer than the trials I posted about in this thread. That said, I think everybody who tried vaping is convinced that the method works - it's just a question of how well.

For getting a lot of b12 into your body, there is really no replacement for injections IMO.

 

[garyfritz]

@ahmo, so the nasal delivery is working well for you? I haven't used it since I realized that, due to poor absorption, I'd have to snort some blood-red stuff every 20-30 minutes all day long. Did you find it worked better than my short experiment suggested?

@skwag, I think the oil is a very good alternative to injection. It's not cheap at the dosages I need, but neither was injection and (for me at least) the oil works much better. But if you're talking about 10-20mg/day or more, then yeah, the oil isn't the perfect answer.

 

[ahmo]

@garyfritz Please remind me what your experiment is. When I got a decent spraybottle (Snoot), I've found this method my favorite so far. I'm using it twice a day. I tried more, but didn't feel any gains, and my body never asks for additional. I've increased my folate to meet the B12.

Injection would be my next step. But given my general level of wellness, I just don't get the impression that B12 injections is going to be the thing that *cures* me. I've noticed a few places on my back that are at times super sensitive, as if there's a tick, but there's nothing there. That has been relieved w/ B12, so it seems to be nerve issues. But what I'm looking for is physical and mental gains, and I now believe that's at the level of mitochondria, don't see B12 helping.

 

[garyfritz]

@ahmo, I tried replacing my oil doses with nasal, using a Snoot spray bottle. I applied as many mg nasally as I get in the oil. Within a day I started feeling bad. After two days I had to go back to the oil, and I immediately felt better. When I found that nasal probably only delivers about 2-3% absorption (vs Greg's claim of 80% for the oil), I understood why replacing the same # of mg didn't work.

I currently take about 1.5mg methyl and 4.5mg adenosyl (injected equivalent). If nasal absorption is about 2-3% as reported, I would have to take about 40x more, or 60mg/day methyl. Since we seemed to be limited to about 20mg/ml concentration, that means I would have to administer 3.0 ml = 30 shots. (And I might need to supplement with adenosyl sublinguals.)

If I take 2 shots per nostril, I would have to dose 7-8 times per day. Not quite the "every 20-30 minutes" I was remembering but still pretty darn inconvenient. Especially since I often look like I've got a nosebleed after spraying 2x per nostril. Because of those logistical issues, I never tested 60mg/day. 3 squirts/day of oil is a lot more workable for me, even if it costs about 2x more than 60 mg/day of crystals.

 

[ahmo]

Thanks @garyfritz I only used the oil 1 squirt at a time, per day. I found no difference between B12oils, DIY trnasdermal, and nasal spray. I got an rx for injections, but never filled it. I baulk at the cost. I guess I could try it, see if it it's life-changing. But since I'm not having any other symptoms beyond poor energy, I'm a bit reluctant.