Alternative Ways of Administering High Dose Vitamin B12

[Freddd]

I have some questions related to B12 levels!

. This may have been discussed on another thread but how many people get follow-up levels of B12 done after they have been on it for awhile?
. Are measurements even useful?
. Do various forms of administration, such as those being discusssed in this thread, produce better serum/blood levels?
. What about intracellular levels?
. Do blood levels belie effectiveness or otherwise of the B12?
. Why do some people continue to take mega-doses when their levels are elevated or high in range?
. Is it better to take several types of B12 such as methyl, cyan, hydroxy - rather than just one type of cobalamin?

Hi Francelle,

how many people get follow-up levels of B12 done after they have been on it for awhile?
Are measurements even useful?

Mine was never measured and would be pretty pointless now. At my previous dose of 10mg injected SC 3x per day an estimate of serum level is about 200,000pg/ml. At 10mg x3 per day I get sustained healing activity in the CNS. Twice a day allows fallback. I am doing higher doses currently as a trial. To pay a sizable price to be told my serum cobalamin level is >1100pg/ml is rather pointless.

Do various forms of administration, such as those being discusssed in this thread, produce better serum/blood levels?

A mg put into serum injected IM would produce an instantaneous serum level of about 200,000 pg/ml decreasing by 75% each hour for several hours and start slowing down after that. An SC injection takes up to 10 hours or so to largely enter serum. A 5mg Jarrow held for 2 hours also puts about 1mg into serum over 2 hours so the peak isn't as high but lasts longer. Other methods could likely achieve something similar. I did a urine colorimetry set of tests of sublingual compared to SC injection in order to come up with the sublingual absorption rate.

What about intracellular levels?

High serum levels well in excess of what can be carried by HTC2 allows all tissues to be saturated via diffusion. Even the CNS/CSF is penetrated in the 100,000pg/ml to 200,000pg/ml range or more.

Why do some people continue to take mega-doses when their levels are elevated or high in range?

The serum halflife of high levels is about 30 minutes until it gets down to an estimated 25,000pg/ml or thereabouts and then starts falling off. It takes high levels to provoke CNS healing especially in some disorders such as FMS/CFS where the CSF has low serum level despite relatively high serum levels. In other words it works.

Do blood levels belie effectiveness or otherwise of the B12?

I don't know what you are asking.

Is it better to take several types of B12 such as methyl, cyan, hydroxy - rather than just one type of cobalamin?

It is more effective on more symptoms to take mb12 and adb12, the ONLY 2 active forms in the human body. All others are temporary but inactive forms and cyanocbl is post cyanide detox waste form that is excreted especially rapidly.

 

[dannybex]

So, who's going to be the first one to get game enough to try the "back door" method of taking these tablets, and then be game enough to report back?!

Yes, I'm wondering if anyone has tried this?

Also wondering if anyone has started a thread re this issue, and asking Jarrow (and others) if they'd consider making a sublingual without the citric acid or unnecessary fructose-type sweetners?

 

[sandralee]

Hi All,

I just posted this on another thread. I have absolutely no problem with the rectal administration method of B12, but I'm concerned that the other substances in the sublinguals might afect the lining of the rectum. Does anyone more knowledgeable than I have any thoughts on this issue?

Best wishes,

Sandraf

 

[dannybex]

good question...

Good question SandraLee,

If the citric acid in the sublinguals chelates minerals (calcium) as Rich hypothesized, might it do the same to the calcium, etc., in the tender mucosal skin of the rectum?

Also, wondering if anyone has tried this or other alternative methods yet and has reported back, perhaps on another thread?

d.

 

[Freddd]

Hi Dan,

I have talked to them about this (removal of citric acid etc). We shall see.

 

[Richard Lee]

I have talked to them about this (removal of citric acid etc). We shall see.

Hi Freddd

I wonder to what extent sublingual absorption would be affected by reduced acidity.

By increasing the pH from 3.4 stepwise up to pH 9 there is a gradual decrease in buccal absorption and also uptake into buccal mucosal cells. Vitamin C is only 13.7% ionized at pH 3.4 but over 99.99% ionized at pH 9.
http://journals.cambridge.org/article_S0007114579000052

absorption of some drugs via the buccal mucosa is shown to increase when carrier pH is lower (more acidic)
http://www.positivehealth.com/article/colon-health/sublingual-absorption

 

[hixxy]

This is a really interesting thread I missed out on. I have a lot of trouble getting supplements down my throat because of MCS. I may have to do some experimentation I think.

hixxy

 

[Lynn_M]

.
I was going to try DMSO, but put it aside, mainly as a I read in this old study that B12 cyanocobalamin was not absorbed all that well across the skin using DMSO, no better than using water (but that ethanol worked quite well). Whether this applies to other forms of B12 I don't know.

I'm not sure how reliable that study is. DMSO I understand carries many things though the skin and into the body.

Hip,
I think that may be a relevant study, in that the researchers concluded that cyanocobalamin appears to be readily absorbed through the skin. But I don't understand some of the techniques and conclusions of that study. First of all, it appears that in experiments 4-7, as described in the left column of p. 262, the researchers excised the skin from the area of application, the bandage and skin section were washed with a detergent solution, diluted to 100 ml with water, and then assayed for radioactivity as a measure of absorption of cyanocobalamin. Now why would they include washings from the bandage in a measure of absorption of the skin? Doesn't make any sense to me.

Because the skin absorption, as they measured it, was so high for ethanol, and total absorption was a measure of skin (which included bandage), carcass, urine, and feces, the 10x higher skin average obtained with ethanol made ethanol look like the star solvent.

But aside from the issue of whether bandage washings should be included, is total absorption the best measure of the effectiveness of the various solvents measured (water, ethanol, 90% DMSO)? Maybe the amount of radioactive cyanocobalamin that makes it into the excreta would be the best measure of the functional absorption?

In the first growth experiment, the researched found that 5 micrograms of cyanocobalamin in 0.03 ml DMSO, or in 0.03 ml water, applied daily topically, yielded the same 28-day weight gain as adding 10 microgram cyanocobalamin/kg to the diet of weanling rats. A weanling rat weighs around 60 g.

What really matters is whether these results translate to humans. Has there been any follow-up research with people?

Does anyone else have an opinion about this study? Rich?

Disappointingly from our perspective, the researchers say that preliminary experiments with radioactive hydroxycobalamin applied to the rat indicated considerably higher percutaneous absorption of cyanocobalamin.

 

[Hip]

Hip,
.... First of all, it appears that in experiments 4-7, as described in the left column of p. 262, the researchers excised the skin from the area of application, the bandage and skin section were washed with a detergent solution, diluted to 100 ml with water, and then assayed for radioactivity as a measure of absorption of cyanocobalamin. Now why would they include washings from the bandage in a measure of absorption of the skin? Doesn't make any sense to me.

Because the skin absorption, as they measured it, was so high for ethanol, and total absorption was a measure of skin (which included bandage), carcass, urine, and feces, the 10x higher skin average obtained with ethanol made ethanol look like the star solvent.

But aside from the issue of whether bandage washings should be included, is total absorption the best measure of the effectiveness of the various solvents measured (water, ethanol, 90% DMSO)? Maybe the amount of radioactive cyanocobalamin that makes it into the excreta would be the best measure of the functional absorption? ....

Hi Lynn

My guess is that in the study in question: Percutaneous Absorption of Vitamin B12 in the Rat and Guinea Pig, they measured the amount of B12 remaining in the bandage just in order to check that the total B12 measured adds up to 100%. So in table 5 (page 265), you can see that they are adding up the percentage amounts of B12 measured in the urine + feces + skin + carcass + bandage to get a total, and the total comes close to 100%, as you would expect.

Whether the amount of radioactive cyanocobalamin that makes it into the excreta is the best measure of functional absorption, I am not sure. You can see in table 2 of the above study that by far the largest portion of B12 gets absorbed into the skin, and I presume the skin is acting a some kind of storage depot for the B12. So maybe that B12 in the skin, although large in amount, is not available for use?

I would imagine that the amount of B12 found in the excreta is a better measure of the blood levels of B12, and that the B12 found in the skin and carcass is a measure of the B12 that the body has stored. Presumably it is the blood levels of B12 that are important in ME/CFS, rather than the body stores?

And in which case, in table 2, for the two-day absorption period, it seems that B12 in water has the highest absorption, if judged by the quantities of B12 measured in the feces.

Though in this study: Absorption of Vitamin B12 from the Colon of the Pig, in which they introduce B12 into the colon and measure its absorption, they say (page 1037) that 49.2% was absorbed, and 50.8% was excreted in the feces. In this study, they seem to count the 49.2% figure as the absorption. But I suppose this pig study is a different scenario, as they are introducing the B12 in to the colon, and so the excreted B12 is probably just the B12 that was not absorbed at all, which was purged out of the colon (whereas in the rat skin absorption study, the fecal B12 is a measure of the B12 that was absorbed though the skin, passed through the blood, and finally excreted).

I guess the nearest practicable thing that we can do imitate colon absorption would be a rectal suppository tablet or capsule. And I found a study that said rectally administered B12 in human subjects "was absorbed to a significant extent". See here: Absorption of Vitamin B12 in a Rectal Suppository (I don't have the full paper, just the abstract you see in the link).

Another interesting study is this one: Nasal absorption of hydroxocobalamin in healthy elderly adults, in which they find that the nasal absorption of hydroxocobalamin B12 is 2 to 5%.

 

[Lynn_M]

Quotes from The Journal of Nutrition study under discussion:
From pg. 262, Experiment 4 (Table 3): After the designated time they were killed, the skin was excised from the area of application and the bandage and skin section were washed with portions of detergent solution.5 Combined skin and bandage washings were diluted to 100 ml with water, as were urine samples, and the fecal samples were suspended in 100 ml water for assay. All radiometrie measurements were made by gamma-ray scintilla tion counting. Urine, feces, washings and whole carcasses were measured in a Tobor large-volume counter, and the washed skin samples were measured in the Autogamma instrument for small volune.

Page 265: Values for skin plus bandage washings were recorded in tables 5 and 6 as an indication of the radioactivity accountability achieved in these experiments. Although somewhat variable, an average of 96% of the activity is accounted for.

 

[Lynn_M]

Hip,
In experiment 4 (Table 3) and experiment 5 (Table 4), they washed the skin and bandage together in detergent solution, diluted it, and measured it - I think that's the washings they refer to. Then they measure the washed skin sample separately. In Table 3, where they list the skin measurements, I presume that's the washed skin sample and doesn't include the cyB12 that got washed out of it. I don't understand why they wouldn't have taken a separate measurement of the skin washings, apart from the bandage, and included the skin washing measurement with the washed skin sample measurement. I don't understand why they combined skin and bandage washings together.

In table 6, I agree, they were accounting for total dosage of radioactive cyB12. In that case, the column Wash+bandage appears to include the combined total of skin and bandage washings plus what was still in the bandage, and Skin is what's left of the cyB12 in the excised sample after the detergent washing.

If my interpretation of their methodology is correct, then what is listed as Skin percentages seems to be a spurious figure. I do agree with you that what is in skin seems to be a storage depot, perhaps only slowly absorbed into the tissues. Rather than blood or body stores of B12 being the significant measure, I would think the tissue stores is what is important. I don't know which parameter would best reflect that.

Tables 1 and 2 don't have the ambiguity of the skin measurement. All 3 solvents look close for weight gain. I don't understand how the researchers say rats given 0.1 ug cyB12 had maximal growth, because their weight figures are roughly 20 g less than the rats given 5 ug cyB12.

You say

"And in which case, in table 2, for the two-day absorption period, it seems that B12 in water has the highest absorption, if judged by the quantities of B12 measured in the feces."

I think you mean Table 3, and that's true at the .025 ug amt. of B12, but it's not true at the 5 day absorption period. Nor is it true at the 2.2-2.5 ug amount of B12, at either the 2 or 5 day absorption periods. The solvent with highest absorption rate depends on dosage and days absorption. I don't know that there's a clear winner identified for the solvent with highest absorption.

Several different times I tried tucking a 1000 mcg or a 5000 mcg Jarrow mB12 tablet up my vagina. Each time I had a pink-tinged clear fluid leaking out for about 1.5 days afterwards. Because it was so watery and free-flowing, it got on my underwear and bed sheets, despite wearing a sanitary napkin. I don't consider it to be a practical application method. I think a rectal application would have the same drawback.

I wouldn't think a person could apply much fluid nasally, so I don't see that as a way to deliver much volume of B12.

Based on Rich's report of David Gregg's use of B12 diluted in DMSO, I had bought some 70% DMSO/30% water before I read this study. I dissolved six 5,000 mcg Jarrow mB12 tablets in 1 oz of DMSO and apply 1 ml of that solution to various skin areas every day, giving me 1,000 mcg of mB12 per application. The enamel on my teeth is very thin - I have what is called translucent teeth, not very white - so I don't want to erode them any more.






.

 

[Crux]

Hi Lynn_M ;

I have also found Dr. Gregg's method to be effective. Although I'm fine with a 5 mg. sub. of Mb12 daily, in the past I have tried increasing the amount transdermally. After a day or two with additional transdermal B12, I began to have symptoms of excess. They were : mild anxiety, sleep delay, and feeling a bit overstimulated.

I consider this method to be good for people who have any sort of difficulties with sublinguals. I buy my DMSO from a chemical supply store. They sell a 99% DMSO. I sometimes apply a barrier coat of castor oil because the DMSO can sting. Even the feet can be a good area to apply this solution.

 

[Hip]

Lynn, that study does seem to be a bit confusing regarding their methods, but I don't think it is too important anyway.


In terms of what B12 applications work well:

• I have used a Jarrow 5000 mcg B12 methylcobalamin tablet simply as a rectal suppository, and it works.

• Another thing you can do is crush a Jarrow 5000 mcg B12 methylcobalamin tablet into fine powder (using a mortar and pestle if you happen to have one, else crushing with a tablespoon also works), and then rubbing this fine powder across an area of body skin (I use the top of my thighs), adding around a teaspoon of water to help this fine powder dissolve and sink into the skin. This B12 will then slowly absorb over the next 24 hours or so (it should go on absorbing until you next take a bath, when it will be washed off).

• I found intranasal application of B12 works very well, but you need to use a liquid B12 that has 1000 mcg per drop. If you tilt your head right back, so that you are looking up at the ceiling, and place a dropper pipette filled with B12 liquid inside your nose, you can squeeze some B12 drops directly into the openings inside your nose that lead into your nasal cavity. Each nasal cavity will hold about 4 or 5 drops, I have found (if you use more, you'll find some of the liquid B12 runs down the back of your throat). So with 5 drops per cavity, you can easily put a dose of 10,000 mcg of B12 into your nose, which is a good dose, assuming that you get 2 to 5% absorption. Note that if the B12 liquid has a citric acid preservative, this may sting the nose like hell, so cautiously try one drop first. In fact, taste the liquid on the tongue first: if it has any sharp tang, it will sting in the nose. What I have done in the past is added a pinch of sodium bicarbonate to the liquid B12 to neutralize the acid, and that makes it possible to put the liquid B12 into the nasal cavities without any stinging.

All these three methods are very viable, I have found.

 

[Lynn_M]

Crux,
I interpret your symptoms of overstimulation to mean that the transdermal B12/DMSO applications are being absorbed. That's good!

Hip,
I take it the rectum doesn't secrete a lot of fluid in response to the mB12 tablet.

Good to know all three of the methods are viable.

 

[Hip]

I take it the rectum doesn't secrete a lot of fluid in response to the mB12 tablet.

No, there are no problems like that. Taking medicines by rectal suppository is very common in countries like France.

 

[iacyi]

I have been trying B12 lozenges as suppositories, with some aloe vera gel to help it on its merry way.

One day when I forgot to take one I did notice feeling worse, which seems promising.

However, particularly after switching to Jarrow B12, I get quite a bit of pink mucous and sometimes bloating. I don't know if it is just the unabsorbed portion or a reaction to the additives. Would mucous significantly reduce the absorption or is it to be expected?

 

[Hip]

I have been trying B12 lozenges as suppositories, with some aloe vera gel to help it on its merry way.

One day when I forgot to take one I did notice feeling worse, which seems promising.

However, particularly after switching to Jarrow B12, I get quite a bit of pink mucous and sometimes bloating. I don't know if it is just the unabsorbed portion or a reaction to the additives. Would mucous significantly reduce the absorption or is it to be expected?

Jarrow Methyl B12 has citric acid as a preservative, and the acidity may be irritating the rectal mucous membranes.

Not sure if this might affect absorption or not.

 

[Lotus97]

I have been experimenting with some alternative methods of absorbing high doses of vitamin B12

Great idea for a thread. I assume no one has a problem expanding this beyond just B12 since many of us here take a lot of different supplements and are looking to save money by increasing their efficacy. I've actually been trying some of these for the past few days and by pure coincidence I stumbled upon this thread. This thread has given me a lot of new ideas and I also have some other ideas that might not have been mentioned yet.

Intranasal. Placing some liquid B12 into your mucous membrane-lined nasal cavity, using a dropper pipette. You need to place the tip of the pipette inside the openings to the nasal cavity; these openings are found at the end of each nostril. Lying down on your back and tilting your head backwards while administering allows the B12 drops to better enter the nasal cavity. Note: test any B12 liquid on your tongue first, and if there is any harshness or acidic sharpness to the taste, it may sting once in the nasal cavity. If it passes the tongue sharpness test, then next test a small amount in the nose, to ensure it does not sting, before taking a larger dose.

Intranasal. Snorting up powder from a finely crushed B12 tablet via a drinking straw. (Best not performed outside a police department). Again, if the powder tastes acidic, it may sting the nose. Test a small amount of powder in the nose first, to ensure it does not sting.

Intrasinus administration. Vitamin B12 powder or B12 drops dissolved in mildly saline water, and administered into nasal and sinus cavities via nasal irrigation (yoga neti). Both the nasal and sinus cavities are lined with mucous membranes. Very wasteful, as much of the administered liquid tends to drip out of the nose.

Wellllllllll, I've done my fair share of snorting in the past so I don't mind doing it again except that I have chronic sinus problems and I'm concerned that would make it worse. If anyone is thinking of doing this DON'T use rolled up money. They are one of the most contaminated things you can use. The suggestion of using a straw is better, but straws are kind of hard which means they are sharp enough to cut the inside of your nose if you're not careful. What I've found works the best is cutting a piece of computer paper and rolling it up. This can be a little sharp too so you also have to be careful. You can try is bending inward the part of the paper going into your nose. You also need to make sure it is not too short and not too long. Same with a straw, you're going to want to cut it down to a shorter length too. The right size might vary depending on the individual, but I suppose a place to start would be 2 inches/5 cm.

I was actually considering putting various supplements in an empty saline nasal spray bottle, but I some questions about that:

Are there certain supplements that either become unstable or lose their effectiveness if they remain in water too long? I was thinking about mixing up everything I was going to use for the day and then taking them in divided doses throughout the day. I remember reading that glutathione becomes unstable in water after a certain time and also creatine. I'm not sure how much time on either of those are, but I'm wondering if anyone knows which things can stay stable/potent in water or some other kind of liquid. Are other liquids better?. I've read that lecithin increases absorption, but I don't know if it's necessary for this kind of method. There's various liquid phospholipids supplements that can either be used individually or mixed with other supplements. I also mix various supplements up in a water bottle and drink it throughout the day. Off the top of my head, here's the ones I have questions about either for a nasal spray or a water bottle: NAC, Alpha Lipoic Acid, B vitamins, Vitamin C, Amino Acids, Minerals. Another thing I'd like to know is if I mix something that's acid and alkaline together and their pH changes will that change other properties of the substances? Of course you should probably try each supplement individually if you're using a nasal spray before you do multiple things.

 

[Hip]

Are there certain supplements that either become unstable or lose their effectiveness if they remain in water too long? I was thinking about mixing up everything I was going to use for the day and then taking them in divided doses throughout the day. I remember reading that glutathione becomes unstable in water after a certain time and also creatine.

Vitamin B12 in the methylcobalamin form is very unstable when light shines on it; it breaks down in a matter of hours by the action of light (photodecomposition). So if you were going to dissolve methylcobalamin into water, you'd want to store your solution in a dark opaque bottle, so that no light gets in.

 

[Hip]

Here is a new thread describing a more efficient way to absorb vitamin B12 and other supplements sublingually:

Sublingual Massage — Absorbing B12 Fast & Efficiently Under the Tongue