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Creatine - It's All About Absorption!

The trick with any supplementation is to allow for maximum absorption, which is why the general rule is that the lightest molecular weight will usually get absorbed the best. Here I am going to talk about creatine absorption and studies relating to it.

By: Dr. David Ryan

A world-class lifting friend of mine had a very significant "occurrence" with creatine once.

He was trying to mix creatine with phosphorous, to make phosphocreatine, which is what the body uses to make massive gains in endurance and size. He found the creatine, but went to a veterinarian-grade magazine and bought 2 kilos of phosphorus.

A few weeks later he was in my clinic, complaining about extreme stomachaches. I explained to him that he wasn't a horse, in spite of his desires to eat and act like one; that he remained a human and that he was basically eating soap. He later ended up losing his gall bladder over the whole situation.

The point here is that what works for one species as food, can be toxic to another. It is all about absorption.

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When you take any supplement, you want to maximize the body's absorption of the material. If you take a 1000 mg of some product, likely only 50% or less will actually get absorbed. Most is filtered out by the kidneys or the liver and is then flushed down the toilet during the next bathroom call.

The trick with any supplementation is to allow for maximum absorption, which is why the general rule is that the lightest molecular weight will usually get absorbed the best.

If you are still questioning the topic of "Does Creatine Work?", then read these following related articles and specifically their cited studies.

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Is Creatine A Steroid?

Recently a very popular political official was offering advice on the public airwaves, and used the terms "steroid" and "creatine" interchangeably. Let's make a point, right here, right now - Creatine Is An Amino Acid Only!

In other words, it is just food... protein to be exact. It is not a steroid, and isn't even in the same class of molecules. So that particular political official should take a basic organic chemistry course. If you eat steak, you get L-Creatine.

So, are we going to put creatine in the right perspective now? Telling kids they can't use this product is insane. This product works, and education on the product and how to properly use it is the way to go, not sensationalism and misguided information about ill effects.

Bodybuilding.com has asked me to uncover the mystery of probably the fastest growing supplement next to protein, that being creatine.

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What Do Cr And PCr Do?

Our muscles run on an energy system that are based on ATP (adenosine triphosphate)/High Energy and ADP (adenosine diphosphate)/Low Energy. The process of changing ATP to ADP is energized by PCr. Now it doesn't take a rocket scientist to see that PCr donates its P to ADP to make ATP.

What Do Cr And PCr Stand For?
"Cr" is short for Creatine, and "PCr" is short for Phosphocreatine (creatine phosphate).

Creatine has been studied for many decades now. Most of the strongest research comes from a Dr. Walker who has identified the activities of Cr in the human body.

Along with Dr. Walker, Guerrero-Ontiveros, Wallimann, as well as others have established important factors regarding the transport and absorption mechanisms of creatine.

  • Cr is produced by hormones or is obtained from diet.

  • Most people produce around 1 gram of Cr/day.

  • Taking Cr as a supplement raises the body's levels of Creatine and returns to normal levels when the Cr supplementation is stopped.

  • Cr and Phosphocreatine (PCr) are both primarily stored in the skeletal muscle and specifically Type 2 muscle.

  • Catecholamines (hormones/neurotransmitters), insulin-like growth factor 1 (IGF-1), insulin, and exercise can influence the net uptake of Cr into skeletal muscle.

What Is IGF-1?
IGF-1 is a protein hormone similar in molecular structure to insulin. IGF-1 plays an important role in childhood growth and continues to have anabolic effects in adults.

IGF-1 is produced by the liver upon stimulation by HGH (human growth hormone), and stimulates and regulates cell growth and multiplication in bones, cartilage, and nerve cells, among other things.

  • Once in the blood, Cr is transported into tissues against a concentration gradient through a sodium and chloride-dependent transporter (CreaT). CreaT is similar to the transporters for dopamine, guanidino, γ-aminobutyric acid, and taurine.

Several theories exist about how Creatine actually increases muscle cell mass. Most are related to Cr attracting water and then resulting in an anabolic (muscle building) reaction to activate protein synthesis.

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Dosing

The problem with supplementation is that no one offers much information on what amount of creatine you should take. Lucky for us, creatine has medical uses for muscular dystrophy and other muscle wasting diseases.

Currently, manufacturers' instructions for athletes' use of Cr follows a dosing regimen of a "loading" phase of 20 g/day (4 x 5 grams) for 5 days and a maintenance dose of 3 to 5 g/day thereafter.

The actual dosing has been reviewed due to the fact that many researchers are looking at the medical benefits of Cr. This allows for all of us to benefit, due to the millions of dollars spent on this topic, which doesn't usually occur with most nutritional supplements.

  • Investigators have found that intramuscular Cr levels increase from 17 to >20% with a dosing regimen of 20 to 30 g for 2 or more days. It has also been reported that up to 20% of this increase is due to PCr.

  • More recent studies have shown that supplementing 3 g/day of Cr over 30 days, after ~2 days of loading, maximal accumulation of intramuscular Cr occurs and therefore amounts of >20 g/day are unnecessary. It would appear that this initial loading is necessary, but only at 20g for two days. This research is related to powdered form of Cr and does not correspond to the liquid form Cr.

  • The maximal accumulation of intramuscular Cr in humans is reflected in the progressive increase in urinary Cr with continuous Cr ingestion.

  • Ingestion of 5g of creatine will show maximum blood level capacities in less than one hour and will last for several hours. Taking glucose with Cr will result in a reduced absorption.

  • Research has also shown that Cr levels in humans can remain elevated for up to 1 month post-supplementation.

  • The activities of the Cr have been shown to be similar between men and woman, but no real studies have been processed for athletes below the age of 18. However, the same principles of creatine supplementation would still apply.


Factors Associated With
Cr Absorption & Removal

One major concern is how Cr is absorbed and then removed from the body. The entire process is related to the molecular weight of any substance. The actual molecular weight of Cr is 113 and it is slightly positively charged.

To obtain maximum absorption, the manufacturer must obtain the lowest molecular weight to imitate the original molecule, which should be a consideration when you start researching the different substances offered on the market.

Also remember that the addition of other substances with creatine can delay or prevent the absorption of Cr through the intestinal tract.

Clearance of Cr from the blood is dependent on intramuscular Cr levels, hormone levels, muscle mass, and kidney function/glomerular filtration rate (GFR). The removal of Cr is relative to kidney function. The more water you drink, the more water you release and the Cr is removed from the blood.

The only way to improve the absorption of Cr is to inject it directly into the blood stream. This is the current interest of the pharmaceutical companies. This is extremely important for the treatment of various diseases such as muscular dystrophy. Most of the future research and advances will be spun off of these clinical studies.

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Liquid Vs. Powdered Creatine

Let me just say this; I offered a significant amount of time to the manufacturers of liquid creatine to produce information to support their product. As of now, no information has been produced. So let me go off on a Dr. Ryan opinion poll: Which form of creatine works for you?

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Which Form Of Creatine Works For You?

Liquid.
Powder.

One odd job I worked at for a while was for the Chemical Abstracts Services here in Columbus, Ohio. This company collects abstracts from around the world and translates the research abstracts into any language. Every piece of research literature comes into this office from every lab.

So I have access to all the chemical research in the world, literally. So for this topic of liquid creatine I asked for available information.

There were no abstracts available, except one: "The Creatine Content Of Creatine Serum And The Change In The Plasma Concentration With Ingestion Of A Single Dose" by Harris et al.

It stated that liquid creatine offers no increase in blood creatine levels after ingestion.1 I then went after information on the available data and found that much of this information is related to a third-world entity, which strikes my scientific nature the wrong way.

orange juice While the debate on this topic goes on, the manufacturers still need to establish their data on this topic.

Nutritional scientific data is not a strong suit of third-world countries. Sorry, but there are not a lot of muscle men walking around the Gaza Strip!

As for a precursor to liquid creatine, I was told that the model for it is from the invention of liquid Vitamin C. Well I have to say this: What the heck is orange juice? Isn't that stable liquid vitamin C?

Fig. 1.  Pathway Of Creatine Metabolism.
Pathway Of Creatine Metabolism
Click Image To Enlarge.
Catalyzed by AGAT, catalyzed by GAMT, catalyzed by creatine kinase (CK), spontaneous, catalyzed by creatine amidohydrolase, catalyzed by glycine oxidase, and catalyzed by semicarbazide-sensitive amine oxidase (SSAO). Dotted pathway indicates recently hypothesized toxic formation of formaldehyde by Yu and Deng (2000).


Conclusion

Let me finalize this on this topic. In spite of all this, I have used liquid Creatine, but I will change to powdered creatine after writing this article. Gotta use what works and that is that!

    To View Top-Selling Creatine Products, Click Here.

Additional Reading

  1. "The Creatine Content Of Creatine Serum And The Change In The Plasma Concentration With Ingestion Of A Single Dose.", Harris RC, Almada AL, Harris DB, Dunnett M, Hespel P.J.; Sports Sci. 2004 Sep; 22(9):851-7. School of Sports, Exercise and Health Sciences, University College Chichester, College Lane, Chichester PO19 6PE, UK.
  2. "Acute Creatine Loading Enhances Human Growth Hormone Secretion.", Schedel JM, Tanaka H, Kiyonaga A, Shindo M, Schutz Y.; Laboratory of Exercise Physiology and Biomechanics, Graduate School of Physical Education, Chukyo University, Toyota, Japan. Jean-Marc. J Sports Med Phys Fitness. 2000 Dec; 40(4):336-42.

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Creatine - It's All About Absorption!
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