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from: http://www.labrada.com/members/week228.htm#art3
The Truth About Creatine Stability
By Dr Mark J Tallon PHd BSc, MSc, CBiol, MIBiol, CES
The facts about creatine monohydrate and pH stable formulations.
“Is there such a thing as “pH stable creatine” formulas? Here we examine the REAL evidence behind issues causing waves in the sports nutrition industry”.
Of late scientific attacks on creatine, its absorption, safety and subsequent uptake into muscle have hit overdrive with the release of so called pH stable and pH correct creatine. However, there comes a point when you have to take a stand and put pseudo-scientists in their place when the information being touted as scientific FACT has the potential to harm the sports supplementation industry as a whole. If you have wasted you hard earned cash on these overpriced products your going to be really P***ed by the time you finish reading this article. In this weeks issue of the LBC I am going to provide you with the REAL science behind how much creatine really are absorbed when given in the only PROVEN performance enhancing form of creatine. That’s right plain old “creatine monohydrate”. So if you want to know the influence of low pH, stomach acids, and fluids on creatine levels don’t stop reading just yet as this is the article you have all been waiting for…
The reason these companies have been able to play on your insecurities about the uptake of creatine and its so-called instability is that there have been relatively few studies that assessing the pharmacokinetics of creatine [1,2]. However, there is data to qualify many of these issues including:-
1. How long does it take for a 5 gram dose to get through the gut and how much reaches the muscle transport system?
2. What is the effect of pH on creatine and its subsequent breakdown to Creatine?
3. What amount of creatine is absorbed into muscle during loading?
4. What is the effect of cooking on creatine and creatinine in meats?
The answer to these questions will provide you with concrete evidence of just how effect and stable creatine really is.
Myth # 1: Creatine breaks down massively in low pH!
Work presented by Professor Roger Harris way back in 1999 at a meeting in Milan [3] gave some great insights into creatine metabolism but more than that unequivocal scientific PROOF that creatine is highly stable in low pH environments. In figure (1) you can see the effect of creatine monohydrate placed into A low pH environment (pH <2) to simulate gastric juice, the exact environmental/physiological conditions experienced by creatine once ingested. This measurement period represents the typically time it would take for a full 5 gram dose to pass from the gut into your plasma (see figure 2). As you can see in fig.1 the actual breakdown / loss of creatine is less than a few %. “Hardly the huge loss you have been lead to believe occurs by so called stable creatine manufactures”.
Figure.1 Adapted from. Harris et al. 1999 [3]
Myth # 2: Creatine is 100% converted into creatinine at low pH in minutes if not seconds!
Well in the last myth we have looked at the short-term or typical time a 5g dose of creatine would take to pass into the blood stream (<6hours Persky et al. 2003 [2]. see figure 2). But what about at other pH levels not found in the gut but maybe in drinks of other fluid suspension for your creatine? Well it’s suggested by so called pH creatine stable specialists that in many of these delivery forms creatine is degraded 100% to creatinine across a whole selection of pH values in seconds? Well again guys lets take a look at some real data and not just looking at minutes or hours or even day but what about months? Again here is some further data from the Milan conference [3] also available from Patent data [4]. As you can see in figure (3) we have a description of creatine in a selection of pH fluids ranging from 3 – 7 (2g Cr.H20 in100ml of 0.1M citrate phosphate buffer heated to 90oC for 30 minutes). In figure (1) creatine was shown to be so stable its breakdown was accelerated in this next experiment by heating on day 0 then monitoring the subsequent breakdown of creatine in different pH’s over time (see the effect of heating in figure 4). Even with this extreme method you can clearly see after 120 days of suspension in a range of pH’s levels creatine degradation is never 100% to creatinine. In fact we see equilibrium develops (creatine /creatinine) with at worst a 70% loss of initial values at 35 days (yep not seconds or minutes). Only a slight change in the citrate buffer content (to 0.2M) can actually cause creatine to increase at pH 5, 6, 7 further more at lower pH’s as found in the gut (pH <3) maximum loss by day 100 is only in the order of only 40%.
Figure.2 Adapted from Persky et al. 2003 [2
So what does that mean for you? Well practical application wise you could place 17g of creatine monohydrate in any pH fluid of between 3-7 and worse case scenario (gut pH 3.0) after 4 months of your creatine just sitting there you still would have enough creatine to maintain your muscle creatine stores following a loading phase (i.e. 5 grams worth). Best-case scenario at a pH 7.0 solution (such as tap water) you will have 85% of the original creatine dose you placed in your drink at day 120. So anyone claiming a 100% breakdown of creatine in fluids, juices or similar liquids in minutes or seconds are pulling your chain, or more importantly your purse strings…don’t be fooled!
Myth # 3: Most creatine is broken down to creatinine before it ever reaches your muscles!
If myth #3 were for real then we would expect no change in muscle or plasma creatine levels during the loading phase. Its common sense right but let’s take a look at some evidence just to make our point!
The first real study to examine this in detail was by Harris et al. (1992) [1] showing 5g taken 4-6 times per day for 4 days increased total muscle creatine stores by as much as 50%. Interestingly, what was also demonstrated was that in day 1 of supplementation 60-80% of the administered dose was retained in the body’s tissues meaning only 20-40% was lost in urinary output. This loss steadily increased over the subsequent days reflecting the muscle creatine concentrations reaching their upper storage capacity rather than conversion of creatine to creatinine due to the effect of low gut pH on creatine stability. If it was an issue of pH rather than muscle tissue having a finite capacity for retention we would see much less uptake on day one of supplementation. Again this is real evidence proving “Creatine is not degraded 100% to creatinine in low pH environments such as the gut”.
On a secondary note many companies have further exaggerated poor absorption of creatine by calculating creatine taken up into muscle versus the total grams of creatine given as a supplement. However, as the published absorption studies in humans use creatine monohydrate not pure creatine you are only giving 0.88 grams of pure creatine per gram of creatine monohydrate. Another way of looking at this is to say for every 20g of creatine monohydrate (a creatine molecule attached to a water molecule) you are in real terms giving 17.5 grams of pure creatine. Therefore, unless actually base you calculation on pure creatine delivered you will underestimate the actual creatine retention levels. Because many of these supplement companies know this they can provide incorrect figures for absorption so be aware.
Figure.3 Adapted from Harris 1999 [3]
Myth # 4: Creatinine is a toxic waste product that should only be formed from your muscles!
Bulls**@… this is the worst lie of them all! Creatinine is a natural byproduct of creatine metabolism and any product; I mean any product that tells you they can increase your creatine levels without substantially increasing your excretion of creatinine is lying. But that said what about the claims creatinine is a toxic waste product? Causes cramps or bloating? AND finally should creatinine only be formed in your muscle cells and not before (as claimed)? That’s right guys these factors are all claimed to be a consequence of creatinine formation from supplemental creatine but are they correct?
Again these claims are scientifically incorrect and darn right inflammatory. Creatinine is formed not only from creatine metabolism in muscle tissue but also from other tissues that metabolize creatine such as your brain. So what about the cramps and bloating? Well again no literature to back this up either with regards creatinine being the source of these problems. The likelihood is that creatine is the causative factor especially when it comes to cramps due to associated increases in intracellular fluid levels during loading (0.5 – 2 kg). However, this is not a new phenomenon as the same occurs with glycogen loading. Hence, the recommendation during the initial loading phase that extra water should be taken on board maybe beneficial. However, the whole issue of muscle cramping has been covered in the scientific literature with no evidence of cramping presented in a study of US college football players monitored for up to 84 days taking 2-25g Cr.H2O/ d (Greenwood et al. 2003) [5]. Finally, what of the main claim of creatinine being toxic? Again evidence to the contrary folks. The confusion and misrepresentation of the facts about creatinine have been used to pull the proverbial scientific mask over your eyes for some time.
Figure.4 Adapted from Harris 1999 [3]
Because creatinine is used as a by physicians as a marker of kidney function when elevated levels are found automatically physicians can jump to the conclusion of kidney malfunction. The fact is this could not be further from the truth because as creatine intake is increased (either through meat intake or supplementation) creatinine excretion will also increase concomitantly. In fact numerous papers have been published of which I am sure many of you are well aware of proving the safety of creatine supplementation including: Juhn and Tarnopolsky, 1998 [6], Kamber et al. 1999 [7], Kreider et al. 2003 [8]; Mayhew et al. 2002 [9]; Mihic et al. 2000[10]; and Volek et al. 2000 [11] to name a few. These studies up to 10 years in length have assessed kidney function and many other markers of health and no negative impact of supplementation was seen.
The recent suggestions and statement that so-called new data is backing up creatinine toxicity is not backed by any reference material in anyway shape or form. Even though there is some data within the literature as hypotheses or case studies these so called incidences of toxic creatine supplementation on closer inspection reveal subjects were already on medication that influences creatine metabolism such as cyclosporin and/or had pre-existing kidney malfunction (nephritis syndromes). Therefore, we have no choice based on all the available evidence to conclude creatine is safe and effective when taken in recommended quantities.
Now for something new...
Beyond the so called inert and toxic claims against creatinine it is actually a metabolite beneficial to our bodies in many ways; let me shed some light on something you may not have heard before. For some years now the bacteria in our gut and intestinal tract know as intestinal flora has been shown to be vital for optimum immune system function [12] as well as absorption of many important nutrients with respect to bone health and muscle metabolism e.g. Calcium [13]. So how is this related to creatinine formation? Well creatinine is simply not just finished regarding its metabolism in our bodies once it is broken down from creatine. It can take many pathways in our bodies, one of which is to chemicals (1- methylhdantoin) that provide a nitrogen source for or gut flora [14 - 17]. So in some ways creatinine is a natural and beneficial resource for our bodies and not a TOXIN some are tying to make us believe. We already know that this beneficial bacterial flora has adapted to exist in an acid environment i.e. Gut. Therefore that constant use of highly alkaline (circa pH 12) may damage the efficiency and or kill many of these beneficial bacteria leading to decreased absorption of many vital vitamins and minerals. Over time it is even possible the damage to the gut flora by excessive alkaline pH could decrease the uptake of the metabolite they are claiming is absorbed better at alkaline pH “CREATINE”.
A Final Word
“Fraudulent claims threaten the foundations of our industry!”
With the sports nutrition industry under increasing governmental pressure on the safety and self regulation of our supplements widely inaccurate claims can add further fuel to the FDA fire. Suggesting a supplement that has been the saving grace of our industry for the past decade is a toxin producing compound; threatens the very core of research proven efficacious products. The worst part of all is they cite not one specific reference to back their claims on toxicity of creatinine. Now it seems to me if this stuff is so fantastic why have no peer reviewed studies been ran on it? The typical reply from charlatans like this is oh its in press. Well as in what journal then contact the journal guys and you will find that there is no actual submission at all.
I am all for innovation as long as compounds are proven safe; but when clinically valid nutrients such as creatine are attacked by pseudo-scientists with no academic qualifications something has to be done. The future of the industry is in your hands as well as scientists like me, so lets spread the word and protect the nutrients that provide the foundations of which our industry and lifestyle are built.
Nb. For your interest other studies on creatine stability confirming the work of Professor Harris are listed in additional materials following the central reference list.’
REFERENCES
Mark Tallon is an applied nutritional biochemist and a specialist on the application of dietary supplements for performance and physique enhancement. He is the CEO and founder of Oxygenics, Ltd., which provides scientific and technical intelligence services to the dietary food and supplement industry, as well as providing one of the most comprehensive dietary supplement newsletters today.
Contact Dr. Tallon at www.oxygenix.com
