An interesting bit of info I received from a friend who has a PhD in Biochem.It discusses the potential dangers and (flawed marketing picture) associated with the use of Creatine Ethly Ester:
1) CEE is a true covalently bonded ester and is absorbed into blood and
tissues as the intact molecule. This is the picture that the
manufacturers would have us believe and is the basis for why they claim
CEE is superior to creatine monohydrate. However, inside cells CEE
will be unreactive with creatine kinase and may be a potential
competitive or non-competitive inhibitor to the enzyme. This would
make it toxic to brain, heart, testes, muscle and all other CK
containing tissues. People by now should be dying, but clearly are not
and this means 2) and 3) are the more likely. Nonethess, CEE should be
treated as a potentially toxic phrarmaceutical and in the US should be
treated as a drug, which requires multi species studies
to estimate LD50's and potential sites of tissue damage etc. However, recently I have been told that CEE did get new dietary ingredient status (scary).
2) CEE is hydrolysed to creatine on absorption from the gut. In this
case CEE offers no advantage over creatine monohydrate which has a
bioavilability of 100%. Indeed if hydrolysis of CEE is less than 100%
then it will be inferior to the monohydate. But in the case of
hydrolysis there are no circumstances in which it could be better than
the monohydrate in increasing tissue creatine levels. Obviously CEE
manufacturers would prefer 1) except that they then shoot themselves in
the foot over the issue of potential toxicity.
3) CEE is not a true covalently bonded ester. The whole of this is a scam with the compound ionizing in solution to free creatine, as does the monohydrate and all salts of creatine. In this case CEE would again
represent no advantage over creatine monohydrate, except to the seller
who can double the price.
The failure of the US sports nutrition community (industry and the
universities) to call for closer examination of CEE seriously questions its
credibility in the eyes of many scientist in this country and the world. A simple water solvation test would answer 3), i.e. whether or not it was a covalent or ionisable derivative of creatine. The work time would be about one hour. Investigation of whether CEE is a competitive or non-competitive inhibitor of creatine kinase would take 2-3 hours. If either of these occured then clearly CEE must be investigated in at least two species to investigate lethality and potential organ damage. If on the other hand CEE is ionisable then I see no reason why a bioavailability study should not be undertaken comparing this, on a molar/molar basis, with
creatine monohydrate. My guess is that plasma AUC would be identical.
Again a very simple study.
Here is an interesting study on CEE that might be of interest to you:
Creatine ethyl ester rapidly degrades to creatinine in stomach acid
Child R and Tallon MJ
1Department of Life Sciences, Kingston University, Penrhyn Rd, Kingston-upon-Thames, United Kingdom. 2University of Northumbria, Sport Sciences, Northumbria University, Northumberland Building, Newcastle upon Tyne, United Kingdom,
[email protected]
Creatine ethyl ester (CEE) is a commercially available synthetic creatine that is now widely used in dietary supplements. It comprises of creatine with an ethyl group attached and this molecular configuration is reported to provide several advantages over creatine monohydrate (CM). The Medical Research Institute (CA, USA) claim that the CEE in their product (CE2) provides greater solubility in lipids, leading to improved absorption. Similarly San (San Corporation, CA, USA) claim that the CEE in their product (San CM2 Alpha) avoids the breakdown of creatine to creatinine in stomach acids. Ultimately it is claimed that CEE products provide greater absorption and efficacy than CM. To date, none of these claims have been evaluated by an independent, or university laboratory and no comparative data are available on CEE and CM.
This study assessed the availability of creatine from three commercial creatine products during degradation in acidic conditions similar to those that occur in the stomach. They comprised of two products containing CEE (San CM2 Alpha and CE2) and commercially available CM (CreapureÒ). An independent laboratory, using testing guidelines recommended by the United States Pharmacopeia (USP), performed the analysis. Each product was incubated in 900ml of pH 1 HCL at 37± 1oC and samples where drawn at 5, 30 and 120 minutes. Creatine availability was assessed by immediately assaying for free creatine, CEE and the creatine breakdown product creatinine, using HPLC (UV)
After 30 minutes incubation only 73% of the initial CEE present was available from CE2, while the amount of CEE available from San CM2 Alpha was even lower at only 62%. In contrast, more than 99% of the creatine remained available from the CM product. These reductions in CEE availability were accompanied by substantial creatinine formation, without the appearance of free creatine. After 120minutes incubation 72% of the CEE was available from CE2 with only 11% available from San CM2 Alpha, while more than 99% of the creatine remained available from CM.
CEE is claimed to provide several advantages over CM because of increased solubility and stability. In practice, the addition of the ethyl group to creatine actually reduces acid stability and accelerates its breakdown to creatinine. This substantially reduces creatine availability in its esterified form and as a consequence creatines such as San CM2 and CE2 are inferior to CM as a source of free creatine.
Supported by Cr-Technologies, LLP, London, England
