Creatine High-Test

Among the multitude of food supplements on the market, none can match the research data associated with creatine. Since its introduction in the late ’80s, countless articles have appeared in science journals extolling its benefits. Not all studies have shown that creatine is clearly beneficial for athletic and exercise purposes, but the vast majority have. Based on those studies, the consensus is that supplemental creatine will produce a good response in about 70 percent of those who use it. Of the 30 percent who don’t respond, most eat considerable amounts of red meat and other foods naturally rich in creatine, so they have already gradually loaded their muscles with it.

Creatine is a natural substance made in the body from three amino acids: arginine, methionine and glycine. It’s primarily synthesized in the liver, secondarily in the kidneys and pancreas. The body synthesizes an average of one gram of it a day and gets another gram from food sources. All commercial creatine is synthetic.

The research on the benefits of creatine is impressive. One study looked at all existing studies pertaining to effective food supplements for those engaged in strength training and concluded that only two had enough solid data to prove that they worked. One was creatine; the other was an amino acid derivative called HMB.

Lately, a number of studies have discovered potential medical uses for creatine, such as in the treatment of certain neurological diseases, and even as a type of nootropic, or brain booster, in normal people. I try to stay current on all the published research on creatine, so I was recently nonplussed to hear about a form of creatine that I had no knowledge of.

It’s called creatine ethyl ester. You may notice that a number of advertisements are touting this new form as being superior to the more common creatine monohydrate. The ads say that creatine ester is much more efficient than other forms of creatine. Other claims are that it’s more soluble in water and doesn’t degrade in solution, as do other forms, and that because of its heightened absorption characteristics, you need to take far less. That, in turn, results in a total absence of side effects often attributed to other forms of creatine, such as bloating, gastrointestinal distress, muscle cramps and so on.

So what is the truth about creatine ester supplements? To answer that question, you must first understand what the ester part of creatine does. To produce a creatine ester, creatine monohydrate reacts with alcohol in an acidic environment. That removes the water attachment to creatine and changes its absorption effects. Generally, esters are more soluble in fat, including the fat contained in cellular membranes. That’s the reason long-acting injectable anabolic steroids are often esters. The ester attachment increases the dispersion and absorption of the drug in the body and extends its activity level.

You’d think that with all the claims being made about this new form of supplemental creatine, there’d be an impressive array of studies to back them up. At present writing, however, there are precisely zero published studies’although I did find a patent application pertaining to creatine ester.

According to that application, creatine ester was developed by two men from Omaha. In stating the reasons they were applying for a patent, they noted that other forms of creatine are poorly absorbed in a water solution, averaging only 1 to 14 percent absorption. Consequently, users have to take large amounts of creatine, starting with five grams, or about a teaspoon. The larger doses often lead to the commonly reported side effects mentioned above.

The patent application further says that other forms of creatine have poor membrane solubility, meaning that they cannot readily penetrate lipid barriers’such as cell membranes. The acidity of the stomach also presents a formidable natural barrier, rendering much of the creatine dose into useless creatinine.

The scenario changes with creatine ester, say the inventors. The ester protects creatine from degradation in the harsh acid environment of the stomach. Once it gets past there, enzymes in the intestinal lining and in the blood called esterases liberate the creatine from the ester, producing bioactive creatine, which then travels to the muscle. Far more creatine is absorbed, so considerably smaller doses of creatine ester can pack a greater metabolic punch than what you get with normal creatine supplements. The authors call creatine ester a pronutrient because of its absorption characteristics. ALL Thanks to the greater absorption, the average dose drops to only two grams, and users don’t have to do a loading phase, say the inventors. It all sounds good, so I decided to ask a renowned creatine researcher who has no commercial ties to any company selling creatine. This scientist didn’t think that increased lipid solubility made a difference with creatine, since its uptake in muscle is limited by the creatine transporter protein in muscle, which is mainly powered by sodium. But that doesn’t mean it doesn’t work; all it means is that more research is needed.

In other words, it’s too soon to tell if creatine ester is superior. I’d like to see some studies that directly compare creatine esters with the old-fashioned creatine monohydrate supplements. You may want to experiment with it and see what kind of results you get.

The inventors of creatine ester also applied for another patent related to creatine ester. It involves using creatine ester as an anti-inflammatory substance. They say that creatine reduces inflammation in a manner different from the usual drugs used for that purpose’and unlike those drugs, creatine ester causes no side effects. The best guess as to how creatine ester does that is through an antioxidant activity that leads to a reduction of inflammatory mediators in the body. Creatine has never been used for that purpose because it would take huge amounts. Because of the alleged greater uptake of creatine ester, however, that problem is eliminated.

Remember, all present creatine forms rapidly degrade into creatinine. If creatine ester remained stable in liquids, though, it could be used in the formulas for ready-made drinks and other liquid products. There’s lots of promise there.

Rumors are circulating that the Food and Drug Administration is already taking a hard look at creatine esters. Some in the FDA think that the ester characteristic of the supplement comes a bit too close to having drug activity. If that proves true, any emerging popularity of creatine ester may spell its doom, since the FDA would likely order the product removed from sale to ‘protect’ consumers. If you’re going to give it a shot, do so soon or you may never get the chance.