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Protecting the Quarterback

Protecting the Quarterback
Delivery systems are a huge factor in delivering a bioavailable product

By Susan Colebank

Imagine relaxing on a nice Sunday afternoon watching your favorite football team square off against its latest opponents. The team is headed by one of the best quarterbacks in the NFL. Theyre on the 5-yard line, with only 15 feet separating them from the winning touchdown. The quarterback gets snapped the ball and ... his teammates step back and allow the other team to sack him. The time, money and care that went into coaxing the best performance out of that quarterback was thrown out the window since the guys who were supposed to defend him didnt do their jobs when he most needed it.

The same could be said about supplements. As is the case when faced with achieving a pivotal touchdown, if a supplement backed by time, money and care is not able to deliver its formula at the right moment, the supplement cant do its proper job. No matter how much science backs up the ingredients in a capsule, tablet or powder, if those nutrients arent absorbed at the right place in the body, a person may not experience the same beneficial effects as they would have from a properly delivered supplement. This is why the importance of a delivery system should not be taken lightly nor should the idea of bioavailability.

According to Redmond, Wash.-based SCOLR Inc., oral dosage forms represent the vast majority of the drug-delivery market in the United States and Europe because of the safety, efficacy, economic and consumer compliance advantages they possess over alternative routes of delivery. Beyond just capsules, tablets and powers, the delivery system market is filled with sophisticated oral options that offer a manufacturers product more efficacy and, truth be told, a better chance of differentiation from a competitors product.

According to Clearfield, Utah-based Albion Advanced Nutrition, bioavailability is important because all nutritional intake must be available to various body systems for growth, maintenance of body tissues, reproduction and other performance factors. No matter how high the nutrient levels or how well formulated the product, if [a nutrient] is not available, then money and effort have been wasted, the company reported.

One such delivery system that helps with bioavailability is chelation. A mineral that is chelated may be more bioavailable than one that is not chelated, said DeWayne Ashmead, Ph.D., Albions president. In order to have a true chelate, you have to have the mineral and other atoms forming a ring. The chelating agent, such as ligands that include ascorbic or citric acid, bonds to the mineral at two points like a claw hanging onto a marble.

However, Ashmead said that many companies will say they have a chelate, but theyll only have taken protein powder, mixed it with mineral salts, and call it a chelate. They may have a complex, but a chelate has to have that ring structure, Ashmead said. Thats one criterion. Two other criteria: the number of atoms in the ring, no more and no less than fiveif so, the chelate is too unstable and will break apart, which is of no value. The second is the molecular weightanything over 1,500 daltons cannot be absorbed intact. A true amino acid chelate will have a molecular weight of less than 800 daltons.

There are many types of chelates, Ashmead said, that are really not bioavailable, so to lump everything in and say Because its chelated its automatically absorbed is a fallacy.

How does a chelated ingredient work? The body believes an amino acid chelate is a small protein molecule, and so treats it as such. The mineral is therefore protected from going through a chemical reaction in the stomach and reaches the small intestine intact, where it is then absorbed by the body through active transport. Once in the tissue, some metabolism will take place and the mineral will be removed from the chelating agent and bond to other transport molecules to move throughout the body.

How does a chelated mineral stack up against an unchelated one? In an instance such as iron sulfate, which is electronically active, it goes around looking for things to join. One possibility is it could meet up with an amino acid from digested meatforming a chelation, which is the best case scenario. Or, it can join to phytic acid from vegetables and wheat, where it then becomes unabsorbable and is eliminated.

For manufacturers looking to put together a multivitamin/mineral formula, chelation may offer more than just more bioavailable minerals. When you use amino acid chelates, they do not cause deterioration of vitamins, but when you use nonchelated minerals, the vitamins begin to deteriorate immediately, Ashmead noted. If that vitamin/mineral product sits on a shelf for any period of timetwo, three monthsyoure going to have a significant loss in the amount of vitamin activity in that product because the nonchelated minerals are causing oxidation.

He added that a manufacturer would have to compensate for the erosion caused by nonchelated minerals by adding more vitamins to the formula to meet the label amounts. However, the mineral density is not as high in an amino acid chelate (20 percent) as in a nonchelated mineral (35 percent), and so a manufacturer needs to account for that in its formula.

Another delivery technology that can be applied to increase bioavailability is controlled delivery technology (CDT), offered by SCOLR. CDT technology is a suite of three patents specific to capsules and tablets; the most dominant form chosen is tablet because of lower costs in manufacturing and greater flexibility in size. SCLOR chooses the most appropriate patent for a manufacturers needs.

Any compound that can be consumed orally and would benefit the body from staying around longer makes sense for a drug delivery technology, according to Stephen Turner, SCOLRs director of product development. One example is vitamin C, according to Turner. This vitamin offers a gamut of benefits, but it is watersoluble and doesnt naturally stick in the body for a long time. As its absorbed, it is virtually metabolized and excreted at the same rate. If you can prolong the time for which it is available, you can get improved performance out of it, he said.

Putting more of an ingredient into a tablet or capsule without delayed delivery technology will not effectively deliver the dose, either. According to Turner, the larger the dose, the less is actually absorbed.

Delivery systems are more than just delaying or prolonging the time in which a tablet is dissolved. Delivery systems have the ability to enhance the solubility of a poorly soluble compound and to improve the effectiveness of a product by keeping it in the body longer. Theres more to delivery systems than just coating a tablet, which is really popular, Turner said.

In fact, one of the more common oral delivery systems being used is a simple matrix that incorporates hydrophilic polymers which swell in water and uses waxes to control the release of active components in a tablet or capsule, creating a Swiss cheese effect that allows active ingredients to seep from the pill into the body.

While this is a relatively simple system utilized by many in the supplement industry, delayed delivery systems are not as frequently seen here as in the drug industrywhere cost is less of an issue for manufacturers. For example, one popular option currently being used in the drug market is a tablet that has osmotic layers within a semi-permeable membrane that is bored with a lasera mechanical delivery system in pill form that will squirt the active ingredient out of the pill. Youre talking about $5 to $10 per pill just in technology alone, Turner said. What we have to offer [CDT] is the cost of a simple wax matrix but the ability of the reservoir-style devices.

The case for looking into a delivery system that extends beyond deciding between a tablet or capsule should be at the forefront of a supplement manufacturers mind. Especially since the industry is a commodity market where no one has rights to the ingredients. Since you dont have a way to control the flow of the active ingredients, you have to be extremely sensitive about the way you put products together, because just by putting them into a pill doesnt protect you from someone else making the same product, Turner said.

While tablets and capsules are one way to target delivery of nutrients, there is also effervescent technologywhich may offer nutrients at a higher rate of speed. Typically, you get much faster rates of absorption at much higher levels into the blood stream in about half the time that you would with tablets or capsules, said Fred Wehling, president of Amerilab Technologies in New Hope, Minn. Although not many studies have been done on effervescent nutritional products, Wehling said clinical studies indicate effervescent technology works to deliver analgesics and decongestants in half the time of a tablet.

The science indicates when stomach acid levels arent adequate, a good portion of a tablet can go through the system before a nutrient like calcium is broken down and absorbed into the system. In those cases, an effervescent product is the only way to make sure that 1,000 mg of calcium is available for the body to absorb, Wehling said.

Anything that can be finely distributed or dissolved in water can be made into an effervescent, which can come in the form of a tablet or powder. One nutritional system that wouldnt work as an effervescent are the green foods, which are sold mainly in powder form for people to mix into a gooey slurry to drink, Wehling reported. Ingredients that do fairly well include high-dose amino acids. Anytime theres a high dose of material that you want to get into water but want to be transportable, effervescence is the perfect way to go, he said. The market in the last three years [for effervescents] has evolved faster than the last 20 years. I think the nutritional industry is growing up a little bit and consumers are more informed today. Companies are now looking at ways to diversify product lines. Traditionally you have capsules, tablets, softgels and liquids, and theres really nothing else. Well, effervescent technology allows somebody to have a differentiation nobody else has.

Typically, an effervescent product is more expensive. But if people really sat down and did the math, Wehling said they would find that taking the equivalent of a calcium tablet, a glucosamine tablet and a multivitamin tablet in one effervescent dosage would cost the same or less than taking all of those pills together.

Making an efficacious supplement goes beyond using high-quality ingredients supported with sound science. Delivery systems that effectively target a product so that it gets absorbed when it needs to be and at the amounts it was formulated to release is more complicated than deciding between a tablet and a capsule. Make sure to have technology in place that protects the product you worked so hard to formulate and market. Otherwise, the quarterbackyour productmay be sacked before it can do its job.


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