Protecting the Quarterback

Protecting the Quarterback
Delivery systems are a huge factor in delivering a bioavailableproduct

By Susan Colebank

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

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

According to Redmond, Wash.-based SCOLR Inc., oral dosageforms represent the vast majority of the drug-delivery market in the UnitedStates and Europe because of the safety, efficacy, economic and consumercompliance advantages they possess over alternative routes of delivery. Beyondjust capsules, tablets and powers, the delivery system market is filled withsophisticated oral options that offer a manufacturers product more efficacyand, truth be told, a better chance of differentiation from a competitorsproduct.

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

One such delivery system that helps with bioavailability ischelation. A mineral that is chelated may be more bioavailable than one thatis not chelated, said DeWayne Ashmead, Ph.D., Albions president. Inorder to have a true chelate, you have to have the mineral and other atomsforming a ring. The chelating agent, such as ligands that include ascorbic orcitric acid, bonds to the mineral at two points like a claw hanging onto amarble.

However, Ashmead said that many companies will say they have achelate, but theyll only have taken protein powder, mixed it with mineralsalts, and call it a chelate. They may have a complex, but a chelate has tohave that ring structure, Ashmead said. Thats one criterion. Twoother criteria: the number of atoms in the ring, no more and no less than fiveifso, the chelate is too unstable and will break apart, which is of no value. Thesecond is the molecular weightanything over 1,500 daltons cannot be absorbedintact. A true amino acid chelate will have a molecular weight of less than 800daltons.

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

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

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

For manufacturers looking to put together amultivitamin/mineral formula, chelation may offer more than just morebioavailable minerals. When you use amino acid chelates, they do not causedeterioration of vitamins, but when you use nonchelated minerals, the vitaminsbegin to deteriorate immediately, Ashmead noted. If that vitamin/mineralproduct sits on a shelf for any period of timetwo, three monthsyouregoing to have a significant loss in the amount of vitamin activity in thatproduct because the nonchelated minerals are causing oxidation.

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

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

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

Putting more of an ingredient into a tablet or capsule withoutdelayed 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 thetime in which a tablet is dissolved. Delivery systems have the ability toenhance the solubility of a poorly soluble compound and to improve theeffectiveness of a product by keeping it in the body longer. Theres moreto delivery systems than just coating a tablet, which is really popular,Turner said.

In fact, one of the more common oral delivery systems beingused is a simple matrix that incorporates hydrophilic polymers which swell inwater and uses waxes to control the release of active components in a tablet orcapsule, creating a Swiss cheese effect that allows active ingredients to seepfrom the pill into the body.

While this is a relatively simple system utilized by many inthe supplement industry, delayed delivery systems are not as frequently seenhere 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 atablet that has osmotic layers within a semi-permeable membrane that is bored with a laseramechanical delivery system in pill form that will squirt the activeingredient out of the pill. Youre talking about $5 to $10 per pill just intechnology alone, Turner said. What we have to offer [CDT] is the cost ofa simple wax matrix but the ability of the reservoir-style devices.

The case for looking into a delivery system that extendsbeyond deciding between a tablet or capsule should be at the forefront of asupplement manufacturers mind. Especially since the industry is a commoditymarket where no one has rights to the ingredients. Since you donthave a way to control the flow of the active ingredients, you have to beextremely sensitive about the way you put products together, because just byputting them into a pill doesnt protect you from someone else making the sameproduct, Turner said.

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

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

Anything that can be finely distributed or dissolved in watercan be made into an effervescent, which can come in the form of a tablet orpowder. One nutritional system that wouldnt work as an effervescent are thegreen foods, which are sold mainly in powder form for people to mix into agooey slurry to drink, Wehling reported. Ingredients that do fairly wellinclude high-dose amino acids. Anytime theres a high dose of material thatyou want to get into water but want to be transportable, effervescence is theperfect way to go, he said. The market in the last three years [for effervescents] hasevolved faster than the last 20 years. I think the nutritional industry isgrowing up a little bit and consumers are more informed today. Companies are nowlooking 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 elsehas.

Typically, an effervescent product is more expensive. But ifpeople really sat down and did the math, Wehling said they would find thattaking the equivalent of a calcium tablet, a glucosamine tablet and amultivitamin tablet in one effervescent dosage would cost the same or less thantaking all of those pills together.

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