Dietary Supplement Tablets and Capsules: Helping the Nutrients Go Down

June 3, 2013
Alan Richman

A spoonful of sugar is no match for today’s sophisticated dietary supplement delivery formats.

In nutrient delivery, as in the fable of the tortoise and the hare, “slow and steady wins the race.” The goal of today’s leading vitamin, mineral, and supplement delivery systems is not merely to get past the gateway of the mouth, but to make sure they have maximum effect once ingested. Makers of tablets, capsules, softgels, and more esoteric formats are always on the lookout for formulations and physical characteristics that will provide optimum absorption and bioavailability.

Except in rare instances where a burst may be best-think effervescents-ingredient suppliers tend to favor sustained-release products or products that protect contents from destructive digestive acids. They don’t want to just dump full doses into the stomach where powerful acids may destroy potency. Ideally, they strive for components that will reach the intestines, or even the cellular level, before giving up their goodies.

 

Acid Resistance

In July, capsules supplier CapsCanada (Tecumseh, ON, Canada) will introduce AR Caps, a line of acid-resistant capsules. “These are enteric capsules that resist stomach digestion and disintegrate in the duodenum or small intestine,” says executive vice president Gabriel Eilemberg. “The new capsules eliminate the need for the coating process after capsules are filled.”

According to Eilemberg, AR Caps are especially ideal for probiotics and enzymes because they protect these nutritional ingredients from the acidic environment of the stomach. He predicts that growing interest in gut health will enable AR Caps to capture a sizable share of the estimated 400 billion empty capsules sold each year.

Protecting capsule contents from stomach acid is also the target of Capsugel’s (Greenwood, SC) DRcaps line. Marketing manager Missy Lowery says DRcaps’ slow disintegration enables most of the capsule’s contents to release in the small intestine, not the stomach. Capsugel’s DRcaps also benefit products such as probiotics and enzymes that might be susceptible to stomach acid. While DRcaps are not an enteric capsule, the capsules protect contents for at least 30 minutes in the stomach’s pH of 1.2, fully opening at an intestinal pH of 6.8.

Capsugel also supplies Licaps capsules, which offers two approaches specifically intended to benefit ingredient combinations or highly targeted delivery times. The first option features beads in a liquid-filled capsule; the second is a capsule within a capsule. The liquid dose in the liquid-filled capsule is designed to offer quick release of an ingredient, while the beads provide for a controlled or delayed time release. The company recommends the capsule-within-a-capsule version for products containing incompatible ingredients or ingredients that would separate if mixed together. “It’s different from beads-in-a-capsule in that all the ingredients are in liquid form,” says Lowery. She identifies products combining a probiotic and a prebiotic as ideal for this technology.

The probiotic connection also has caught the fancy of Robinson Pharma Inc. (Santa Ana, CA). In March, the company introduced its new Unique IS-2 probiotic softgel, which was developed in collaboration with B&D Nutritional Ingredients Inc. (Vista, CA), Unique Biotech USA (Davie, FL), and Unique Biotech Ltd. India (Hyderabad, India).

The new capsule is based on the Unique IS-2 Bacillus coagulans strain, a trademarked bacterium that has demonstrated high resistance to extreme temperature and humidity, the companies say. In addition to temperature stability, the strain is also resistant to gastric acids and can survive transit through the gastrointestinal tract.

In a press release, Fred Jamee, Robinson Pharma’s senior vice president and chief quality officer, described how the creation of a stable, active probiotic softgel was both multifaceted and rigorous. “First, one must identify a strain type that has the potential to survive the manufacturing process. More challenging is testing for the presence and viability of the probiotic after encapsulation. Recovery of the active probiotic from the lipid matrix of a softgel is not easy. Finally, and more rigorous still, is creating a product that can withstand the challenges of time, in this case passing an accelerated stability study.”

 

Other Types of Protection

Supplement delivery systems also protect ingredients in other ways. On its website, supplier Ingredion (Westchester, IL), which incorporates both Corn Products and National Starch, lauds modern encapsulation technology for providing the following benefits: protection against oxygen, oxidizing agents, other ingredients, enzymes, temperatures, and light.

The company’s newest offering is Q-Naturale SF, an emulsifier derived from the quillaja tree, which grows abundantly in Chile and is free from the price and supply chain pressures of gum arabic. According to Ingredion, the new ingredient enables improved oxidation protection.

Like capsule-in-a-capsule and other types of capsule technologies that can guard against premature ingredient interaction, tablets, too, can help keep ingredients separate.

Not long ago, Sabinsa Corp., (East Windsor, NJ) introduced a line of bi-layered tablets designed to deliver stable dosage forms of actives that may not otherwise be compatible. These Integrated Nutritional Composites (INCs, for short) are multirelease products that were initially offered in five off-the-shelf varieties: Blood Sugar Support INC Actives, containing the company’s Silbinol (pterostilbene 5%, 30%, or 90%), cinnamon extract, zinc monomethionine, and BioPerine, a proprietary black pepper extract; Weight Management INC Actives, containing ForsLean (Coleus forskohlii), GarCitrin (Garcinia cambogia), and BioPerine; Heart Health INC Actives, containing policosanol and niacin; Heart Health+ INC Actives with L-carnitine, beetroot extract, policosanol, and niacin; and NiLitis SR INC Actives, containing Boswellin (Boswellia serrata), Curcumin C3 Complex (curcuminoids 95%), and ginger extract.

Existing formulas notwithstanding, the company believes that the true potential for INC technology lies in its ability to allow customers to work with Sabinsa scientists to tweak existing offerings and/or come up with brand new formulas. By targeting specific market needs, finished-product manufacturers can differentiate their products from the competition. 

 

Also: Read about how coloring capsules can make a difference.

 

Sidebar: Improving Absorption

Several companies specialize in ingredients to improve nutrient absorption or bioavailability.

Sabinsa Corp.’s (East Windsor, NJ) patented BioPerine ingredient is sourced from piperine found in black pepper and long pepper plants. What makes the ingredient special, says Sabinsa, is its ability to increase the bioavailability of nutritional compounds, an effect that has been substantiated in clinical studies.

AstraGin, offered by NuLiv Science USA Inc. (Walnut, CA), also claims to improve absorption of amino acids, minerals, and vitamins. The company describes AstraGin as an all-natural plant-derived compound extracted from highly fractionated Panax notoginseng and Astragalus membranaceus using a proprietary pharmaceutical extraction and processing technology. NuLiv’s Richard Wang, M.P.H., says AstraGin has been included in multiple preworkout and recovery formulations, with preclinicals demonstrating that the substance supports absorption of arginine, citrulline, folate, glucosamine, and more.

Wang explains, “AstraGin has a positive influence on the transporter molecules in the small intestines. By activating more of these molecules, it allows more nutrients to pass through the intestinal lumen and directly into the bloodstream for utilization.”

Jesse Lopez, president and CEO of SourceOne Global Partners (Chicago), says his company’s VESIsorb delivery system mimics the human fat digestion and absorption process. It’s common knowledge that fat-soluble vitamins are better absorbed when administered after a meal containing fat. Lopez says SourceOne’s VESIsorb is a lipid-based formulation that naturally self-assembles on contact with an aqueous phase into a colloidal system, helping to improve oral drug or natural bioactive bioavailability.

According to Lopez, use of VESIsorb has enabled SourceOne to broaden the food product, drink mix, beverage, and personal care product applications of certain bioactive ingredients.

Noting that SourceOne has already employed VESIsorb in enhancing its CoQSource and OmegaChoice products, with more to follow soon, Lopez says, “We have succeeded in this area by addressing issues such as water solubility, oxidative stability, shelf life, and uniformity of dispersion in the delivery medium.”