Joerg Gruenwald & Cordula Mueller01.01.06
New Supplement Opportunities in Europe
A new generation of dietary supplements in Europe is possible through the physiologically scheduled release of compounds.
By Joerg Gruenwald & Cordula Mueller
The human diet is composed of many nutrients and substances. It is well known that minerals and trace elements, in physiological concentrations, can interact during digestion. The result is usually impaired bioavailability. This can be circumvented through galenically controlled, time-release formulations, which take these interactions into account and optimize bioavailability.
Absorption of Essential Nutrients
The absorption of essential nutrients occurs primarily in the small intestine. The entire small intestine is capable of this, but most of the absorption occurs in the upper sections. There are various mechanisms for the uptake of nutrients from the intestine into the blood. During simple passive diffusion, the uptake of nutrients follows a concentration gradient. This is mainly the case for higher dosages. In general, absorption occurs mainly against a concentration gradient with the aid of an “active transporter.”
Due to the limited number of transporters, sometimes even a lesser concentration can lead to overloading this transporter system. This is particularly true when two similar substances compete for the same transporter. Many essential nutrients are then absorbed by passive diffusion. However, this is less effective. This leads to limited bioavailability, particularly when competition occurs during passive diffusion.
Interaction of Vitamins & Minerals
Mutual interactions are not known for vitamins. Vitamins can, however, influence the absorption of trace elements (For example: positive—iron und vitamin C; negative—vitamin C and selenium). It is also well known that fat-soluble vitamins (A, D, E, K) are only efficiently absorbed in the presence of fat and bile acids. The presence of bioflavonoids improves the bioavailability of vitamins C and E by protecting them from oxidation. Additionally, both are antioxidants and act synergistically to protect the body from free radicals.
In contrast, the bioavailability of most trace elements and minerals varies considerably and depends upon many factors, such as the amount taken up, the type and solubility of the chemical form used, the composition of the diet, duration of intestinal passage, interactions with other elements and the status of nutrient supply in the body. In particular, plant components (lignin, oxalic acid, phytate, phosphate), which occur for example in grains and legumes, can build complexes with minerals and trace elements that are difficult to dissolve and thereby inhibit absorption. Polyphenols, such as tannins found in coffee, black tea or red wine, can similarly impair absorption. Iron, zinc, copper, chromium, calcium and magnesium are particularly affected. Overall there are numerous, mostly negative, interactions between the individual minerals and trace elements known. For example, the absorption of zinc and manganese is impaired in the presence of iron.
Vitamin and mineral preparations should always be taken together with a meal. This is because a mixed meal will contain nutritional components that can significantly improve the absorption of micronutrients. Proteins and amino acids can build easily absorbable complexes with several minerals and protect against the undesirable bonding with phytate. In particular, it is known that the bio-availability of zinc and copper can be clearly improved by the presence of amino acids, such as histidine and cysteine. Iron profits from sulfur containing amino acids and other reducing nutritional components (e.g., vitamin C). Further, calcium uptake is improved by the simultaneous intake of vitamin D, lactose from milk products, fructo-oligosaccharide and the amino acids lysine and arginine.
Optimized Bioavailability of Essential Nutrients Through Controlled Release
The described absorption processes and interactions make it clear that selective timed release of essential nutrients in the gastrointestinal tract leads to a significant increase in their bioavailability.
The newly developed and patented “Chrono-Depot“ technology (chronos, latin = time) uses this knowledge to incorporate essential nutrients, which could otherwise be inhibited, into various matrixes. These are multi-layered tablets, where the layers are completely separated from one another, allowing for the phase-controlled release of complex combinations of essential nutrients in a single tablet. In addition, it is possible to connect an “immediate release phase” with a “depot-phase.” Essential nutrients that should flood the body as quickly as possible (i.e., magnesium for rapid increase in muscle endurance) are incorporated in the “immediate release phase.” Those for which a delayed release is advantageous (e.g., vitamin C) would be in the “depot phase.”
For very complex combinations of multiple essential nutrient preparations, it can also be advantageous to have the various essential nutrients in three separate matrixes with different release times. As opposed to the conventional multiple-essential nutrient combinations, the individual nutrients are not just thrown together in a single phase, but the negative and positive interactions would be taken into account. Such a “smart tablet” could for example incorporate the fat-soluble vitamins in the first immediate release phase, so that they can interact unhindered with fat molecules. Vitamin C would be released over a longer period in phase 2. And its presence can simultaneously improve the absorption of iron. Selenium is incorporated into phase 3, thereby preventing its undesirable oxidation by vitamin C. Chromium is separated from the interfering influence of zinc and iron, as well as iron from that of calcium, copper and zinc. Possible interactions between calcium and magnesium would also be impeded. Because of the many, partially overlapping interactions, various combinations are possible.
Outlook
So how does improved bioavailability present new opportunities for supplements? First of all, improved bio-availability ensures that lower dos-ages are sufficient to meet the nutrient requirements of the body. This is of major importance with regards to the harmonization process in the European Union (EU). There are large differences regarding the legal maximum levels of vitamins and minerals in dietary supplements between the European countries (i.e., supplements from the Netherlands will usually contain high dosages that cannot be legally sold in Germany due to the country’s strict view of supplemental vitamins). Therefore better bioavailable formulations with lower dosages present the opportunity to offer these “smart” dietary supplements to all European consumers. This is also important in light of the trend toward additional intake of essential nutrients as part of a healthy lifestyle or as self-medication. Demographic developments, such as the aging of the large baby boomer population, and increased education attainment shows that this trend will continue. Thus, the development of new galenic forms with optimized bioavailability is of particular importance both for the individual consumer and the marketer of dietary supplements in Europe. This also represents a great opportunity for global companies looking to differentiate with science-based innovation.NW