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Effervescent Delivery Form

Based upon the success with the effervescent calcium product which provides a completely solubilized form of ionized calcium, this technology has been extended into other nutrients for the promotion of bioavailability. Comparative absorption of an effervescent, multi-vitamin, mineral replacement prototype product - KidsC 100 by Performing Science - to normal tablet delivery forms has recently been accomplished.

In one such bioavailability study, equal potencies of vitamin B2, vitamin B6, and zinc were taken as the effervescent product (KidsC 100) versus two of the most common name brand tablet forms of multi-vitamin products. Results of comparative absorption for each of these nutrients can be seen in Figures 1, 2 and 3. This study employed six normal, healthy male subjects who were not taking any previous nutritional supplements and were fasted overnight and then administered either the effervescent tablet or one of the two tablet delivery forms in a random fashion. Serum levels of the vitamin were then evaluated at one to four and eight hours after supplementation, and urinary 24-hour samples were taken. Urinary output indicated that the effervescent delivery form resulted in a 94 percent absorption as compared to 73 and 78 percent for equal potencies of the normal tablet delivery form. (See Figure 4.)

Overall bioavailability is measured by excretion of riboflavin at 24 hours, according to the method of Drs. Morrison and Chapman.19 Comparative urinary excretion data indicates that the effervescent multi-vitamin preparation was 16 percent better absorbed than tablet A and 21 percent better absorbed than tablet B. This would support previous work that indicates that those vitamin products which dissolve more rapidly in conditions which mimic gut contents have higher bioavailability.20



Additional benefits realized with the effervescent nutrient delivery form included better acceptance of the supplement by the subjects. These preparations were very easy on the stomach and easily consumed, as well as very bioavailable. It can be seen from Figures 1, 2 and 3 that the absorption of riboflavin, pyridoxine, and zinc was more rapid with the effervescent delivery form than the normal tablet delivery forms. Enhanced rates of absorption from 15-42 percent were observed among the different nutrients in different subjects. Work by Drs. Xi in China and Stozek in Poland has indicated that more rapid dissolution of the B vitamin nutrients promotes increased absorption in human subjects.21, 22 This is certainly confirmed in the comparative studies of the effervescent delivery form to normal tablet forms in human subjects.


Extension of the Effervescent Delivery Technology

This technology has been applied to two basic nutrient formulations which include a multi-vitamin mineral and electrolyte replacement preparation-KidsC 100; and a soluble, well tolerated vitamin C product-ConvenienC 2000. It is interesting that ConvenienC 2000 contains 2,000mg of vitamin C and is tolerated very well by individuals who have had problems with other vitamin C preparations. This is undoubtedly due to the fact that by being completely dissolved prior to supplementation, it reduces hyperosmolarity in the stomach and intestines that is found with normal tablet delivery forms. This reduces inflammation or diarrhea complications that are commonly seen with high dose tablet forms of vitamin C.

By delivering the nutrients in solution, the effervescent preparations afford immediate opportunity for these nutrients to be absorbed, starting in the mouth and moving through the stomach into the duodenum, which is entirely different from the absorptive ability of normal tablet delivery forms. These effervescent products are also buffered against pH change so that they do not create regions of high acidity or alkalinity in the intestinal tract as do many other nutrient delivery forms. This, then, improves tolerance and reduces nausea after supplementation.


Conclusion Concerning Nutrient Bioavailability

Based upon the physiology of nutrient digestion and absorption, it can be concluded that there are specific regions within the intestinal tract where various nutrients are optimally absorbed. The delivery of the nutrient in a bioavailable state at the region for absorption results in enhanced efficiency of transport and increased overall nutrient efficacy.

There are many new delivery forms that are being explored to promote improved nutrient absorption, with one of the most exciting being the effervescent delivery form which provides the nutrients in a buffered, solubilized state for rapid, immediate absorption. These forms are readily tolerated and well received by individuals who have had problems with tablet delivery forms. The effervescent calcium product is extremely useful for providing an ionized source of bioavailable calcium in a single drink, which should help promote compliance for individuals involved in calcium supplemental regimes.

Taken as a whole, it can be seen that significant progress is now being made in promoting better absorption of both the water- and fat-soluble vitamins and the trace elements in those individuals who have impaired nutrient absorption. Advances like the effervescent delivery system are very helpful for augmenting the absorption of all three of these families of nutrients and overcoming problems that may be associated with low stomach acid output, pancreatic insufficiency, or bile acid secretory difficulties.


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R E F E R E N C E S

1F. Moog, "The Lining of the Small Intestine," Scientific American, October, 1981, pp. 154-176.

2R. Recker, "Calcium Absorption and Achlorhydria," New England Journal of Medicine, 313, July, 1985, p. 70.

3H.M. Middleton, "Uptake of Pyridoxine by In Vivo Perfused Segments of Rat Small Intestine: A Possible Role for Intracellular Vitamin Metabolism," J. Nutrition, 115, p. 1079 (1985).

4K.J. Breen, B. Wood, et al., "Jejunal Uptake of Thiamine Hydrochloride in Man: Influence of Alcoholism and Alcohol," Amer J. Clin. Nutr., 42, p. 121 (1985).

5N. Stevenson, "Active Transport of L-Ascotic Acid in the Human Ileum," Gastroenterology, 67, p. 952 (1974).

6S. Yung, M. Mayersohn, and J.B. Robinson, "Ascotic Acid Absorption in Humans: A Comparison Among Several Dosage Forms," J. Pharm. Sciences, 71, p. 242 (1982).

7N.E. Bateman and D.A. Uccellini, "Effect of Formulation on the Bioavailability of Riboflavin," J. Pharm. Pharmacol., 36, p. 461 (1984).

8H.E. Gallo-Torres, "Obligatory Role of Bile for the Intestinal Absorption of Vitamin E," Lipids, 5, p. 379 (1970).

9M.T. MacMahon, "Comparison of the Absorption of a Polar Lipid, Oleic Acid, With a Non-Polar Lipid, Alpha-Tocopherol, Mixed Micellular Solution," European J. Clinical Investigation, 1, p. 161 (1970).

10J. B. Bieri, "Kinetics of Tissue Alpha-Tocopherol Depletion and Repletion," Ann. N. Y Academy Sciences, 203, p. 18 (1972).

11J. Bland and E. Prestbo, "Vitamin E-Comparative Absorption Studies," Intl. Clin. Nutr. Reviews, 4, p. 82 (1984).

12B.G. Shah, "Chelating Agents and Bioavailability of Minerals," Nutrition Research, 1, p. 617 (1981).

13"Picolinic Acid in the Treatment of Disorders Requiring Zinc Supplementation," Nutrition Reviews, 38, p. 148 (1980).

14G. Starich, "Dietary Chromium-Forms and Availabilities," Science of Total Environ., 28, p. 443 (1983).

15L.H. Allen, "Calcium Bioavailability and Absorption: A Review,' Amer J Clinical Nutrition, 35, p. 783 (1982).

16A.W. Mahoney and D.G. Hendricks, "Effects of Calcium Solubility on Absorption by Rats with Induced Achlorhydria," Nutr. Metabolism, 18, p. 310 (1975).

17O. Epstein and S. Sherlock, "Vitamin D, Hydroxyapatite, and Calcium Gluconate in Treatment of Cortical Bone Thinning in Postmenopausal Women," Amer. J. Clin. Nutrition, 36, p. 426 (1982).

18J.S. Fordtran and T.W. Locklear, "Ionic Constituents and Osmolarity of Gastric and Small-intestinal Fluids After Eating," Am. J. Digestive Diseases, 11, p. 503 (1966).

19A.B. Morrison and D.G. Chapman, "Further Studies on the Relation Between In Vitro Disintegration Times of Tablets and the Urinary Excretion Rates of Riboflavin," J. Amer Pharm. Assoc., 68, p. 634 (1959).

20D.G. Chapman and J.A. Campbell, "The Relation Between In Vitro Disintegration Time of Sugar-Coated Tablets and Physiological Training," J. Amer. Pharm. Assoc, 60, p. 374 (1956).

21N. Xi, J. Lu, and G. Chen, "Bioavailability and Pharmacokinetic Analysis of Riboflavin Preparations," Shanghai Diyi Yixueyuan Xuebao, 10, p. 193 (1983).

22T. Stozek and J. Wielgus, "Comparative Study on the Release of Riboflavin From Tablets in Vitro and its Bioavailability," Farm. Pol., 38, p. 465 (1982).




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