Calcium taurate as a dietary supplement

Details Calcium taurate as a dietary supplement Calcium taurate as a dietary supplement

1999-12-10

2001-03-20

Harrison, Robert H. (Department: 1619)

Drug, bio-affecting and body treating compositions

Inorganic active ingredient containing

Aluminum, calcium or magnesium element, or compound containing

C514S711000, C562S104000

Reexamination Certificate

active

06203823

ABSTRACT:

FIELD OF THE INVENTION
The present invention relates to the use of calcium taurate as a nutritional supplement and antihypertensive agent.
BACKGROUND OF THE INVENTION
Calcium is vital to normal bone formation and maintenance of bone density. Long-term dietary calcium insufficiency almost always results in net loss of calcium from the bones. The U.S. recommended daily allowance (RDA) for calcium is 800 mg/day, with an additional 400 mg advisable for pregnant and lactating women. A large proportion of the over-60 population consumes less than one-half of the RDA for calcium. This is also the age group most at risk of developing osteoporosis, which is characterized by loss of the organic matrix as well as progressive demineralization of the bone. Some studies suggest that postmenopausal women may need up to 1,200 mg calcium/day just to maintain calcium balance (
Textbook of Biochemistry With Clinical Correlations
, Second Edition, T. Devlin, Ed., John Wiley & Sons, New York, 1986, pp. 983-984).
Calcium has also been demonstrated to have an antihypertensive effect (McCarron,
Am. J Clin. Nutr
. 65(suppl.):712S-716S, 1997). Calcium is also required for many enzymes, mediates some hormonal responses, and is essential for muscle contractility and normal neuromuscular irritability.
Taurine is an amino acid present in high concentrations in excitable and secretory tissue. Its role in cardiac finction has received particular attention (Huxtable,
Physiol. Rev
., 72:101-163, 1992; Schaffer et al.,
Taurine in Health and Disease
, pp. 171-180, 1994). Although taurine can be synthesized endogenously from the amino acid cysteine, in mammals it is derived principally from the diet and is thus considered a “conditionally essential” nutrient. Conventional diets supply 40-400 mg of taurine daily, while vegetarian diets are extremely low in this amino acid.
The main function of taurine in mammals appears to be the regulation of transmembrane ionic movements, especially the regulation of calcium distribution (Schaffer et al., supra.; Huxtable, supra.; Schaffer et al.,
Taurine: functional Neurochemistry, Physiology and Cardiology
, pp. 217-225, 1990). However, the mechanisms of this regulation are not well understood. Taurine has also been shown to have antihypertensive properties (Fujita et al.,
Circulation
75:525-532, 1987; Inoue et al.,
Cardiovascular Res
., 22:351-358, 1988 ). Taurine also exerts a platelet stabilizing effect both in vitro and, after oral administration, ex vivo (Hayes et al.,
Am. J. Clin. Nutr
., 49:1211-1216, 1989; Atahanov,
Arzneim
-
Forsch/Drug Res
., 42:1311-1313, 1992). Acute intravenous administration of taurine reduces the incidence of arrythmias in animals treated with arrhythmogenic agents and multi-gram doses have been shown to be effective in the treatment of ischemic congestive heart failure (Azurna et al.,
Curr Ther. Res
., 34:543-557, 1983). Thus, increased taurine intake appears to be beneficial to vascular health.
Many sources of calcium, including calcium carbonate and calcium citrate, have less than optimal bioavailability. In addition, these sources of calcium require require an acidic environment for calcium release. Ordinarily, this does not present a problem. However, in individuals with achlorohydria, a condition in which stomach acid cannot be produced, these sources of calcium have very poor bioavailability because calcium ions cannot be released from the compounds. The present invention provides a calcium taurate complex for use as a dietary calcium supplement and antihypertensive agent. This complex has excellent calcium bioavailability and does not require an acidic environment for calcium release.
SUMMARY OF THE INVENTION
One embodiment of the present invention is a method for supplementing dietary calcium in an individual, comprising orally administering calcium taurate to the individual. Preferably, the calcium tarot provides between about 600 mg and 1,200 mg calcium. More preferably, the calcium taurate provides about 800 mg calcium.
Another embodiment of the present invention is a method of treating hypertension in an individual in need thereof, comprising administering an effective daily antihypertensive amount of calcium taurate to the individual. Preferably, the daily antihypertensive amount of calcium taurate provides between about 600 mg and about 1,200 mg calcium. More preferably, the daily antihypertensive amount of calcium taurate provides about 800 mg calcium.
The present invention also provides a pharmaceutical composition for treatment of hypertension, comprising an effective therapeutic dose of calcium taurate in conjunction with an antihypertensive drug. Preferably, antihypertensive drug is a diuretic, &bgr; blocker, calcium antagonist or angiotensin converting enzyme inhibitor.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
The present invention provides a calcium taurate salt for the nutritional and therapeutic administration of calcium and taurine, both of which are have beneficial antihypertensive effects. The calcium taurate complex dissolves rapidly and completely at acid, neutral or slightly alkaline pH, indicating extremely good bioavailability. This complex is particularly useful for administration to individuals unable to produce stomach acid because the calcium can be released at neutral and slightly alkaline conditions.
The reaction of taurine with calcium oxide, calcium hydroxide or calcium salts, under appropriate conditions, yields calcium taurate having the formula (H
2
N—CH
2
—CH
2
—SO
3
)
2
Ca
2+
. This compound may be used both as a source of the essential nutrient calcium, and as a source of the conditionally essential amino acid taurine. The oral administration of these compounds delivers calcium and taurine to appropriate sites of action. Calcium taurate is also useful as a therapeutic agent for hypertension and can be used as an adjuvant to conventional anihypertensive drugs. There are four categories of antihypertensive drugs: diuretic agents (e.g., bendroflumethiazide, chlorothiazide, cyclothiazide), &bgr; blockers (e.g., atenolol, propanolol), calcium antagonists (e.g., verapamil, nifedipine) and angiotensin converting enzyme (ACE) inhibitors (e.g., captopril, enalapril). A more complete listing of antihypertensive drugs may be found in
The Merck
Manual, 16th edition, pp. 422-425, 1992). The calcium taurate of the invention is highly soluble in water and provides excellent nutritional availability of both calcium and taurine.
The synthesis of calcium taurate is described in Example 1. Calcium hydroxide and taurine are mixed and heated in an aqueous solution, preferably water. Most of the water is removed by evaporation, and then alcohol is added to precipitate the product and allow it to be separated by filtration. The elemental analysis is provided in Table 1 and confirms isolation of a compound having the formula (H
2
N—CH
2
—CH
2
—SO
3
)
2
Ca
2+
. In addition, the
1
H-NMR (500 MHz, D
2
O) spectrum of calcium taurate showed the equivalence of the two methylene groups which resulted in one signal (type A
4
) with the center at 3.029 ppm. The absence of other signals indicates that no degradation products were produced during the synthesis.
TABLE 1
Elemental analysis of calcium taurate
% C
% H
% N
% S
% Ca
Calculated
16.66
4.19
9.71
22.24
13.89
1st analysis
16.61
4.38
9.35
19.34*
13.35
2nd analysis**
16.90
4.34
9.68
22.16
*Elemental analysis performed by Desert Analytics showed consistently less sulfur content due to potential calibration error.
**Repeated analysis of the same product performed by NuMega Resonance Labs confirmed the correct sulfur content in the product
Since two taurine molecules combine with one calcium atom, it is preferred that the molar ratio of taurine to calcium be about 2:1, although ratios of between about 1.5:1 and about 2.5:1 are contemplated. The product is extremely water soluble.
For oral administration as a nutritional supplement or antihypertensive agent, calcium taurate may be provided as a tablet, aqueous or oil suspension, dispersible powder or

Affiliated with

Also associated with

Rating

Calcium taurate as a dietary supplement does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Calcium taurate as a dietary supplement, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Calcium taurate as a dietary supplement will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2494595