Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Reexamination Certificate
2002-04-22
2002-10-22
Henley, III, Raymond (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
C514S562000, C514S566000
Reexamination Certificate
active
06468965
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to chelators for metals and, more particularly, to a pharmaceutical composition for oral administration of a mixture of chelators to a subject.
BACKGROUND OF THE INVENTION
Chelating agents, or chelators, constitute a well known type of multifunctional organic compounds that are capable of forming complexes of multivalent metal ions such as, for example, calcium, magnesium zinc, iron, chromium, and lead. Chelators find use in a variety of commercial applications, for example, photographic processing solutions, to which they can be added to form soluble complexes with metal ions that would otherwise produce undesirable precipitates or sludges.
A well known and widely used chelator is ethylenediaminetetraacetic acid, (HO
2
CCH
2
)
2
NCH
2
CH
2
N(CH
2
CO
2
H)
2
, commonly referred to as EDTA, commercially available both as the free acid and as various salts, for example, disodium EDTA, tetrasodium EDTA, dipotassium EDTA, calcium disodium EDTA, etc. Other commercial chelators are the naturally occurring amino acid L-cysteine, HSCH
2
CH(NH
2
)CO
2
H, and its acetylated derivative N-acetyl-L-cysteine, HSCH
2
CH(NHCOCH
3
)CO
2
H, commonly referred to as NAC.
In addition to their industrial applications, chelators have also been extensively employed therapeutically in the treatment of human subjects. For example, injections of EDTA have been used to remove high levels of toxic lead from the bloodstream of individuals who have been exposed to lead paint. Intravenous injection of chelators has also been employed in the treatment of other medical conditions. For example, U.S. Pat. No. 5,114,974 to Rubin discloses the treatment of atherosciereosis with MgNa
2
EDTA.
Chelation therapy to remove potentially harmful metal ions from the body of an individual is today frequently proposed as a means for gaining and maintaining good health and avoiding surgery for heart disease. Although chelation therapy of human patients is most commonly carried out by intravenous injection, oral chelation therapy is also well known. For example, U.S. Pat. No. 5,080,906 to Carenzi et al. discloses a method and composition for oral administration of N-acetylcysteine (NAC).
Various formulations containing one or more chelators for oral administration are commercially available. Typically, these formulations contain a low dosage of chelators, along with a mixture of other purportedly beneficial ingredients. The list of ingredients for one such product, Life Glow Plus™ from Vibrant Life contains, per capsule, 25 mg disodium dihydrate EDTA, 15 mg L-cysteine, and 15 mg NAC, and specified amounts of 48 additional substances, including other amino acids, vitamins, minerals, herbs, glandular substances, and “special items.” The recommended daily dosage of Life Glow Plus™ is 20 capsules.
Another available oral chelation product is Kelation Plus® from Kelation Plus International, Jacksonville Fla., a powder packaged in individual daily servings and said to contain 26 pharmaceutical grade vitamins, minerals, amino acids, and glandulars. The list of 26 ingredients, all in unspecified amounts, for Kelation Plus® includes L-cysteine. A footnote to the ingredients list states: “EDTA used as a preservative.”
U.S. Pat. No. 6,114,387 to Cutler discloses a solid pharmaceutical composition for the oral administration of chelating agents to an individual that consists essentially of at least 100 milligrams of ethylenediaminetetraacetic acid (EDTA) or a molar equivalent amount of pharmaceutically acceptable salts or hydrated salts of EDTA, at least 75 milligrams of N-acetylcysteine (NAC), and an appropriate amount of at least one pharmaceutical formulating agent.
Lactoferrin is an 80 kDa mammalian iron-chelating glycoprotein that can be obtained on a commercial scale from the whey protein of cow's milk. The anti-viral, anti-microbial, anti-cancer, and immune modulating/enhancing effects of orally administered lactoferrin have been extensively reported. Because many pathogenic bacteria require a supply of free iron to grow, they can, in the presence of the strongly iron-chelating lactoferrin, be inhibited or killed. For example, as reported in Shi et al., “Human Lactoferrin Binds and Removes the Hemoglobin Receptor Protein of the Peridontopathogen
Porphyromonas gingivalis
”, J. Biol. Chem., 2000, Vol. 275, No. 39, pp. 30002-30008, lactoferrin exhibits an inhibiting action on growth of the bacteria responsible for gingivitis.
In regard to its anti-cancer effects, lactoferrin exhibits a capability for inhibiting angiogenesis, a well-establish prerequisite for tumor growth, as discussed in Norby et al., “Orally Administered Bovine Lactoferrin Systemically Inhibits VEGF
165
-Mediated Angiogenesis in the Rat”, Int. J. Cancer, 2001, Vol. 91, pp. 236-240. Also, as reported in Kuhara et al., “Orally Administered Lactoferrin Exerts an Antimetastatic Effect and Enhances Production of IL-18 in the Intestinal Epithelium”, Nutrition and Cancer, 2000, Vol. 38, No. 2, pp. 192-199, lactoferrin has been found to exert a significant inhibiting effect on the lung colonization of colon 26 carcinoma.
The anti-viral, anti-cancer, and anti-microbial effects of lactoferrin, as well as its antioxidant characteristics, are discussed in Brink, “Lactoferrin: The Bioactive Peptide that Fights Disease”, Life Extension magazine, October 2000, which also includes an extensive listing of recent publications regarding the beneficial effects of lactoferrin.
There remains a need for a convenient, orally administered pharmaceutical composition that contains an effective dosage of a combination of selected chelators, in particular, ethylenediaminetetraacetic acid, N-acetyl-L-cysteine, and lactoferrin, without included extraneous ingredients that may impair their effectiveness. This need is met by the present invention.
SUMMARY OF THE INVENTION
In accordance with the present invention, a solid pharmaceutical composition for the oral administration of chelating agents to an individual consists essentially of: at least 100 milligrams of ethylenediaminetetraacetic acid (EDTA) or a molar equivalent amount of pharmaceutically acceptable salts or hydrated salts of EDTA, at least 75 milligrams of N-acetyl-L-cysteine, at least 10 milligrams of lactoferrin, and an appropriate amount of at least one pharmaceutical formulating agent.
The pharmaceutical composition of the present invention provides a convenient alternative to intravenous injection of chelating agents, which is time-consuming and requires visitation to a medical facility.
REFERENCES:
patent: 6114387 (2000-09-01), Cutler
Will Brink, “Lactoferrin: The Bioactive Peptde that Fights Disease”,LE Magazine, pp. 1-10, (Oct. 2000).
Yixin, Shi, et al., “Human Lactoferrin Binds and Removes the Hemoglobin Receptor Protein of the Periodontopathogen Porphyromonas Gingivalis”,The Journal of Biological Chemistry, vol. 275, pp. 30002-30008, (Sep. 29, 2000).
Klas Norby, et al., “Orally Administered Bovine Lactoferrin Systemically Inhibits VEGF—Mediated Angiogenesis in the Rat”, Publication of the International Union Against Cancer,Wiley-Liss, Inc., vol. 91, pp. 236-240, (2001).
Tetsuya Kuhara, et al., “Orally Administered Lactoferrin Exerts an Antimetastatic Effect and Enhances Production of IL-18 in the Intestinal Epithelium”, Nutrition and Cancer,Lawrence Erlbaum Associates Inc., vol. 38(2), pp. 192-199, (2000).
Henley III Raymond
Jaeckle Fleischmann & Mugel LLP
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