Title: Formulations and methods for treating chronic
United States Patent: 6,517,832
Issued: February 11, 2003
Inventors: Marrongelle; Jeffrey L. (1629 Long Run Rd.,
Orwigsburg, PA 17972); Staverosky; Thomas J. (1537 Mineral Springs Rd.,
Reading, PA 19602)
Appl. No.: 935945
Filed: August 24, 2001
A prophylactic treatment for the human malady clinically described as
migraine headache comprising daily administration in unit dosage form of a
first formulation which comprises a major amount of bioactive peptides and a
minor amount of probiotics. Concurrently, daily administration in dosage
form of a second formulation of a major amount of active components like
malic acid, sylibum marianum, acetyl-L-cysteine, copper chelate, zinc
gluconate, aspartate and bromelain. A minor amount of plant derivatives
excipients comprise the balance of the second formulation. Preferably, these
plant derivatives include beet root, powder, watercress, celery, dandelion,
capsicum and artichoke extract.
DETAILED DESCRIPTION OF A PREFERRED EMBODIMENT
Accordingly, the inventive methods provides for concurrent administration
of two discrete formulations of known beneficial substances, the first
formulation is a blend of select ingredients and is thought to improve
digestion in most patients.
Formulation I is a unique blend of two ingredients in a gelatin capsule,
which blend primarily serves to focus on returning the digestive system to
normal function. The first composition of Formulation I is a fish protein
concentrate of bioactive peptide. The second composition of the group are
probiotics, which are known to be beneficial bacteria, that normally inhabit
a mammalian digestive (intestinal) tract, such as the acidophilus
microorganism found in yogurt. It is an important agent, shown to be
effective in absorbing toxins from both the small intestine and the bowel.
This two part formulation is assembled in the weight ratios set out in
Working Example I, as in Foundation Formula of The Forever Well entity,
The second formulation (II) is a combination of as many as 21 substances,
all known to be both benign and beneficial, included selected vitamins,
trace minerals, herbs, micronutrients, and macronutrients (Renew Formula.RTM.,
of the Foreverwell entity). They are assembled in the weight ratios set out
in Working Example II. They are well adapted to using standard gelatin
capsules as the unit dosage form.
Of the vitamins, included are vitamin B complex species, like B1, B6, and
inositol (cis-1,2,3,5-trans, 4, 6, cyclohexanehexol). The trace minerals
include magnesium as the aspartate, copper as a chelate, manganese as
glycerolphosphate, and zinc as the gluconate. Herbs include silybum marianum
(milk thistle), beet root powder, watercress, celery, dandelion, parsley,
and capsicum. Micro-nutrients are malic acid, proanthocyanidins, N-Acetyl-L-Cysteine,
and SOD (superoxide dismutase). The macro-nutrients include pyridoxal-5
phosphate, and Agaricus Blazei.
Pharmaceutically acceptable formulations for oral administration may take
the form of, for example, tablets or capsules prepared by conventional
means, with acceptable excipients, such as binding agents, for example,
maize starch, or hydroxymethyl cellulose; fillers, for example, lactose,
sucrose, mennitol, and maize starch; lubricants, for example, stearic acid,
polyethylene glycol, magnesium stearate, metallic or silica, disintegrants,
for example, potato starch, or wetting agents, e.g., sodium lauryl sulfate.
The tablets may be coated by methods well known in the arts.
Liquid preparations for oral administration may take the form of, for
example, aqueous or oily solutions, syrups, elixirs, emulsions or
suspensions, or they may be presented as a dry product for reconstitution
with water or other suitable vehicle before use. Such liquid preparations
may be prepared by conventional means, with pharmaceutically acceptable
additives, such as suspending agents, for example, sorbitol syrup,
glucose-sugar syrup, or gelatin; emulsifying agents such as lecithin,
acacia, or sorbitan mon-oleate; non-aqueous vehicles like oily esters, or
ethyl alcohol; and preservatives like methyl or propel p-hydroxy benzoates,
or sorbic acid. Such liquid preparations may also contain conventional
buffers, flavoring, coloring, and sweetening agents, as appropriate. The
prophylactic effects for relief of migraine are effected by taking three
capsules (500 mg each) of Formulation I, along with two capsules of
Formulation II (400 mg each) before each of the two largest meals of the
day, on a daily basis, longer term for an adult in the weight range of
125-200 lb. To limit initial digestive disturbances, take a reduced regimen
for the first week. For the initial regime, the reduced dosage of the two
capsules is 1400 mg daily.
A proposed dose of the compounds of the invention for oral administration to
a human (about 160 lb.) body weight, for the treatment of migraine, is
2300-4600 mg of capsule daily of the ingredients, which dose could be
administered up to eight times per day, but more usually one to four times a
day, in divided dosages, as noted. It should be understood that unless
otherwise indicated, the dosages are referred to in terms of the weight of
the active components of the two formulations.
WORKING EXAMPLE I - FOUNDATION FORMULA .RTM.
COMPOSITION AMOUNT PER CAPSULE
Bioactive peptides 375 mg
Probiotics 62.5 mg
Bioactive peptides which as are available in a particular predigested fish
protein concentrate are sold under the trade name Seacure and made available
by Proper Nutrition, Inc., Reading, Pa.
Probiotics such as are made available in various strains and custom blends
by Nebraska Cultures and other providers. These beneficial intestinal
bacteria assist in the digestion and absorption of food. the selected blend
used in Foreverwell Foundation formula includes the DDS-1 strain of
acidophilus, Lactobacilus bulgaricus, Bifido bacterium, and Enterococcus
The DDS-1 strain of the acidophilus is described in product sheets and is
available from Nebraska Cultures, Walnut Creek, Calif. L. bulgaricus is also
available from Nebraska Cultures, as is bifidobacterium bifidum and
enterococcus faecium. The last species is also sourced in U.S. Pat. No.
5,589,168, granted Dec. 31, 1996 to Allen et al, titled "PROBIOTIC.".
WORKING EXAMPLE II - RENEW FORMULA .RTM.
COMPOSITION AMOUNT PER CAPSULE
Malic Acid 70 mg
Silybum marianum 15 mg
N-Acetyl-L-cysteine1 40 mg
Copper chelate 1 mg
Zinc gluconate 5 mg
Magnesium aspartate 10 mg
Proanthocyanidins2 10 mg
Manganese glycerolphosphate 1 mg
B1 thiamine mononitrate 5 mg
B2 -Riboflavin 5 mg
Inositol (hexahydroxycyclohexane) 5 mg
Beet root powder 10 mg
Watercress 5 mg
Celery 5 mg
Dandelion 5 mg
Capsicum 5 mg
Artichoke Extract 100 mg
SOD (superoxide dismutase)3 250 mcg
Pyridoxal 5 Phosphate (B6) 25 mg
Agaricus Blazei 75 mg
Bromelain 100 mg
TOTAL 498 mg
1 Acetyl derivative of L-cysteine, an amino acid. Osilated as the HCl
salt preparation per Monograph 2787, Merck Index, Eleventh Ed. (1989).
2 An analog of cyandin chloride, a substituted benzyopyrylium
preparation and properties Monograph 2694, Merck Index, 11th Edition
3 Superoxide dismutase extracts of ox erythroctes are disclosed in the
scientific literature. French patent application Ser. No. 73.13670, filed
April 16, 1973, describes superoxide dismutase extracts from marine
bacteria strains, as well as a process for their preparation, which
process does not form any part of the present invention.
The other ingredients are readily available from various suppliers of
natural supplement components. Proanthocyanidins are an antioxidant
component of grape seed. Capsicum is cayenne pepper, and Agaricus Blazei is
a mushroom. Bromelain is a digestive enzyme derived naturally from
pineapple, and which is commercially available from makers of nutritional
The several components of the Renew Formula (Working Example II) recite the
optimal number of elements blended for a unit dosage, such as per capsule.
Still, the essential components are malic acid, silybum marianum, the L-cysteine
derivative, magnesium aspartate, copper chelate, and zinc gluconate (Cu/Zn
ratio of 1:5). The other minor concentration elements are useful adjuncts
for optimal effectiveness, but they are not essential to an effective unit
dosage. For the Foundation Formula (R), unit dosages, both the bioactive
pepides and probiotics are needed for their efficacy.
Claim 1 of 8 Claims
What is claimed is:
1. A first pharmaceutical composition, in unit dosage form which comprises a
major percent by weight of bioactive peptides consisting essentially of fish
protein concentrate and a minor percent by weight of probiotics selected
from the group consisting of DDS-1 strain of Lactobacillus acidophilus,
Lactobacillus bulgaricus, Bifidobacterium bifidum and Enterococcus faecium.
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