Title: Integrated comprehensive hemorrhoid treatment compositions and regimen
United States Patent: 6,228,387
Inventors: Borod; Murray (1420 Capri Ave., Petaluma, CA 94954)Appl. No.: 641884
Filed: August 18, 2000A first composition for topical application and a second for oral administration, make up a comprehensive program for the treatment and relief of hemorrhoids. The topical application composition contains supplements for healing of hemorrhoids including an agent for the enhancement of the formation of collagen and elastin, an antioxidant having a proanthocyanidin as the active agent in combination with vitamin C, one or more anti-inflammatory agents, and vitamin E. In the preferred embodiment, the composition is made from gotu kola extract, grape seed extract, horse chestnut extract, aloe vera, vitamin C, and vitamin E. A few drops each of Essential Oils of Chamomile and Lavender may be included. The composition may be formulated as an ointment, cream or gel for external application. The components of the composition work synergistically to relieve the pain, discomfort and swelling associated with hemorrhoids while enhancing the connective tissue sheathes surrounding and supporting the veins and capillaries. The composition for topical application is used in combination with a second composition of supplements for oral administration which includes gotu kola extract, grape seed extract, bilberry extract, vitamin C and vitamin E. The second composition is administered as a daily dosage, and may be formulated as one or more tablets, capsules, softgels or gelcaps.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
The invention is a comprehensive, integrated hemorrhoidal
treatment and relief program, made up of two important components, these
being a first composition for topical application, and a second, equally
important, composition of supplements for oral administration.
1. Composition for Topical Application
The topical application composition is composed of an agent for the
enhancement of the formation of collagen and elastin, an antioxidant
having a proanthocyanidin as the active agent in combination with vitamin
C, and an anti-inflammatory agent in combination with vitamin E.
The agent for the enhancement of the formation of collagen and elastin is
preferably gotu kola (Centella asiatica) extract. Gotu kola is described
in The Healing Power of Vitamins, Minerals and Herbs, (Readers Digest
Association, Ltd., Pleasantville, N.Y., 1999) at pp. 306-307 and The
Healing Power of Herbs, 2nd ed., M. T. Murray (Prima Publishing, Rockin,
Calif., 1995), at pp. 173-183. (The foregoing is incorporated into this
disclosure by reference.) Centella is a perennial plant native to India,
China, Madagascar, Africa and Australia. Gotu kola extract contains a
number of pharmacologically active triterpene compounds, including asiatic
acid, madecassic acid, asiaticoside, and madecassoside. In addition, gotu
kola contains the flavonoids kaempferol, quercetin, and their glycosides.
As used in the present invention, the gotu kola extract is preferably
standardized to contain at least 10% asiaticoside. Numerous studies have
shown gotu kola to be effective in the treatment of varicose veins. Gotu
kola appears to aid the formation of collagen and elastin, resulting in
improved strength of the connective tissue sheath surrounding the veins
and capillaries, reduction in hardening and improved elasticity of the
blood vessels, improved blood flow through the veins and capillaries, and
improved permeability of the vessel walls.
The antioxidant used in the composition of the present invention is
preferably grape seed extract, although Pycnogenol.RTM. may be used in
alternative embodiments. Both grape seed extract and Pycnogenol contain
proanthocyanidins, which are a group of polyphenols having a flavonoid
structure, and particularly are made from chains of catechins and
epicatechins, resulting in at least ten hydroxyl groups.
The proanthocyanidins are powerful antioxidants, and therefore useful in
scavenging free radicals, primarily O2-, hydrogen
peroxide, and hydroxyl radicals. Free radicals are formed in the
hemorrhoid sufferer, either as the result of dietary insufficiencies,
stress, inflammation or aging. Free radicals are highly reactive and
damage the connective tissue and the blood vessels. Proanthocyanidins
neutralize free radicals, either by reducing them directly, or by an
addition reaction in which the proanthocyanidin is oxidized by the free
radicals to incorporate the additional oxygen into their structure.
Proanthocyanidins are flavonoids which are thought to enhance vitamin C
concentrations in the blood and to promote vitamin C's role in the
formation of collagen.
Grape seed extract is preferred to Pycnogenol.RTM. because (1) grape seed
extract contains a higher proanthocyanidin concentration than
Pycnogenol.RTM. (about 10% higher); (2) grape seed extract contains the
gallic esters of proanthocyanidins, which are regarded as the best free
radical scavengers; and (3) grape seed extract may be more economically
produced than Pycnogenol. In the preferred embodiment of the present
invention, the grape seed extract is standardized to contain 92 to 95%
proanthocyanidins.
The main pharmacological constituent of horse chestnut seeds, twigs,
sprouts and leaves is the saponin escin or aescin, a mixture of triterpene
saponins. Aescin is known to have anti-inflammatory and edemic actions,
and is used in topical ointments. Topical gels are standardized to contain
2% aescin.
The composition further contains vitamin C (ascorbic acid). Vitamin C is
known to strengthen capillaries and cell walls, and is crucial to the
formation of collagen. Vitamin C works synergistically with the powerful
antioxidant agent, either grape seed extract or Pycnogenol. The
proanthocyanidins in the antioxidant agent serve to protect vitamin C,
thereby enabling the vitamin C to perform its role in forming collagen in
order to strengthen the blood vessels.
The composition also contains an additional anti-inflammatory agent,
preferably aloe vera. Aloe vera is a succulent plant of the Lily family
which is native to Africa and grown commercially in warm regions
throughout the world. The inner layer of the plant leaf contains a clear
gel. Aloe vera gel is known to contain a number of anti-inflammatory
agents useful for topical applications. The gel produces
anti-inflammatory, moisturizing and emollient effects which help to
relieve pain and stop itching. Aloe vera--dilates capillaries allowing
more blood to get to the diseased area, thus speeding up the healing
process.
The composition contains vitamin E, which is reported to have
anti-inflammatory effect when applied topically. Vitamin E, either an
.alpha.-tocopherol or mixed tocopherols, is also an antioxidant. Studies
have shown that vitamin E appears to work synergistically with vitamin C,
so that vitamin E helps to maintain vitamin C levels, and vice versa.
If desired, the composition may include a few drops of Essential Oil of
Chamomile. Used externally, chamomile is known to help soothe skin
inflammation and chamomile contains bacteria-fighting compounds that may
speed the healing of infections as well.
Also, the composition may include a few drops of Essential Oil of
Lavender, which has properties similar to those of chamomile, and is quite
soothing to the skin.
The inventive concept of the composition according to the present
invention is intended to extend to any composition containing an agent for
the enhancement of the formation of collagen and elastin, an antioxidant
having a proanthocyanidin as the active agent in combination with vitamin
C, and an anti-inflammatory agent in combination with vitamin E. A
preferred example of percentage content of the composition is listed in
Table 1 below, although the invention is not limited to the percentages
supplied in the table.
TABLE 1
Composition for Topical Application
Component Supplements Daily Dosage
Gotu kola extract, 40-100 mg
standardized
Grape seed extract, 40-100 mg
standardized
Horse Chestnut 40-100 mg
Extract, standardized
Aloe vera gel 40-100 mg
Vitamin C 30-60 mg
Vitamin E 50-200 IU
Essential Oil of a few drops
Chamomile
Essential Oil of a few drops
Lavender
The composition may be made in the form of an ointment, a cream, or a gel. For this purpose, the composition may contain a pharmaceutically acceptable topical carrier which has substantially non-irritating compatible components, either alone or in mixtures, which are suitable for delivering the active components topically. Thus, the composition may contain solvents, fatty bodies, thickening agents, emulsifiers, an emulsion, or other excipients which do not alter the therapeutic effect of the active ingredients. The composition may be packaged in jars, squeeze tubes, suppositories, pads, or in wipes infused with the formula which may be used in place of toilet tissue. Since the components of the composition are soluble, they will be absorbed through the hemorrhoidal tissues and tissues of the anal-rectal region, entering the blood stream through the capillaries. Thus, although the composition is applied topically, the composition will also have systemic effects.
2. Composition for Oral Administration
The effectiveness of topical application of the composition is accompanied by an equally important, daily regimen of a second composition of supplements administered orally. A preferred regimen of supplements is set forth in Table 2 as follows. For purposes of this application, the oral regimen of supplements can be in the form of one or more tablets, capsules, softgels or gelcaps containing the component nutrients in the approximate dosages listed in Table 2.
TABLE 2
Oral Regimen of Supplements
Supplement Daily Dosage
Gotu kola extract, 100-300 mg
standardized
Grape seed extract, 100-300 mg
standardized
Bilberry extract, 100-300 mg
standardized
Vitamin C 250-1000 mg
Vitamin E 250-1000 I.U.
The preferred regimen should be administered orally, daily. The dosages may be formulated as one or more tablets, capsules, softgels or gelcaps. For this purpose, the second composition may additionally contain fillers and other excipients.
Bilberry, or Vaccinium myrtillus, is a shrubby perennial plant of the berry family endogenous to Europe. The active ingredients in bilberry are flavonoid compounds known as anthocyanosides, which are composed of an anthocyanidin and a sugar. The flavonoids are known to have an antioxidant effect and to work synergistically to maintain vitamin C levels. Bilberry extract exhibits collagen stabilizing activity and reduces capillary permeability and fragility. A standardized extract of bilberry contains at least 25% anthocyanoside content. The remaining components of the oral regimen have been described above.
Advantageously, the compositions of the present invention for topical application and the regimen of supplements are nontoxic vitamins and natural plants extracts which are safe at the dosage levels described herein. Thus, the compositions for hemorrhoid treatment and relief of the present invention provide for temporary relief of pain and discomfort while actively promoting healing through correcting deficiencies.
It is to be understood that the present invention is not limited to the sole embodiments described above, but encompasses any and all embodiments within the scope of the following claims.
Claim 1 of 8 Claims
I claim:
1. A topical composition for hemorrhoid treatment and relief comprising:
a) a plant derivative for the enhancement of the formation of collagen and
elastin consisting of from about 40 to 100 mg gotu kola extract;
b) an antioxidant having a proanthocyanidin as the active agent consisting
of from about 40 to 100 mg grape seed extract;
c) an anti-inflammatory agent consisting of about 40 to 100 mg horse
chestnut extract and about 40 to 100 mg weight aloe vera gel;
d) from about 30 to 60 mg vitamin C; and
e) from about 50 to 200 IU vitamin E.
____________________________________________
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