Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution...
Reexamination Certificate
2001-12-12
2003-08-19
Weber, Jon P. (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Reexamination Certificate
active
06607753
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to the field of therapeutic compounds for the treatment of diseases of the skin and mucosal tissue. In particular the present invention relates to creams, ointments, eye and ear drops made from the herb
Tribulus Terrestris
that have a high content of spirostanol-type steroidal saponins and are useful in the treatment of conditions related to viral, fungal, yeast, parasitic and bacterial infections, particularly genital, skin (including acne) and eye and ear infections.
2. Description of the Related Art
Tribulus Terrestris
, commonly known as “Puncture Vine” or Caltrop fruit, is an herb that has been used for centuries in Europe for hormone insufficiency in men and women. It has also been used in the treatment of liver, kidney and urinary tract disease. In recent years
Tribulus Terrestris
has been touted as a dietary supplement for improving athletic performance. It has been discovered that ingestion of
Tribulus terrestris
significantly elevates the level of several hormones: Testosterone; Luteinizing Hormone; Follicle Stimulating Hormone; and Estradiol. Clinical studies on Tribulus, conducted at the Chemical Pharmaceutical Institute in Sofia, Bulgaria, showed improved reproductive functions, including increased sperm production and Testosterone levels in men. Among women,
Tribulus terrestris
L. increased the concentration of hormones including Estradiol, with Testosterone being very slightly influenced, thereby improving reproductive function, libido and ovulation.
The active components of the
Tribulus terrestris
L. plant also have a stimulating effect on the immune, sexual and reproductive systems, leading to improved muscle building, stamina and endurance. Other positive changes observed in a number of cases were a reduction in cholesterol, enhanced mood and well-being. No adverse effects to the central nervous or cardiovascular systems were noted in any of the clinical studies.
The Tribulus plant is also of interest due to the increasing clinical importance of emerging pathogens as well as drug-resistant microorganisms, which lend additional urgency to identify novel, active compounds. Currently available drugs for the treatment of fungal infections include amphotericin B (a macrolide polyene), which interacts with fungal membrane sterols, flucytosine (a fluoropyrimidine), which interferes with fungal protein and DNA biosynthesis, and a variety of azoles (e.g. ketoconazole, itraconazole, and fluconazole) that inhibit fungal membrane-sterol biosynthesis (see e.g. Alexander, B. D. et al., Drugs, 1997, 54:657-678). Although amphotericin B has a broad range of activity and is viewed as the “gold standard” of antifungal therapy, its use is limited due to infusion-related reactions and nephrotoxicity (see Alexander, B. D. et al., Drugs, 1997, 54:657-678). Flucytosine usage is also limited due to the development of resistance and its narrow spectrum of activity. Further, the widespread use of azoles is causing the emergence of clinically-resistant strains of Candida spp. (see Alexander, B. D. et al., Drugs, 1997, 54:657-678). This problem is particularly important in treating vaginal infections due to bacteria, parasitis and fungi.
Other commonly used agents in treating vaginal infections include dimethylalkybenzalkonium choloride, nonylphenololyoxyethylene or nonoxynol-9. The use of these bacteriocidal agents in vaginally inserted suppositories, creams, foams or the like, however, is also not without problems inasmuch as these agents tend to diminish or destroy the healthy bacterial flora of the vagina, and cause a tendency to develop yeast infections (candidasis). Further, many of the prior art compositions have a narrow spectrum of action in that they cover only some of the microorganisms responsible for a particular condition.
In this respect, the
Tribulus terrestris
L. plant has been a promising alternative to existing “chemical” anti-microbials.
Tribulus terrestris
L. contains saponins, which in plants, are formed from a sapogenin core linked with a sugar. The sapogenin, or glycoside, may be a steroid or a triterpene and the sugar moiety may be glucose, galactose, a pentose or a methyl pentose. Samples of
Tribulus terrestris
L. extract prepared according to the invention disclosed herein have been found to include tigogenine, diosgenin (a steroid sapogenin), desoxydiosgenin astragalin, kampferol (a flavanoid), dioscin (a furostanol that converts to diosgenin and glucose under hydrolysis), protodioscin (a furostanol), harmine (a bioflavanoide), linoleic acid, galactoolysaccharide, protogracillin and kampferol biofavanoide compounds. As with many secondary plant compounds, the concentration of saponins within a plant will vary depending upon the identity of the plant, the source of saponin within the plant (e.g. seed, fruit, leaves) and the conditions under which the plant is grown. The method of extraction will also affect the concentration of saponins. Generally, however, saponins are present in conventional extracts at about 15 to 25 percent by weight and average at about 20% by weight.
Saponins are also found in soybeans, alfalfa, and ginseng have been studied extensively for their effect of lowering cholesterol. For example, U.S. Pat. No. 4,242,502 issued to Malinow et al (1980) relates to the use of saponins to inhibit cholesterol absorption. According to this reference, modification of the oligosaccharide portion of the saponin by hydrolysis under mild acid conditions affects the saponins' ability to affect cholesterol absorption. More particularly, when the sugar moiety of the saponin molecule is removed, i.e., the glycosidic linkage is cleaved, it was found that the cholesterol is no longer removed. Therefore, hyrolysis of saponin in the stomach or intestine is an important factor in considering the efficacy of saponin-containing therapeutic compound, for example, in the treatment of hypercholesterolemia. To this effect, U.S. Pat. No. 5,760,009 (Allen et al., 1998) discloses a crystalline monohydrate of a spirostanol glycoside that is not degraded in the digestive system and is useful for the control of hypercholesterolemia or atheroscerosis. Topical application of saponins also presents special consideration for therapeutic efficacy since not all saponins are topically bio-active.
The steriodal saponins found in the herb
Tribulus terrestris
are two types; furostanols and spirostanols. Furostanol steroidal saponins from
Tribulus terrestris
L. are not topically bio-active and must be first converted to spirostanols to become bio-active, for example, via enzyme hydrolysis. The instant invention discloses the use of
Tribulus terresteris
L. compositions having a high spirostanol saponin content useful in treating fungal, bacterial viral and parasitic infections and methods for making the same.
SUMMARY OF THE INVENTION
The present invention includes pharmacologic compositions derived from the herb
Tribulus Terrestris
L. that have a high content of spirostanol-type steroidal saponins and/or balance the ratio of furostanol to spirostanol-type saponins in the resulting composition. The compositions may be used topically, orally and on mucosal tissues and exhibit a strong anti-bacterial, anti-inflammation, anti-viral, and anti-herpes effect. They are highly useful in treating vaginal infections, skin disorders and viral infections such as herpes simplex I and herpes simplex II, and in some cases may block cancer cells from growing.
The compositions disclosed herein may be combined with ingredients known in the art to provide creams, ointments, and eye and eardrops. For example, the present invention discloses a cream made from
Tribulus Terrestris
L. that has a very strong anti-bacterial, anti-inflammation, anti-virus, anti-herpes effect, represents a great improvement in the fields of dermatology and gynecology and satisfies a long felt need of dermatologists and gynecologists. Additionally, the compounds and methods disclosed herein are useful in treating cervical woun
Alexis Brian
Cislo & Thomas LLP
Patten Patricia D
Weber Jon P.
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