Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution...
Reexamination Certificate
2001-06-27
2004-05-18
Patten, Patricia (Department: 1654)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
C424S773000, C424S776000
Reexamination Certificate
active
06737084
ABSTRACT:
DESCRIPTION OF THE INVENTION
While increased understanding of the pathophysiology of male erectile dysfunction progressed rapidly in the past decade and led to new therapeutic modalities, little has been done to address similar issues in women. Accordingly, the present invention relates to all aspects of modulating the female sexual response, including female sexual dysfunction, such as female sexual arousal disorders (FSAD), orgasmic disorders, and sexual pain disorders, and enhancing the female sexual experience. In particular, the present invention relates to compositions, articles of manufacture, methods of preparation thereof, methods of use thereof, etc., for conditions, disorders, and diseases related to female reproductive physiology systems, especially those involved in the female sexual response.
Compositions comprising botanical extracts, active agents, etc., can be produced and used in accordance with the present invention that are useful to treat or affect the female sexual response. For example, the present invention relates to compositions, preferably for topical or local use, which comprise one or more of the following ingredients, including, but not limited to, borage seed oil and other sources of gamma linolenic acid (GLA),
Angelica pubescens
root,
Coleus forskohlii
extract, vinpocetine, and other naturally-occuring cyclic adenosine monophosphate (cAMP) and cyclic guanine monophosphate (cGMP) phosphodiesterase (PDE) inhibitors and equivalents thereof. The compositions can produce one or more of the following pharmacological effects, including, but not limited to, increases in localized nitric oxide, cAMP production and/or elevation, cGMP production and/or elevation, prostaglandin E
1
production, inhibition of prostaglandin E
1
breakdown, calcium channel antagonism, phosphodiesterase inhibition, anti-oxidation, vasodilation, smooth muscle relaxation, etc.
A useful composition in accordance with the present invention can comprise borage seed oil or other borage plant parts, preferably from
Borago officianalis
. The borage plant (e.g., leaves, roots, and seeds) comprises a complex mixture of defined and undefined constituents, including, e.g., acetic acid; alkaloids; allantoin; amabiline; arabinose; ascorbic-acid; beta-carotene; bomesitol; calcium; choline; cobalt; dhurrin; fat; fiber; galactose; gamma linolenic acid; glucose plant; intermedine; lycopsamine; magnesium; malic acid; mucilage; niacin; phosphorus potassium; protein; pyrrolizidines; resin; riboflavin; rosmarinic acid; silicic acid; sodium; supinine; supinine viridiflorate; thiamin and zinc. A preferred bioactive ingredient of Borage is gamma linolenic acid (GLA) having a molecular weight of 278. GLA is a polyunsaturated fatty acid (PUFA) belonging to the group of fatty acids called omega-6 or N-6 fatty acids because of the presence of a double bond between the 6th and 7th carbon. GLA is found predominantly in the seed of the Borage plant, but is also found in evening primrose seed oil and other botanical and natural sources.
Borage seed oil can be prepared by any suitable method, preferably methods which extract GLA and other bioactive agents, such as cold pressure extraction, screw pressure extraction, solvent extraction, supercritical fluid extraction, etc. A borage seed oil can comprise any amount of GLA, preferably, e.g., by weight, at least about 10%, 15%, 20%, 25%, 30%, etc. The oil preferably is free of compounds which are toxic, or deleterious to mammals, such as alkaloids, pyrrolizidine, etc.
Borage seed oil can be present in a composition of the present invention in any effective amount, e.g., 1-100%, 10-95%, 20-95%, 30-95%, 50-95%, 70-90%, 60-90%, 80%, 81%, 82%, 83%, 84%, 84.25%, 85%, 86%, 87%, etc., w/w (i.e., weight of ingredient/weight of total composition).
In addition to borage seed oil, other sources of GLA can be utilized, including, e.g., purified or isolated GLA, botanical extracts, such as evening primrose oil (e.g.,
Oenothera biennis
and
Oenothera lamarckiana
), black currant oil, spirulina, oils from the seeds of the Ribes family, etc.
Borage seed oil has a variety of beneficial effects and activities, including, but not limited to, e.g., inhibiting platelet aggregation, lowering blood pressure, anti-inflammatory activity, vasodilation, prostaglandin promoting activity, PGE
1
promoting activity (see, below), promoting circulating hormones, causing smooth muscle relaxation, etc. Borage seed oil can be included in a composition of the present invention in amounts which are effective to achieve one or more of the aforementioned effects.
A composition of the present invention can also comprise Angelica, such as
Angelica archangelica, Angelica sinensis, Angelica sylvestris, Angelica officinalis
, archangel, European angelica, garden Angelica,
Angelica acutiloba
, preferably
Angelica pubescens
which is also known as Du Huo or Du Huo Radix. Angelica root is preferred, but other parts of the plants can be used as well. Angelica contains a wide and complex variety of different constituents, of a defined and undefined nature. Preferred bioactive compounds are flavinoids, flavones and coumarins, preferably, osthole or 7-methoxy-8-(3-methylpent-2-enyl)coumarin, and alpha-angelicalactone. Other coumarins, include, e.g., meranzin hydrate, nodakentin, marmesinin, columbianadin, columbianetin, bergapten, heramandiol, 6-alkylcoumarins, angelol-type coumarins, byak-angelicin, ferulin, oxypeucedanin, umbelliprenin, imperatorin, neobyakangelicin, prenylcourmarins, glabralactone, anpubesol, angelical, angelin, furanocourmins, and derivatives thereof. Other bioactive agents include, e.g., linoleic acid, osthenol, falcarindiol, numerous flavinoids and flavones, 11(S), 16(R)-dihydroxyoctadeca-9Z, 17-diene-12,14-diyn-1-yl-acetate, xanthotoxin, umbelliferone, ferulic acid, magnesium, and derivatives thereof.
Angelica possesses a number of pharmacological activities, including, but not limited to smooth muscle relaxant activity, phosphodiesterase inhibition, calcium antagonist activity, cycloxygenase and 5-lipoxygenase inhibition (e.g, Liu et al.,
Pharm. Bio
., 36(3):207-216, 1998), etc. Coumarins, and osthole in particular, have been identified to display activities such as, inhibition of platelet aggregation, inhibition of smooth muscle contraction, smooth muscle relaxation (e.g., Che-Ming et al.,
Naunyn
-
Schmiedeberg's Arch. Pharmacol
., 349:202-208, 1994), inhibition of calcium flux, cyclic nucleotide (such as cGMP and cAMP) phosphodiesterase inhibition, increase in cAMP and cGMP levels, anti-proliferative, anti-inflammatory (Yuh-Fung et al.,
Planta Medica
, 61(1):2-8, 1995), enhancement of the increase of cAMP and cGMP induced by forskolin, vasorelaxation, neurotransmitter receptor binding, such as GABA, 5HT-1A, D-2, and D-1 receptors (Jyh-Fei et al.,
Proceedings of the National Science Council Republic of China, Part B, Life Sci
., 19(3):151-158, 1995), etc. Alpha-angelicalactone also possesses various activities, including, e.g., calcium antagonism. See, e.g., Entman et al.,
J. Clin. Invest
., 48:229-234, 1969. Ferulic acid, another component of Angelica root also has been shown to scavenge oxygen free radicals and increase intracellular cAMP and cGMP. See, e.g. Zheng R L, Zhang H.,
Free Radic Biol Med
., 22(4):581-586, 1997. Preferred activities of Angelica are cyclic nucleotide phosphodiesterase inhibition, calcium antagonism, oxygen free radical scavenging, smooth muscle modulation, as either vasorelaxant or vasodilatory.
A composition of the present invention can comprise any effective amount of Angelica, preferably
Angelic pubescens
root, e.g., 0.1-99%, 0.1-80%, 0.1-50%, 0.5-8%, 1%, 2%, 3%, 4%, 5%, etc. w/w.
In another embodiment of the present invention, a composition can further comprise
Coleus forskohlii
, preferably from its tuber or roots. The plant is a member of the Labiatae family and grows as a perennial. It is native to India, Nepal, Sri Lanka, and Thailand. See, e.g.,
The Wealth of India
, Vol. II, C.S.I.R., India, 1950, Page 308
. Coleus forskohlii
Bennett Robert M.
Crosby Martin G.
Millen White Zelano & Branigan P.C.
Patten Patricia
Qualilife
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