Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from a root – bulb – tuber – corm – or...
Reexamination Certificate
1999-04-29
2001-07-31
Lilling, Herbert J. (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Containing or obtained from a root, bulb, tuber, corm, or...
C435S091500, C435S091500, C435S091500, C435S091500
Reexamination Certificate
active
06267996
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention is directed to novel pharmaceutical and cosmetic formulations which exhibit antimicrobial activity comprising hydrophilic or pure extracts of Krameria and lipophilic extract of
Mesua ferrea
in a sufficient amount to exhibit antimicrobial activity.
Extracts of the roots, bark, and leaves of different species of Krameria are enriched in neolignanes which have antimicrobial activity against gram negative, gram positive bacteria, fungi, and anaerobic strains. (Martindale, The Extrapharmacopeia, 28th Ed. 1982; Cannizaro, Boll. Soc. Ital. Biol. Sperim. 1, 22, 1964; V. Hoppe, Drogenkunde Bdl Walter De Gruyter Ed., 1975; and British Patent 2,184,353 A). A preferred species of Krameria is
Krameria triandra
, and a particularly active neolignane is Eupomatenoid. The extracts are obtained by extraction with chlorinated solvents, aliphatic ethers and ketones, as well as aliphatic and aromatic esters.
The extracts of Krameria's roots, bark, and leaves are naturally hydrophilic due to the phenol character of their active components. Nevertheless, the extraction can be carried out with protic solvents. Pure Eupomatenoid 6 and 2-(2,4-dihyroxyphenyl)-5-propenylbenzofuran can be recovered from these extracts using chromatographic techniques on silica gel, as reported in EP 0 464 297 B1.
Flowers, and particularly the buds, of
Mesua ferrea
, yield a lipophilic extract containing substituted coumarins and xanthones. These extracts are particularly active on gram negative, gram positive, and anaerobic bacterial strains, with an activity comparable to that of the extract prepared from
Krameria triandra.
The extraction can be carried out with aprotic solvents such as hexane, methylene chloride. However, for better results, the extraction process can be carried out with carbon dioxide in hypercritic conditions. For example, the extraction of vegetable material is conducted under pressures ranging from 110 to 260 bar, mainly at 200 bar and at temperatures ranging from 35° C. to 65° C., preferably at 45° C.
Despite improvements in the extraction process of Krameria, the use of the extract or compounds within the extract with medications is still mostly undeveloped. Shortcomings include the absence of medications which use Krameria extracts in combination with other medications and a clear understanding of the effect of extract of Krameria upon other compounds. The present invention is directed to overcoming these shortcomings by providing cosmetic and pharmaceutical formulations comprising extract of Krameria and extract of
Mesua ferrea
and demonstrating their superior antimicrobial activity as compared to conventionally prepared compounds, i.e. compounds lacking extract of Krameria and extract of
Mesua ferrea.
SUMMARY OF THE INVENTION
The present invention is directed to an antimicrobial or preservative formulation comprising an extract of Krameria in combination with an extract of
Mesua ferrea.
The extracts are present in a combined amount sufficient to inhibit microbial growth, including weight ratios of between about 10:1 to about 1:10, preferably between about 2:3 to about 3:2, and more preferably about 1:1. The Krameria extract is present in an amount of between about 0.01% to about 1% by weight, and is an extract of Krameria sp., extract of
Krameria triandra,
a neolignane, a pure compound of the extract, or a mixture thereof. The neolignane may be Eupomatenoid 6, 2-(2,4-dihydroxyphenyl)-5-propenylbenzofuran, or a mixture thereof. The
Mesua ferrea
extract is present in an amount of between about 0.1% to about 0.5% by weight.
The formulation may also comprise at least one ximeninic acid, in a amount of between about 0.1% to about 0.5% by weight; lauric acid, in an amount of between about 0.1% to about 0.4% by weight; and an anti-inflammatory saponin, in an amount between about 0.1% to about 1% by weight. Preferably, the anti-inflammatory is an extract from
Olax dissitiflora, Aesculus hippocastanum, Centella asiatica, Terminalia sericea, Glycyrrhiza glabra,
or a mixture thereof.
Pharmaceutical or cosmetic compositions may contain the formulation in sufficient amounts to inhibit microbial growth and a pharmaceutically acceptable carrier or excipient. Pharmaceutical, food, or cosmetic compositions can be preserved using the formulation when applied in sufficient amount to inhibit microbial growth. Particularly, a pharmaceutical composition containing the formulation can be used in the treatment of acne.
DETAILED DESCRIPTION OF THE INVENTION
Surprisingly, it has been found that the combination of extracts of some plants naturally having low antimicrobial activity alone or with compounds with antimicrobial activity, leads to a synergistic effect that enhances antimicrobial activity. In particular, combinations comprising hydrophilic extract of Krameria and lipophilic extract of
Mesua ferrea
have demonstrated superior results against gram positive, gram negative, and anaerobic bacterial strains as compared to compounds lacking extract of Krameria.
The present invention provides several benefits over the conventionally prepared antimicrobial formulations. One embodiment of the present invention enhances the effect of preservatives on food and cosmetic products. Another advantage of the present invention is that the cosmetic and pharmaceutical formulations reduce inflammation. Yet another advantage of the present invention is that the pharmaceutical and cosmetic formulations are particularly effective as antiacne medications.
As used herein, “extract of Krameria” means one or more compounds obtained from the extraction of roots, bark, leaves, or a combination thereof of Krameria with a suitable solvent. The compounds within the formulation obtained by extraction may be hydrophilic, hydrophobic, or a combination thereof.
As used herein, “pure compound from an extract of Krameria” means neolignanes such as Eupomatenoid 6 and 2-(2,4-dihydroxyphenyl)-5-propenylbenzofuran).
As used herein, “formulation” means a composition comprising more than one compound which may be homogeneous or heterogenous.
One embodiment of the invention is directed to pharmaceutical and cosmetic formulations with enhanced antimicrobial activity comprising extracts of Krameria and extracts of
Mesua ferrea
in a sufficient amount to be therapeutically effective. Yet another embodiment of the present invention is directed to formulations comprising hydrophilic extract of Krameria, lipophilic extracts of
Mesua ferrea,
and substances exhibiting anti-inflammatory activity.
The formulations comprising extract of Krameria and extract of
Mesua ferrea
exhibiting enhanced antimicrobial activity may be directed to food and cosmetic preservatives and used in the alimentary and cosmetic industries. Formulations, as applied to alimentary or cosmetic industries, comprise: hydrophilic extract of Krameria, and lipophilic extract of
Mesua ferrea.
As used in the present invention, “extract of Krameria” include extracts from Krameria sp.,
Krameria triandra,
pure compounds from the extract including but not limited to Eupomatenoid 6 and 2-(2,4-dihydroxyphenyl)-5-propenylbenzofuran, and mixtures thereof. Preferably, the extract is from
Krameria triandra
or a pure compound from Krameria extract. Extract of Krameria should be used in an amount which is therapeutically effective to exhibit antimicrobial activity.
As used in the present invention, “compounds exhibiting antimicrobial activity” include compounds that are capable of destroying or inhibiting the growth of microorganisms. The compounds exhibiting antimicrobial effect should be used in sufficient amounts to deter microbial growth.
As used in the present invention, “extract of
Mesua ferrea”
include extracts from the flowers, buds, and other parts of the
Mesua ferrea
plant. Extract of
Mesua ferrea
should be used in an amount which is therapeutically effective to exhibit antimicrobial activity; one of ordinary skill in the art with little or no experimentation can determine the amount necessary. When extract of K
Bombardelli Ezio
Cristoni Aldo
Morazzoni Paolo
Seghizzi Roberto
Indena S.p.A
Lilling Herbert J.
Pennie & Edmonds LLP
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