Patent Grant
7597915
The present invention relates to compositions containing medicinal plant extracts or purified or standardized fractions thereof, useful in the treatment of atopic dermatitis, skin allergic conditions and acne.
Atopic dermatites are characterized by persistent inflammatory conditions which may cause lacerations of the skin with possible infections. Inflammation is often accompanied by intense itching; the consequent scratching by the patient may further irritate the affected area.
Dermatites, which are also frequently referred to as eczema, are superficial skin inflammations, with acute or chronic course and variable clinical and histological manifestations, which affect an unnegligible percentage of population (2-3%).
The etiology of the various forms of dermatitis is still partly unclear, although the immune component is definitely one of the factors. The pathological manifestations are often alike, and are mainly characterized by the presence of papules, erythematous spots and vesicles, which can form plaques, edema, scaling-crusting lesions and the like. The most common dermatites comprise atopic dermatitis, contact allergies, contact dermatitis, stasis dermatitis, seborrheic dermatitis, lichen simplex and acne vulgaris.
The choice treatment consists in the use of corticosteroids, which involve well-known side effects (possible secondary infections, inefficacy after prolonged use, and the like).
It has now been found that compositions containing:
exert immediate, beneficial effect to the patient and induce the fast remission of the pathological condition, even compared with known medicaments such as topical anti-inflammatories and steroids.
More precisely, the compositions of the invention comprise:
According to the present invention, the Ginkgo biloba content can range from 0.1 to 2%; the floroglucinols content can range from 0.1 to 1%; and the Zanthoxylum bungeanum or Echinacea angustifolia lipophilic extract content can range from 0.01 to 0.5%.
According to the invention, Ginkgo biloba terpenes are present in the free form or preferably in the form of complex with natural or synthetic phospholipids. “Ginkgo biloba terpenes” herein means the terpenes, either pure or in a mixture wherein the total triterpenes content ranges from 60 to 100%, preferably 90%, the bilobalide content ranges from 20 to 70%, preferably 45%, and ginkgolides A, B, C and J total content ranges from 25 to 75%, preferably 50%.
Ginkgo biloba terpenes, in addition to the antinflammatory action, also exert antiallergic action, as observed in a number of models both in animals and humans, thereby reducing one of the symptoms involved, which keep irritation and the continuous recidivation. This antiallergic action makes said terpenes particularly useful when an immune factor is involved in the etiology.
Floroglucinols, either pure or in a mixture thereof extracted from Humulus lupulus, Hypericum sp and Mirtus sp., are active against anaerobic bacteria such as Propionibacterium acnis and the like and on Candida albicans strains, at concentrations of 0.5-4 μg/mL.
In particular, Humulus lupulus extracts are characterized by a floroglucinols content of 20 to 80%, preferably 60%. Among the extracts of Hypericum sp., particularly preferred is a Hypericum perforatum extract with a floroglucinols (adhyperforin/hyperforin) content ranging from 20 to 80%, preferably 60%. Among the extracts of Mirtus sp, particularly preferred is an extract of Mirtus communis leaves prepared by extraction with carbon dioxide under pressure ranging from 235 to 260 bars, at a temperature ranging from 40 to 60° C., preferably a 45° C. The resulting extract usually contains about 35% of mirtocumulone.
The compositions of the invention containing a Zanthoxylum bungeanum or Echinacea angustifolia lipophilic extract enriched in isobutylamides, active as topical analgesics inhibiting the nervous conduction proved particularly effective in the treatment of localized itching. Therefore, according to a preferred aspect, the compositions of the present invention will contain, as component c), a Zanthoxylum bungeanum or Echinacea angustifolia lipophilic extract enriched in isobutylamides. The Zanthoxylum extract can be prepared for example as disclosed in WO 00/02570, while the Echinacea extract can be prepared for example as disclosed in EP 0 464 298.
The compositions of the invention further containing natural compounds with estrogenic and/or antiandrogenic action proved particularly effective in the treatment of seborrheic dermatitis and acne. Therefore, according to a preferred aspect, the compositions of the present invention will contain, in addition to components a), b) and c) above, also natural compounds with estrogenic action, such as ferutinine and/or extracts of various Ferula species, and/or natural compounds with antiandrogenic action, such as lauric acid.
According to a further preferred aspect, the compositions of the present invention will contain Oenothera biennis oil as lipophilic excipient.
The present invention, therefore, relates to topical compositions for the treatment of atopic dermatitis, skin allergic conditions and acne, containing the combinations described above. Said compositions will be prepared according to conventional methods well known in the pharmaceutical technique, such as those described in “Remington's Pharmaceutical Handbook”, Mack Publishing Co., N.Y., USA, together with suitable excipients commonly used in the art.
The examples reported hereinbelow further illustrate the invention.
Ginkgo biloba terpenes in form
Humulus lupulus extract
Zanthoxylum bungeanum extract
Oenothera biennis oil
Ginkgo biloba terpenes in form
Mirtus communis lipophilic extract
Zanthoxylum bungeanum extract
Oenothera biennis oil
Ginkgo biloba terpenes in form
Humulus lupulus extract
Echinacea angustifolia extract
Oenothera biennis oil
Ginkgo biloba terpenes in form
Hypericum perforatum extract
Echinacea angustifolia extract
Oenothera biennis oil
Ginkgo biloba terpenes in form
Humulus lupulus extract
Zanthoxylum bungeanum extract
Oenothera biennis oil
| Number | Date | Country | Kind |
|---|---|---|---|
| MI2003A2286 | Nov 2003 | IT | national |
| Filing Document | Filing Date | Country | Kind | 371c Date |
|---|---|---|---|---|
| PCT/EP2004/012608 | 11/8/2004 | WO | 00 | 5/23/2006 |
| Publishing Document | Publishing Date | Country | Kind |
|---|---|---|---|
| WO2005/053720 | 6/16/2005 | WO | A |
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| 7008627 | Castelli et al. | Mar 2006 | B1 |
| 7166310 | Koch et al. | Jan 2007 | B2 |
| 20040185123 | Mazzio et al. | Sep 2004 | A1 |
| 20060275246 | Bombardelli et al. | Dec 2006 | A1 |
| Number | Date | Country |
|---|---|---|
| 0 870 507 | Oct 1998 | EP |
| 108642 | Jul 1994 | RO |
| Number | Date | Country | |
|---|---|---|---|
| 20070071839 A1 | Mar 2007 | US |
