Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules
Reexamination Certificate
2000-12-28
2002-07-16
Lilling, Herbert J. (Department: 1651)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Capsules
C424S725000, C424S043000, C424S059000, C424S073000, C424S455000, C424S465000
Reexamination Certificate
active
06419950
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to a novel extract obtained by extraction of the pericarp of
Zanthoxylum bungeanum
with carbon dioxide and to the pharmaceutical and cosmetic formulations containing it. This extract has anti-inflammatory and analgesic activities and can be used for the treatment of itching.
BACKGROUND OF THE INVENTION
Pericarp of
Zanthoxylum bungeanum
is commonly used in China in spices for seasoning food. Moreover, in Chinese and Indian folk medicine, this part of the plant is used as local anesthetic and for the treatment of dysentery. The essential oil, which contains a series of monoterpenes such as 1,8-cimol, linalool, 4-terpinol, caryophyllene, limonene and the like, is also reported as a strong repellent against insects.
Recently, EP 568001 disclosed the antiviral activity of the skin of this fruit. In U.S. Pat. No. 5,137,912, chelcrythrine extracted from the root bark of
Zanthoxylum simulans
(synonym of
bungeanum
) was disclosed to be active in the prevention of thrombosis. According to JP 01294657, the extraction of the pericarp with organic solvents provides an extract containing isobutylamides that exerts a local anesthetic effect 30 seconds after application on the tongue and lasting up to 20-80 minutes.
Despite this, there remains a need for additional anti-inflammatory and analgesic formulations, and the present invention satisfies this need.
SUMMARY OF THE INVENTION
It has now surprisingly been found that the extract of the pericarp of
Zanthoxylum bungeanum,
prepared by extraction with carbon dioxide under supercritical conditions, has remarkable analgesic activity without exerting the local anesthetic activity characteristic of the extracts obtained by solvent means. The product of the present invention is prepared by extracting the pericarp of
Zanthoxylurn bungeanum,
finely ground or transformed into pellets, with carbon dioxide under pressure conditions ranging from 150 to 300 bars, preferably under 180-230 bars, at temperatures ranging from 35 to 55° C., preferably at 35-40° C.
The resulting extract can either be used as it is, after removing the extraction water, or it can further be purified by partitioning it with immiscible solvents such as aliphatic alcohols and aliphatic hydrocarbons, preferably n-hexane or petroleum ether.
The resulting extracts proved to exert a marked analgesic activity when applied percutaneously to humans; therefore they are valuable for use both in the pharmaceutical and cosmetic fields.
In the pharmaceutical field, these extracts are useful for alleviating pain resulting from diabetic microangiopathy, hemorrhoids, burns, or due to any other local causes. A further application of the extracts of the invention is in the treatment of itching.
In the cosmetic field, the extracts according to the invention are useful in depilatory creams, after-sun formulations, shaving lotions and creams, and in all types of skin treatments requiring local analgesic or anti-itching action.
REFERENCES:
patent: 01 294657 (1989-11-01), None
Computer DWPI Abstract 1990-012982 JP01294657A Nov. 1989.*
Computer IFSCC Abstract 23627 Cristoni et l “In-Cosmetics” Apr. 20-22, 1999 P342-353.*
Kenji Mizutani et al. “Amides from Huajiao; Pericarps of Zanthoxylum Bungeanum Maxim.” Chemical and Pharmaceutical Bulletin, vol. 36, No. 7, 1988, pp. 2362-2365.
Xin-Li Huang et al. “Effects of Extracts of Zanthoxylum Fruit and their Constituents on Spontaneous Beating Rate of Myocardial Cell Sheets in Culture.” Phytotherapy Research, vol. 7, No. 1, 1993, pp. 41-48.
Bombardelli Ezio
Gabetta Bruno
Indena SpA
Lilling Herbert J.
Pennie & Edmonds LLP
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