Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from piper
Reexamination Certificate
2000-05-31
2001-10-16
Lilling, Herbert J. (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Containing or obtained from piper
Reexamination Certificate
active
06303157
ABSTRACT:
BACKGROUND
The plant kava-kava (piper methysticum Forst. Piperaceae) is native to Polynesia. An intoxicating beverage made from its crushed roots has been used in ceremonies since ancient times.
Kava-kava has been found to have significant analgesic and anesthetic effects via non-opiate pathways. It also can be used as phytotranquilizer to reduce nervousness and overexcitement. However, kava-kava's most popular application is as a natural anxiolytic and has compared favorably to a number prescription medications such as benzodiazepines. Kava-kava's pharmacological activity has been attributed to lactones present in the plant roots.
Several kava-kava products are available, such as kava-kava-based beverages, kava-kava ethanol extract solutions, kava-kava emulsions with glycerin and coconuts oil dispersed in water, and kava-kava extract tablets. Unfortunately, the active lactones in kava-kava-based products have low bioavailability since the lactones themselves are practically insoluble in water. For example, the maximum solubility of kawain at 21° C. is about 2.2 mg/100 ml water. Accordingly, high doses of kava-kava-based products or the active lactones are required to obtain therapeutic effects.
SUMMARY
In one aspect, the invention features a method of obtaining a kava-kava lactone-containing product by heating pulverized kava roots in an aqueous solution which contains a cyclodextrin-based solubilizing agent to extract kava-kava lactones from the pulverized kava-kava roots.
In another aspect, the kava-kava lactone-containing product in dried form includes greater than about 50 parts by weight (e.g., about 50 to about 99 parts by weight) of one or more of the active kava-kava lactones and has a solubility of at least about 0.05 mg/ml (e.g., about 0.05 mg/ml to about 25 mg/ml), preferably greater than about 0.1 mg/ml, and most preferably greater than about 1 mg/ml in water at about 25° C.
The cyclodextrin-based solubilizing agent includes &agr;, &bgr;, or &ggr; forms of cyclodextrin and derivatives thereof. &agr;-cyclodextrin is a ring of six glucose residues, &bgr;-cyclodextrin is a ring of seven glucose residues, and &ggr;-cyclodextrin is a ring of eight glucose units. Examples of cyclodextrin-based solubilizing agents, include but are not limited to, &agr;, &bgr;, or &ggr; forms of cyclodextrin, hydroxypropylcyclodextrin, hydroxyethylcyclodextrin, glucosylcyclodextrin, maltosylcyclodextrin, and maltotriosylcyclodextrin. See, for example, U.S. Pat. No. 5,997,856.
In another aspect, the invention features a method of removing flavokawains from a crude kava-kava lactone-containing preparation. The method includes heating the crude kava-kava lactone-containing preparation in an aqueous solution which contains a cyclodextrin-based solubilizing agent to solubilize kava-kava lactones and thereby produce an aqueous kava-kava lactone-containing solution; and removing flavokawains from the solution, such as by filtering. Crude kava-kava lactone-containing preparations, typically, are produced by extracting pulverized kava-kava root with an organic solvent and are commercially available as kava-kava extracts.
In yet another aspect, the invention features a solubilized kava-kava root extract in aqueous form including active kava-kava lactones in a concentration greater than 0.05, preferably greater than about 0.1, and most preferably greater than about 1 weight percent of the extract, and flavokawains in a concentration of less than about 0.3 weight percent of the extract.
In still another aspect, the invention features a solubilized kava-kava root extract in dried form including active kava-kava lactones in a concentration greater than about 50 weight percent of the extract, and flavokawains in a concentration of less than about 0.3 weight percent of extract.
The kava-kava lactone-containing product (i.e., kava-kava root extract) of this invention exhibits desirable composition and performance. It has a high content of kava-kava lactones and a low content of flavokawains, and increased bioavailability and skin permeability of kava-kava lactones when used as an ingredient in a food, pharmaceutical, or cosmetic product.
Other features and advantages of the invention will be apparent from the following detailed description, and from the claims.
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Chen Lan Bo
Ono Mitsunori
Fish & Richardson P.C.
Kava Pharmaceuticals, Inc.
Lilling Herbert J.
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