Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Patent
1992-05-07
1994-03-22
Rollins, John W.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
514456, A61K 3578
Patent
active
052962245
DESCRIPTION:
BRIEF SUMMARY
The invention relates to an extract of low flavokawin content from the rhizome of Piper methysticum Forst. (pepper intoxicant, Piperaceae family) called "kava-kava", having a high content of kava lactones and good bioavailability.
In Polynesia, the home of the kava bush, since ancient times the natives have used an aqueous extract (cold macerate) of the drug for ritual and therapeutic purposes.
The relaxing action of the drug, which is used as phytotranquilizer for relaxing in cases of nervousness and overexcitement and as an agent for including sleep, is based on the occurrence of several 6-substituted 4-methoxypryones, that is the kava lactones kawain, dihydrokawain, methysticin, dihydromethysticin, yangonin and desmethoxyyangonin (cf. Hansel et al., Deutsche Apothekerzeitung 125, No. 41, pages 2056-2058 (1985)). In addition, in the kava drug the yellow compounds flavokawin A and flavokawin B are contained to which skin-specific secondary effects are assigned (Shulgin, Bulletin on Narcotics, Vol. XXV, No. 2, pages 59-74 (1973)). Finally, the drug contains a series of further contents which have not yet been fully clarified and which are pharmacologically inert and referred to as "matrix substances".
Some kava lactones have also been synthesized, including kawain, the racemate being available commercially as psychopharmacological agent in the form of capsules containing 200 mg of the active agent.
The kava lactones are practically insoluble in water. For example, the maximum solubility of kawain at 21.degree. C. is 2.2 mg/100 ml water. In the cold macerate used by the Polynesians, however, there is up to about 70 mg kava pyrones (total pyrone content) in every 100 ml macerate. It was concluded from this that the pharamacologically inert "matrix substances" contained in the drug act as solubilizers for the kava pyrones (cf. Hansel et al., loc. cit.).
Because of its low bioavailability, the therapeutic effect obtainable with the kava lactone preparations hitherto on the market is unsatisfactory. The individual pure substances, irrespective of whether they are synthesized or isolated from the drug, must be administered in high doses because of their poor solubility whilst the dry extracts recovered from the drug have a total lactone content of only about 5 to 30% by weight so that in spite of the better solubility compared with the pure substances high doses must again be used to obtain the desired minimum titer in the blood or plasma.
The invention is therefore based on the problem of providing a dry extract having a substantially higher total lactone content but nevertheless good water solubility, with high bioavailability after oral administration and as low a flavokawin content as possible, as well as a simple process for the production thereof. The invention is further based on the problem of making pharmaceutical preparations with a high content of readily soluble and bioavailable kava lactones and as low as possible in flavokawin content, which can be administered orally and with which the danger of secondary effects due to discolouring of the skin is greatly reduced compared with the preparations known hitherto.
This problem is solved according to the invention by a dry extract from the rhizome of Piper methysticum Forst. which is characterized by a total content of kava lactones of at least 50% by weight and a flavokawin content of at the most 0.3% by weight. Preferably, the dry extract has a total content of kava lactones of 50 to 90% by weight and/or a flavokawin content of less than 0.3% by weight. An extract is particularly advantageous which has a total content of kava lactones of 60 to 80% by weight and the flavokawin content of which is less than 0.2% by weight.
Although the extract according to the invention is highly enriched compared with the extracts known hitherto and has a total content of kava lactones of up to 90% by weight and thus comes very close to the pure preparations, consisting for example of 100% kawain, it has surprisingly been found that the bioavailability of the extract a
Dr. Wilmar Schwabe GmbH & Co.
Rollins John W.
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