Aphios
Granted United States Patent for Making
an Enhanced St. John’s Wort Product
October
24, 2001
— Aphios
Corporation announced today that it was granted United States
Patent No. 6,291,241, entitled “Method for Making Hypericum
Fractions and St. John’s Wort Products,” on September 18,
2001.
St.
John’s Wort (Hypericum perforatum) is a bushy
perennial with yellow flowers that blooms around St. John
the Baptist’s day in June. An oil extract of the
fresh flowers contains liposoluble napthodianthrones, such
as hypericin and hyperforin. These compounds are thought
to be responsible for St. John's Wort reputation as an effective
antidepressant.
St.
John’s Wort extracts are in fact among the most popular
OTC “phytomedicines” sold throughout Europe
and the United States. Among the most widely prescribed
antidepressants in the United States are Prozac® from Eli Lilly, Zoloft® from Pfizer and Paxil® from SmithKline Beecham. The worldwide
sales of the top selling antidepressants exceed $8 billion
per year. As people experience adverse side effects from
prescription antidepressants, there has been a concomitant
rise in the use of St. John’s Wort and other herbs
as natural antidepressants. However, St. John’s Wort products
are not being manufactured with any significant regard to
efficacy, safety and standardization. Often, these products
are not standardized to the correct bioactive ingredient,
and their content and quality are not reproducible from
one batch to the next.
Aphios
has discovered and developed a method for standardizing
and manufacturing an enhanced efficacy St. John’s Wort product.
This method utilizes supercritical fluids and near-critical
fluids with or without polar cosolvents such as alcohols
(SuperFluids™ ). These fluids are gases such
as carbon dioxide which, when compressed, exhibit enhanced
thermodynamic properties that can be “fine-tuned” for rapid
and selective extraction of bioactive molecules. Such fluids
provide for more rigorous standardization of nutraceuticals
and potential herbal Rx products such as St.
John’s Wort and for achieving formulations that may not
be produced with conventional organic phase manufacturing.
These products are free of toxic organic solvents, environmentally
friendly and truly “green.”
In
vitro serotonin reuptake inhibition assays, conducted
by an independent testing laboratory, have shown that Aphios’
SuperFluids St. John’s Wort product is as effective
as Prozac and Zoloft at the 10 to 25 mg level. The bioactive
ingredient of the St. John’s Wort product has been identified
to be hyperforin with chromatographic and absolute purities
as high as 80%. This hypericin-free St. John’s Wort product
demonstrates a linear dose-response curve in the in vitro
bioactivity assay.
Research
leading to this invention was funded, in part, by a Fast
Track SBIR grant from the National Center for Complementary
and Alternative Medicine (NCCAM) of the National Institutes
of Health (NIH).
Aphios
Corporation is a biopharmaceutical company which is developing
enhanced therapeutics for health maintenance and the treatment
of human diseases with a focus on infectious diseases, cancer,
CNS disorders. Aphios Corporation has developed several
enabling technology platforms for improving the discovery,
manufacturing, delivery and safety of therapeutic drugs,
and has several enhanced therapeutic drugs in development.
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