Xantol™ is an enhanced St. John’s Wort product, which is standardized by hyperforin content [U.S. Patent No. 6,291,241 B1, Castor et al., 2001]. Aphios utilized its patented SuperFluids™ fractionation and manufacturing technologies to develop this product. Aphios is developing Xantol™ for mild to moderate depression, as a natural alternative to prescription antidepressants with adverse side-effect profiles.

St. John’s Wort (Hypericum perforatum, SJW) is an over-the-counter herbal remedy, which is often self-prescribed for the treatment of depression, anxiety, and sleep disorders. SJW has comparable efficacy to the selective serotonin re-uptake inhibitors (SSRI) for the treatment of mild to moderate depression (Pepping, 1999). Hypericum perforatum is a bushy perennial with yellow flowers that bloom around St. John the Baptist’s day in June. An oil extract of the fresh flowers contains liposoluble napthodianthrones and phloroglucinols, such as hypericin and hyperforin. These compounds are thought to be responsible for St. John’s reputation as an effective antidepressant.

In our research, we identified and patented an enriched SJW fraction of Hypericum perforatum that is quite effective as a serotonin reuptake inhibitor (SRI). The bioactive ingredient was identified through an in vitro serotonin reuptake inhibition assay, and by HPLC chemical analyses and Mass Spectra analyses to be hyperforin.

Xantol™ has been shown in an in vitro serotonin reuptake inhibition assays to exhibit linear dose-response curves with respect to hyperforin content. Hyperforin is a clear, honey-colored and honey-like material that becomes waxy at 4°C; it is insoluble in water and only partially soluble in absolute ethanol.

Permeability measurements, using the in situ single pass perfusion technique in rats, determined that Xantol™ is very permeable, perhaps 5 to 6 times higher permeability than metoprolol, which is recommended as the “high permeability” internal standard by the FDA in the BCS guidance. Xantol™ will be most likely classified as BCS 2, high permeability and low solubility, by the FDA. Aphios has established a standardized formulation of Xantol™ in opaque hard-gel capsules that contain natural antioxidants and are purged with nitrogen to enhance stability. The capsules are contained in an amber bottle or blister paks to minimize light intrusion and improve shelf life.

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