An enhanced St. John's Wort botanical product standardized by hyperforin for use as an alternative to prescription antidepressants

Xantol™ - An Enhanced St. John's Wort Botanical Drug

Xantol Hyperforin-Molecular-Structure smXantol™ is an enhanced St. John's Wort (SJW) product standardized by hyperforin content [US Patent]. Aphios utilized its patented SuperFluids™ fractionation and manufacturing  technologies to develop Xantol™.

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

nanoHYP St.-Johns-Wort-FlowersSJW (Hypericum perforatum) is an over-the-counter herbal remedy often self-prescribed for the treatment of depression, anxiety and sleep disorders. It has comparable efficacy to selective serotonin re-uptake inhibitors (SSRIs) for the treatment of mild to moderate depression.

SJW 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 SJW's reputation as an effective antidepressant.

SJW extracts are sold in pharmacies throughout Europe and they are in fact among the most popular OTC "phytomedicines" sold in EEC countries. Among the most widely prescribed antidepressants in the United States are Prozac® from Eli Lilly, Zoloft® from Pfizer and Paxil® from GlaxoSmithKline. Worldwide sales of the top-selling antidepressants are approximately $4.8 billion. As people experience adverse side effects from prescription antidepressants, there has been a concomitant rise in the use of SJW and other herbs as natural antidepressants. Several herbal formulations, purporting to be natural substitutes for Prozac®, are already being marketed.

An Effective Serotonin Re-Uptake Inhibitor

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

Xantol Serotonin-Re-Uptake-Inhibition-of-Hyperforin smXantol™ has been shown in in vitro serotonin re-uptake 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, with permeability perhaps 5 to 6 times higher than metoprolol, which is recommended as the "high permeability" internal standard by the Food and Drug Administration (FDA) in the Biopharmaceutics Classification System (BCS) guidance. Xantol™ will be most likely classified as BCS 2, high permeability and low solubility, by the FDA.

Xantol™ - A Standardized, Stabilized Formulation of SRI Hyperforin

Xantol Xantol-CapsulesXantol™, an enhanced St. John's Wort botanical drug for mild to moderate depression, is standardized by the serotonin re-uptake inhibitor hyperforin, which is the active pharmaceutical ingredient of St. John's Wort.

Xantol™ is formulated with natural antioxidants and emulsifiers and it is encapsulated in clear gel capsules that are purged with nitrogen to minimize oxygen and enhance stability. The capsules are contained in opaque bottles or blister packs to minimize light intrusion and improve shelf life.


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