Friday, December 17, 2010

Potratz on SHR: Grape Fruit Oil for Enhanced Oral Steroid Resorption

Just for those of you who are not yet addicted to the Super Human Channel, i.e. Carl Lenore's radio program on exercise, nutrition and longevity: Wednesday, 15 December 2010, Carl had Eric Potratz from Primordial Performance on the show and talked to him about what could be the future of oral drug/steroid delivery. Although the show certainly smacks of a product pimpjob, the general information Potratz provides is scientifically correct.

Audio 1: Super Human Radio - 631 - Oral Hormone Delivery And Bioavailability
Potratz main argument that grape fruit blocks the intestinal esterase, i.e. the removing of the ester attached to a steroid to render it absorbable via the lymphatic system, has been confirmed in several studies. More recently, Li et. al. (Li. 2009) reported:
[..]oral coadministration of GFJ [Grape Fruit Juice] or an esterase inhibitor, bis-(p-nitrophenylphosphate), with the prodrugs led to respective increases in plasma area under the curve by 70% or 57% for enalaprilat and 279% or 141% for lovastatin acid. In addition, portal vein-cannulated rats pretreated with GFJ at –15 and –2 h before lovastatin administration (10 mg/kg p.o.) as a solution, 1) in water and 2) in GFJ, showed, respectively, a 49% increase (CYP3A-inhibited) and a 116% increase (both CYP3A and gut esterase-inhibited) in the portal plasma exposure to the active acid, compared with a non-GFJ pretreatment group. Overall, along with the CYP3A inactivation by GFJ, the decreased esterase activity also played a significant role in increasing the metabolic stability and permeability of esters leading to enhancement of exposure to the active drugs in rats.
Yet, obviously, the claims Potratz makes on a 15x-20x enhanced bioavailability of the "new" esterified designer-prohormones of the Andro Series still have to be confirmed by independent testing. Also, his claim that the specific oil (from the rind of the grape fruit) Primordial will be using is much more potent than the juice itself, seems logical, but has - to my knowledge - not been scientifically investigated, yet. What certainly is false, however, is Carl's ad-hoc calculation of a compound exhibiting a oral bioavailability of 2% suddenly having one of 60%-70% - probably his personal excitement that made him miscalculate ;-)