ACTIVE SUBSTANCE CONTENTS-TRIBULUS TERRESTRIS Tribulus terrestris ext.compound is a non-hormonal complex. Its active components are saponins of furastanol type, standardized on the basis of predominating compound, prododioscine. The structural formula of prododioscine is (2:1), 26-0-beta-1-glucopiranosil, 22-hydroxyfurost-5-en-3-beta, 26-diol, 3-0-beta diglucoramnoside. The substance is yellow-brown amorphous powder with specific aroma and bitter taste, soluble in water, sparingly soluble in methyl alcohol and insoluble in chloroform. PROPERTIES OF THE PREPRATION Pharmacological Effect, Mode of Action Tribulus terrestris Tribulus terrestris enhance endogenous testosterone levels through the increase in luteinizing hormone (LH), a gonad stimulating hormone produced by the anterior pituitary gland. Tribulus terrestris in recommended dose leads to elevate testosterone levels within approximately 60 minutes after dosing. Tribulus peak levels are achieved in 3 to 4 hours post dosing. Clinical studies have shown that tribulus terrestric increase endogenous testosterone production levels by 30% or more then five days. Tribulus terrestris improves the spermatogenesis and increases the number of spermatogonia, spermatocytes and spermatids in the testes without producing any effect on the diameter of semeniferous tubules. Regular use of tribulus terrestris result in an intensification of spermatogenesis, improve the sperm quality. It enhances the sperm motility and percentage of actively mobile spermatozoa and prolongs sperm viability. Hypothesis of the central effects of tribulus in lead by the elevated LH levels. It may realize its effects by being metabolized into androgen-like metabolites or stimulating the physiological transformation of testosterone into dehydrotestosterone (DHT). Tribulus terrestris may exert a direct action on the hypothalamus and other superior brain structure that regulate the ganadotrophic releasing factors. An important feature of pharmacodynamics of tribulus is the regulation of the body’s hormonal balance without any interference with its functional mechanism. PHAMACOKINETICS Absorption, Distribution, Metabolism & Elimination
The active substance of protodioscine is shown to be rapidly eliminated from the plasma, since its concentration is almost insignificant after180 minutes. The clinical test revealed the 24 hours excretion of active substances show after 12-24 % of compound is being excreted with the bile, whereas urinary excretion is about 6-7 % for 50-200mg/kg body mass as single intravenous dose administration. Following oral administration of similar doses, quantity of prododioscine being excreted through bile range from 2-5 % in 24 hours. Following the oral administration, no measurable concentration of any unaltered protodioscine was found in urine after 24 hours. The experimental studies suggest that the hepatic route is the preferred route of unchanged protodioscine. The rapid elimination of protodioscine, the active content of tribulus terrestris and the lower percentage of unchanged protodioscine in relation to the doses reveals the intensive biotransformation of protodioscine within the body.