Development and Study of an Extemporaneous Form of 20-Hydroxyecdysone

In this research, we develop and study an extemporaneous (main) form of 20-hydroxyecdysone, along with drafting of prescription forms. Preclinical studies were conducted using 20-hydroxyecdysone and its extemporaneous form. The latter proved its harmlessness (the drug belongs to class VI of relatively harmless substances according to Hodge and to class V of toxicity in accordance with GOST 32644-2014) and efficacy in a model of experimental hyperglycemia. The developed extemporaneous form of 20-hydroxyecdysone was studied in the form of a nanostructured clathrate complex with arabinogalactan with improved pharmaceutical and pharmacological properties. The nanostructured clathrate complex of 20-hydroxyecdysone with arabinogalactan at a mass ratio of 1:10 was obtained as a finely-dispersed white powder with a light-yellow tint and the average particle size of 35.3 nm. In terms of bioavailability, the extemporaneous form of 20-hydroxyecdysone exceeds the similar value of the original compound by 1.91 times. 20-hydroxyecdysone is involved in the phosphatidylinositol-3-kinase signaling pathway of activation of serine-threonine protein kinase B. In the activated form, this kinase phosphorylates various protein substrates in the cytosol, thereby modulating their functions and playing a central role in various cellular processes. The extemporaneous form of 20-hydroxyecdysone allows its dose to be reduced, thus ensuring high compliance with the drug. Low doses of the drug minimize the probability of side effects and their rapid elimination in case of their emergence. Instructions for the medical use of the developed extemporaneous form of 20-hydroxyecdysone are provided, and prescription forms are developed. Based on the results obtained, the extemporaneous form of 20-hydroxyecdysone can be recommended for use as independent therapy or in combination with other metabolic agents. The established physiological efficacy and safety render the developed extemporaneous form of 20-hydroxyecdysone a metabolic agent for practical use.