The Synthesis Of Diosgenin Solvates And Their Influence Factors

Polymorphic drugs are refered to the active pharmaceutical ingredient(API) of the solid drugs exiting in a specific crystalline state. Different physicochemical property of polymorphism can cause the difference of solubility, dissolution rate, bioavailability. More and more people are concerned about the polymorphic drug because of its advantages on pharmaceutics.This article choose steroid hormone drug Diosgenin as API to synthesis novel polymorphic drug. Three sovaltes and three hydrates of Diosgenin were be synthesized. One of them is powder state and others are crystalline state. The six polymorphic drugs have been thoroughly characterized by single crystal X-ray diffraction, powder X-ray diffraction, Fourier transform infrared spectroscopy, thermogravimetry. More importantly, three controlling factors including initial concentration, water volume fraction, and solvent have been investigated in the crystallization of diosgenin polymorphs have been reported. The crystallization experiments in ethanol displays that as the initial concentration increases, polymorph 4, 7, and 6 appear in order and with the increase of water content polymorph 7, 4, 9, and 5 are obtained correspondingly. When acetone is used as solvent, polymorph 8 was synthesized.In conclusion, polymorphic drugs have broad applications in pharmaceutical. It can help people to find the most suitable polymorph by exploring the synthesis conditions and controlling the transformation.