Control over Polymorph Formation of Polydatin in Binary Solvent System and Structural Characterization

Ningbo Gong; Xue Wang; Ying Wang; Shiying Yang; Junke Song; Yang Lu; Guanhua Du

doi:10.1016/j.jpba.2020.113260

Control over Polymorph Formation of Polydatin in Binary Solvent System and Structural Characterization

J Pharm Biomed Anal. 2020 Oct 25:190:113260. doi: 10.1016/j.jpba.2020.113260. Epub 2020 Mar 17.

Authors

Ningbo Gong¹, Xue Wang¹, Ying Wang¹, Shiying Yang¹, Junke Song², Yang Lu³, Guanhua Du⁴

Affiliations

¹ Beijing Key Laboratory of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
² Beijing City Key Laboratory of Drug Target Identification and Drug Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College. Beijing, 100050, China.
³ Beijing Key Laboratory of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China. Electronic address: luy@imm.ac.cn.
⁴ Beijing City Key Laboratory of Drug Target Identification and Drug Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College. Beijing, 100050, China. Electronic address: dugh@imm.ac.cn.

PMID: 32846398
DOI: 10.1016/j.jpba.2020.113260

Abstract

Polydatin is a natural product used for anti-oxidant, anti-inflammatory and anti-tumor purposes, and often added in medicine, nutraceutical, cosmetics, and dietary supplement. Polymorphism is a key feature of solid-state pharmaceutical products. Polymorphic modifications may exhibit different physical and chemical properties. Here we report two different polymorphs, and the amorphous form of Polydatin. Polymorphs were prepared in binary solvent system. The crystal structures of the two forms were revealed for the first time. The structure and 3D packing were determined with single crystal X-ray diffraction analysis. The batch consistency and stability were identified with Powder X-ray diffraction analysis. Various functional groups present in the polymorphs were analyzed with fourier transform infrared spectroscopic method. The thermal properties were investigated with DSC and TGA. HPLC-MS was used for the pharmacokinetic study. Results show that form B has the faster absorption, and can be maintained in animal bodies for a longer time than form A.

Keywords: Characterization; Pharmacokinetic study; Polydatin; Polymorphism; X-ray diffractometry.

MeSH terms

Calorimetry, Differential Scanning
Crystallization
Crystallography, X-Ray
Glucosides*
Solvents*
Spectroscopy, Fourier Transform Infrared
Stilbenes*
X-Ray Diffraction

Substances

Glucosides
Solvents
Stilbenes
polydatin