Crystal habit, characterization and pharmacological activity of various crystal forms of arteether

Acta Pharmaceutica Sinica B

Geeta Shukla¹  Renu Chadha²  Sushma Gupta² 

[1] Department of Microbiology, Panjab University, Chandigarh 160014, India;Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India;

关键词: Arteether;    Polymorphism;    Solubility;    Antimalarial activity;   

DOI  :  10.1016/j.apsb.2011.06.010

来源: DOAJ

【 摘 要 】

The aim of this study was to investigate and characterize different crystal forms of arteether, a rapidly acting, highly potent antimalarial drug for the treatment of acute Plasmodium falciparum malaria. Six different crystal forms were prepared utilizing various polar and non-polar solvents. Scanning electron microscopy (SEM) revealed differences in the surface characteristics of the six forms from those of a commercial sample. Differential scanning calorimetry (DSC) revealed the absence of a desolvation endotherm indicating that the forms were neither hydrates nor solvates. Powder X-ray diffraction (PXRD) patterns of the forms showed much weaker major peaks than in the commercial sample indicating them to be less crystalline. Solubility and dissolution studies showed that the most amorphous form was the most soluble and possessed the highest antimalarial activity.

【 授权许可】

Unknown