Preformulation study on anti-smallpox drug tecovirimat
Author(s):LI Xiao-xi, SHAO Shuai, YANG Mei-yan, GAO Chun-sheng, ZHONG Wu, Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences Pages:557-561 Year:2016
Issue:3 Journal:International Journal of Pharmaceutical Research Keyword:tecovirimat; study preformulation; crystal characterization; solubility; permeability; Abstract:Objective To study the preformulation properties of tecovirimat for formulation design. Methods The appearance,crystal structure,solubility and permeability of the drug were investigated. The UV method was established to determine the content of tecovirimat in vitro. The solubilization experiment was also conducted. Results Tecovirimat is white and odorless powder with crystalline hydrate structure and low water-solubility with high permeability. The morphology of tecovirimat is six-prismatic-shape. The linearity range of established UV method was 4.14-24.83 μg/ml(r=0.9996). The 1∶1 soluble complex was formed with tecovirimat and hydroxypropyl-β-cyclodextrin. Conclusion Tecovirimat is poorly water-soluble drug with high permeability and the established method could be used to determine the content of the drug. Hydroxypropyl-β-cyclodextrin could be used for the solubilization of tecovirimat.