抗天花病毒药物特考韦瑞处方前研究

目的：对特考韦瑞进行处方前研究，为设计制剂处方奠定基础。方法对特考韦瑞的外观、晶体、溶解性、渗透性进行考察，采用紫外分光光度法建立了特考韦瑞的体外含量测定方法，并进行了初步增溶实验。结果特考韦瑞为含结晶水的白色粉末，无臭味，具有六棱形晶体结构，难溶于水，渗透性高。含量测定方法在4.14~24.83μg/ml范围内有良好线性关系（r=0.9996）。特考韦瑞可与羟丙基β环糊精形成摩尔比为1∶1的可溶性包合物，温度升高有利于包合反应进行。结论特考韦瑞为低溶解性高渗透性的BCSⅡ类药物，建立的方法准确可靠。羟丙基β环糊精为较理想的增溶剂。

Preformulation study on anti-smallpox drug tecovirimat

[Abstact] Objective To study the preformulation properties of tecovirimat for formulation design. Methods The appear?ance,crystal structure,solubility and permeability of the drug were investigated. The UV method was established to determine the con?tent 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 4.14-24.83μg/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 meth?od could be used to determine the content of the drug. Hydroxypropyl-β-cyclodextrin could be used for the solubilization of tecovirimat.