目的 开发与格列美脲片体内溶出行为相关的体外溶出方法,并预测两种片剂的人体生物等效性.方法 采用GastroPlusTM软件建立格列美脲片人体药代动力学(PK)模型;基于模型预测原研片剂在人体中的溶出行为;以预测结果指导体外溶出方法开发;通过虚拟生物等效性试验,利用体外溶出数据预测B、C两种格列美脲片的人体生物等效性(BE)结果;利用比格犬BE进行佐证.结果 模型的准确性与可靠性良好;原研片剂在人体胃肠道中呈线性溶出,于2h时溶出完全;流通池开环模式(pH 7.0缓冲液,14 mL·min-1)可基本模拟格列美脲片在人体中的溶出行为;经虚拟生物等效性试验,预测B与原研片剂生物等效,而C与其不等效;比格犬BE试验结果与人体虚拟BE结果一致.结论 基于体外溶出数据,预测格列美脲片人体生物等效性的方法具有一定可行性.
Object A systematic study on the chemical constituents ofFuscoporia oblique Fr. Te. LáT was carried out. Methods The constituents were isolated on silica gel column chromatography, identified by physico-chemical properties and structurally elucidated by spectral analysis (MS, 1H，13CNMR and IR). Results 9 compounds were identified, namely fuscoporine (Ⅰ), lanosterol (Ⅱ), 3β-hydroxy-lanosta-8, 24-diene-21-al (Ⅲ), 3β, 21-dihydroxy-lanosta-8, 24-diene (Ⅳ), 3β-hydroxy-lanosta-8, 24-diene-21-acid (Ⅴ), 3β, 22R-dihydroxy-lanosta-8, 24-diene (Ⅵ), ergosterol peroxide (Ⅶ), analog of sphingin (Ⅷ) and mannitol(Ⅸ). Conclusion Compound I is a new pigment and named as fuscoporine.
从云衫针层孔菌Phellinus yamanoi(Tamz.)shaw分离得到12个化合物,借助光谱分析鉴定为:8,11,13-abietadien-18-oic acid(1),1,2-benzenedi-carboxylic acid bis(2-ethylhexyl )ester (2) ,ergosterol peroxide(3) ,ergosta 7,22 (E)-dien-3-ol (4), ergosta 7,22 (Z)-dien-3- ol (5), octadecanoic acid- 1,3-propanediyl ester (6), octadecanoic acid ( 7), 8 ( 19), 14-1abdadien-13-ol(8),ergosta-4,6,8(14),22-tetraen-3-one(9),化合物(10)为鞘氨醇类似物以及mannitol(11)和D-mannose(12).
