利培酮口溶膜的制备及体内外评价

发布时间：2018-08-24 13:16

【摘要】：首先测定了国外市售利培酮口溶膜和国内市售口崩片在不同溶出介质中的溶出曲线,结果在水中具有较大的区分力,因而用水作为溶出介质测定溶出曲线并结合溶化时间和物理性能进行处方筛选,制备了利培酮口溶膜。结果表明,自制口溶膜在4种不同pH值的溶出介质中1 min均溶出80%以上,2 min内溶出完全,与国外市售口溶膜的体外溶出行为基本一致。差示扫描量热(DSC)和X射线衍射(XRD)研究结果显示,利培酮以无定形态分散于载体材料中。Beagle犬体内药动学试验结果表明,自制口溶膜与国外市售口溶膜具有相似的药代动力学行为;自制口溶膜的相对生物利用度以利培酮计为(109.1±9.5)%、以活性代谢物9-羟基利培酮计为(102.0±17.3)%。
[Abstract]:The dissolution curves of risperidone film sold abroad and domestic risperidone tablets in different dissolution media were determined. Therefore, the risperidone oral dissolution film was prepared by determining the dissolution curve with water as the dissolution medium and combining with the dissolution time and physical properties. The results showed that the membrane was completely dissolved in more than 80% of the 1 min in 4 kinds of dissolving media with different pH values in 2 min, which was basically consistent with the in vitro dissolution behavior of the film sold in foreign markets. The results of differential scanning calorimetry (DSC) and X-ray diffraction (XRD) showed that risperidone was dispersed in the carrier material in an amorphous form. The pharmacokinetics of risperidone was similar to that of the foreign market. The relative bioavailability of the membrane was (109.1 卤9.5) and (102.0 卤17.3), respectively, and that of the active metabolite, 9-hydroxyrisperidone, was (102.0 卤17.3).
【作者单位】：中国医药工业研究总院药物制剂国家工程研究中心;山东省注射用微粒给药新技术重点实验室;
【基金】：国家“重大新药创制”科技重大专项(2013ZX09301302-001-002) 上海市科委研发平台专项(15DZ2290600)
【分类号】：R943

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