目的研制银杏叶总黄酮的自微乳化口腔速溶膜,并考察其体外性质。方法采用溶解度法和伪三元相图法筛选确定银杏叶总黄酮自微乳化给药系统处方;在此基础上,以成膜性和体外崩解时间为指标筛选固体载体,制备能在口腔中迅速自微乳化的固体膜剂。考察其自微乳化性能、崩解时间、体外释放度等体外性质,采用差示扫描量热法和扫描电子显微镜表征药物晶型和膜的表面形态。结果光子相关光谱法测得本制剂微乳液的平均粒径为(48.1±5.45)nm,与银杏叶总黄酮自微乳化给药系统的微乳粒径无差异;崩解时间为(9.94±0.26)s;体外释放度在5 min时即可达到(70.98±0.31)%,显著快于市售片。结论银杏叶总黄酮自微乳化口腔速溶膜结合了自微乳化给药系统和口腔速溶膜的双重优点,是具有应用前景的新剂型。

To prepare the total ginkgo flavonoid (TGF) self-microemulsifying oral fast dissolving films (SMEOFDF) and evaluate its in vitro properties. Methods The formulation of TGF self-microemulsifying drug delivery system (SMEDDS) was optimized based on the solubility method and the pseudo-ternary phase diagram, and then the influence of formulation on disintegration time and film forming property were observed by single factor test. Microemulsified performance, disintegration time, content uniformity, and release profiles in vitro were investigated. The surface feature of TGF SMEOFDF was detected by scanning electron microscope and the crystal form of drug was characterized by differential scanning calorimetry. Results The average particle size was (48.1 ± 5.45) nm with non-difference from SMEDDS. The average time to disintegrating was (9.94 ± 0.26) s and the releasing drug at 5 min of TGF SMEOFDF was (70.98 ± 0.31)% in vitro. Conclusion SMEOFDF which has both advantages of SMEDDS and fast dissolving oral films is a new dosage form with profound application prospect.

重庆市自然科学基金项目(CSTC2009BB5106);中央高校基本科研业务费专项资金资助(XDJK2009C076);西南大学博士基金项目(SWUB2008032);重庆市卫生局中医药科技项目(2010-2-135)