枸橼酸坦度螺酮口腔速溶膜的制备与质量评价
Preparation and Quality Evaluation of Tandospirone Citrate Orodispersible Films
刘圆圆 1杜欢欢 2尹民 2施斌 2贺敦伟3
作者信息
- 1. 中国海洋大学医药学院,山东青岛 266003
- 2. 则正(上海)生物科技有限公司,上海 201807
- 3. 中国海洋大学医药学院,山东青岛 266003;则正(上海)生物科技有限公司,上海 201807
- 折叠
摘要
采用溶剂浇铸法制备枸橼酸坦度螺酮口腔速溶膜(ODFs).通过单因素试验筛选了成膜材料、掩味剂和增塑剂,确定优化处方为:10.8％的枸橼酸坦度螺酮、37.5％的HPMC E5、7.5％的羟丙纤维素、27.0％的羟丙基倍他环糊精、15％的甘油和2.2％的三氯蔗糖.所得ODFs成膜性好,崩解时间约40 s,含量均匀度和有关物质符合规定,15 min时水中的溶出率超过85％,与市售片剂的溶出行为相似.基于羟丙基倍他环糊精的包合作用,药物的掩味效果较好.在光照、高温和高湿条件下进行ODFs的稳定性试验.结果显示,除60 ℃高温条件外,ODFs在其他条件下稳定性良好,外观、含量和有关物质未发生显著变化.在40℃、相对湿度75％条件下放置1个月,ODFs中的药物晶型保持稳定.
Abstract
The orodispersible films(ODFs)of tandospirone citrate were prepared by solvent casting method.The film-forming materials,taste masking agent and plasticizer were screened and optimized by single factor tests.The optimal formulation was as follows:10.8％of tandospirone citrate,37.5％of HPMC E5,7.5％of hydroxypropyl cellulose,27.0％of hydroxypropyl-β-cyclodextrin,15％of glycerin,and 2.2％of sucralose.The obtained ODFs had good film properties with a disintegration time of about 40 s.The requirements for content uniformity and related substances were met.The dissolution rate in water at 15 min exceeded 85％,which was similar to that of the commercially available tablets.The bitterness of the drug was well masked on the basis of the inclusion effect of hydroxypropyl-β-cyclodextrin.The stability tests were conducted under photolysis,high temperature,and high humidity conditions.The results showed that the ODFs had good stability except for high temperature at 60 ℃.The appearance,drug content and related substances of the ODFs stored under other conditions had not significantly changed.After being stored for one month under accelerated test condition(40 ℃ and 75％of relative humidity),the API crystal form remained stable.
关键词
枸橼酸坦度螺酮/口腔速溶膜/掩味/溶剂浇铸法/体外溶出/稳定性Key words
tandospirone citrate/orodispersible film/taste masking/solvent casting method/in vitro dissolution/stability引用本文复制引用
出版年
2024
NETL
NSTL
万方数据