氢溴酸东莨菪碱温敏型鼻用原位凝胶的制备  

Preparation of temperature-sensitive nasal in situ gel of scopolamine hydrobromide

作　　者：李美燕[1] 林於[1] 欧阳雪[1] 郑欣[1] 

机构地区：[1]重庆医科大学,重庆400016

出　　处：《中成药》2015年第3期517-521,共5页Chinese Traditional Patent Medicine

摘　　要：目的制备氢溴酸东莨菪碱的温敏型鼻用原位凝胶。方法用不同质量浓度和配比的壳聚糖、β-甘油磷酸钠制备不同pH的原位凝胶,并测定其凝胶化时间、黏度变化情况与载药凝胶的累积释放度。结果质量浓度为2%的壳聚糖和56%的β-甘油磷酸钠体积比为6∶1,pH 7.1时原位凝胶黏度达到5 Pa·s,初始凝胶温度为34℃,随着温度的升高、壳聚糖质量浓度的增加、β-甘油磷酸钠含量的增加、pH升高(由6.5升至7.2),凝胶化时间减少;以氢溴酸东莨菪碱为模型药物,载药凝胶中药物10h累积释放度为71%,释放曲线符合一级动力学方程。结论壳聚糖/β-甘油磷酸钠制备的氢溴酸东莨菪碱温敏型原位凝胶对药物具有缓释作用,适合制成鼻用制剂。AIM To prepare temperature-sensitive nasal in situ gel containing scopolamine hydrobromide.METHODS In situ gel containing different mass concentration ratios of chitosan and β-glycerophosphate were prepared under the condition of different pH values,and their gelation time,viscosity changes and the cumulative release were measured.RESULTS The in situ gel viscosity reached 5 Pa · s in the condition with pH valued7.1,and volume ratio of 2% chitosan and 56% β-glycerophosphate reached 6 ∶ 1.Meanwhile,the gelation time after its initial gelation at 34 ℃ in the previously mentioned condition tended to be shorter with the temperature elevation,and increasement in mass concentration of chitosan,content of β-glycerophosphate and p H value rising from 6.5 to 7.2.When scopolamine hydrobromide as model drug was loaded to temperature-sensitive gel,its cumulative release amounted to 71% in 10h,and the release curve was in conformity to the first-order kinetic equation.CONCLUSION Temperature-sensitive in situ gel containing scopolamine hydrobromide,formed by chitosan andβ-glycerophosphate,shows sustained-release effect and therefore is suitable for the preparation of nasal formulation.

关 键 词：壳聚糖 β-甘油磷酸钠 温敏型凝胶 氢溴酸东莨菪碱 缓释 

分 类 号：R944[医药卫生—药剂学]