摘要
目的系统考察药物、载体和附加剂的性质对泊洛沙姆溶液体系胶凝行为的影响,为眼用温敏型原位凝胶的处方设计提供参考。方法以搅拌子法测定相变温度,流变仪分析温度变化对体系凝胶黏度的影响,分别考察泊洛沙姆配比、黏附性材料、药物及其载体、以及常用附加剂对体系胶凝行为特征的影响。结果黏附性材料甲基纤维素和壳聚糖使凝胶相变温度升高,羟丙甲纤维素和海藻酸钠的作用则相反;枸杞多糖能升高凝胶相变温度;枸杞籽油微乳和黄芩苷纳米结晶也会提高体系相变温度和黏度;但槐定碱、抑菌剂苯扎氯铵和pH调节剂(硼酸-硼砂缓冲对)却无明显影响;渗透压调节剂氯化钠和甘露醇降低了相变温度的同时能增加黏度值。结论通过选择改变泊洛沙姆溶液的胶束数量和状态影响眼用温敏型原位凝胶体系的胶凝行为可使药物较长时间滞留在眼部并缓慢释放。
AIM To design ophthalmic thermosensitive in situ gel formulation by a systematic study on influences of different drugs,carriers,and additives to gelation behavior of poloxamer solution. METHOD Phase transition temperature was determined by stirring method,and the effect of temperature on system viscosity change was analyzed by the rheometry. The influence of poloxamer ratio,adhesive materials,drugs,carriers and other additives on phase transition temperature and behavior were studied. RESULTS Difference in performance was noticed by variant adhesion materials-methyl cellulose and chitosan increased the phase transition temperature,but hydroxypropyl methyl cellulose and sodium alginate held the converse situation. Wolfberry seed oil microemulsion and baicalin nanocrystalline increased both viscosity and phase transition temperature of the system. Lycium barbarum polysaccharides only raised the phase transition temperature. Sophoridine,benzalkonium chloride and the pH adjusting agents（ boracic acid-borax buffer） had little effect. The osmotic pressure regulator,sodium or mannitol,decreased the phase transition temperature but increased the viscosity. CONCLUSION The numbers and the micelles status of poloxamers can influence the gelation behavior of ophthalmic thermosensitive in situ gels,and an optimized scheme can prolong the ophthalmic drug retention time and slow its release.
出处
《中成药》
CAS
CSCD
北大核心
2014年第7期1397-1401,共5页
Chinese Traditional Patent Medicine
基金
2011年宁夏自然科学基金项目(NZ11103)
2012宁夏自然科学基金项目(NZ1226)
关键词
眼用原位凝胶
温敏型
胶凝行为
药物载体
附加剂
ophthalmic in situ gel
thermosensitive
gelation behavior carriers
additives
