摘要
目的研究壳聚糖/羧甲基壳聚糖/甘油磷酸钠（CS/CMCS/GPS）体系水凝胶的温敏性,载药凝胶以及共混β-环糊精（β-CD）包合物对药物的缓释性能。方法试管倒置法研究不同配比,不同pH值对CS/CMCS/GPS体系温敏凝胶化性能的影响;饱和水溶液法制备吲哚美辛/β-CD包合物,红外光谱表征包合物;紫外分光光度法测定包合物载药量和药物的累积释放度。结果 2%CS-2%CMCS-56%GPS体积比从10∶1∶2变为10∶10∶2（体系pH6.8）,37℃下凝胶化时间由370s升至490s,后又降至90s;三者体积比从10∶3∶1变为10∶3∶6（体系pH6.8）,37℃下凝胶化时间从407s降至66s。pH值在6.8~7.2范围适合于体系凝胶化。调节体积比及合适的pH值,在37℃下可实现CS/CMCS/GPS体系快速凝胶化。以吲哚美辛和吲哚美辛/β-CD包合物为模型药物,载有吲哚美辛温敏凝胶12h的累积释放度为65.2%,载有吲哚美辛/β-CD包合物温敏凝胶累积释放度为52.8%,而吲哚美辛原药12h的累积释放度为87.6%,吲哚美辛/β-CD包合物的累积释放度为82.1%。结论一定体积配比CS/CMCS/GPS体系在37℃具有快速凝胶特性,β-CD包合物与温敏性凝胶共混,对药物具有更加明显的缓释作用。
OBJECTIVE To investigate temperature sensitivity of chitosan（CS）/carboxymethylchitosan（CMCS）/ glycerphosphate（GPS） hydrogel and study drug release profile of CS/CMCS/GPS hydrogel loading indomethacin and indomethacin/β-cyclodextrin inclusion complex. METHODS Using the method of inversion of test tube, temperature sensitivity of CS/CMCS/GPS hydrogel was studied under different ratio of CS and CMCS and GPS at various pH of the mixture solutions. β-cyclodextrin inclusion complex of indomethacin was prepared and characterized by IR. Drug loading and cumulative release of drug was detected by ultraviolet spectrophotometry. RESULTS The gelation time （GT） of CS/CMCS/GPS hydrogel was first increased from 370 s to 490 s and then decreased to 90 s at the considition of 37 ℃ and pH 6.8 when the ratio in volume of 2%CS-2%CMCS-56% GPS from 10 ∶ 1 ∶ 2 to 10 ∶ 10 ∶ 2. The GT was within 66-407 s when the volume ratio of CS-CMCS-GPS was from 10 ∶ 3 ∶ 1 to 10 ∶ 3 ∶ 6. The suitable pH to gelate for CS/CMCS/GPS system was at 6.8-7.2. This system could rapidly be gelated at 37 ℃ under the appropriate volume ratio of CS/CMCS/GPS and pH. The in vitro dissolution showed that the cumulative release at 12 h of thermosensitive CS/CMCS/GPS gel loading indomethacin or indomethacin/β-cyclodextrin inclusion complexes was 65.2% and 52.8%, respectively, which was significantly lower than that of raw indomethacin for 87.6% and inclusion compound of indomethacin for 82.1%. CONCLUSION CS/CMCS/GPS system with appropriate the volume ratio and pH can be gelable fastly at 37 ℃ . Thermosensitive gel incorporating β-CD inclusion compound of drug showed more significant sustained release, and can be a good potential drug carrier for temperature sensitive and sustained drug delivery system.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2010年第7期626-630,共5页
Chinese Journal of Modern Applied Pharmacy
基金
福建省自然科学基金计划资助项目(C0710026)
关键词
壳聚糖
温敏性
吲哚美辛
Β-环糊精
缓释
chitosan
thermosensitive
indomethacin
β-cyclodextrin
sustained release
