本文選題：氯雷他定 + 透明質(zhì)酸�。� 參考：《中國醫(yī)院藥學(xué)雜志》2016年15期

【摘要】：目的:制備氯雷他定(LOR)透明質(zhì)酸(HA)微囊和微球,并對其進(jìn)行體外評價。方法:HA和聚乙二醇6000(PEG6000)為材料,以粒徑,載藥量,載藥率,溶解度,體外累積釋放度來評價載藥微囊和微球;利用DSC和XRD考察載藥微囊和微球中LOR的晶型變化。結(jié)果:HA、PEG6000和LOR的比例為16∶1∶2時,LOR的溶解度和溶出效果最佳。LOR微囊的水中溶解度為(23.12±0.15)μg·mL~(-1),載藥量為(8.07±0.44)%,載藥率為(76.69±0.44)%,體外累積釋放度達(dá)到(87.00±3.34)%;LOR微球的水中溶解度為(5.58±0.15)μg·mL~(-1),載藥量為(11.87±0.46)%,載藥率為(112.78±0.46)%,體外累積釋放度達(dá)到(63.16±0.63)%。晶型變化分析結(jié)果,微囊中LOR大部分以無定型狀態(tài)存在,小部分以結(jié)晶狀態(tài)存在;微球中LOR以無定型狀態(tài)存在。結(jié)論:采用噴霧干燥法成功制備LOR-HA微囊和微球,顯著改善LOR的溶解度和體外釋放度的,利用此方法制備微囊(或微球)成本較低、操作簡單,易于實(shí)現(xiàn)大規(guī)模工業(yè)化生產(chǎn)。
[Abstract]:Aim: to prepare and evaluate hyaluronic acid (HA) microcapsules and microspheres of loratadine. Methods the microcapsules and microspheres were evaluated by particle size, drug loading, drug loading rate, solubility and cumulative release in vitro, and the crystal types of LOR in drug loaded microcapsules and microspheres were investigated by DSC and XRD. Results at 16:1:2, the solubility and dissolution of LOR were the best. The solubility of LOR microcapsules was 23.12 鹵0.15) 渭 g / ml, the drug loading was 8.07 鹵0.44 渭 g / L, the drug loading rate was 76.69 鹵0.444.The cumulative release degree in vitro was 87.00 鹵3.34) 渭 g / mL / L ~ (-1), and the solubility of LOR microspheres was 5.58 鹵0.15) 渭 g / mL / L ~ (-1). The drug loading rate was 112.78 鹵0.46 and the cumulative release in vitro was 63.16 鹵0.63. The results showed that most of LOR in microcapsules existed in amorphous state and a small part in crystalline state, while in microspheres LOR existed in amorphous state. Conclusion: LOR-HA microcapsules and microspheres were successfully prepared by spray drying method, and the solubility and in vitro release of LOR were significantly improved. The preparation of LOR-HA microcapsules (or microspheres) by this method was relatively low in cost, easy to operate and easy to realize large-scale industrial production.
【作者單位】： 延邊大學(xué)藥學(xué)院;
【分類號】：R943

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本文編號：1985436