壳聚糖交联微球的制备

发布时间：2019-05-27 11:38

【摘要】：微球剂型是目前制剂研究的重点方向之一。微球可以降低药物的降解速率,提高药物的稳定性。单一交联剂制备的微球具有良好的缓释性,但其不能实现有效的控释。本文采用京尼平与香草醛复配交联制备5-氟尿嘧啶载药微球,通过调节交联剂的比例控制微球的释放速度。本课题首先通过对单一交联剂制备微球的条件进行筛选。在该条件的基础上,确定了复配交联剂制备微球的最佳条件,最后加入5-氟尿嘧啶制备载药微球,利用HPLC测定载药微球的最高载药量为2.97%,包封率为20.27%。通过SEM图谱表征,制备的微球分散性良好,粒径分布均匀,粒径范围为10-20μm左右;FT-IR图谱结果显示,京尼平和香草醛均与壳聚糖交联;溶胀性能结果显示,不同复配比例交联剂制备的微球溶胀率不同,证明不同复配比例交联剂制备的微球具有不同的释放速率;XRD图谱结果显示,微球成功交联;DSC-TGA图谱证实了5-氟尿嘧啶在微球内部,并提高了5-氟尿嘧啶的稳定性。参考已有的国家标准,研究了5-氟尿嘧啶载药微球的释放性能,在pH=3.6缓冲溶液中,微球在24 h内最高累积释放率为97.2%,在pH=7.4缓冲溶液中,微球在24h内最高累积释放率为94.2%。因此,通过控制交联剂复配比例可以达到控制释放速率的效果。在高温、高光和高湿条件下对微球的稳定性进行了研究,证明5-氟尿嘧啶微球的稳定性良好。
[Abstract]:Microsphere dosage form is one of the key directions of the present preparation. The microspheres can reduce the degradation rate of the medicine and improve the stability of the medicine. The microspheres prepared by the single cross-linking agent have good slow-release property, but can not realize effective controlled release. In this paper,5-fluorouramide drug-loaded microspheres were prepared by cross-linking of Beijing-Niping and vanillin, and the release rate of the microspheres was controlled by adjusting the cross-linking agent. In this paper, the conditions of the preparation of microspheres by a single cross-linking agent are selected. On the basis of this condition, the optimal conditions for preparing the microspheres by the compound cross-linking agent were determined, and the drug-loaded microspheres were prepared by adding 5-fluorouramide. The highest drug-carrying amount of the drug-loaded microspheres was 2.97% and the encapsulation rate was 20.27% by HPLC. The prepared microspheres have good dispersivity and uniform particle size distribution, and the particle size range is about 10-20 & mu; m; and the FT-IR spectrum results show that both the Jingyi and the vanillin are cross-linked with the chitosan; and the swelling performance results show that the swelling rate of the microspheres prepared by the cross-linking agent of different compounding proportions is different, The results show that the microspheres have different release rates. The results of the XRD pattern show that the microspheres were successfully cross-linked, and the DSC-TGA pattern confirmed that the 5-fluorouramide was inside the microspheres, and the stability of the 5-fluorouramide was improved. With reference to the existing national standard, the release performance of 5-fluorouramide drug-loaded microspheres was studied. The maximum cumulative release rate of the microballoon was 97.2% in the buffer solution of pH = 3.6, and the maximum cumulative release rate was 94.2% in the buffer solution of pH = 7.4. Therefore, the effect of controlling the release rate can be achieved by controlling the compounding ratio of the cross-linking agent. The stability of the microspheres was studied under the conditions of high temperature, high light and high humidity.
【学位授予单位】：河北科技大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：TQ460.1;O636.1

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