酵母细胞壁的盐酸氯丙嗪微囊的制备和稳定性考察

Preparation of chlorpromazine hydrochloride microcapsules with yeast cell wall and evaluation on their stability

目的以酵母细胞壁为囊材,制备盐酸氯丙嗪微囊,并观察其稳定性。方法以载药量为评价指标,采用正交试验设计确定制备盐酸氯丙嗪微囊最佳处方和工艺,并对微囊含量的检测方法进行精密度、稳定性及准确性验证。光学显微镜观察微囊形态,考察其体外释放、高湿度和强光照射的稳定性。结果在40℃,盐酸氯丙嗪与酵母细胞壁质量比为1∶3,时间为6 h,微囊的平均载药量可达41.76%。改进的含量检测方法精密度、稳定性、准确性良好。光学显微镜下可见微囊囊壁完整,呈球形或椭球形,形态均一。盐酸氯丙嗪微囊500 min体外累积释放为94.89%。盐酸氯丙嗪微囊对湿度和光度稳定性显著增加。结论酵母细胞壁可作为囊材用于制备微囊,且能增加药物的稳定性。

Objective To prepare chlorpromazine hydrochloride microcapsules by using yeast cell wall and observe their stability.Methods The formula and procedure were optimized by orthogonal design,serving drug-loading rate as an index for evaluation.The method for determination of drug-loading was verified for precision and stability.The microcapsules were observed for morphology by optical microscopy,and evaluated for drug release in vitro as well as the drug stabilities to high humidity and highlight exposure.Results The optimal temperature,ratio of chlorpromazine hydrochloride to yeast cell wall and time for preparation of microcapsules were 40 ℃,1 ∶ 3 and 6 h respectively.The drug-loading rate of microcapsules prepared under the optimal condition was 41.76%.The modified method for determination of drug-load showed high precision,stability and accuracy.Optical microscopy showed that the microcapsules were in even sphere or oval shape,with intact walls.A portion of 94.89% of total drug in the microcapsules were released in vitro within 500 min.The drug stability in microcapsules to humidity and light increased.Conclusion Yeast cell wall may be used as a material for preparation of microcapsule and may increase the drug stability.