S. K. Patel College of Pharmaceutical Education and Research, Ganpat University, Mehsana-Gozaria Highway Kherva, Gujarat, India.
Acta Pharm. 2010 Dec;60(4):455-65. doi: 10.2478/v10007-010-0034-7.
The purpose of the present study was to design muco-adhesive chitosan microspheres containing amoxicillin. Chitosan microspheres with a small particle size and good sphericity were prepared by a spray-drying method followed by chemical treatment with a chemical crosslinking agent (glutaraldehyde). Parameters affecting the crosslinking extent of the crosslinking time and the concentration of the crosslinker agent. Crosslinked spray-dried chitosan microspheres were analyzed for their morphological aspects, particle size, drug entrapment efficiency, swelling percent and in vitro drug release. Batch M4 with a drug polymer ratio of 1:2, dissolved in minimum concentration of acetic acid solution treated with glutaraldehyde, was found to be optimal giving controlled drug release for 10 h. It was found that both the increase of glutaraldehyde concentration and crosslinking duration decreased the swelling capacity of chitosan microspheres. This could be directly correlated to drug release from the microspheres.
本研究旨在设计含有阿莫西林的粘膜黏附性壳聚糖微球。通过喷雾干燥法制备粒径小、球形好的壳聚糖微球,然后用化学交联剂(戊二醛)进行化学处理。考察了交联时间和交联剂浓度等参数对交联程度的影响。对交联喷雾干燥壳聚糖微球的形态学、粒径、药物包封效率、溶胀率和体外药物释放进行了分析。发现药物-聚合物比为 1:2 的批次 M4,溶解在最低浓度的乙酸溶液中,用戊二醛处理,是最佳的,可控制药物释放 10 小时。结果发现,戊二醛浓度和交联时间的增加都会降低壳聚糖微球的溶胀能力。这与微球中药物的释放直接相关。