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目的研制阿魏酸和黄芪甲苷缓释长效制剂用于植入给药。方法以明胶和阿拉伯胶为囊材,分别以阿魏酸和黄芪甲苷为囊心物采用复凝聚法制备微囊,制备处方为胶药比5∶1(质量比),胶液浓度为每30 ml蒸馏水溶解1.0 g囊材,将阿魏酸和黄芪甲苷分别凝聚成囊,按一定比例混合后固化,用胶原海绵吸收,冷冻干燥制得植入剂并评价其体外释放效果。结果植入剂中阿魏酸的含量为(1.02±0.13)%(w/w下同),黄芪甲苷的含量为(3.15±0.06)%(n=3)。与单用微囊相比,将微囊分散于胶原海绵中能够显著降低释药速度,实现缓释效果,并且释药动力学拟合Higuchi方程。结论将微囊分散于胶原海绵骨架中可以实现缓释长效。
Objective To develop ferulic acid and astragaloside long-acting sustained-release preparation for implantation. Methods The gelatin and gum arabic were used as the capsular material, and the ferulic acid and astragaloside were used as the core material respectively to prepare the microcapsules by complex coacervation method. Dissolving 1.0 g capsule material with 30 ml distilled water, the ferulic acid and astragaloside were respectively aggregated into capsules, mixed in a certain proportion, then solidified, absorbed by collagen sponge, and lyophilized to prepare implants and evaluated the in vitro release effect. Results The content of ferulic acid in implants was (1.02 ± 0.13)% (w / w) and the content of astragaloside was (3.15 ± 0.06)% (n = 3). Dispersing the microcapsules in the collagen sponge significantly reduces the rate of drug release compared to the single microcapsules, achieves a sustained release effect, and the release kinetics fits the Higuchi equation. Conclusion The microcapsules dispersed in the collagen sponge skeleton can achieve long-term sustained release.