卵磷脂/果胶钙凝胶球的制备及性能研究  

Preparation and evaluation of lecithin/calcium-pectin composite beads

作　　者：赵远航[1] 盛林杰[1] 谌晨 李维爽[1] 刘敏[1] 武文洁[1] 

机构地区：[1]天津科技大学材料科学与化学工程学院,天津300457

出　　处：《中国新药杂志》2015年第6期713-720,共8页Chinese Journal of New Drugs

摘　　要：目的：本研究旨在探讨卵磷脂对载药果胶钙凝胶球的改性作用。方法：采用单因素法分析了果胶与卵磷脂比例、交联剂浓度和果胶与药物比例等因素对卵磷脂／果胶钙凝胶球载药释药性能的影响。本研究选择Ca^2＋为交联剂，卵磷脂为改性剂，制备卵磷脂／果胶钙凝胶球，作为结肠定位给药载体；选择吲哚美辛、酮洛芬和姜黄素3种模型药物，考察配方及工艺参数对小球的形态、载药量、包封率和在模拟胃肠道中释药性能的影响，并比较了卵磷脂改性果胶钙体系和果胶锌体系的性能。结果：果胶凝胶球基本成球形，平均粒径1．2～1．6mm，平均粒重1．3～2．9mg，包封率范围37％～92％，载药量范围5％～27％。果胶与卵磷脂比例、交联剂浓度和果胶与药物比例对复合凝胶球的形态、载药、包封率及释药性能均有影响。在分别载荷吲哚美辛、酮洛芬和姜黄素的果胶钙凝胶球中，卵磷脂改性对果胶钙凝胶球载药量的影响不明显，对药物包封率有明显提高。吲哚美辛的包封率从61．77％提高到91．83％；酮洛芬的包封率从61．15％提高到75．97％；姜黄素的包封率从64．21％提高到77．76％。卵磷脂／果胶钙凝胶球对酮洛芬和姜黄素的释药性能影响较小，但明显降低了吲哚美辛的释药速率，吲哚美辛在模拟胃肠道中10h的累积释药率由62．78％降低到3．40％。结论：通过果胶与卵磷脂复合，可以改变药物的释放速率。但是，卵磷脂对载荷不同模型药物体系的影响不同，卵磷脂／果胶钙凝胶球对吲哚美辛的释药性能有明显的改善作用，而对酮洛芬和姜黄素的释药影响较小。相对于果胶钙体系，卵磷脂对果胶锌体系的释药性能影响较大。Objective ： To investigate the influence of lecithin on drug loading of calcium-pectin gel beads. Methods ： The influences of the ratio of pectin to lecithin, crosslinking agent concentration and the ratio of pectin to drug on drug loading and drug release of lecithin/calcium-pectin beads were investigated by single factor analysis. As a colon-specific carrier, lecithin/calcium-pectin beads were prepared with pectin and lecithin in the presence of calcium by ionotropic gelation method. Indomethacin, ketoprofen and curcumin were used as model drugs. The influences of these formulation parameters upon bead shape, size, encapsulation efficiency, drug loading and drug release pattern were investigated in simulated gastro-intestinal conditions. Properties of lecithin/calcium-pectin and lec- ithin/zinc-pectin were compared. Results： Pectinate gel beads were nearly spherical with diameter of 1.2 - 1.6 mm, weight of 1.3 - 2.9 mg, encapsulation efficiency of 37% - 92% , and drug loading of 5% - 27%. The ratio of pectin to lecithin, crosslinking agent concentration and the ratio of pectin to drug significantly affected the bead shape, size, encapsulation efficiency, drug loading and drug release pattern. In the systems loading indomethacin, ketoprofen or curcumin, lecithin almost showed no influence on drug loading, but significantly improved encapsulation efficiency of the three drugs. The encapsulation efficiency of indomethacin increased from 61.77% to 91.83% , that of ketoprofen increased from 61.15% to 75.97% , and that of curcumin increased from 64.21% to 77.76%. The lecithin/calcium-pectin beads significantly decreased the drug release rate from 62.78% to 3.40% at 10 h in the system loading indomethacin in simulated gastro-intestinal conditions, but it did not affect drug re- lease from the systems loading ketoprofen and curcumin. Conclusion： Lecithin can interact with pectin forming complex which can change drug release rate. However, the influence of lecithin on systems loading different drugs is different

关 键 词：果胶钙 卵磷脂 结肠给药 吲哚美辛 酮洛芬 姜黄素 

分 类 号：R943.4[医药卫生—药剂学]