黄连素海藻酸钙凝胶小球制备工艺及释药特性研究  

Preparation and release characteristics of berberine calcium alginate gel beads

作　　者：熊富良[1] 靳文运[1] 何广华[1] 张雪琼[1] 万志敏[1] 

机构地区：[1]武汉理工大学化工学院,湖北武汉430070

出　　处：《中成药》2010年第4期573-576,共4页Chinese Traditional Patent Medicine

摘　　要：目的:考察不同条件下制备的黄连素海藻酸钙凝胶小球的pH值依赖性释放。方法:用浸渍法制备黄连素的海藻酸钙凝胶小球。通过黄连素溶液的浓度,海藻酸钠溶液的浓度和交联时间这三个因素,来考察黄连素凝胶小球的制备工艺,并在模拟胃液和肠液pH环境下,测试其释放行为。结果:黄连素浓度的提高,有利于载药量的提高;而海藻酸钠浓度的提高,会使载药量降低;交联时间对载药量的影响很小。实验证明,载药量最高可以达到16%,与黄连素同类药物相比,显著提高了载药量。最佳工艺小球在pH 1.0的介质中几乎不溶胀,2个小时累积释放不到10%,而在模拟肠液的pH7.4环境中,6个小时的累积释放达到70.14%,24 h累积释放达到98.21%。结论:该黄连素凝胶小球具有较好的缓控释效果,可以降低黄连素对胃部的刺激并可应用于黄连素对溃疡性结肠炎的治疗。AIM： To study pH-sensitive release of berberine from Ca-alginate gel beads prepared under differ-ent condition.METHODS： Ca-alginate gel beads containing berberine were prepared by dipping method.In com-bination of the concentration of berberine solution,of sodium alginate solution and cross-linking time,release prop-erty was studied in simulated gastric juice and enteric juice pH conditions.RESULTS： The increase in the con-centration of berberine was beneficial to the improvement in drug loading;The increase in the concentration of sodi-um alginate reduced in drug loading;cross-linking time has little influence on drug loading.The experiment showed that the maximum drug loading achieved 16%,which significantly improved the drug loading compared with other berberine preparation.Moreover,In 0.1 mol/L HCL（pH 1.0） solution,the release amount of berberine from the beads was less than 10% in 2 h.In simulated enteric juice（pH7.4） solution,the release amount of berberine from the beads was 70.14% in 6 h,the release amount of berberine from the beads was 98.21% in 24 h.CONCLUSION： Calcium alginate gel beads containing berberine has very good sustained,and controlled release effect.It can be used in the treatment of ulcerative colitis with lower gastric discomfort.

关 键 词：黄连素 海藻酸钙 凝胶小球 

分 类 号：R944[医药卫生—药剂学]