含甘草总黄酮效应组分微丸的制备及性质考察

目的应用挤出滚圆法制备含甘草总黄酮效应组分微丸,采用Eudragit RS 100为包衣材料,制备含甘草总黄酮效应组分缓释微丸.方法采用Mini Glatt流化床底喷包衣法制备包衣微丸,对其包衣工艺及处方进行单因素考察,评价微丸的粉体学性质和体外释放行为.结果当聚合物包衣增重6%,增塑剂用量为10%时,药物具有明显的缓释作用,体外释放曲线符合Peppas和Higuchi方程.结论制备的含甘草总黄酮效应组分微丸具备较理想的缓释效果.     

流化床包衣法制备芍药总苷缓释微丸的研究

目的 应用挤出滚圆法制备芍药总苷速释微丸,用Eudragit RS 100作为包衣材料,制备芍药总苷缓释微丸。方法 采用mini Glatt流化床底喷包衣法制备缓释微丸,对其包衣工艺及处方进行单因素考察,评价微丸的粉体学性质和体外释放行为。结果 当聚合物包衣增质量为6%,增塑剂用量为10%时,药物具有明显的缓释作用,体外释放曲线符合Peppas和Higuchi方程。结论 制备的芍药总苷缓释微丸具备较理想的缓释效果。     

含甘草酸效应组分微丸的制备及其性质考察

目的:应用挤出滚圆法制备含甘草酸效应组分速释微丸,采用Eudragit RS 100与Eudragi RL 1002种包衣材料,制备含甘草酸效应组分缓释微丸。方法:采用Mini Glatt流化床底喷包衣法制备缓释微丸,对其包衣工艺及处方进行单因素考察,评价微丸的粉体学性质和体外释放行为。结果:当Eudragit RS 100与Eudragit RL 100的质量比为4∶1,聚合物包衣增重为5%,增塑剂用量为15%时,药物具有明显的缓释作用,体外释放曲线符合Pep-pas和Higuchi方程。结论:通过调整Eudragit RS 100与Eudragit RL 100的比例,或提高聚合物包衣增重等手段,能使含甘草酸效应组分缓释微丸具备较理想的缓释效果。     

载米诺环素纳米羟基磷灰石/壳聚糖复合体的体外释放及抑菌性

BACKGROUND: Hydroxyapatite/chitosan (HA/CS) complex may act as a drug carrier for drug release, but little is reported about the release amount and antibacterial effect of minocycline-HA/CS (Mino-HA/CS) complex. OBJECTIVE: To investigate the in vitro release and antibacterial property of Mino-HA/CS complex. METHODS: HA/CS and Mino-HA/CS were prepared using co-precipitation method. The surface and cross-section features of the complexes were observed under scanning electron microscopy. The porosities were measured according to Archimedes Principle. The release of minocycline hydrochloride was measured by high performance liquid chromatography with the simulated saliva as drug release media. In vitro antibacterial effect on Porphyromonas gingivalis and Staphylococcus aureus were measured by bacteria-inhibiting ring method. Biological toxicities were evaluated via cell counting kit-8cell proliferation assay. RESULTS AND CONCLUSION: The porosity of Mino-HA/CS was larger than that of HA/CS, with the average porosity of 53.99%. Single-day release amount of Mino-HA/CS could maintain at the level of 0.5-1 μg per day for a long-term. Bacteriostatic rings of Porphyromonas gingivalis and Staphylococcus aureus still existed clearly after 7 days. Cell proliferation assays showed that Mino-HA/CS extract had the significant effect on promoting cell proliferation. These findings indicate that the Mino-HA/CS sustains the release of minocycline at a relatively stable level within a longer period, shows good inhibitory effect on Porphyromonas gingivalis and Staphylococcus aureus and promotes the proliferation of periodontal ligament cells.     

流化床包衣法制备芍药总苷缓释微丸的研究

目的 应用挤出滚圆法制备芍药总苷速释微丸,用Eudragit RS 100作为包衣材料,制备芍药总苷缓释微丸.方法 采用mini Glatt流化床底喷包衣法制备缓释微丸,对其包衣工艺及处方进行单因素考察.评价微丸的粉体学性质和体外释放行为.结果 当聚合物包衣增质量为6%,增塑剂用量为10%时,药物具有明显的缓释作用,体外释放曲线符合Peppas和Higuchi方程.结论 制备的芍药总苷缓释微丸具备较理想的缓释效果.     

挤出滚圆法制备芍药甘草方微丸的处方工艺研究

目的应用挤出滚圆法制备芍药甘草方微丸。方法在考察提取物的物理性质的基础上,用挤出滚圆造粒机分别制备芍药、甘草微丸;采用单因素试验优化制剂处方及工艺条件;评价了微丸的粉体学性质、收率和体外溶出度。结果用挤出滚圆法制备的芍药、甘草微丸在30min内体外溶出均达90%以上,且圆整度好,收率高。结论挤出滚圆法制备芍药甘草方微丸工艺简便易行,制得的微丸质量好,收率高,体外释药迅速。     

载5-氟尿嘧啶纳米微球治疗荷H22腹水瘤小鼠的实验研究

目的 观察自制载5-氟尿嘧啶(5-FU)纳米微粒对荷H22小鼠恶性腹水的治疗作用以及对小鼠生存期、小鼠体重、H22细胞周期、小鼠肝脏毒性的影响.方法 168只荷H22腹水瘤昆明小鼠随机分为7组,即空白对照组、溶剂对照组、辅料对照组、5-FU阳性药组(5 d共3 mg),低(5 d共0.12 mg)、中(5 d共0.6 mg)、高(5 d共3 mg)剂量微粒缓释组.药物经腹腔注入,微粒缓释组只给药一次,其他组均为连续给药5 d,每天一次.观察各组小鼠生存情况,比较各组小鼠平均生存时间、小鼠体重、细胞增殖指数(PI)以及肝脏毒性.结果 与对照组比较,微粒缓释组能明显提高小鼠的生存时间(P<0.05)、减小小鼠体重(P<0.05)和增殖指数(PI)、减小肝毒性.与阳性药物组比较,中、高剂量微粒缓释组对小鼠H22腹水瘤的抑制作用增加,表现为明显延长生存时间(P<0.05)、减缓小鼠体重增长(P<0.05)和减小增殖指数(PI),药物对肝脏毒性影响也有减小,表现为中剂量组肝脏毒性明显降低,高剂量组肝脏毒性与阳性药物组相当.结论 5-FU载药缓释纳米微球在治疗荷H22腹水瘤小鼠时可以在小鼠体内持续释放,与阳性药物组相比减少了给药次数,增加了药物对H22肿瘤细胞的抑制作用,并减小对肝脏的毒性.     

挤出滚圆法制备芍药甘草方微丸的处方工艺研究

目的应用挤出滚圆法制备芍药甘草方微丸。方法在考察提取物的物理性质的基础上,用挤出滚圆造粒机分别制备芍药、甘草微丸;采用单因素试验优化制剂处方及工艺条件;评价了微丸的粉体学性质、收率和体外溶出度。结果用挤出滚圆法制备的芍药、甘草微丸在30min内体外溶出均达90%以上,且圆整度好,收率高。结论挤出滚圆法制备芍药甘草方微丸工艺简便易行,制得的微丸质量好,收率高,体外释药迅速。