载三联抗结核药物硫酸钙/聚氨基酸人工材料体外缓释性能的观察

被引:19
作者
刘海涛 [1 ]
施建党 [2 ]
王骞 [3 ]
王自立 [2 ]
耿广起 [2 ]
德向研 [2 ]
王洁 [4 ]
杨宗强 [2 ]
机构
[1] 宁夏医科大学总医院创伤骨科
[2] 宁夏医科大学总医院脊柱骨科
[3] 美国南佛罗里达大学药学院
[4] 宁夏医科大学科学技术实验中心
关键词
抗结核药; 硫酸钙/聚氨基酸; 缓释; 体外;
D O I
暂无
中图分类号
R529.2 [骨和关节结核];
学科分类号
100201 [内科学];
摘要
目的:探讨载三联抗结核药物硫酸钙/聚氨基酸人工材料在模拟体液中的药物缓释性能。方法:避光环境下以100:3:3:12的比例称取硫酸钙/氨基酸复合材料500mg、异烟肼(isoniazid,INH)15mg、利福平(rifampicin,RFP)15mg、吡嗪酰胺(pyrazinamide,PZA)60mg制备载药人工缓释材料,将其置于模拟体液中,分别于浸泡3h、12h、24h、36h、48h、60h、72h、1~14周时取材料浸提液,应用高效液相色谱法(HPLC)检测其中INH、RFP、PZA三种药物的浓度,并据其计算单位时间段内药物释出质量。结果:载三联抗结核药的硫酸钙/聚氨基酸人工材料在模拟体液中浸泡3h时浸提液中释出INH、RFP、PZA的浓度分别达到152.96±1.32μg/ml、92.90±2.17μg/ml和334.90±12.3μg/ml,在8周前各时间点的浸提液中,3种药物浓度均较高;至8周时PZA的释出浓度、10周时RFP释出浓度、11周时INH的释出浓度仍高于其10倍的最小抑菌浓度,之后逐渐降低;未载药硫酸钙/聚氨基酸人工材料在有效检测时间内药物出峰时间处未见有意义杂质峰出现。结论:载三联抗结核药硫酸钙/聚氨基酸人工材料具有较为平稳、持续时间较长的有效缓释性能,三种药物在模拟体液中释出药物的浓度均可达到体内杀死结核分枝杆菌的浓度。
引用
收藏
页码:239 / 244
页数:6
相关论文
共 22 条
[1]
Delivery of rifampicin–PLGA microspheres into alveolar macrophages is promising for treatment of tuberculosis.[J].Keiji Hirota;Taizo Hasegawa;Takehisa Nakajima;Hiroyuki Inagawa;Chie Kohchi;Gen-Ichiro Soma;Kimiko Makino;Hiroshi Terada.Journal of Controlled Release.2009, 3
[2]
Measurement of the concentration of three antituberculosis drugs in the focus of spinal tuberculosis [J].
Ge, Zhaohui ;
Wang, Zili ;
Wei, Mingji .
EUROPEAN SPINE JOURNAL, 2008, 17 (11) :1482-1487
[3]
Efficient drug delivery to alveolar macrophages and lung epithelial lining fluid following pulmonary administration of liposomal ciprofloxacin in rats with pneumonia and estimation of its antibacterial effects [J].
Chono, Sumio ;
Tanino, Tomoharu ;
Seki, Toshinobu ;
Morimoto, Kazuhiro .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2008, 34 (10) :1090-1096
[4]
Treatment of spinal tuberculosis with ultrashort-course chemotherapy in conjunction with partial excision of pathologic vertebrae [J].
Wang, Zili ;
Ge, Zhaohui ;
Jin, Weidong ;
Qiao, Yongdong ;
Ding, Huiqiang ;
Zhao, Haoning ;
Lin, Zhikai ;
Chen, Jun ;
Yang, Weiyu .
SPINE JOURNAL, 2007, 7 (06) :671-681
[5]
Mechanical properties of calcium sulphate/hydroxyapatite cement [J].
Lei, Dang ;
Wardlaw, D. ;
Hukins, D. W. L. .
BIO-MEDICAL MATERIALS AND ENGINEERING, 2006, 16 (06) :423-428
[6]
The fusion rate of calcium sulfate with local autograft bone compared with autologous iliac bone graft for instrumented short-segment spinal fusion [J].
Chen, WJ ;
Tsai, TT ;
Chen, LH ;
Niu, CC ;
Lai, PL ;
Fu, TS ;
McCarthy, K .
SPINE, 2005, 30 (20) :2293-2297
[7]
Modeling small-molecule release from PLG microspheres: effects of polymer degradation and nonuniform drug distribution.[J].Chandrashekar Raman;Cory Berkland;Kyekyoon (Kevin) Kim;Daniel W. Pack.Journal of Controlled Release.2004, 1
[8]
Evaluation of an in situ setting injectable calcium phosphate as a new carrier material for gentamicin in the treatment of chronic osteomyelitis: Studies in vitro and in vivo.[J].U. Joosten;A. Joist;T. Frebel;B. Brandt;S. Diederichs;C. von Eiff.Biomaterials.2003, 18
[9]
EVALUATION OF THE RISK OF INSTRUMENTATION AS A FOREIGN-BODY IN SPINAL TUBERCULOSIS - CLINICAL AND BIOLOGIC STUDY [J].
OGA, M ;
ARIZONO, T ;
TAKASITA, M ;
SUGIOKA, Y .
SPINE, 1993, 18 (13) :1890-1894
[10]
高效液相色谱法测定复方非洛地平控释片中2个组分释放度 [J].
狄忠 ;
李志平 ;
刘燕 ;
喻芳邻 ;
孔华 ;
梅兴国 .
中国药学杂志, 2013, 48 (12) :1015-1018