摘要
目的研究他莫昔芬微胶囊的制备工艺及体外释放性能。方法通过向明胶溶液中加入硫酸钠溶液的单凝聚方法制备了他莫昔芬微胶囊;观测其形态、尺寸,鉴别其组分,测定他莫昔芬含量、包封率和回收率,并进行体外释放实验。结果他莫昔芬与明胶的质量比为1∶2,明胶溶液浓度为5%,体系pH值为3.6,以30%硫酸钠溶液为稀释液时能得到他莫昔芬/明胶微胶囊;光学显微镜观察可见得到的微胶囊具有很好的圆形形态,微胶囊的平均包封率为87.12%,他莫昔芬平均含量为29.04%,平均粒径尺寸为16.79μm。并对微胶囊在模拟胃液和肠液的释放特征进行模拟,体外释放曲线都符合一级动力学释放规律,完全释放时间可达12h以上。结论以他莫昔芬为囊心、明胶为囊材能够制得具有良好的圆形形态和较好缓释效果的他莫昔芬/明胶微胶囊。
Abstract
OBJECTIVE To study the preparation and the in vitro release profile of tamoxifen (TAM)/gelatin microcapsules. METHODS TAM microcapsules were prepared through single coacervation by adding sodium sulfate solution to gelatin solution. The morphology and size of the microcapsules were observed, and the content, encapsulation efficiency and recovery efficiency of the microcapsules were measured. Moreover, their in vitro release experiments were carried out.RESULTS TAM/gelatin microcapsules were obtained when the weight ratio of TAM to gelatin loaded was 1∶2. The concentration of gelatin solution was 5%. The pH value of the mixed system was 3.6 and the mixed system was diluted with 30% of sodium sulfate solution. FTIR spectra of the microcapsules confirmed the existence of TAM. The microcapsules had good sphericity morphology and distribution. The size of the microcapsules was in the range of 10～25 μm with an average size of 16.79 μm. The encapsulation efficiency and recovery efficiency of the microcapsules were 88.3% and 99.3% respectively. The release kinetics of microcapsules was studied in false gastric and intestines juice. The in vitro release profile was fitted with the first-order kinetic equation well in both conditions, and TAM was completely released after about 12 h.CONCLUSION TAM/gelatin microcapsules with good morphology and sustained release effect can be obtained by single coacervation method.
关键词
他莫昔芬 /
微胶囊 /
模拟胃肠液 /
体外药物释放
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Key words
tamoxifen /
microcapsule /
false gastric and intestines juice /
in vitro release profile
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马宗会;樊在霞;聂华丽;朱利民.
他莫昔芬微胶囊的制备及体外药物释放性能研究[J]. 中国药学杂志, 2008, 43(16): 1248-1251
M Zong-hui;FN Zi-xi;NIE Hu-li;ZHU Li-min.
Preparation of Tamoxifen Microcapsules and their in Vitro Release Profile [J]. Chinese Pharmaceutical Journal, 2008, 43(16): 1248-1251
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脚注
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