谢先运. 硝硫氰胺固体分散物的溶解速度和吸收J. 药学学报, 1979, 14(1): 45-48.
引用本文: 谢先运. 硝硫氰胺固体分散物的溶解速度和吸收J. 药学学报, 1979, 14(1): 45-48.
Xie Xian-yun. THE DISSOLUTION RATE AND ABSORPTION OF NITHIOCYAMINE SOLID DISPERSIONJ. Acta Pharmaceutica Sinica, 1979, 14(1): 45-48.
Citation: Xie Xian-yun. THE DISSOLUTION RATE AND ABSORPTION OF NITHIOCYAMINE SOLID DISPERSIONJ. Acta Pharmaceutica Sinica, 1979, 14(1): 45-48.

硝硫氰胺固体分散物的溶解速度和吸收

THE DISSOLUTION RATE AND ABSORPTION OF NITHIOCYAMINE SOLID DISPERSION

  • 摘要: 硝硫氰胺难溶于水,其吸收受溶解速度所限制。微粉化减低粒子大小后,通常可增加吸收和总生物利用度。但由微粉化而得到粒子的巨大表面上所附有的自由能,使其成为热力学不稳定体系。选择无生理活性、易溶载体聚乙二醇6000,以熔融法制备成固体分散物。X-射线衍射实验证实为热力学稳定的间充固体溶液。发现硝硫氰胺-聚乙二醇6000(1:9)固体分散物的溶解速度,分别为微粉化和纯硝硫氰胺的10.6倍和15倍。小白鼠体内研究,微粉化硝硫氰胺24小时血浓曲线下的总面积,只有硝硫氰胺-聚乙二醇6000固体分散物的59%。

     

    Abstract: Nithiocyamine is poorly soluble in water, whose GI absorption is rate limited bydissolution. Reduction of the particle size by micronization generally increases the rateof absorption and/or total bioavailability. The large surface area of the particles whichresults from the micronization is associated with surface free energy which makes thesystem thermodynamically unstable. Selecting a physiological inert, easily soluble carriersuch as polyethylene glycol 6,000, solid dispersions are prepared by melting method.The formation of thermodynamically stable interstitial solid solution was demonstratedby X-ray diffraction. The dissolution rate of nithiocyamine-polyethylene glycol 6,000(1:9) was found respectively to be 10.6 and 15 times than that of micronized and purenithiocyamine. In the in vivo studies on mouse, the total areas under the blood concentration curves in 24 hrs for micronized nithiocyamine were found to be approximatly only 59% of those obtained from nithiocyamine-polyethlene glycol 6,000 soliddispersions.

     

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