作为改善阿苯达唑生物药剂学行为策略的固体分散体的开发及体外评价
Development and in vitro evaluation of solid dispersions as strategy to improve albendazole biopharmaceutical behavior.
作者信息
Simonazzi Analía, Cid Alicia Graciela, Paredes Alejandro Javier, Schofs Laureano, Gonzo Elio Emilio, Palma Santiago Daniel, Bermúdez José María
机构信息
Instituto de Investigaciones para la Industria Química, Universidad Nacional de Salta - Consejo Nacional de Investigaciones Científicas y Técnicas, Av. Bolivia 5150, Salta 4400, Argentina.
Unidad de Investigación y Desarrollo en Tecnología Farmacéutica, Universidad Nacional de Córdoba - Consejo Nacional de Investigaciones Científicas y Técnicas, Haya de la Torre y Medina Allende, Ciudad Universitaria, Córdoba 5000, Argentina.
出版信息
Ther Deliv. 2018 Sep;9(9):623-638. doi: 10.4155/tde-2018-0037.
AIM
Solid dispersions using Poloxamer 407 as carrier were developed to improve albendazole (ABZ) solubility and dissolution profiles.
METHODS
ABZ/poloxamer solid dispersions were prepared, and dissolution profiles were mathematically modeled and compared with physical mixtures, pharmaceutical ABZ and a commercial formulation.
RESULTS
Poloxamer 407 increased exponentially ABZ solubility, in about 400% when 95% w/w of polymer compared with its absence. Solid dispersions initial dissolution rate was three to 20-fold higher than physical mixtures, the drug and the commercial formulation. All the solid dispersions required less than 2.2 min to reach an 80% of ABZ dissolution, while the commercial formulation needed around 40 min.
CONCLUSION
Solid dispersions improved ABZ solubility and dissolution rate, which could result in a faster absorption and an increased bioavailability.
目的
开发以泊洛沙姆407为载体的固体分散体，以改善阿苯达唑（ABZ）的溶解度和溶出曲线。
方法
制备ABZ/泊洛沙姆固体分散体，并对溶出曲线进行数学建模，与物理混合物、药用ABZ和市售制剂进行比较。
结果
泊洛沙姆407使ABZ溶解度呈指数增加，与无聚合物时相比，当聚合物含量为95%（w/w）时，溶解度增加约400%。固体分散体的初始溶出速率比物理混合物、药物和市售制剂高3至20倍。所有固体分散体达到80% ABZ溶出所需时间少于2.2分钟，而市售制剂需要约40分钟。
结论
固体分散体改善了ABZ的溶解度和溶出速率，这可能导致更快的吸收和提高生物利用度。
Zotero 插件