Galenika a.d., Institute for Research and Development, Batajnicki drum b.b, Belgrade, Serbia.
Arch Pharm Res. 2009 Dec;32(12):1767-74. doi: 10.1007/s12272-009-2215-9. Epub 2010 Feb 17.
Using mixture experimental design, the effect of carbomer (Carbopol((R)) 971P NF) and hydroxypropylmethylcellulose (Methocel((R)) K100M or Methocel((R)) K4M) combination on the release profile and on the mechanism of drug liberation from matrix tablet was investigated. The numerical optimization procedure was also applied to establish and obtain formulation with desired drug release. The amount of TP released, release rate and mechanism varied with carbomer ratio in total matrix and HPMC viscosity. Increasing carbomer fractions led to a decrease in drug release. Anomalous diffusion was found in all matrices containing carbomer, while Case - II transport was predominant for tablet based on HPMC only. The predicted and obtained profiles for optimized formulations showed similarity. Those results indicate that Simplex Lattice Mixture experimental design and numerical optimization procedure can be applied during development to obtain sustained release matrix formulation with desired release profile.
采用混合物实验设计,研究了 Carbomer(Carbopol((R)) 971P NF)和羟丙甲纤维素(Methocel((R)) K100M 或 Methocel((R)) K4M)组合对释放曲线的影响,以及药物从基质片中释放的机制。还应用数值优化程序来建立和获得具有所需药物释放的配方。TP 的释放量、释放率和机制随总基质中 Carbomer 比例和 HPMC 黏度的变化而变化。增加 Carbomer 分数会导致药物释放减少。在所有含有 Carbomer 的基质中都发现了异常扩散,而仅基于 HPMC 的片剂则主要是 Case-II 转运。优化配方的预测和获得的曲线具有相似性。这些结果表明, Simplex Lattice 混合物实验设计和数值优化程序可应用于开发中,以获得具有所需释放曲线的持续释放基质配方。