Faculty of Pharmacy, Department of Drug Form Technology, Wroclaw Medical University, Borowska 211A, 50-556, Wroclaw, Poland.
Department of Pharmacognosy and Phytochemistry, Medical University of Silesia in Katowice, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, ul. Jagiellonska 4, 41-200, Sosnowiec, Poland.
AAPS PharmSciTech. 2018 Feb;19(2):951-960. doi: 10.1208/s12249-017-0912-0. Epub 2017 Nov 2.
The presented work describes the formulation and characterization of modified release glassy solid dosage forms (GSDFs) containing an amorphous nifedipine, as a model BCS (Biopharmaceutical Classification System) class II drug. The GSDFs were prepared by melting nifedipine together with octaacetyl sucrose. Dissolution profiles, measured under standard and biorelevant conditions, were compared to those obtained from commercially available formulations containing nifedipine such as modified release (MR) tablets and osmotic release oral system (OROS). The results indicate that the dissolution profiles of the GSDFs with nifedipine are neither affected by the pH of the dissolution media, type and concentration of surfactants, nor by simulated mechanical stress of biorelevant intensity. Furthermore, it was found that the dissolution profiles of the novel dosage forms were similar to the profiles obtained from the nifedipine OROS. The formulation of GSDFs is relatively simple, and the dosage forms were found to have favorable dissolution characteristics.
本工作描述了含有非那吡啶的改良释放玻璃状固体剂型（GSDF）的配方和特性，作为模型 BCS（生物药剂学分类系统）II 类药物。GSDF 通过将非那吡啶与八乙酰蔗糖熔融制备。在标准和生物相关条件下测量的溶解曲线与从含有非那吡啶的市售制剂（如缓释（MR）片剂和渗透释放口服系统（OROS））获得的那些进行了比较。结果表明，含有非那吡啶的 GSDF 的溶解曲线不受溶解介质 pH 值、类型和浓度的表面活性剂以及生物相关强度的模拟机械应力的影响。此外，发现新型剂型的溶解曲线与非那吡啶 OROS 获得的曲线相似。GSDF 的配方相对简单，并且发现这些剂型具有良好的溶解特性。
