Research and Development unit, Nafas Zist Pharmed Pharmaceutical Company, Science and Technology Park of Islamic Azad University, Tehran, Iran.
Pharm Nanotechnol. 2021;9(2):157-163. doi: 10.2174/2211738509666210114160941.
Ferric carboxymaltose (FCM) formulation consists of iron-carbohydrate nanoparticles where iron-oxyhydroxide as a core is covered by a carbohydrate shell. The present work provides an improved synthesis process of FCM as an intravenous iron, active pharmaceutical ingredient.
Water-soluble FCM complex was prepared from the reaction of ferric hydroxide precipitation with an aqueous solution of oxidized maltodextrin (MD) at optimum temperature and pH conditions. A systematic approach was followed to obtain the optimal weight ratio of the maltodextrin/ ferric chloride for FCM synthesis process with suitable-sized nanoparticles. Physical characterization of newly synthesized ferric carboxymaltose (FCM-NP) was performed to establish its equivalency with the reference product (Ferinject).
The size distribution of the whole nanoparticles determined by dynamic light scattering (DLS) was in the range of 15-40 nm with an average particle size of 26 ± 6.6 and 25.8 ± 4.9 for FCM-NP and Ferinject, respectively. X-ray diffraction (XRD) results of FCM-NP and Ferinject indicated the Akaganeite structure of iron-oxyhydroxide. The iron content of particles (cores) measured by Atomic absorption spectroscopy (AAS) was almost equal for the two formulations. The Fourier transform infrared (FTIR) spectra of Ferinject and FCM-NP were approximately similar.
Various analytical methods, including FTIR spectroscopy, XRD analysis, DLS technique, TEM, and AAS were employed. It was observed that the specifications of FCM-NP obtained by these analyses were almost identical to those of Ferinject. Accordingly, the two formulations were considered comparable.
三价铁羧基麦芽糖（FCM）制剂由铁碳水化合物纳米颗粒组成，其中铁氧氢氧化物作为核心，被碳水化合物外壳覆盖。本工作提供了一种改进的 FCM 作为静脉铁、活性药物成分的合成工艺。
水溶性 FCM 复合物是由氢氧化铁沉淀与氧化麦芽糊精（MD）水溶液在最佳温度和 pH 条件下反应制备的。采用系统的方法获得了最佳的麦芽糊精/氯化铁重量比，以获得适合尺寸的纳米颗粒的 FCM 合成工艺。对新合成的铁羧基麦芽糖（FCM-NP）进行物理特性表征，以确定其与参比产品（Ferinject）的等效性。
动态光散射（DLS）测定的整个纳米颗粒的粒径分布在 15-40nm 范围内，平均粒径分别为 26±6.6nm 和 25.8±4.9nm，用于 FCM-NP 和 Ferinject。FCM-NP 和 Ferinject 的 X 射线衍射（XRD）结果表明铁氧氢氧化物的纤铁矿结构。原子吸收光谱（AAS）测量的颗粒（核）的铁含量对于两种制剂几乎相等。Ferinject 和 FCM-NP 的傅里叶变换红外（FTIR）光谱大致相似。
采用傅里叶变换红外（FTIR）光谱、X 射线衍射（XRD）分析、动态光散射（DLS）技术、透射电子显微镜（TEM）和原子吸收光谱（AAS）等多种分析方法。观察到通过这些分析获得的 FCM-NP 的规格几乎与 Ferinject 相同。因此，认为这两种制剂是可比的。
