Yan Xin, Zhang Qi, Wang Tao, Luo Yu, Sha Xianyi
School of Pharmacy, Fudan University, Shanghai 201203, China.
Pharmaceutics. 2025 Feb 23;17(3):292. doi: 10.3390/pharmaceutics17030292.
: Iron-deficiency anemia is one of the most common nutritional deficiencies worldwide. Polysaccharide-iron complexes (PICs), as novel organic iron supplements, have garnered increasing attention due to their high bioavailability, minimal gastrointestinal irritation, and favorable tolerability. However, different formulations of PICs can show significant variations in their physicochemical properties and bioavailability. These factors are crucial for clinical efficacy and safety. : This study selected two formulations of polysaccharide-iron complexes: Formulation A (PIC-coated pellets) and Formulation B (PIC powders), with ferrous succinate tablets (Formulation C) used as a control. The focus was on evaluating the molecular weight of the polysaccharides, the levels of free iron, and the dissolution across various dissolution media. Physicochemical properties were compared through particle size analysis, dissolution rate testing, and free iron content determination. Additionally, the pharmacokinetic properties of the two PIC formulations were assessed in a beagle dog model of iron-deficiency anemia. : Significant differences were observed in particle appearance and content structure between the two PIC formulations. Formulation A, prepared using pellet technology, exhibited a uniform particle size distribution. Its dissolution rate in acidic environments was significantly lower than that of Formulation B. In simulated gastric fluid, the cumulative iron dissolution rate of Formulation A was less than 15% within two hours, while that of Formulation B exceeded 50%, with substantial batch-to-batch variability. In various dissolution media, Formulation A released 12% of its dissolved iron content in gastric fluid within two hours. In contrast, the absolute free iron content of Formulation B was 8.5 times higher than that of Formulation A in simulated gastric fluid. In the beagle dog model of iron-deficiency anemia, Formulation A showed significantly higher bioavailability, which suggests that the pellet preparation technology improves both the acid resistance and bioavailability of the PIC formulation. : The study revealed that Formulation A, prepared using pellet technology, possesses unique quality characteristics. This technology significantly reduces the release of free iron from PICs due to gastric acid action, potentially minimizing gastrointestinal irritation. Moreover, the pellet preparation process improves the acid resistance and bioavailability of PIC formulations, offering a more effective therapeutic option for iron-deficiency anemia. Future research may further explore the potential applications of pellet technology in other iron supplement formulations.
缺铁性贫血是全球最常见的营养缺乏症之一。多糖铁复合物（PICs）作为新型有机铁补充剂，因其高生物利用度、最小的胃肠道刺激和良好的耐受性而受到越来越多的关注。然而，不同配方的PICs在物理化学性质和生物利用度上可能存在显著差异。这些因素对临床疗效和安全性至关重要。
配方A（PIC包衣微丸）和配方B（PIC粉末），以琥珀酸亚铁片（配方C）作为对照。重点评估多糖的分子量、游离铁水平以及在各种溶出介质中的溶出情况。通过粒度分析、溶出速率测试和游离铁含量测定来比较物理化学性质。此外，在缺铁性贫血的比格犬模型中评估了两种PIC配方的药代动力学性质。
两种PIC配方在颗粒外观和含量结构上存在显著差异。采用微丸技术制备的配方A呈现出均匀的粒度分布。其在酸性环境中的溶出速率明显低于配方B。在模拟胃液中，配方A的铁累积溶出率在两小时内低于15%，而配方B超过50%，且批次间差异较大。在各种溶出介质中，配方A在两小时内在胃液中释放其溶解铁含量的12%。相比之下,在模拟胃液中，配方B的绝对游离铁含量比配方A高8.5倍。在缺铁性贫血的比格犬模型中，配方A显示出显著更高的生物利用度，这表明微丸制备技术提高了PIC配方的耐酸性和生物利用度。
该研究表明，采用微丸技术制备的配方A具有独特的质量特性。该技术显著减少了胃酸作用下PICs中游离铁的释放，可能将胃肠道刺激降至最低。此外，微丸制备工艺提高了PIC配方的耐酸性和生物利用度，为缺铁性贫血提供了更有效的治疗选择。未来的研究可能会进一步探索微丸技术在其他铁补充剂配方中的潜在应用。
