Ferric maltol   中文名称: 麦芽酚铁

Metabolic Disease

服用麦芽酚铁后，血清铁蛋白、血液血红蛋白、网织红细胞血红蛋白、血清铁和血清铁蛋白水平均升高[1]。

根据动物研究，麦芽酚铁中未被吸收的铁至少可以以螯合形式留在小肠中，降低局部毒性的可能性和游离铁损伤肠粘膜的风险[1]。

Introduction: Iron deficiency anemia affects up to three quarters of patients with inflammatory bowel disease (IBD). It can significantly impact the quality of life and the ability to work by impairing physical, emotional, and cognitive functioning. The etiology of iron deficiency anemia is multifactorial and oral or intravenous iron replacement is necessary. However, oral iron supplements are often discontinued prematurely due to poor tolerability or insufficient efficacy. Moreover, intravenous supplementation is inconvenient, associated with potentially serious safety risks, and a burden on healthcare resources.[1]

Areas covered: Ferric maltol is a novel ferric iron compound with potential use as an oral therapy for iron deficiency anemia. This overview explains how the molecule’s design impacts clinical outcomes and summarizes available clinical data (ranging from early comparisons with ferrous sulfate to randomized, placebo-controlled, Phase III data in patients with IBD known to be intolerant of oral ferrous products).[1]

Expert opinion: Ferric maltol offers the ability to treat iron deficiency anemia in mild-to-moderate IBD without resorting to intravenous therapy, even in those who are intolerant of oral ferrous products. This clinical benefit has the potential to change treatment pathways and increase choice, not only in IBD but also perhaps in many areas beyond gastroenterology.

Absorption, Distribution and Excretion
Ferric maltol dissociates in the gastrointestinal tract, leading to a Tmax of 1.5-3.0 hours for iron concentrations. Mean serum iron increases by 14±6µmol/L in iron deficient patients following a single dose. a 60mg dose is approximately 14% bioavailable. 60 minutes after injection of radiolabelled ferric maltol, 11+2% of the dose is present in the bone marrow, 18±1% is present in the liver, and 2.6±1% is in the urine. Maltol has an AUC of 0.022-0.205h\*µg/mL and maltol glucuronide has an AUC of 9.83-30.9h\*µg/mL.
39.8-60% of an oral dose of ferric maltol is excreted in the urine as a glucuronide conjugate. Iron and ferric maltol are not excreted in the urine and unabsorbed ferric maltol is eliminated in the feces.
Data regarding the volume of distribution of ferric maltol is not readily available.
Data regarding the clearance of ferric maltol is not readily available.

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Metabolism / Metabolites
_In vitro_, ferric maltol metabolism is predominantly glucuronidation of maltol by UGT1A6 and sulfation.

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Biological Half-Life
Maltol has a half life of 0.7h.

Protein Binding
Data regarding the protein binding of ferric maltol is not readily available.

[1]. Stallmach A, et al. Ferric maltol (ST10): a novel oral iron supplement for the treatment of iron deficiency anemia in inflammatory bowel disease. Expert Opin Pharmacother. 2015;16(18):2859-67.

Ferric maltol is an iron(III) atom complexed with 3 maltol molecules to increase the bioavailability compared to iron(II), without depositing it in the duodenum as insoluble ferric hydroxide and phosphate. Ferric maltol has been described in literature since at least the late 1980s as a potential treatment for iron deficiency. Ferric maltol was granted FDA Approval on 25 July 2019.
See also: Ferric cation (has active moiety).

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Drug Indication
Ferric maltol is indicated to treat iron deficiency in adults.
Feraccru is indicated in adults for the treatment of iron deficiency.
Treatment of iron deficiency

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Mechanism of Action
Ferric maltol dissociates as the iron atom is donated to unknown iron uptake mechanisms, possibly beta 3 integrin or divalent metal transporter 1, in the ileum and duodenum. Once the iron is in circulation, it then associates with transferrin and ferritin.

C₁₈H₁₅FEO₉

431.15

431.006

C, 50.14; H, 3.51; Fe, 12.95; O, 33.40

33725-54-1

169535

Typically exists as Purple to purplish red solids at room temperature

148Ų

0

9

0

28

200

0

Cl.CC1C=CC(C(C(N2CCCCC2)C)=O)=C(C)C=1

AHPWLYJHTFAWKI-UHFFFAOYSA-K

InChI=1S/3C6H6O3.Fe/c3*1-4-6(8)5(7)2-3-9-4;/h3*2-3,8H,1H3;/q;;;+3/p-3

iron(3+);2-methyl-4-oxopyran-3-olate

Ferric maltol; Iron (III) maltol; ST10; ST 10021; WHO 9974ST-10; ST 10-021ST-10021; WHO-9974ST; 10 ST10-021; ST-10-021; ST10021; WHO9974; Ferric maltol; 33725-54-1; Iron (III) maltol; st10; iron maltol; MA10QYF1Z0; Ferric maltol [INN]; Ferric maltol [USAN];

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~12.5 mg/mL (~28.99 mM)

配方 1 中的溶解度: ≥ 1.25 mg/mL (2.90 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 12.5 mg/mL澄清的DMSO储备液加入到400 μL PEG300中，混匀；再向上述溶液中加入50 μL Tween-80，混匀；然后加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: 1.25 mg/mL (2.90 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 悬浊液; 超声助溶。
例如，若需制备1 mL的工作液，可将 100 μL 12.5 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。