Iron Sucrose Supplement

English name：Iron saccharate

CAS number：8047-67-4

Molecular formula: C18H24Fe2O24

Molecular weight: 736.06

EINECS number: 232-464-7

Related category

Monosaccharides; Pharmaceutical raw materials; Pharmaceutical raw materials; Biological chemicals; Raw materials; Other chemical products; Chemical raw materials ; API;Carbohydrates & Derivatives; Intermediates & Fine Chemicals; Pharmaceuticals

Mol file：8047-67-4.mol

Structural formula:

Iron sucrose property

Melting point: 168-171°C

Storage condition: Refrigerator

Solubility: slightly soluble in water

Form: solid

Color: Brown to dark brown

InChI：InChI=1/3C6H10O8.2Fe/c3*7-1(3(9)5(11)12)2(8)4(10)6(13)14;;/h3*1-4,7-10H,(H,11,12)(H,13,14);;/q;;;2*+3/p-6/t3*1-,2-,3-,4+;;/s3

InChIKey：ADQSUDSYBZBMFT-JMMWHMDLNA-H

CAS DataBase: 8047-67-4(CAS DataBase Reference)

(IARC) Carcinogen classification: 3 (Vol. 2, Sup 7) 1987EPA

Chemical Information: Iron saccharate (8047-67-4)

Intravenous iron supplementation

Iron sucrose has been safely used abroad for many years, and has been marketed in 68 countries and regions around the world, and its injection preparation is the oldest intravenous iron supplement used. Iron sucrose injection in the treatment of iron deficiency anemia can promote the rapid entry of iron into endothelial cells, which is of great significance for erythropoiesis. Injection of iron sucrose injection is one of the most clinically used methods of iron supplementation. Compared with oral ferrous succinate, the absorption effect of iron is better, and the intestinal symptoms are not easy to appear. Compared with other types of iron supplements, iron sucrose has a safe, rapid and effective iron supplement treatment effect, its side effects are far lower than other dosage forms of iron supplements such as dextran iron, iron sucrose has become the fastest growing class of products in the domestic iron supplement market. In addition, the study found that the treatment of diabetes patients with iron deficiency anemia by iron sucrose injection can obtain ideal therapeutic effect, which is conducive to improving the clinical indicators of patients, and is worthy of clinical promotion and application.

Iron sucrose injection is an effective drug for the treatment of iron deficiency anemia, and it has achieved good clinical effect as an iron supplement in practical medical activities.

Action effect

Iron sucrose is more suitable for people who are intolerant to oral iron or those who are not well absorbed by oral iron. If you inject it directly, you can effectively supplement iron for the human body. What's more, it should be noted that when we use injection, the following infusion formula is generally transfused with normal saline. Understand the relevant blood loss or the amount of iron that needs to be added, etc., after calculation, use it according to the doctor's guidance. Control the injection speed when using iron sucrose injection, if the injection is too fast, it may lead to hypoglycemia.

Backdrop

Anemia is an important complication of chronic renal failure, and the application of recombinant erythropoietin has greatly improved the anemia of patients, but many dialysis patients do not respond to erythropoietin treatment or have poor efficacy. Iron deficiency is the most common cause of erythropoietin resistance, and appropriate iron supplementation is crucial to obtain the efficacy of erythropoietin. There are two ways to supplement iron, oral and intravenous. The patients who still have moderate anemia after oral iron administration were examined for serum ferritin, serum iron, folic acid and vitamin B12, and the results showed that the folate and vitamin B12 in the patients with anemia were at normal levels, while serum ferritin and serum iron were significantly lower than normal. After long-term oral iron administration, serum ferritin and serum iron in the blood of patients are still obviously insufficient, which may be an important reason for the substandard HB in patients with kidney replacement therapy despite regular use of erythropoietin. Before the use of intravenous iron, the vast majority of patients took oral iron supplementation. Studies have shown that oral iron supplementation is difficult to achieve or maintain the therapeutic goals of renal anemia. The reasons may include: insufficient intake, the average daily intake of iron is only 10 to 15mg, and only 10% to 20% of it can be absorbed; Excessive loss, such as repeated blood tests, residual blood in dialyzers and pipelines, gastrointestinal bleeding, etc.; The application of rhEPO increases the demand for iron in the body.

More and more studies have shown that intravenous iron can significantly improve anemia, and the K/DOQI guidelines recommend that patients with hemodialysis should be routinely given intravenous iron supplementation to treat anemia. Iron sucrose injection polynuclear iron hydroxide (Ⅲ) -sucrose complex solution, after intravenous use of iron sucrose in patients with moderate anemia, which could not be corrected by oral iron supplementation, serum iron and serum ferritin were significantly increased, and hemoglobin and HcChemicalbookt were significantly increased. Therefore, iron sucrose injection is more effective in correcting anemia than oral iron. Iron sucrose is the safest intravenous iron agent at present. It has the advantages of fast acting, not easy allergic reaction and acute iron poisoning. It is widely used in clinic. After intravenous iron supplementation, iron agent binds to transferrin and quickly reaches bone marrow, which can quickly replenish iron deficiency in patients, maintain iron reserve and improve patients' responsiveness to EPO.

Pharmacological action

Iron sucrose is a polynuclear ferric hydroxide (III), the core surface is surrounded by a large number of non-covalent bonded sucrose molecules, forming a complex with an average molecular weight of 43kDa. This macromolecular structure can avoid being eliminated from the kidney. The complex is structurally stable and releases iron ions under reasonable conditions.

Pharmacokinetics

Absorption: A single intravenous dose containing 100mg of this product reached the highest level after 10min, averaging 538μmol/L.

Distribution: the central chamber distribution volume is about 3L, and the steady state distribution volume is about 8L.

Metabolism and excretion: The injected iron is rapidly eliminated in the plasma, with a half-life of about 6h; The iron removal was less than 5% of the total removal 4 hours before injection, and about 75% of sucrose was excreted after 24 hours.

Indication

It is clinically suitable for the treatment of iron deficiency anemia that can not be effectively alleviated by oral iron, such as severe iron deficiency requiring rapid iron supplementation, oral iron absorption disorders and oral iron intolerance.

Preparation

Route 1: Ferric hydroxide colloids are prepared by the reaction of ferric salt and inorganic base at 5 ~ 20℃. Ferric hydroxide colloids are then complexed with sucrose at 100 ~ 120℃ to obtain ferric sucrose solution. Ferric sucrose solution is spray dried to obtain solid state.

preparation

Route 2:

1. Crystals: Adjust the pH value of sucrose solution to 1 ~ 4 with acetic acid, add the iron salt solution to the sucrose solution to form a mixture, adjust the pHChemicalbook value of the mixture to 1 ~ 3 with Na2CO3 solution, stir, continue to add Na2CO3 solution until turbidity appears in the mixture and the pH value of the mixture is adjusted to 4 ~ 7, filter. Add water to get discus solution;
2. Complexation: heating the sucrose solution, adding lye for alkalization, adding discus solution to the alkalized sucrose solution, standing still overnight to obtain complexation solution;
3. Refining: The complex liquid after the rest of the night is filtered, the filtrate is precipitated with 2 to 3 times 95% ethanol, and filtered, that is, iron sucrose.

Safety information

Customs Code: 29400090

Toxicity: LD50 in mice (mg Fe/kg): >2500 orally; >200 i.v. (Geisser)

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