Use of sialic acid in promoting iron absorption of iron supplements
By combining sialic acid with sodium ferrous citrate, iron absorption is promoted, solving the problem of low absorption rate of non-heme iron supplements and achieving efficient iron utilization and health promotion effects.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- CABIO BIOTECH (WUHAN) CO LTD
- Filing Date
- 2022-11-11
- Publication Date
- 2026-06-05
AI Technical Summary
Existing non-heme iron supplements have low absorption rates, leading to widespread iron deficiency, which affects the health of organisms. Furthermore, conventional iron supplements may cause gastrointestinal discomfort.
Sialic acid is combined with ferrous drugs, especially sodium ferrous citrate, with a daily intake of 0.8-3.5 mg/kg to promote iron absorption.
It significantly improves iron bioavailability, enhances red blood cell and hemoglobin production, improves immune function and gut health, and reduces gastrointestinal discomfort.
Smart Images
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Abstract
Description
Technical Field
[0001] This invention relates to the field of sialic acid application technology, and more particularly to the application of sialic acid in promoting the absorption of iron from iron supplements. Background Technology
[0002] Iron is one of the essential trace elements for living organisms. As the most abundant trace element, it plays a vital role in maintaining normal metabolism and growth and development. The physiological functions of iron in the body include participating in oxygen transport and electron transport processes, maintaining normal hematopoietic function, and enhancing the body's immune function. Furthermore, as a transition metal, iron can switch between different valence states, making it an important cofactor for the physiological functions of many heme proteins and non-heme iron-containing proteins. The body requires approximately 25-30 mg of iron daily for erythrocyte production, and loses another 1-2 mg of iron due to bleeding, mucosal and skin cell shedding, etc. However, the body absorbs only 1-2 mg of iron daily through diet. Further iron loss, impaired dietary absorption, or increased demand, such as frequent blood donation, gastrointestinal diseases, physical activity, vegetarianism, or pregnancy, may exceed the gastrointestinal tract's capacity for iron absorption, leading to iron deficiency.
[0003] Iron deficiency anemia is a common micronutrient deficiency in the population, especially in growing children and pregnant women. It can lead to a range of other symptoms such as fatigue, hair loss, and difficulty swallowing. The condition is particularly severe for patients with chronic diseases, resulting in a deterioration in quality of life and poor prognosis. It is associated with reduced work capacity and impaired cognitive function, and has become a global public health problem affecting over 2 billion people. Iron absorption depends on its form, gastrointestinal conditions, the amount and chemical form of iron digested, and the quantity and characteristics of other dietary components.
[0004] Oral iron supplements are a common method for relieving and treating iron deficiency anemia. Heme iron and non-heme iron are two forms of dietary iron supplementation, and their absorption processes differ due to their different forms. Both heme and non-heme iron are primarily absorbed in the duodenum, but they cross the intestinal cell mucosa through completely independent pathways. Although heme iron has a higher bioavailability, it only accounts for about 15% of total dietary iron, while non-heme iron accounts for 85%, with an absorption rate of only about 10%. Currently available iron supplements are mainly non-heme iron, including ferrous sulfate, ferrous gluconate, ferrous fumarate, ferrous succinate, iron dextran, and sodium ferrous citrate. While ferrous iron supplements have a high iron content and are very helpful in treating iron deficiency anemia, they often cause upper abdominal pain, diarrhea, and constipation, which can be severe enough to lead to discontinuation of treatment. Therefore, improving the digestibility and absorption of non-heme iron is of great significance. Summary of the Invention
[0005] This invention provides the application of sialic acid in promoting iron absorption in iron supplements. The purpose of this invention is to overcome the shortcomings of existing iron supplements, such as low absorption rates and negative impacts on gastrointestinal function.
[0006] In a first aspect, the present invention provides the application of sialic acid in promoting the efficiency of iron absorption by the human body.
[0007] In the applications provided by this invention, the daily intake of sialic acid is 0.8-3.5 mg / kg.
[0008] In the application provided by this invention, Fe 2+ Calculate, Fe 2+ The daily intake is 0.2-0.5 mg / kg.
[0009] Secondly, the present invention provides the application of sialic acid in the preparation of iron supplements at a daily intake of 0.8-3.5 mg / kg.
[0010] Thirdly, the present invention provides an iron supplement comprising a ferrous drug and sialic acid, wherein the daily intake of sialic acid is 0.8-3.5 mg / kg. Preferably, the daily intake of sialic acid is 1.5-3.5 mg / kg.
[0011] In the iron supplement provided by this invention, the ferrous drug is sodium ferrous citrate.
[0012] This invention explores the effects of different combinations of iron supplements and sialic acid, and finds that sodium ferrous citrate as a suitable iron supplement... 2+ When used as a donor, sialic acid has the most significant effect on promoting iron absorption.
[0013] In the iron supplement provided by this invention, Fe 2+ The recommended daily intake of sodium ferrous citrate is 0.2-0.5 mg / kg.
[0014] Fourthly, the present invention provides the application of the above-mentioned iron supplement in increasing the production of red blood cells and hemoglobin in organisms.
[0015] And the application of the aforementioned iron supplements in the preparation of drugs for treating anemia.
[0016] As understood by those skilled in the art, this invention also claims protection for the use of iron supplements containing sodium ferrous citrate and sialic acid in increasing erythrocyte and hemoglobin production in organisms. The iron supplements containing sodium ferrous citrate and sialic acid in this invention, which increase erythrocyte and hemoglobin production in organisms, are for non-disease treatment purposes.
[0017] The present invention claims the use of an iron supplement containing sodium ferrous citrate and sialic acid in increasing the production of red blood cells and hemoglobin in organisms for non-disease treatment and diagnostic purposes.
[0018] The beneficial effects of this invention are as follows:
[0019] (1) This invention is the first to propose that ferrous iron absorption can be promoted by combining sialic acid and ferrous citrate.
[0020] (2) This invention combines sialic acid with ferrous drugs to supplement iron, which not only improves the bioavailability of iron, but also allows sialic acid to play a variety of biological activities such as regulating immunity and promoting intestinal health while supplementing iron. Detailed Implementation
[0021] To make the objectives, technical solutions, and advantages of this invention clearer, the technical solutions of this invention are described clearly and completely. Obviously, the described embodiments are only some, not all, of the embodiments of this invention. Based on the embodiments of this invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of this invention.
[0022] Example
[0023] This embodiment provides an evaluation of the improvement effect of SA compound iron supplement using anemic mice.
[0024] The experimental method is as follows:
[0025] (1) Animal model establishment and sample collection
[0026] a) Experimental animals: 100 female KM mice, 4 months old.
[0027] b) Feed: Low iron feed formula (iron content < 5.7 mg / kg feed): 20.0% casein, 65.0% corn starch, 5% corn oil, 5% cellulose powder, 4.0% mineral mixture, 0.5% vitamin mixture and 0.5% choline chloride.
[0028] Mineral mixture content (g%): MgSO4 73.758, ZnSO4 7H2O 19.67, MnSO4 H2O 5.778, CuSO4 5H2O 0.7315, KClO3 0.0625.
[0029] Vitamin mixture content (g%): Retinol acetate (5×10) 4 IU / g) 1.0, cholecalciferol (2×10) 5IU / g) 0.75, Tocopherol Acetate (75% V) 12.5, Phytonaphthoquinone 0.04, Thiamine Hydrochloride 0.6, Riboflavin 0.6, Pyridoxine Hydrochloride 0.6, Nicotinic Acid 3.0, Folic Acid 0.1, Cyanocobalamin Hydrochloride (0.1% V) 2.0, Sucrose 78.81.
[0030] c) Test substances: Sialic acid SA (preferably in the form of N-acetylneuraminic acid, wherein the source of N-acetylneuraminic acid is microbial fermentation); Sodium ferrous citrate SFC.
[0031] d) Establishment of the iron deficiency anemia (IDA) model: The room temperature was 24±2℃, and the humidity was 55±5%. Iron contamination was avoided during the rearing process. Hard plastic cages were used, and mice were allowed free access to food and ultrapure water. After 7 days of acclimatization, a low-iron diet was introduced for one week, followed by bloodletting (1.5 ml / day) for four consecutive days to establish the IDA model. The low-iron diet was continued for two weeks. IDA mice gradually showed signs of lethargy. Hemoglobin (Hb) was measured in tail blood from the mice. A successful model was defined as Hb < 90 g / L, with a success rate of 100%.
[0032] e) IDA model recovery experiment
[0033] Iron-deficiency anemia mice (IDA) and healthy mice were divided into groups. The IDA mice were fed with sodium ferrous citrate (SFC), ferrous sulfate (FS), sialic acid (SA), sodium ferrous citrate (SFC) + sialic acid (SA), and ferrous sulfate (FS) + sialic acid (SA). The treatment groups are shown in Table 1, where L is the low dose, M is the medium dose, and H is the high dose.
[0034] Table 1 shows the effect of iron supplementation on iron-deficiency anemic mice (IDA).
[0035]
[0036]
[0037] The dosage of SFC and FS iron supplements is 3 mg / kg body weight (bw). The low, medium, and high doses of sialic acid are 10 mg / kg bw, 20 mg / kg bw, and 40 mg / kg bw, respectively.
[0038] Based on the equivalent dose conversion between animals and between animals and humans in pharmacological experiments in the literature, Huang Jihan et al., Anhui Provincial Drug Clinical Evaluation Center, Yijishan Hospital of Wannan Medical College, Chinese Journal of Clinical Pharmacology and Therapeutics, 2004, 9(9):1069–1072, calculated the daily human intake of sialic acid based on the standard weight of 60kg for normal adults as follows: low dose 48.66mg, medium dose 97.32mg, high dose 194.65mg; the daily human intake of iron was 14.60mg.
[0039] Mice in each group were housed separately and administered iron orally for three weeks, while also having free access to a low-iron diet and ultrapure water. All supplements were freshly prepared daily, and body weight was monitored every three days during the feeding period, with supplementation administered according to body weight. A total of 8 mice perished during the experiment.
[0040] (2) Detection indicators and methods
[0041] ① Red blood cell count (RBC): Blood cell counting method
[0042] ② Hemoglobin level (Hb): Spectrophotometry
[0043] ③ Hemocytocyte ratio (Ht): Blood analyzer method
[0044] (3) Test results
[0045] Table 2 shows the weight changes of mice from 1 to 7 weeks of feeding.
[0046] Table 2. Changes in body weight of mice in each treatment group.
[0047] Group 1 week 2 weeks 3 weeks 4 weeks 5 weeks 6 weeks 7 weeks Group 1 blank 27.8 30.9 32.5 33.9 35.2 35.6 36.2 Group 2 IDA 28 29.8 30.3 30.8 31.5 31.3 31.9 <![CDATA[Group 3 (Fe 2+ )]]> 28.3 30.1 30.5 30.5 31.7 32.6 34 Group 4(M-SA) 27.9 29.8 30.8 31.8 30.8 31.5 31.2 <![CDATA[Group 5 (Fe 2+ -L-SA)]]> 27.8 28.5 29.7 30.9 30.7 32.8 33.6 <![CDATA[Group 6 (Fe 2+ -M-SA)]]> 27.8 29.7 31.9 31.6 32.2 32.8 34.7 <![CDATA[Group 7 (Fe 2+ -H-SA)]]> 28.1 29.2 30.6 30.8 32.7 33.8 35 <![CDATA[Group 8 (Fe 2+ )]]> 28.1 28.7 30.2 31.5 32.7 33.1 33.7 <![CDATA[Group 9 (Fe 2+ -L-SA)]]> 27.8 29.2 29.6 29.6 31.0 32.2 33.2 <![CDATA[Group 10 (Fe 2+ -H-SA)]]> 28.2 28.9 29.3 29.3 31.4 32.0 32.8
[0048] Analysis of the results in Table 1 showed that there was no significant difference in mouse body weight among the groups in week 7 (p > 0.05).
[0049] The rate of change in red blood cell count (RBC) is shown in Table 3.
[0050] Table 3. Successful IDA Modeling—RBC Change Rate After 3 Weeks of Iron Supplementation
[0051]
[0052] The results in Table 3 show that neither sodium ferrous citrate nor sialic acid alone could restore the red blood cell count of IDA mice to normal levels. However, the synergistic effect of sodium ferrous citrate and sialic acid was able to restore the red blood cell count of IDA mice to near-normal levels within 3 weeks.
[0053] Furthermore, in groups 5-7, the iron supplementation groups treated with sialic acid (SA) showed a significantly higher rate of change in red blood cell count compared to groups 1 and 2. This large rate of change in red blood cell count confirms that sialic acid combined with ferrous citrate increases red blood cell count by 6-40% compared to ferrous citrate supplementation alone. Low doses showed little effect, but medium- to high doses of SA synergistically enhanced the body's utilization of iron and increased red blood cell production. In the ferrous sulfate group, the increase in red blood cell count after combined administration with SA was only 2-6% compared to ferrous sulfate supplementation alone.
[0054] The rate of change in hemoglobin (Hb) values is shown in Table 4.
[0055] Table 4. Successful IDA Modeling—Hb Change Rate After 3 Weeks of Iron Supplementation
[0056] Group Initial Hb (g / L) End of Hb (g / L) Rate of change (%) Group 1 blank <![CDATA[132.46 a ]]> <![CDATA[134.05 a ]]> 101.2 Group 2 IDA <![CDATA[84.68 b ]]> <![CDATA[49.45 c ]]> 58.4 <![CDATA[Group 3 (Fe 2+ )]]> <![CDATA[86.64 b ]]> <![CDATA[98.67 b ]]> 113.9 Group 4(SA) <![CDATA[88.24 b ]]> <![CDATA[54.09 c ]]> 61.3 <![CDATA[Group 5 (Fe 2+ -L-SA)]]> <![CDATA[86.68 b ]]> <![CDATA[103.94 b ]]> 119.9 <![CDATA[Group 6 (Fe 2+ -M-SA)]]> <![CDATA[84.48 b ]]> <![CDATA[116.08 a ]]> 137.4 <![CDATA[Group 7 (Fe 2+ -H-SA)]]> <![CDATA[87.01 b ]]> <![CDATA[126.34 a ]]> 145.2 <![CDATA[Group 8 (Fe 2+ )]]> <![CDATA[88.34 b ]]> <![CDATA[90.25 b ]]> 102.2 <![CDATA[Group 9 (Fe 2+ -L-SA)]]> <![CDATA[89.02 b ]]> <![CDATA[93.92 b ]]> 105.5 <![CDATA[Group 10 (Fe 2+ -H-SA)]]> <![CDATA[86.73 b ]]> <![CDATA[100.23 b ]]> 115.6
[0057] The results in Table 4 show that neither sodium ferrous citrate nor sialic acid alone could restore the hemoglobin level of IDA mice to normal. In addition, the combination of low-dose sialic acid and ferrous citrate was not significantly effective compared with the ferrous citrate alone group. Sodium ferrous citrate and medium-high sialic acid showed a synergistic effect, and were able to restore the hemoglobin level of IDA mice to near normal within 3 weeks.
[0058] Furthermore, the iron treatment groups (groups 5-7) with added sialic acid showed a significantly higher rate of change in hemoglobin levels compared to groups 1 and 2. This large rate of change in hemoglobin levels confirms that sialic acid and sodium ferrous citrate have a synergistic effect, enhancing the body's utilization of iron and producing hemoglobin.
[0059] In the ferrous sulfate group, when administered in combination with SA, the hemoglobin levels of IDA mice did not show a significant increase compared to ferrous sulfate supplementation alone.
[0060] The changes in hemoglobin ratio (Ht) are shown in Table 5.
[0061] Table 5. Changes in Ht levels 7 days before successful IDA modeling and 3 weeks after iron supplementation.
[0062]
[0063]
[0064] Analysis of the results in Table 5 shows that in group 3, iron supplementation in IDA mice gradually increased the hemoglobin ratio from 11.3 to 15.7 within 3 weeks. The effect of low-dose sialic acid was not significant, but with medium- to high-dose sialic acid, the hemoglobin ratio gradually increased from 11.3 to 23.1 within 3 weeks. Therefore, the iron-treated groups (groups 6 and 7) with added sialic acid showed a significantly faster increase in hemoglobin ratio than groups 3 and 4. This rapid increase in hemoglobin ratio confirms that sialic acid and sodium ferrous citrate have a synergistic effect, enhancing the body's utilization of iron in iron-deficient mice.
[0065] In the ferrous sulfate group, although the blood cell ratio of IDA mice was increased when ferrous sulfate was administered in combination with SA compared with ferrous sulfate supplementation alone, no significant difference was observed.
[0066] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention, and not to limit them; although the present invention has been described in detail with reference to the foregoing embodiments, those skilled in the art should understand that modifications can still be made to the technical solutions described in the foregoing embodiments, or equivalent substitutions can be made to some of the technical features; and these modifications or substitutions do not cause the essence of the corresponding technical solutions to deviate from the spirit and scope of the technical solutions of the embodiments of the present invention.
Claims
1. Application of iron supplements in the preparation of drugs that increase the production of red blood cells and hemoglobin in organisms; The iron supplements used in this application contain sialic acid and sodium ferrous citrate; The daily intake of sialic acid in the aforementioned applications is 0.8-3.5 mg / kg; In the application, Fe 2+ The recommended daily intake of sodium ferrous citrate is 0.2-0.5 mg / kg.
2. Application of iron supplements in the preparation of drugs for treating anemia; The iron supplements used in this application contain sialic acid and sodium ferrous citrate; The daily intake of sialic acid in the aforementioned applications is 0.8-3.5 mg / kg; In the application, Fe 2+ The recommended daily intake of sodium ferrous citrate is 0.2-0.5 mg / kg.