Ferrous Ascorbate- One of the most widely prescribed oral iron supplement

INTRODUCTION

Iron deficiency anaemia (IDA) is a major public health problem in India. Iron deficiency can easily be corrected with iron supplementations. WHO & UNICEF have recommended taking iron supplements for adolescents and young children in the countries where 40% of anaemia is prevalent in population. Oral iron preparations are used for mild to moderate anaemia and available for the supplementation of iron in clinical practice. Most of the oral?iron?formulations are available in the form of ferrous as well as in the form of ferric compounds. Ferrous ascorbate is the most widely prescribed oral iron supplement as it has a good efficacy and is well tolerated in both adults and children. Oral iron preparations have followed the conventional ‘prolonged-release’ formulation, which improves the toleration capacity of the gastrointestinal tract and enhances the bio-availability. After the ferrous form absorption, iron reaches its maximum in the blood for about 7 hours and stays in that state for 24 hours.

WHY FERROUS ASCORBATE (FAS)?

Ferrous Ascorbate?supplement restores the body’s important nutrients. It is especially vital during pregnancy because of its function in developing the unborn baby’s brain and spinal cord. FAS functions as a catalyst in various metabolic activities in our bodies, accelerating oxygen delivery and use and aiding cell development and proliferation. FAS promotes the synthesis of red blood cells and is used in the treatment of anaemia caused due to iron deficiency in the body. It acts as a health supplement for those with low iron content in their diet. Iron increases the production of red blood cells and haemoglobin. Vitamin C present in FAS aids in the effective and maximum absorption of dietary iron.?

Advantages of Ferrous Ascorbate

Ferrous Ascorbate?results from the reaction of Ascorbic Acid with Iron.?Iron?is absorbed very well in the presence of ascorbic acid, as this compound is known to convert ferric iron into ferrous iron.

1. Ferrous form of iron is soluble at neutral pH and can be absorbed three times higher than the ferric form. Oxidation is prevented by Ascorbic acid, which can thus act as reducing agent as well as maintain the iron in ferrous form.
2. FAS is known to exist intact inside the gastrointestinal tract due to the stable chelation of iron with ascorbate. This compound does not dissociate due to any of the food inhibitors.?Iron gets absorbed easily in vivo from FAS than from?Ferrous Sulphate.
3. It is found that FAS dissociates in aqueous solution into ascorbate ion and ferrous ion where ascorbate ion acts as a monodentate. FAS is known to dissociate at pH5. At pH6 to 8, the solubility effect is enhanced by ascorbate, which is beneficial for the absorption of iron.

IMPLEMENTATION OF FERROUS ASCORBATE(FAS)

Ferrous ascorbate has a better bioavailability, as high as 67%. FAS is a stable chelate that does not dissociate in the gastrointestinal tract. Higher absorption of iron from FAS can be explained by the ascorbate component that prevents oxidation of the iron to a ferric state. A mean rise in haemoglobin (Hb) greater than 5.0 g/dL in 60?days and greater than 2.0 g/dL within 45 days is reported with once-daily therapy of FAS. FAS is also efficacious for the prophylaxis of anaemia in patients who undergo surgical procedures. Thus, FAS has an important place in the clinical management of IDA in real-life scenarios.?The increase in haemoglobin levels after prescribing 100mg dosage of iron for 28 days was higher in the case of divalent formulations than that of the trivalent formulations. A few other similar studies have proved that divalent form of iron or FAS has greater bio-availability than the trivalent form of iron. Hence, ferrous salts and especially FAS is chosen over other iron forms for preparing the drugs as they are efficient, cost effective and have tolerability.

STUDY ON FERROUS ASCORBATE FORMULATIONS (FAS)

Ferrous ascorbate is widely used in clinical practice. In a retrospective analysis of hospital records of 250 patients with anaemia (15–35?years of age) being treated in a teaching hospital in India, FAS was most commonly prescribed (69.2%), FASs has shown good efficacy in an open-label, prospective study in clinical settings in India. Once daily administration of a fixed-dose combination tablet of FAS (equivalent to 100?mg iron) and folic acid (1.1?mg) for 45?days showed a rapid rise in Hb (mean: 2.37?g/?dL; 95% CI: 2.25–2.49) in 1,461 women (IDA without pregnancy: 508; anaemia during pregnancy: 613; pregnancy with IDA: 204; not specified: 136) who had a mean baseline Hb of 8.53?±?1.46?g/dL (95% CI: 8.45–8.61) and mean age of 27?±?8?years. In this study, FAS was well tolerated, and a significant improvement in Hb was reported as early as 15?days (mean: 1.67; 95% CI: 1.56–1.78). The largest rise in Hb (3.60?g/dL) was seen in women with Hb less than 6?g/dL at baseline followed by those with baseline Hb of 6–8?g/dL (2.91?g/dL), 8.1–10 g/dL (2.23 g/dL), and greater than 10?g/dL (1.25?g/dL). In addition, there was a marked improvement in fatigue and pallor. In an open-labelled, randomized study, FAS (n =?30) was compared to carbonyl iron (n =?30) for IDA (Table 3).33 Patients received the two preparations in doses equivalent to 100?mg elemental iron for 60?days.?

Another?clinical study was conducted comparing the FAS formulation with that of ferrous sulphate in 18 healthy volunteers. The intestinal absorption was not different when measured after 21 days. But, haemoglobin content has come to baseline values in both the groups.

?Another study by the same research group was conducted in which the bio-availability of trivalent iron form (Ferric Hydroxide Polymaltose Complex) was compared with the bivalent form?(Ferrous Ascorbate). The iron absorption in the intestines was evaluated in the fasting state by the estimation of plasma iron tolerance curves and whole body iron retention values. The estimation of plasma iron showed lower Fe (III) content (1.2+/-0.1percent) compared to 43.7+/-7.1percent of FAS. After taking a meal, there was a change in divalent iron absorption than the trivalent iron absorption.

• These iron compounds differ in the bio-availability, safety, cost and side effects. Apart from the different chemical states of iron formulations available in the market, they also exist in different generic forms.
• Clinically, iron salts that are bivalent like Ferrous Sulphate, Ferrous Fumarate and Ferrous Gluconate are widely used than the ferric iron forms. The bio-availability of ferric forms of iron is 3-4 times less than the ferrous forms (10 to 15% bio-availability).
• Ferric forms of iron are poorly soluble in alkaline solutions and hence they have to be transformed into ferrous forms before they are absorbed.

FERROUS ASCORBATE (FAS) IS ALSO USED IN AGRICULTURAL AND PLANTATION INDUSTRY

With the increasing shortage of global available resources, efficient and sustainable agricultural production represents a major challenge. Mineral nutrients must be sufficiently available to ensure efficient crop productivity and maintain product quality. FAS plays an important role in cellular function, and represents one of the essential micro-elements in plants and animals. Plants use Fe to ensure electron flow through the PSII-PSI complex during photosynthesis and FAS plays a critical role in plant development because of its activity in regulating redox status. It is an indispensable cofactor in the respiratory chain and enzymes of tricarboxylic acid cycle, nitrate metabolism, biosynthesis of gibberellins and ethylene, amongst others. Improvement in FAS utilization or enhancement of tolerance to FAS deficiency are important agronomic objectives.

Ferrous, is the most abundant type of iron in soil. However, due to the poor solubility of Ferrous ions under aerobic conditions, especially in high pH and calcareous soils, plants usually display a shortage of Iron. In order to adapt to Ferrous deficiency stress, plants have evolved two strategies to take up Ferrous from the soil, strategy in non-graminaceous plants; including cotton,?Arabidopsis, and pea. Another strategy in graminaceous; such as rice and maize and so on Both strategies depend on the action of plasma membrane proteins in the cells of root epidermis.

WEST BENGAL CHEMICAL INDUSTRIES LIMITED (WBCIL) & FERROUS ASCORBATE (FAS)

West Bengal Chemical Industries Limited?is one of the leading manufacturer of Ferrous Ascorbate in India for the pharmaceutical & nutritional supplements. FAS is available in both powder and?DC Grade forms.

Central Drugs Standard Control Organisation(CDSCO)?has decided to include?Ferrous Ascorbate?in?Indian?Pharmacopoeia (IP).?WBCIL have successfully developed the IP grade in powder form and corresponding DC Grade. West Bengal Chemical Industries Ltd. have supplied the said material among Indian majors who have successfully concluded clinical trials.?

Customization and documentation support is available as per customer requirement. West Bengal Chemical Industries Ltd. ensures that the product maintains an excellent microbial profile.?WBCIL’s?DC grade?material is ready for direct compression.

?

FREQUENTLY ASKED QUESTIONS

Question 1. How does FAS Look like?

Answer: FASis a?free flowing powder with Blackish tint.

Question 2. Is FAS Soluble or insoluble in Water?

Answer: FAS is Soluble in Water.

Question 3: what should the?pH(of a 2.0% w/v solution) of FAS be?

Answer: The Iron content as ferrous in FAS depends on the grade. However, as per IP grade ph should be between 5.5% w/w – 7% w/w.

Question 4.?What should?the?Iron Content?in FAS be?

Answer- the Iron content as ferrous in FAS depends on the grade. However, as per IP grade the iron content should be between (13.5% w/w- 15.5% w/w)

Question 5.?Can FAS tablets be consumed for tiredness?

Answer: A drop in the iron levels in the body decreases haemoglobin synthesis. It leads to the reduced oxygen-carrying capacity of the blood, due to which you feel tired. FAS can boost iron levels, which in turn, will boost energy levels and relieve you from tiredness.

Question 6. When should I take FAS?

Answer: You should take FAS tablets at least one hour before or two hours after meals. Do not consume dairy products or antacids for at least two hours after taking FAS as they may reduce the efficacy of this drug. Avoid laying down immediately after using the drug. Measure dose carefully if using FAS in liquid form.

Question 7. Is FAS safe during pregnancy?

Answer: Yes. FAS is safe during pregnancy if used under the supervision of a health care professional. Consuming the recommended dosage of FAS during pregnancy improves iron utilization and satisfies the increased demand for iron in a pregnant woman’s body. Hence it prevents iron deficiency in pregnant women.

Question 8. Why is FAS better?

Answer: FAS is better when compared to other iron supplements, as it causes minimal gastrointestinal tract problems. Also, it is easily absorbed in the human body with less troublesome interactions with dietary products and other medicines. FAS is also suitable for long-term use as compared to other iron supplements.

Question 9: Can I take FAS for anaemia and iron deficiency?

Answer: Yes, FAS is recommended for iron deficiency anaemia. It is not recommended for other types of anaemia. Take FAS in the dose and duration advised by your doctor.

Question 10: What is FAS + Folic acid used for?

Answer:?FAS + Folic acid is used to treat iron-deficiency anaemia.