Regulatory approvals for ascorbic acid 

Food and beverage industry

  • The US FDA classifies it as Generally Recognized as Safe (GRAS) for use as a food additive and preservative.

  • European Food Safety Authority (EFSA): Approved under food additive code E300.

  • Codex Alimentarius: Considered an effective antioxidant for food applications.

Pharmaceutical and nutritional uses

  • FDA-approved for treating Vitamin C deficiency (scurvy) and as a significant element in dietary supplements.

  • World Health Organization (WHO): Included on the Essential Medicines List (EML) for its ability to cure scurvy and enhance iron absorption.

  • European Medicines Agency (EMA): Approved for oral and injectable medicinal formulations.

Cosmetic and Skincare Applications

  • FDA and EU Regulations: Cosmetic formulations are permitted because of their antioxidant capabilities, which help protect the skin from aging and environmental harm.

PHARMACOKINETICS:

Absorption

Primarily absorbed in the small intestine via active transport and passive diffusion 

Bioavailability:

  • High at low doses (~70-90% for 30-180 mg/day).

  • Decreases with higher doses (>1g/day) as absorption saturates.

  • Excess is excreted in urine.

Distribution

  • Free ascorbic acid is the primary form in which it circulates in the bloodstream.

  • High-demand organs, such as the brain, adrenal glands, liver, and leukocytes, actively absorb tissue.

  • Storage There is no considerable long-term storage; any excess is promptly eliminated.

Metabolism

  • DHA is mostly metabolized in the liver and can be converted back into ascorbic acid or further broken down. 

  •  Metabolized into oxalic and diketogulonic acids, which are eliminated in urine. 

Excretion

  • Kidneys expel primarily through urine. 

  • Renal reabsorption occurs through SVCT1 transporters. 

  • Excess quantities (>1g) are quickly removed without metabolization.

  • High doses may increase oxalate levels and cause renal stones in predisposed persons.

DOSAGE AND ADMINISTRATION

Adults: The recommended daily allowance (RDA) for vitamin C is 90 mg/day for men and 75 mg/day for women. Smokers may require an additional 35 mg/day.

Children: 1-3 years: 15 mg/day, 4-8 years: 25 mg/day, 9-13 years: 45 mg/day, 14-18 years: 75 mg/day (boys) / 65 mg/day (girls)

For Treatment of Scurvy (Severe Vitamin C Deficiency)

Adults: High doses are typically required, often starting with 300-1,000 mg per day until symptoms improve.

Children: Doses are adjusted based on age and severity, typically 100 mg per day.

DRUG INTERACTIONS

  • Iron Supplements: Enhances absorption of non-heme iron.

  • Anticoagulants (e.g., Warfarin): May reduce anticoagulant effects.

  • Chemotherapy Drugs: High doses may interfere with efficacy.

  • Oral Contraceptives: May reduce vitamin C levels.

  • Statins: Could potentially reduce cholesterol-lowering effects.

  • Barbiturates: Can lower vitamin C levels.

  • Corticosteroids: May increase the risk of deficiency.

  • Alcohol: Increases risk of deficiency.

  • Antacids: May reduce absorption when taken together.

  • NSAIDs: Increased risk of kidney damage.

CONTRAINDICATIONS

Contraindications of Ascorbic Acid:

  • Hypersensitivity: Allergy to ascorbic acid or components.

  • Kidney Stones: Risk of stone formation with high doses.

  • Iron Overload Disorders: (e.g., Hemochromatosis, Thalassemia) – increases iron absorption.

  • G6PD Deficiency: High doses may cause hemolysis.

  • Severe Renal Impairment: Risk of accumulation in kidney dysfunction

SIDE EFFECTS

Common Side Effects:

  • Upset Stomach: Nausea, abdominal cramps, and diarrhea (especially with high doses).

  • Heartburn: Acidic nature may cause irritation.

  • Headache: Some people may experience headaches.

Severe Side Effects:

  • Kidney Stones: High doses (over 2,000 mg/day) can increase the risk.

  • Gastrointestinal Issues: Severe abdominal pain, bloating, and diarrhea.

  • Hemolysis: In people with G6PD deficiency, high doses can cause red blood cell destruction.

TOXICITY

Symptoms:

  • Gastrointestinal issues (diarrhea, nausea, cramps)

  • Kidney stones (especially in high doses)

  • Iron overload (in iron-sensitive individuals)

  • Hemolysis (in G6PD deficiency)

Risk of kidney damage with prolonged high doses

Image
Ascorbic acid
CAS Number
98-01-1(freebase)
Alternate CAS Number
721436-53-9 (hydrate)
CAS Number
50-81-7(base libre)
Alternate CAS Number
5743-28-2(sel de calcium dihydraté); 134-03-2(sel de sodium)
CAS Number
342385-52-8(hydrate salt)
Alternate CAS Number
526-98-7(Freebase)
CAS Number
129499-78-1(free base);
Alternate CAS Number
2178105-19-4 (Na salt)
CAS Number
490-83-5(free base)
Alternate CAS Number
51260-76-5 (Na salt)