Alleviation of ascorbic acid-induced gastric high acidity by calcium ascorbatein vitroandin vivo

Abstract

Ascorbic acid is one of the most well-known nutritional supplement and antioxidant found in fruits and vegetables. Calcium ascorbate has been developed to mitigate the gastric irritation caused by the acidity of ascorbic acid. The aim of this study was to compare calcium ascorbate and ascorbic acid, focusing on their antioxidant activity and effects on gastric juice pH, total acid output, and pepsin secretion in an in vivo rat model, as well as pharmacokinetic parameters. Calcium ascorbate and ascorbic acid had similar antioxidant activity. However, the gastric fluid pH was increased by calcium ascorbate, whereas total acid output was increased by ascorbic acid. In the rat pylorus ligation-induced ulcer model, calcium ascorbate increased the gastric fluid pH without changing the total acid output. Administration of calcium ascorbate to rats given a single oral dose of 100 mg/kg as ascorbic acid resulted in higher plasma concentrations than that from ascorbic acid alone. The area under the curve (AUC) values of calcium ascorbate were 1.5-fold higher than those of ascorbic acid, and the Cmax value of calcium ascorbate (91.0 ng/ml) was higher than that of ascorbic acid (74.8 ng/ml). However, their Tmax values were similar. Thus, although calcium ascorbate showed equivalent antioxidant activity to ascorbic acid, it could attenuate the gastric high acidity caused by ascorbic acid, making it suitable for consideration of use to improve the side effects of ascorbic acid. Furthermore, calcium ascorbate could be an appropriate antioxidant substrate, with increased oral bioavailability, for patients with gastrointestinal disorders.

Study Regarding a New Extended-Release Calcium Ascorbate and Hesperidin Solid Oral Formulation

“…Calcium ascorbate was used for vitamin C intake to reduce the high acid side effects at the gastric level [22]. In addition, a slow-release pharmaceutical formulation was chosen to ensure a gradual release of the active ingredients and a prolonged effect (prolonged-release tablets) [23].…”

Multi-center study of residual gastric volume and bowel preparation after the usage of 1L and 2L polyethylene glycol in Korea

“…Vitamin C is a necessary element for our body, but if taken in excess, side effects such as diarrhea, abdominal pain, acid indigestion, and frequent urination may occur. [ 29 , 30 ] Also an increase in gastric juice secretion may lead to a decrease in pH, [ 31 ] which may cause an increase in RGV. Therefore, the causes of the increase in RGV of 1L PEG may be various, but what we know from this study is that it is desirable to reduce water intake within 5 hours before the colonoscopy.…”

Phenytoin Toxicity with High Dose, Concomitant Ascorbic Acid Dosing

“…[6][7][8] However, other studies point to ascorbic acid overall increasing acid output, thus lowering pH. 9 Phenytoin metabolism is multifactorial, being affected by protein binding, oral formulation, pharmacogenomics (CYP2C9, CYP2C19) and possibly altered pH in the stomach and/or small intestine. 6,[10][11] Altered pH from AA affecting absorption and/or phenytoin metabolism could have been contributory to the patient's elevated phenytoin levels.…”

“…6,[10][11] Altered pH from AA affecting absorption and/or phenytoin metabolism could have been contributory to the patient's elevated phenytoin levels. 3,9 The patient was taking 1,600 mg of ascorbic acid with his phenytoin dose. 1,600 mg of ascorbic acid in the stomach likely temporarily changes the acidity of the stomach and possibly the proximal small intestine.…”