Lee Joon-Kyung, Jung Sang-Hyuk, Lee Sang-Eun, Han Joo-Hui, Jo Eunji, Park Hyun-Soo, Heo Kyung-Sun, Kim Deasun, Park Jeong-Sook, Myung Chang-Seon
Department of Physical Pharmacy, College of Pharmacy, Chungnam National University, Daejeon 34134, Korea.
Department of Pharmacology, College of Pharmacy, Chungnam National University, Daejeon 34134, Korea.
Korean J Physiol Pharmacol. 2018 Jan;22(1):35-42. doi: 10.4196/kjpp.2018.22.1.35. Epub 2017 Dec 22.
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 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 C value of calcium ascorbate (91.0 ng/ml) was higher than that of ascorbic acid (74.8 ng/ml). However, their T 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.
抗坏血酸是水果和蔬菜中最著名的营养补充剂和抗氧化剂之一。已开发出抗坏血酸钙以减轻抗坏血酸酸度引起的胃部刺激。本研究的目的是比较抗坏血酸钙和抗坏血酸,重点关注它们在大鼠模型中的抗氧化活性以及对胃液pH值、总酸分泌量和胃蛋白酶分泌的影响,以及药代动力学参数。抗坏血酸钙和抗坏血酸具有相似的抗氧化活性。然而,抗坏血酸钙可提高胃液pH值,而抗坏血酸则会增加总酸分泌量。在大鼠幽门结扎诱导的溃疡模型中,抗坏血酸钙可提高胃液pH值而不改变总酸分泌量。给大鼠单次口服100 mg/kg抗坏血酸剂量的抗坏血酸钙后,其血浆浓度高于单独使用抗坏血酸时的浓度。抗坏血酸钙的曲线下面积(AUC)值比抗坏血酸高1.5倍,抗坏血酸钙的C值(91.0 ng/ml)高于抗坏血酸(74.8 ng/ml)。然而,它们的T值相似。因此,尽管抗坏血酸钙显示出与抗坏血酸相当的抗氧化活性,但它可以减轻抗坏血酸引起的胃部高酸度,使其适合用于改善抗坏血酸的副作用。此外,抗坏血酸钙对于胃肠道疾病患者可能是一种合适的抗氧化底物,具有更高的口服生物利用度。