5-CNAC is an orally active enhancer of absorption, with no pharmacological activity on its own. 5-CNAC can significantly enhance the absorption efficiency of the drug (such as Salmon calcitonin ) when administered together with it in the gastrointestinal tract. 5-CNAC binds reversibly and non-covalently to peptide drugs, protecting them from degradation by gastrointestinal enzymes, increasing their lipid solubility, promoting passive transcellular absorption, and not damaging the integrity of the intestinal epithelium. 5-CNAC can be used in the research of adjuvants for orally administered peptide agents [1] [2].
In Vitro, 5-CNAC (0.01-500 μg/mL; 30 min) exhibits high plasma protein binding (>99%) in human plasma and serum in vitro at concentrations up to 100 μg/mL, with binding site saturation observed at 500 μg/mL[1].
References:
[1]. Gschwind HP, et al. Metabolism and disposition of the oral absorption enhancer 14C-radiolabeled 8-(N-2-hydroxy-5-chlorobenzoyl)-amino-caprylic acid (5-CNAC) in healthy postmenopausal women and supplementary investigations in vitro. Eur J Pharm Sci. 2012 Aug 30;47(1):44-55.
[2]. Karsdal MA, et al. The effect of oral salmon calcitonin delivered with 5-CNAC on bone and cartilage degradation in osteoarthritic patients: a 14-day randomized study. Osteoarthritis Cartilage. 2010;18(2):150-159.
In Vitro, 5-CNAC (0.01-500 μg/mL; 30 min) exhibits high plasma protein binding (>99%) in human plasma and serum in vitro at concentrations up to 100 μg/mL, with binding site saturation observed at 500 μg/mL[1].
References:
[1]. Gschwind HP, et al. Metabolism and disposition of the oral absorption enhancer 14C-radiolabeled 8-(N-2-hydroxy-5-chlorobenzoyl)-amino-caprylic acid (5-CNAC) in healthy postmenopausal women and supplementary investigations in vitro. Eur J Pharm Sci. 2012 Aug 30;47(1):44-55.
[2]. Karsdal MA, et al. The effect of oral salmon calcitonin delivered with 5-CNAC on bone and cartilage degradation in osteoarthritic patients: a 14-day randomized study. Osteoarthritis Cartilage. 2010;18(2):150-159.
















