title: Carboxymethylcellulose sodium improves the pharmacodynamics of 1-deoxynojirimycin by changing its absorption characteristics and pharmacokinetics in rats.
abstract: 1-Deoxynojirimycin (DNJ) has excellent inhibitory activity against alpha-glucosidase and can therefore decrease the postprandial blood glucose level in humans. However, a major limitation of DNJ is its fast absorption rate compared with other alpha-glucosidase inhibitors. In this study, we investigated the effect of adjuvants on the pharmacokinetics of DNJ, and found that carboxymethylcellulose sodium (CMCNa) can remarkably improve the activity of DNJ on glucose levels. When DNJ was used in combination with CMCNa, its absorption was suppressed and delayed by CMCNa. CMCNa can also change the pharmacokinetics of DNJ in rats. Pharmacodynamics were further studied using the oral glucose tolerance test, and the results confirmed that CMCNa can enhance DNJ's modulation of glucose level. All the results indicate that carboxymethylcellulose sodium can improve the pharmacodynamics of 1-deoxynojirimycin by changing the absorption characteristics and pharmacokinetics of DNJ in rats.
authors.affiliation: College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, China.
authors.forename: Liqiang
authors.initials: L
authors.lastname: Wang
authors.forename: Jiamin
authors.initials: J
authors.lastname: Peng
authors.forename: Xin
authors.initials: X
authors.lastname: Wang
authors.forename: Xiaodan
authors.initials: X
authors.lastname: Zhu
authors.forename: Binfeng
authors.initials: B
authors.lastname: Cheng
authors.forename: Jie
authors.initials: J
authors.lastname: Gao
authors.forename: Min
authors.initials: M
authors.lastname: Jiang
authors.forename: Gang
authors.initials: G
authors.lastname: Bai
authors.forename: Yuanyuan
authors.initials: Y
authors.lastname: Hou
mesh_terms: D017485:1-Deoxynojirimycin / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D000277:Adjuvants, Pharmaceutic; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D005079:Excipients; D005951:Glucose Tolerance Test; D065089:Glycoside Hydrolase Inhibitors; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D007408:Intestinal Absorption / Q000187:drug effects; D008297:Male; D013058:Mass Spectrometry; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000277:Adjuvants, Pharmaceutic; D001786:Blood Glucose; D004791:Enzyme Inhibitors; D005079:Excipients; D065089:Glycoside Hydrolase Inhibitors; D007202:Indicators and Reagents; D017485:1-Deoxynojirimycin; D002266:Carboxymethylcellulose Sodium