Carboxymethylcellulose sodium improves the pharmacodynamics of 1-deoxynojirimycin by changing its absorption characteristics and pharmacokinetics in rats.

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.