| Customization: | Available |
|---|---|
| CAS No.: | 864070-44-0 |
| Formula: | C23h27clo7 |
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| Product Name | Empagliflozin |
| CAS | 864070-44-0 |
| Appearance | White crystalline powder |
| MF | C23H27ClO7 |
| MW | 450.9 |
pharmacokinetics
absorb
No clinically meaningful difference was observed in the pharmacokinetic profile of Englizin between healthy volunteers and patients with type 2 diabetes. The peak plasma concentration of Englipzin was reached 1.5 hours after oral administration. After that, the plasma concentration decreased biphasically, with a rapid distribution phase and a relatively slow terminal phase. Steady-state mean plasma AUC and Cmax were 1870 nmol·h/L and 259 nmol/L (10 mg Englipzin once daily) and 4740 nmol·h/L and 687 nmol/L (25 mg englipzin once daily), respectively. Throughout the therapeutic dose range, systemic exposure to Englipzin increased proportionally with dose. The single administration and steady-state pharmacokinetic parameters of enaglipzin were similar, suggesting that the pharmacokinetics were linear over time.
The administration of 25 mg of Englipzin after a high-fat and high-calorie meal resulted in slightly lower exposure, with approximately 16% reductions in AUC and 37% reductions in Cmax compared to the fasting state. The observed effects of food on the pharmacokinetics of enoglizin are not clinically significant, and Enoglizin can be given after eating or on an empty stomach.
distribution
The apparent steady-state distribution volume was estimated to be 73.8 L based on population pharmacokinetic analysis. After oral [14C] -Englizin solution in healthy subjects, erythrocyte zoning was approximately 36.8% and plasma protein binding was 86.2%.
metabolism
No major metabolites of enoglizin have been detected in human plasma, and the most abundant metabolites are the three glucuronide conjugates (2-O-, 3-O-, and 6-O glucuronide). The total body exposure of each metabolite is less than 10% of the total substance associated with the drug. In vitro studies have shown that the main metabolic pathway of enoglizin in human body is glucuronic acid reaction through uridine 5' -diphospho-glucuronyltransferases UGT2B7, UGT1A3, UGT1A8 and UGT1A9.
eliminate
Based on population pharmacokinetic analysis, the estimated apparent terminal elimination half-life of Englipzin was 12.4 hours and the apparent oral clearance was 10.6 L/ hour. After once daily administration, accumulation of up to 22% relative to plasma AUC was observed at homeostasis, which is consistent with the half-life of Englipzin. After oral [14C] -Englizin solution in healthy subjects, approximately 95.6% of drug-associated radioactivity was eliminated with fecal (41.2%) or urine (54.4%). The vast majority of drug-related radioactivity recovered in feces is the maternal drug prototype, and about half of the drug-related radioactivity excreted in urine is the maternal drug prototype.
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