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Relative bioavailability of an empagliflozin 25-mg/linagliptin 5-mg fixed-dose combination tablet .
Int J Clin Pharmacol Ther. 2017 Apr; 55(4):355-367.IJ

Abstract

OBJECTIVE

This relative bioavailability study compared a fixed-dose combination (FDC) tablet of empagliflozin 25 mg/linagliptin 5 mg with the corresponding individual components. In addition, the effect of food on the bioavailability of the FDC was studied, and the standard-dissolving formulation FDC was compared with a slow-dissolving side batch.

METHODS

An open-label, randomized, crossover study design was used (ClinicalTrials.gov Identifier NCT01189201). Healthy volunteers (n = 42) each received three single-dose treatments: FDC standard dissolution, individual tablets, and either FDC standard dissolution with food or FDC slow dissolution. Primary endpoints for relative bioavailability comparisons were area under the plasma concentration-time curve (AUC) over time 0 to the last time point with the plasma concentration above the quantification limit (AUC0-tz) for empagliflozin, AUC from 0 to 72 hours (AUC0-72) for linagliptin, and maximum plasma concentration (Cmax) for both drugs.

RESULTS

In all three comparisons, the 90% confidence intervals for the ratios of AUCs were within the standard acceptance range (80 - 125%) for bioequivalence. Empagliflozin and linagliptin both showed reductions in Cmax after food compared with the fasted state, although overall exposure remained similar. The empagliflozin/linagliptin combinations were well tolerated.

CONCLUSIONS

This study shows that the FDC of empagliflozin 25 mg/linagliptin 5 mg can be regarded as bioequivalent to the individual tablets. Administering the tablet after food or a tablet with a slow-dissolution profile did not have a clinically-relevant impact on the bioavailability of empagliflozin/linagliptin FDC tablets. .

Authors

No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Randomized Controlled Trial

Language

eng

PubMed ID

28290274

Citation

Glund, Stephan, et al. "Relative Bioavailability of an Empagliflozin 25-mg/linagliptin 5-mg Fixed-dose Combination Tablet ." International Journal of Clinical Pharmacology and Therapeutics, vol. 55, no. 4, 2017, pp. 355-367.
Glund S, Mattheus M, Runge F, et al. Relative bioavailability of an empagliflozin 25-mg/linagliptin 5-mg fixed-dose combination tablet . Int J Clin Pharmacol Ther. 2017;55(4):355-367.
Glund, S., Mattheus, M., Runge, F., Rose, P., & Friedrich, C. (2017). Relative bioavailability of an empagliflozin 25-mg/linagliptin 5-mg fixed-dose combination tablet . International Journal of Clinical Pharmacology and Therapeutics, 55(4), 355-367. https://doi.org/10.5414/CP202929
Glund S, et al. Relative Bioavailability of an Empagliflozin 25-mg/linagliptin 5-mg Fixed-dose Combination Tablet. Int J Clin Pharmacol Ther. 2017;55(4):355-367. PubMed PMID: 28290274.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Relative bioavailability of an empagliflozin 25-mg/linagliptin 5-mg fixed-dose combination tablet . AU - Glund,Stephan, AU - Mattheus,Michaela, AU - Runge,Frank, AU - Rose,Peter, AU - Friedrich,Christian, PY - 2017/04/07/accepted PY - 2017/3/16/pubmed PY - 2017/6/20/medline PY - 2017/3/15/entrez SP - 355 EP - 367 JF - International journal of clinical pharmacology and therapeutics JO - Int J Clin Pharmacol Ther VL - 55 IS - 4 N2 - OBJECTIVE: This relative bioavailability study compared a fixed-dose combination (FDC) tablet of empagliflozin 25 mg/linagliptin 5 mg with the corresponding individual components. In addition, the effect of food on the bioavailability of the FDC was studied, and the standard-dissolving formulation FDC was compared with a slow-dissolving side batch. METHODS: An open-label, randomized, crossover study design was used (ClinicalTrials.gov Identifier NCT01189201). Healthy volunteers (n = 42) each received three single-dose treatments: FDC standard dissolution, individual tablets, and either FDC standard dissolution with food or FDC slow dissolution. Primary endpoints for relative bioavailability comparisons were area under the plasma concentration-time curve (AUC) over time 0 to the last time point with the plasma concentration above the quantification limit (AUC0-tz) for empagliflozin, AUC from 0 to 72 hours (AUC0-72) for linagliptin, and maximum plasma concentration (Cmax) for both drugs. RESULTS: In all three comparisons, the 90% confidence intervals for the ratios of AUCs were within the standard acceptance range (80 - 125%) for bioequivalence. Empagliflozin and linagliptin both showed reductions in Cmax after food compared with the fasted state, although overall exposure remained similar. The empagliflozin/linagliptin combinations were well tolerated. CONCLUSIONS: This study shows that the FDC of empagliflozin 25 mg/linagliptin 5 mg can be regarded as bioequivalent to the individual tablets. Administering the tablet after food or a tablet with a slow-dissolution profile did not have a clinically-relevant impact on the bioavailability of empagliflozin/linagliptin FDC tablets. . SN - 0946-1965 UR - https://www.unboundmedicine.com/medline/citation/28290274/Relative_bioavailability_of_an_empagliflozin_25_mg/linagliptin_5_mg_fixed_dose_combination_tablet__ L2 - https://www.dustri.com/nc/journals-in-english?artId=15269 DB - PRIME DP - Unbound Medicine ER -