Effects of food on the pharmacokinetics of a gemigliptin/metformin sustained-release 50/1,000 mg (25/500 mg x 2 tablets) fixed-dose combination tablet in healthy male volunteers

International Journal of Clinical Pharmacology and Therapeutics

Volumn 52, Issue 5, 2014, Pages 381-391

  Choi, Hee Youn ^a   Noh, Yook Hwan ^a   Kim, Yo Han ^a   Kim, Mi Jo ^a   Lee, Shi Hyang ^a   Kim, Jeong Ae ^b   Kim, Bogyeong ^b   Lim, Hyeong Seok ^a   Bae, Kyun Seop ^a  

^a University of Ulsan College of Medicine   (South Korea)

^b LG Chemical Ltd   (South Korea)

Author keywords

DPP 4 inhibitor; Food effect; Gemigliptin; Metformin; Pharmacokinetics

Indexed keywords

CREATINE KINASE; DRUG METABOLITE; GEMIGLIPTIN; GEMIGLIPTIN PLUS METFORMIN; LC 15 0636; METFORMIN; ORAL ANTIDIABETIC AGENT; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; CALIBRATION; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIET RESTRICTION; DIZZINESS; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG TOLERABILITY; FOOD; FOOD DRUG INTERACTION; GEOMETRIC MEAN RATIO; HEMATURIA; HUMAN; HUMAN EXPERIMENT; HYPERTRIGLYCERIDEMIA; LEUKOCYTOSIS; LIMIT OF QUANTITATION; LIPID DIET; LOOSE FECES; MALE; MAXIMUM PLASMA CONCENTRATION; NAUSEA; NECK PAIN; NORMAL HUMAN; OPEN STUDY; PHARMACOLOGICAL PARAMETERS; RANDOMIZED CONTROLLED TRIAL; RETENTION TIME; SIDE EFFECT; SINGLE DRUG DOSE; SUSTAINED RELEASE PREPARATION; TIME TO MAXIMUM PLASMA CONCENTRATION; UPPER RESPIRATORY TRACT INFECTION;

ADMINISTRATION, ORAL; ADULT; AREA UNDER CURVE; CROSS-OVER STUDIES; DELAYED-ACTION PREPARATIONS; DRUG ADMINISTRATION SCHEDULE; DRUG COMBINATIONS; FASTING; FOOD-DRUG INTERACTIONS; HALF-LIFE; HEALTHY VOLUNTEERS; HUMANS; HYPOGLYCEMIC AGENTS; MALE; METABOLIC CLEARANCE RATE; METFORMIN; PIPERIDONES; POSTPRANDIAL PERIOD; PYRIMIDINES; REPUBLIC OF KOREA; SEX FACTORS; TABLETS; YOUNG ADULT;

EID: 84900459506     PISSN: 09461965     EISSN: None     Source Type: Journal    
DOI: 10.5414/CP202038     Document Type: Article

References (26)

1. CDC. National Diabetes Fact Sheet, 2011. US Department of Health and Human Services. In: Services UDoHaH: CDC; 2011. http://www.cdc.gov/diabetes/ pubs/pdf/ndfs-2011.pdf.
2. IDF. Diabetes Atlas. 5th edn: International Diabetes Federation; 2012. http://www.idf.org/diabetesatlas/5e/Update2012.
3. Stratton IM, Adler AI, Neil HA, Matthews DR, Manley SE, Cull CA, Hadden D, Turner RC, Holman RR. Association of glycaemia with macrovascular and microvascular complications of type 2 diabetes (UKPDS 35): prospective observational study. BMJ. 2000; 321: 405-412. CrossRef PubMed (Pubitemid 30609442)
4. Nathan DM, Buse JB, Davidson MB, Heine RJ, Holman RR, Sherwin R, Zinman B. Management of hyperglycemia in type 2 diabetes: A consensus algorithm for the initiation and adjustment of therapy: a consensus statement from the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care. 2006; 29: 1963-1972. CrossRef PubMed (Pubitemid 44156663)
5. Bailey CJ, Turner RC. Metformin. N Engl J Med. 1996; 334: 574-579. CrossRef PubMed (Pubitemid 126537875)
6. Nathan DM, Buse JB, Davidson MB, Ferrannini E, Holman RR, Sherwin R, Zinman B; American Diabetes Association; European Association for Study of Diabetes. Medical management of hyperglycemia in type 2 diabetes: a consensus algorithm for the initiation and adjustment of therapy: a consensus statement of the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care. 2009; 32: 193-203. CrossRef PubMed
7. Turner RC, Cull CA, Frighi V, Holman RR; UK Prospective Diabetes Study (UKPDS) Group. Glycemic control with diet, sulfonylurea, metformin, or insulin in patients with type 2 diabetes mellitus: progressive requirement for multiple therapies (UKPDS 49). JAMA. 1999; 281: 2005-2012. CrossRef PubMed (Pubitemid 29254858)
8. Green BD, Flatt PR, Bailey CJ. Dipeptidyl peptidase IV (DPP IV) inhibitors: A newly emerging drug class for the treatment of type 2 diabetes. Diab Vasc Dis Res. 2006; 3: 159-165. CrossRef PubMed (Pubitemid 44902481)
9. Drucker DJ, Nauck MA. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet. 2006; 368: 1696-1705. CrossRef PubMed (Pubitemid 46048557)
10. Charbonnel B, Karasik A, Liu J, Wu M, Meininger G; Sitagliptin Study 020 Group. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes inadequately controlled with metformin alone. Diabetes Care. 2006; 29: 2638-2643. CrossRef PubMed (Pubitemid 44912191)
11. DeFronzo RA, Hissa MN, Garber AJ, Luiz Gross J, Yuyan Duan R, Ravichandran S, Chen RS; Saxagliptin 014 Study Group. The efficacy and safety of saxagliptin when added to metformin therapy in patients with inadequately controlled type 2 diabetes with metformin alone. Diabetes Care. 2009; 32: 1649-1655. CrossRef PubMed
12. Hinke SA, Kühn-Wache K, Hoffmann T, Pederson RA, McIntosh CH, Demuth HU. Metformin effects on dipeptidylpeptidase IV degradation of glucagon-like peptide-1. Biochem Biophys Res Commun. 2002; 291: 1302-1308. CrossRef PubMed (Pubitemid 34694333)
13. Migoya EM, Bergeron R, Miller JL, Snyder RN, Tanen M, Hilliard D, Weiss B, Larson P, Gutierrez M, Jiang G, Liu F, Pryor KA, Yao J, Zhu L, Holst JJ, Deacon C, Herman G, Thornberry N, Amatruda J, Williams-Herman D, et al. Dipeptidyl pepti-dase-4 inhibitors administered in combination with metformin result in an additive increase in the plasma concentration of active GLP-1. Clin Pharmacol Ther. 2010; 88: 801-808. CrossRef PubMed
14. Yang SJ, Min KW, Gupta SK, Park JY, Shivane VK, Pitale SU, Agarwal PK, Sosale A, Gandhi P, Dharmalingam M, Mohan V, Mahesh U, Kim DM, Kim YS, Kim JA, Kim PK, Baik SH. A multicentre, multinational, randomized, placebo-controlled, double-blind, phase 3 trial to evaluate the efficacy and safety of gemigliptin (LC15-0444) in patients with type 2 diabetes. Diabetes Obes Metab. 2013; 15: 410-416. CrossRef PubMed
15. Lim KS, Kim JR, Choi YJ, Shin KH, Kim KP, Hong JH, Cho JY, Shin HS, Yu KS, Shin SG, Kwon OH, Hwang DM, Kim JA, Jang IJ. Pharmacokinetics, pharmacodynamics, and tolerability of the dipeptidyl peptidase IV inhibitor LC15-0444 in healthy Korean men: a dose-block-randomized, double-blind, placebo-controlled, ascending single-dose, Phase I study. Clin Ther. 2008; 30: 1817-1830. CrossRef PubMed
16. Rhee EJ, Lee WY, Min KW, Shivane VK, Sosale AR, Jang HC, Chung CH, Nam-Goong IS, Kim JA, Kim SW; Gemigliptin Study 006 Group. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor gemigliptin compared with sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes inadequately controlled with metformin alone. Diabetes Obes Metab. 2013; 15: 523-530. CrossRef PubMed
17. Guideline on Clinical Development of Fixed Combinations of Medical Products (Korean). Ministry of Food and Drug Safety, Korea. http://www.mfds.go. kr/index.do?x=17&searchkey=notice-number&mid=560 &searchword=B1- 2009-2-005&y=11&pageNo=1&seq=4510&cmd=v
18. National Institute of Toxicological Research. Guideline on Food-Effect Bioavailability and Fed Bioequivalence Studies (Korean). National Institute of Toxicological Research; 2005. http://www.mfds.go.kr/index.do?seq=714&mid= 102&cmd=v&cd=
19. Guidance for Industry: Food-effect Bioavailability and Fed Bioequivalence Studies U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER); 2002. http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/ Guidances/UCM070241.pdf.
20. Company B-MS. Glucophage XR(metformin hydrochloride extended-release tablets) FDA approved drug products label information. Princeton, NJ: Bristol-Myers Squibb Company; 2008. Available at: http://www.accessdata.fda.gov/ drugsatfda-docs/label/2008/020357s031,021202s016lbl.pdf.
21. International Conference on Harmonisation of technical requirements for registration of pharmaceuticals for human use. ICH harmonized tripartite guideline: Guideline for Good Clinical Practice. J Postgrad Med. 2001; 47: 45-50. PubMed
22. World Medical Association Inc. Declaration of Helsinki. Ethical principles for medical research involving human subjects. J Indian Med Assoc. 2009; 107: 403-405. PubMed
23. Rowland M, Tozer T. N. Clinical Pharmacokinetics and Pharmacodynamics: Concepts and Applications. Philadelphia, Pa: Lippincott Williams & Wilkins 2011.
24. Genser D. Food and drug interaction: consequences for the nutrition/health status. Ann Nutr Metab. 2008; 52 (Suppl 1): 29-32. CrossRef PubMed (Pubitemid 351496702)
25. Won CS, Oberlies NH, Paine MF. Mechanisms underlying food-drug interactions: inhibition of intestinal metabolism and transport. Pharmacol Ther. 2012; 136: 186-201. CrossRef PubMed
26. Noh YH, Lim HS, Jin SJ, Kim MJ, Kim YH, Sung HR, Choi HY, Bae KS. Effects of ketoconazole and rifampicin on the pharmacokinetics of gemigliptin, a dipeptidyl peptidase-IV inhibitor: a crossover drug-drug interaction study in healthy male Korean volunteers. Clin Ther. 2012; 34: 1182-1194. CrossRef PubMed