( g dose. In patients with type 2 d...)An Investigational Study Released at ADA Showed that Initial,Combination Therapy with Januvia (sitagliptin) and Metformin Led to,Improvement in Markers of Beta Cell Function in Patients with Type,2 Diabetes,Health

g dose. In patients with type 2 diabetes administered JANUVIA 100 mg (N=81) or JANUVIA 200 mg (N=63) daily, there were no meaningful changes in QTc interval based on ECG data obtained at the time of expected peak plasma concentration. 12.3 Pharmacokinetics The pharmacokinetics of sitagliptin has been extensively characterized in healthy subjects and patients with type 2 diabetes. After oral administration of a 100 mg dose to healthy subjects, sitagliptin was rapidly absorbed, with peak plasma concentrations (median Tmax) occurring 1 to 4 hours postdose. Plasma AUC of sitagliptin increased in a dose-proportional manner. Following a single oral 100 mg dose to healthy volunteers, mean plasma AUC of sitagliptin was 8.52 ?M-hr, Cmax was 950 nM, and apparent terminal half-life (t1/2) was 12.4 hours. Plasma AUC of sitagliptin increased approximately 14% following 100 mg doses at steady-state compared to the first dose. The intra-subject and inter-subject coefficients of variation for sitagliptin AUC were small (5.8% and 15.1%). The pharmacokinetics of sitagliptin was generally similar in healthy subjects and in patients with type 2 diabetes. Absorption The absolute bioavailability of sitagliptin is approximately 87%. Because coadministration of a high-fat meal with JANUVIA had no effect on the pharmacokinetics, JANUVIA may be administered with or without food. Distribution The mean volume of distribution at steady state following a single 100 mg intravenous dose of sitagliptin to healthy subjects is approximately 198 liters. The fraction of sitagliptin reversibly bound to plasma proteins is low (38%). Metabolism Approximately 79% of sitagliptin is excreted unchanged in the urine with metabolism being a minor pathway of elimination. Following a (14C)sitagliptin oral dose, approximately 16% of the radioactivity was excreted as metabolites of sitagliptin. Six metabolites were detected at trac
'"/>




Page: 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32
Related medicine technology :

1. Phase 3 Results for Dabigatran Etexilate, an Investigational Oral Anticoagulant, Presented Today at the XXIst Congress of the International Society on Thrombosis and Haemostasis
2. Late Breaking Data Released at ADA Showed that the Investigational Use of Januvia and Metformin as Initial Combination Therapy Provided Significant Glucose Lowering Efficacy over 54 Weeks in Patients with Type 2 Diabetes
3. Investigational Study Demonstrated a Re-Establishment of Clinical Improvement with Orencia (Abatacept) in Children with Juvenile Idiopathic Arthritis upon Re-Introduction of Therapy
4. Mercks Investigational Migraine Treatment MK-0974 Significantly Improved Migraine Pain on Several Efficacy Measures in a Phase II Study
5. Data Demonstrated Metastatic Melanoma Response to Investigational Immunotherapy Ipilimumab
6. Investigational Drug Cediranib (AZD2171) Shows Promise in Patients With Recurrent Glioblastoma (GBM)
7. Additional New Data from Satraplatin SPARC Phase 3 Investigational Trial Presented at ASCO Annual Meeting
8. Additional New Data from Satraplatin SPARC Phase 3 Investigational Trial Presented at ASCO Annual Meeting
9. Investigational Cancer Drug Pertuzumab Shows Promising Results in Advanced Breast Cancer When Combined with Herceptin
10. Shire Announces Positive Results of Studies With Guanfacine Extended Release, An Investigational Nonstimulant Medication Filed for the Treatment of ADHD in Children and Adolescents
11. Investigational Study Evaluates the Effectiveness of Aripiprazole in Adolescents With Schizophrenia