Bioequivalence study in healthy Thai male volunteers Sitagliptin 100 mg Film-coated Tablets (SITATIN (100 mg)) and Reference Product (JanuviaTM (100 mg)) in Healthy Thai Volunteers under Fasting Conditions
Conditions
Interventions
Each film-coated tablet contains 128.5 mg of sitagliptin phosphate monohydrate, which is equivalent to 100 mg of free base.,Each film-coated tablet contains 128.5 mg of sitagliptin phosphate monohydra
Experimental Drug,Active Comparator Drug
Generic sitagliptin 100 mg film-coated tablet, SITATIN (100 mg),Sitagliptin 100 mg film-coated tablet, JanuviaTM (100 mg)
Sponsors
International Bio Service Co., Ltd.
Eligibility
Sex/Gender
All
Age
18 Years to 55 Years
Inclusion criteria
Inclusion criteria: 1. Healthy Thai male or female subjects between the ages of 18 to 55 years. 2. Body mass index between 18.5 to 30.0 kg/m2. 3. Normal laboratory values, including vital signs and physical examination, for all parameters in clinical laboratory tests at screening. Any abnormalities from the normal or reference range will be carefully considered clinically relevant by the physician as individual cases, documented in study files prior to enrolling the subject in this study. 4. Non-pregnant woman (negative pregnancy test) and not currently breast feeding. 5. Female subjects abstain from either hormonal methods of contraception (including oral or transdermal contraceptives, injectable progesterone, progestin subdermal implants, progesterone-releasing IUDs, postcoital contraceptive methods) or hormone replacement therapy for at least 28 days prior to check-in in Period 1. Injectable contraceptives e.g. Depo-Provera will be discontinued at least 6 months prior to check-in in Period 1. Subjects agree to use acceptable non-hormonal contraceptive methods such as condom, diaphragm, foams, jellies, or abstinence for at least 14 days prior to check-in in Period 1 until 7 days after the end of study in Period 2. Female subjects of non-childbearing potential must meet at least one of the following criteria prior to check-in in Period 1: - Postmenopausal for at least 1 year or - Surgically sterile (bilateral tubal ligation, bilateral oophorectomy or hysterectomy) at least 6 months 6. Male subjects who are willing or able to use effective contraceptive e.g. condom or abstinence after check-in in Period 1 until 7 days after the end of study in Period 2. 7. Have voluntarily given written informed consent (signed and dated) by the subject prior to participating in this study.
Exclusion criteria
Exclusion criteria: 1. History serious hypersensitivity reactions, i.e., anaphylaxis, angioedema, exfoliative skin conditions including Stevens-Johnson syndrome, to sitagliptin, another dipeptidyl peptidase-4 (DPP-4) inhibitors or any other ingredient of the product. 2. History or evidence of clinically significant renal, hepatic, gastrointestinal, hematological (e.g. anemia), endocrine (e.g. hyper/hypothyroidism, diabetes mellitus), pulmonary or respiratory (e.g. asthma), cardiovascular (e.g. hyper/hypotension), psychiatric, neurologic (e.g. seizures), allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing) or any significant ongoing chronic medical illness. 3. History or evidence of type 1 diabetes mellitus, diabetic ketoacidosis. 4. History or evidence of acute pancreatitis including fatal and non-fatal hemorrhagic or necrotizing pancreatitis. 5. History or evidence of genital mycotic infections, urinary tract infections within 14 days prior to check-in in each period. 6. History or evidence of severe joint pain. 7. History or evidence of bullous pemphigoid. 8. History or evidence of cardiovascular bleeding, gastrointestinal bleeding, gastric or duodenal or peptic ulcer. 9. Investigation with blood sample shows fasting blood glucose level less than 70 mg/dl or more than 99 mg/dl at screening. 10.History of problems with swallowing tablet or capsule. 11.History of sensitivity to heparin or heparin-induced thrombocytopenia. 12.Any condition possibly affecting drug absorption e.g. gastrectomy, enterectomy, gastritis or duodenal or gastric ulceration other than appendectomy. 13.History of diarrhea or vomiting within 24 hours prior to check-in in each period. 14.History or evidence of drug addict or investigation with urine sample shows a positive test for drug of abuse (morphine, marijuana or methamphetamine). 15.12-lead ECG demonstrating QTc >450 msec, a QRS interval >120 msec or with an abnormality considered clinically significant at screening. If QTc exceeds 450 msec, or QRS exceeds 120 msec, the ECG will be repeated two more times and the average of the three QTc or QRS values will be used to determine the subjects eligibility. 16.Investigation with blood sample shows positive test for HBsAg. 17.Abnormal liver function, is greater than or equal to 1.5 times of upper normal limit of reference range for ALT, AST or bilirubin levels at screening laboratory test. 18.Have eGFR (CKD-EPI) < 45 mL/min/1.73 m2 based on serum creatinine results, at the screening laboratory test or during enrollment. 19.History or evidence of habitual use of tobacco or nicotine containing products and cannot abstain for at least 48 hours prior to check-in in Period 1 and continued for entire duration of the study. 20.History or evidence of alcoholism or harmful use of alcohol within 2 years prior to screening i.e., alcohol consumption of more than 14 standard drinks per week for men and 7 standard drinks per week for women (A standard drink is defined as 360 mL of beer or 150 mL of wine or 45 mL of 40% distilled spirits, such as rum, whisky, brandy, etc.). 21.History or evidence of alcohol consumption or alcohol-containing products and cannot abstain for at least 48 hours prior to check-in in Period 1 and continued for entire duration of the study or alcohol breath test shows positive result. In case of alcohol breath test result represents the alcohol concentration range of 1 - 10 mg%
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Cmax, AUC0-tlast and AUC0-infinity 0-48 hrs, Washout period 6-14 days Mass spectrometry (LC-MS/MS) | — |
Secondary
| Measure | Time frame |
|---|---|
| Tmax, t1/2, AUC0-tlast/AUC0-infinity, AUC%extrapolate, lambdaz and MRT 0-48 hrs, Washout period 6-14 days Mass spectrometry (LC-MS/MS) | — |
Countries
Thailand
Contacts
Public ContactThanaporn Wongyai
International Bio Service Co., Ltd.
Outcome results
None listed