Bioequivalence Study of Gefitinib Tablets Under Fasting Conditions

An Open-Label，Randomized, Single-Dose, 2-way Crossover Bioequivalence Study. During each session, the subjects were randomly assigned in a 1:1 ratio to receive a single 250-mg dose of either the test formulation(Hunam Kelun) or the reference formulation(Iressa® Astrazeneca), and vice versa, with a 21-day washout period between administration periods.

Inclusion criteria

• Healthy male subjects.
• At least 18 years of age .
• Weight at least 50kg and body mass index between 19 and 26 kg/m2.
• Informed consent and voluntary to sign a written informed consent.
• Can communicate with researchers and complete the study in accordance with the provisions of the research.

Exclusion criteria

• Abnormal diagnostic findings, and clinical significances determined by researchers (physical examination,vital sign, ECG,X-ray,blood routine examination, urine routine examination,blood biochemical examination and coagulation test).
• Having functional gastrointestinal disease or inadequate secretion of gastric acid or is treated for a acid suppression. Which including gastro upset, dyspepsia, gastritis, gastric ulcer, duodenal ulcer, gastric secrete melanoma, etc.
• Taking drugs that alter the environment of the gastrointestinal，especially alter the gastrointestinal pH，within 30 days before the first dose. Such as Proton pump inhibitors：thiophene, omeprazole, lansoprazole, esomeprazole, etc . and H2 antagonist ranitidine：cimetidine, famotidine, etc .and antacids hydrogen carbonate Sodium, magnesium oxide, aluminum hydroxide, magnesium trisilicate, etc .and gastric mucosal protective agent：sucralfate，and so on.
• Not comply with a unified diet or has swallowing difficulties.
• Allergic to any ingredient or excipients of the study drug.
• History of gastrointestinal disorders and severe liver and kidney diseases ，which affect the absorption or metabolism of drugs so far.
• History of ocular surface damaging diseases (such as corneal perforation, ulcers, etc.).
• History of serious blood diseases.
• With skin, cardiovascular, liver, kidney, digestive, neurological, psychiatric, metabolic disorders, or any other disease that can interfere with the results of the trial.
• History of long-term excessive drinking (more than 8 cups a day, 1 cup = 250 mL) of tea, coffee or caffeinated beverages，or 48 hours before the first dose intake of any food or drink containing caffeine (such as coffee, tea, chocolate, etc.).
• Ingested any drinks or foods that are rich in xanthine and grapefruit or affect the drug absorption, distribution, metabolism and excretion.
• A positive result in breath alcohol test or previous alcohol abuse (ie, men drink more than 28 standard units a week [1 standard unit defined as containing 14 grams of alcohol, such as would be found in a standard shot of hard liquor, a 12-ounce bottle of beer, or a 5-ounce glass of wine] Or regular drinking(more than 14 standard units of alcohol per week) within 6 months before the trial.
• Daily intake of more than 3 cigarettes from 3 months before the study to 48 hours before the first dose or intake of tobacco or any type of tobacco product within 48 hours before the first dose.
• Taking drugs that interact with gefitinib （such as CYP3A4 inhibitors： itraconazole, ketoconazole, clotrimazole, Ritonavir, etc .and CYP3A4/5 inducers：rifampicin, carbamazepine, phenobarbital, phenytoin, dexamethasone, etc .and CYP2D6 inhibitors：Fluoxetine, paroxetine , etc .） within 30 days before the first dose. And use of any prescription drugs, non-prescription drugs, Chinese herbal medicine, health products within 14 days before the first dose.
• Volunteer in any other clinical drug study or taking any clinical trial drug within 3 months prior to this study.
• Blood donation or lost more than 450mL blood within 3 months prior to the study，or has a plan to donate blood or blood components within the study period or within 3 months after the end of study.
• Suffering from a serious illness or having undergone major surgical procedures within 1 years before the firs dose.
• Abnormal blood coagulation, or having a known tendency of severe bleeding.
• A positive result in drug test or existing drug abuse (eg, morphine, marijuana, methamphetamine, dimethylene bisoxamine amphetamines, ketamine, etc.) within 1 year prior to the trial.
• A positive result in hepatitis B surface antigen (HBsAg), anti-hepatitis C virus (HCV) antibodies, a syphilis test, or an human immunodeficiency virus (HIV) test.
• Having fertility planning or reluctant to take appropriate contraceptive during the study or within 6 months after the study.
• Other unfavorable factors diagnosed by investigators.