bioavailability of 5 mg of levamlodipine maleate tablets versus 10 mg of amlodipine besylate tablet in healthy subjects

Conditions: Hypertension

Summary: this study are (1) to assess the relative bioavailability (ba) of a single oral dose of either 5 mg of levamlodipine maleate tablets from cspc or 10 mg of amlodipine besylate tablet (norvasc®) from pfizer inc. under fasting condition in male and female healthy subjects; and (2) to evaluate food effect on the pk profile of levamlodipine maleate tablets from cspc.

this study consists of 2 parts: part 1 will be a randomized, open-label, single-dose, two-way crossover study to assess the relative ba of levamlodipine maleate tablets from cspc (test) versus amlodipine besylate tablet norvasc® from pfizer inc. (reference) after a single oral administration under fasted conditions in male and female healthy subjects. approximately 32 healthy subjects will be enrolled in the us to obtain 27 completed subjects. part 2 will be a single-arm, open-label, single-dose phase to assess food effect on the pk profile of levamlodipine maleate tablets from cspc. subjects who have completed part 1 will be rolled over to part 2 after a wash-out period for at least 14-days since the last dosing. subjects will receive a single oral administration of study drug under a high-fat / high-calorie meal that should derive approximately 150, 250 and 500-600 calories from protein, carbohydrate and fat, respectively.

Eligibility criteria:
key inclusion criteria: 1. women of childbearing potential (wocbp) must have a negative pregnancy test at screening and be practicing a medically acceptable method of contraception with an annual failure rate of less than 1% during the study and 60 days after discontinuation of study treatment. 2. considered healthy by the principal investigator, based on a detailed medical history, full physical examination, clinical laboratory tests, 12-lead ecg and vital signs; 3. nonsmoker, defined as not having smoked or used any form of tobacco in more than 6 months before screening; 4. body mass index (bmi) of 19 to 30 kg/m2 inclusive and body weight not less than 50 kg; exclusion criteria: 1. clinically significant history of gastrointestinal, cardiovascular, musculoskeletal, endocrine, hematologic, psychiatric, renal, hepatic, bronchopulmonary, neurologic, immunologic, lipid metabolism disorders, or drug hypersensitivity; 2. mean systolic blood pressure of three measurements \>140 mmhg, or a mean diastolic blood pressure of three measurements \>90 mmhg at screening. 3. known or suspected malignancy; 4. positive blood screen for human immunodeficiency virus (hiv), or hepatitis b surface antigen (hbsag), or hepatitis c virus (hcv); 5. a history of seizure. however, a history of febrile seizure is allowed; 6. positive pregnancy test result, or plan to become pregnant if female; 7. a hospital admission or major surgery within 30 days prior to screening; 8. participation in any other investigational drug trial within 30 days prior to screening; 9. dsm-v substance use disorder within 6 months prior to screening; 10. a positive result for alcohol or drugs of abuse at screening or admission; 11. tobacco use within 6 months prior to screening; 12. an unwillingness or inability to comply with food and beverage restrictions during study participation; 13. donation or blood collection of more than 1 unit (approximate 450 ml) of blood (or blood products) or acute loss of blood during the 90 days prior to screening; 14. use of prescription or over-the-counter (otc) medications, and herbal medicines (including st john's wort, herbal teas, garlic extracts) within 14 days prior to dosing; 15. a history of suicide attempt in the past 12 months and/or seen by the investigator as having a significant history of risk of suicide or homicide; 16. a history of intolerance or hypersensitivity to amlodipine or any excipients; 17. an unwillingness of male participants to use appropriate contraceptive measures if engaging in sex intercourse with a female partner of childbearing potential during the study and 60 days after discontinuation of study treatment.