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The Objectives of this study is to evaluate the pharmacokinetics and safety of multiple oral doses of probucol in healthy male subjects.
This is a single dose, single period, multiple administration, open-labeled trial in one investigation center.
The screening examination will be completed from Day -14 to Day -2 before investigational medicinal product (IMP) administration. The subjects will be hospitalized on Day -1. From Day 1 (the next day), the subjects will receive probucol twice daily (BID). for 14 consecutive days. On Day 18, the subjects can be discharged after the safety evaluation. The follow-up visit will occur on Day 6, 9, 12, 15, 19, 27 (totally 41 days) after the final dosing day.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| probucol in healthy male subjects | Other | multiple oral doses of probucol in single group of healthy male subjects |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Probucol | Drug | 250mg (1 tablet) bid. p.o for 14 consecutive days |
|
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetic parameters | Pharmacokinetic parameters: Day 1 (Plasma PK parameters over the 24h dosing period): Cmax, Cmax1, Cmax2, tmax1, tmax2, AUC (0-10)h, AUC (10-24)h, AUC24h, C24h; Day3,5,7,9,11,12,13:C24h; Day 14: Cmax, Cmax1, Cmax2, tmax1, tmax2, AUC (0-10)h, AUC (10-24)h, AUC24h, C24h, Clast, tlast, t1/2,z,Lambdaz, DF, CL/F, Vz/F, AUC_%Extrap; Accumulation evaluation parameters: Rpred, R14,ac(AUC24h), R14,ac(Cmax), R14,ac(C24h), R14,ac[AUC(0-10h)], R14,ac[AUC(10-24h)], R14,ac(Cmax1), R14,ac(Cmax2). | Day 1, 3, 5, 7, 9, 11, 12, 13, 14 |
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Inclusion Criteria:
Exclusion Criteria:
Subjects with hypersensitivity or a history of hypersensitivity to any drug (any prescription or over-the-counter [OTC] drug)
Subjects who meet any of the following lipid criteria in the fasting state (at time of screening examination)
LDL-C: ≥ 140 mg/dL
TC: ≥ 220 mg/dL
HDL-C: < 40 mg/dL
TG: ≥ 150 mg/dL
Subjects with electrocardiogram (ECG) results showing AV block or with both QTc and QRS width outside the standard values of the ECG laboratory (at time of screening examination)
Subjects with alcohol or drug dependence or a history of drug abuse
Subjects who have a positive result in an infectious disease test or urine drug test (at time of screening examination)
Use of any of the following within the specified period prior to scheduled investigational medicinal product (IMP) administration
Use of any other investigational drug within 16 weeks prior to scheduled IMP administration in the present trial
Plasmapheresis or plateletpheresis within 2 weeks or whole blood collection (blood donation, etc) cumulatively exceeding 200 mL within 4 weeks, 400 mL within 12 weeks, or 1200 mL within 1 year prior to scheduled IMP administration
Subjects whose body weight is less than 50 kg (at time of screening examination)
Subjects who are scheduled for examination or treatment at any other hospital or clinic during the trial period
Subjects otherwise judged by the investigator or sub investigator to be inappropriate for inclusion in the trial
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| Name | Affiliation | Role |
|---|---|---|
| Pei Hu, PHD | Clinical Pharmacology Research Center of Peking Union Medical College Hospital | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Clinical Pharmacology Research Center, Peking Union Medical College Hospital | Beijing | China |
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| ID | Term |
|---|---|
| D011341 | Probucol |
| ID | Term |
|---|---|
| D010636 | Phenols |
| D001555 | Benzene Derivatives |
| D006841 | Hydrocarbons, Aromatic |
| D006844 | Hydrocarbons, Cyclic |
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| D006838 |
| Hydrocarbons |
| D009930 | Organic Chemicals |