Healthy
Conditions
Brief summary
Comparative pharmacokinetics of dipyridamole in two new formulations of Asasantin ER compared to the present commercial formulation
Interventions
DRUGAsasantin ER, new formulation I
DRUGAsasantin ER, new formulation II
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
DOUBLE
Eligibility
Sex/Gender
ALL
Age
21 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
* All participants in the study should be healthy males or females, range from 21 to 50 years of age and be within ± 20 % of their normal weight (Broca-Index) * Prior to admission to the study all volunteers will have given, in accordance with good clinical practice (GCP) and the local legislation, their written informed consent * Subsequently each subject will have his medical history taken and will receive a complete medical examination (incl. blood pressure and pulse rate measurements) as well as a 12-lead ECG * Hematopoietic, hepatic and renal function tests will be carried out in the laboratory * The subjects will fast for 12 hours before collection of specimens for all laboratory evaluations * The above mentioned examinations will be performed within 14 days before the first administration of the test substance
Exclusion criteria
* Volunteers are excluded from the study if the results of the medical examination or laboratory tests are judged by the clinical investigator to differ significantly from normal clinical values * Subjects with known gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders * Subjects with diseases of the central nervous system (such as epilepsy) or with psychiatric or neurological disorders * History of orthostatic hypotension, fainting spells or blackouts * Subjects with chronic or relevant acute infections * Subjects with allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator * Volunteers who have taken a drug with a long half-life (≥ 24 hours) within one month or less than ten half-lives of the respective drug before enrolment in the study * Volunteers who receive any other drugs which might influence the results of the trial during the week previous to enrolment in the study * Volunteers who participate in another study with an investigational drug within the last two months preceding the study * Volunteers who are unable to refrain from smoking on study days * Volunteers who smoke more than10 cigarettes (or equivalent) per day * Volunteers who drink more than 60 g of alcohol per day * Volunteers who are dependent on drugs * Volunteers who donate blood (≥ 100 mL) within the last four weeks * Volunteers who participate in excessive physical activities within the last week before the study (e.g. competitive sports) * Volunteers who suffer from any other disease or abnormality of clinical relevance * History of hemorrhagic diatheses * History of gastro-intestinal ulcer, perforation or bleeding * History of bronchial asthma * History of glucose-6-phosphate dehydrogenase (G-6-PD) deficiency Female subjects: * Pregnancy * Positive pregnancy test * No adequate contraception (adequate contraception e.g. sterilization, intrauterine devices (IUD), oral contraceptives) * Inability to maintain this adequate contraception during the whole study period * Lactation period
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Area under the concentration-time curve of dipyridamole in plasma at steady state (AUC,ss) | Up to 48 hours after start of drug administration |
| Percent peak trough fluctuation of dipyridamole in plasma (%PTF) | Up to 48 hours after start of drug administration |
Secondary
| Measure | Time frame |
|---|---|
| Minimum measured concentration of the analytes in plasma at steady state over a uniform dosing interval τ (Cmin,ss) | Up to 48 hours after start of drug administration |
| Time from dosing to the maximum measured concentration of the analytes in plasma at steady state over a uniform dosing interval τ Time from dosing to the maximum measured concentration of the analytes in plasma at steady state (tmax,ss) | Up to 48 hours after start of drug administration |
| Percent area under the curve fluctuation of the analytes in plasma (AUCfluct) | Up to 48 hours after start of drug administration |
| Terminal half-life of the analytes in plasma (t1/2) | Up to 48 hours after start of drug administration |
| Ratio of peak concentration of the analytes in plasma over area under the curve at steady state (Cmax,ss / AUC,ss) | Up to 48 hours after start of drug administration |
| Number of subjects with clinically relevant changes in vital signs (blood pressure, pulse rate) | up to 8 days after last study drug administration |
| Number of subjects with clinically relevant changes in 12-lead ECG | up to 8 days after last study drug administration |
| Number of subjects with clinically relevant changes in laboratory values | up to 8 days after last study drug administration |
| Number of subjects with adverse events | up to 8 days after last study drug administration |
| Percent of dose of the analytes recovered unchanged in urine (Ae%) | Up to 24 hours after start of drug administration |
| Maximum concentration of the analytes in plasma at steady state (Cmax,ss) | Up to 48 hours after start of drug administration |
Outcome results
None listed