Dose Tolerance Study in Healthy Male Volunteers After Intranasal Application of Epinastine Nasal

Recruitment & Eligibility

Inclusion Criteria

All participants in the study should be healthy, range from 21 to 50 years of age and be within ± 20 % of their normal weight (Broca -Index)
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. Haematological, hepatic and renal function tests will be carried out in the laboratory (Bioscientia Ingelheim, Germany). 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
In accordance with good clinical practice (GCP) and the local legislation all volunteers will have given their written informed consent prior to admission to the study

Exclusion Criteria

Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
Surgery of the gastro-intestinal tract (except appendectomy)
Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
History of orthostatic hypotension, fainting spells or blackouts
Chronic or relevant acute infections
History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
Intake of drugs with a long half-life (> 24 hours) within at least one month or less than ten half-lives of the respective drug before enrolment in the study
Use of any drugs which might influence the results of the trial (≤ one week prior to administration or during the trial)
Participation in another trial with an investigational drug (≤ two months prior to administration or during the trial
Smoker (> 10 cigarettes or > 3 cigars or > 3 pipes/day)
Inability to refrain from smoking on trial days
Alcohol abuse (> 60 g/day)
Drug abuse
Blood donation (≥ 100 mL within four weeks prior to administration or during the trial)
Excessive physical activities (within the last week before the study)
Any laboratory value outside the reference range of clinical relevance

Study & Design

Arm && Interventions

Group	Intervention	Description
Epinastine nasal	Epinastine nasal	single rising doses
Placebo	Placebo	-

Primary Outcome Measures

Name	Time	Method
Number of patients with clinically relevant findings in vital signs	up to 8 days after drug administration	blood pressure, pulse rate
Number of patients with clinically relevant findings in laboratory parameters	up to 8 days after drug administration
Number of patients with clinically relevant findings in 12-lead ECG	up to 8 days after drug administration
Number of patients with adverse events	up to 8 days after drug administration
Changes in rhinoscopy assessment	up to 8 days after drug administration

Secondary Outcome Measures

Name	Time	Method
Renal clearance (CLR)	up to 48 hours after drug administration
Amount excreted into urine (Ae)	up to 48 hours after drug administration
Total mean residence time in the body (MRTtot)	up to 48 hours after drug administration
Maximum measured concentration in plasma (Cmax)	up to 48 hours after drug administration
Area under the concentration-time curve in plasma (AUC)	up to 48 hours after drug administration
Terminal rate constant of in plasma (λz)	up to 48 hours after drug administration
Apparent terminal half-life in plasma (t1/2)	up to 48 hours after drug administration
Apparent volume of distribution during the terminal phase (Vz/F)	up to 48 hours after drug administration
Time from dosing to the maximum concentration in plasma (tmax)	up to 48 hours drug administration
Total clearance in plasma after extravascular administration (CL/F)	up to 48 hours after drug administration
Assessment of dose-proportionality of epinastine nasal	up to 48 hours after drug administration	based on AUC and Cmax

Recruitment & Eligibility