Effects of 500 mg Immediate Release and Extended Release Methylnaltrexone on Loperamide-induced Delay of the Oro-cecal and Whole-gut Transit Time in Healthy Subjects

• Status: Completed
• Trial end date: 2010-05-01
• Target enrollment: 0
• Participant gender: All

Summary

The purpose of this study is to describe the effects of methylnaltrexone in preventing loperamide-induced delay of the oro-cecal and whole-gut transit time and measure pharmacokinetics of methylnaltrexone after subcutaneous and oral administration of immediate release and extended release capsules.

• Phase: Phase 1
• Accepts Healthy Volunteers?: Accepts Healthy Volunteers

Details

• Lead Sponsor: University Medicine Greifswald
• Treatments: Antidiarrheals; Loperamide; Methylnaltrexone; Naltrexone; Sulfasalazine

Criteria

Inclusion Criteria:

• age: 18 - 45 years

• sex: male and female

• ethnic origin: Caucasian

• minimal body weight: 62 kg

• body mass index: ≥ 19 kg/m² and ≤ 27 kg/m²

• good health as evidenced by the results of the clinical examination, ECG, and the laboratory check-up, which were judged by the clinical investigator not to differ in a clinical relevant way from the normal state

• written informed consent

Exclusion Criteria:

• hepatic and renal diseases and/or pathological findings, which might interfere with pharmacokinetics and pharmacodynamics of the study medication

• gastrointestinal diseases and/or pathological findings, which might interfere with pharmacokinetics and pharmacodynamics of the study medication

• drug or alcohol dependence

• positive drug or alcohol screening

• smokers of 10 or more cigarettes per day

• positive results in HIV, HBV and HCV screenings

• volunteers who were on a diet which could affect the pharmacokinetics of the drug

• heavy tea or coffee drinkers (more than 1 L per day)

• lactation, pregnancy test positive or not performed or women of child-bearing age without safe contraception

• volunteers suspected or known not to follow instructions of the clinical investigators

• volunteers who were unable to understand the written and verbal instructions, in particular regarding the risks and inconveniences they would have been exposed to as a result of their participation in the study

• volunteers liable to orthostatic dysregulation, fainting or blackouts

• participation in a clinical trial during the last 3 months prior to the start of the study

• less than 14 days after last acute disease

• less than 3 months after last blood donation

• any medication within 4 weeks prior to the intended first administration of the study medication which might have influenced functions of the gastrointestinal tract (e.g. laxatives, metoclopramide, loperamide, antacids, H2-receptor antagonists, proton pump inhibitors)

• any other medication within two weeks prior to the first administration of the study medication, but at least 10-time the half-live of the respective drug (except oral contraceptives)

• intake of grapefruit containing food or beverages within 14 days prior to administration of the study medication

• known allergic reactions to the active ingredients used or to constituents of the study medication

• deficiency of glucose-6-phosphate dehydrogenase