Gastrointestinal Behavior of Posaconazol in Healthy Volunteers

Healthy Clinical Trial

Official title:

Gastrointestinal Behavior of Posaconazol in Healthy Volunteers

Clinical Trial Details — Status: Recruiting

Administrative data

• NCT number: NCT02048345
• Other study ID #: DDD13POSA
• Status: Recruiting
• Phase: N/A
• First received: June 23, 2013
• Last updated: January 28, 2014
• Start date: January 2014

Study information

• Verified date: January 2014
• Source: Katholieke Universiteit Leuven
• Contact: Bart Hens, Pharmacist
• Phone: +3216330302
• Email: bart.hens[@]pharm.kuleuven.be
• Is FDA regulated: No
• Health authority: Belgium: Federal Agency for Medicinal Products and Health Products
• Study type: Interventional

Clinical Trial Summary

The aim of this study is to understand the behavior of posaconazol gives as a suspension and solution in the gastrointestinal tract in human volunteers. The investigators know that supersaturation for this compound can be achieved by the influence of the gastrointestinal tract: The acid environment of the stomach creates a optimized environment for the basic compound to reach a high solubility, while the neutral environment of the small intestine creates a low solubility environment for the compound. The transit from stomach to small intestine gives the opportunity for the drug to create a supersaturated solution. Giving the drug as a solution to the healthy volunteer makes sure that precipitation is not occurring in the stomach and that precipitation has to happen in the small intestine. After all, supersaturation is a state that is not thermodynamic stable and always will want to precipitate. Giving the drug as a suspension to the healthy volunteers, can make it possible that still some particles of the drug are not in dissolution and that those particles will flow to the small intestine where other particles easily can bind to. This will make that almost the whole supersaturated solution is immediately precipitated.

The investigators want to give the suspension by the authorized drug called Noxafil. On the other hand an aqueous solution will be made by adjusting the pH to 1.2 (which is conform with the pH of the stomach) and given to the volunteers by the stomach catheter. This 2 formulations will be tested in a fasted state and a fed state (by giving 2 Ensure plus shakes to the volunteers before the experiment starts). After intake of the formulation, gastric and duodenal fluids will be aspirated by the catheters and analyzed at their laboratory. So the four conditions the investigators want to study are:

1. 10 mL Suspension of posaconazol (Noxafil 40mg/mL) together with a glass of 240 mL water in a fasted state

2. 250 mL solution of posaconazol, by dissolving 2.6 mL autohorized suspension (Noxafil) in 247 mL water, adjusted to pH 1.2 by hydrochloric acid given to the volunteer in a fasted state.

3. 10 mL Suspension of posaconazol (Noxafil 40mg/mL) together with a glass of 240 mL water in a fed state (by giving 20 minute before intake of the formulation, 2 ensure plus shakes)

4. 250 mL solution of posaconazol, by dissolving 2.6 mL autohorized suspension (Noxafil) in 247 mL water, adjusted to pH 1.2 by hydrochloric acid given to the volunteer in a fed state (by giving 20 minute before intake of the formulation, 2 ensure plus shakes).

By getting more knowledge about the behavior of posaconazol (interplay supersaturation / precipitation) more insights can be achieved for the development of supersaturating drug delivery systems.

Recruitment information / eligibility

• Status: Recruiting
• Enrollment: 10
• Est. primary completion date: December 2014
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Both
• Age group: 18 Years to 40 Years

Eligibility

Inclusion Criteria:

• 18-40 years Healthy volunteers

Exclusion Criteria:

• disease Hiv, Hepatitis B, Hepatitis C Pregnant Drug abuse

Study Design

Allocation: Randomized, Intervention Model: Crossover Assignment, Masking: Open Label, Primary Purpose: Basic Science

Related Conditions & MeSH terms

• Healthy

Intervention

Drug:
• Suspension Fasted State

• Suspension Fed State

• Solution Fasted State

• Solution Fed State

Locations

Country	Name	City	State
Belgium	UZ Leuven Gasthuisberg	Leuven

Sponsors (1)

Lead Sponsor	Collaborator
Katholieke Universiteit Leuven

Country where clinical trial is conducted

Belgium, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	Concentration-time profile in stomach and small intestine for posaconazol		These concentrations will be measured for 4 hours, together by taking blood samples to see how the drug will be transported to the blood circulation (PK profile for 48 hours)	No