Some aspects of sorbinicate pharmacokinetics

Area of Science:

• Pharmacology
• Gastroenterology
• Biochemistry

Background:

• Nicotinic acid is a vital nutrient with therapeutic applications.
• Understanding the absorption and metabolism of its derivatives is crucial for drug development.
• D-glucitol hexanicotinate (sorbinicate) is a nicotinic acid derivative with potential therapeutic benefits.

Purpose of the Study:

• To investigate the gastrointestinal absorption of D-glucitol hexanicotinate (sorbinicate).
• To determine the hydrolysis of sorbinicate to free nicotinic acid.
• To analyze the plasma kinetics of nicotinic acid after oral sorbinicate administration in rats.

Main Methods:

• Oral administration of D-glucitol hexanicotinate (sorbinicate) to rats.
• Analysis of gastrointestinal absorption and tissue hydrolysis.
• Measurement of plasma nicotinic acid levels over time.
• Comparison with oral administration of nicotinic acid.

Main Results:

• D-glucitol hexanicotinate (sorbinicate) is absorbed intact in the upper gastrointestinal tract.
• Rapid hydrolysis to free nicotinic acid occurs in various tissues.
• Plasma nicotinic acid levels are significantly lower and more constant after sorbinicate administration compared to nicotinic acid.
• Species differences in plasma kinetics were observed, but the trend of lower, stable levels persisted.

Conclusions:

• D-glucitol hexanicotinate (sorbinicate) serves as an effective delivery form for nicotinic acid.
• The unique absorption and hydrolysis pathway leads to a more favorable pharmacokinetic profile.
• Sorbinicate offers a potentially safer alternative for achieving nicotinic acid plasma levels.