Absorption of sulindac from a novel (Pro-SorbTM) liquid formulation

Area of Science:

• Pharmacokinetics
• Drug Delivery Systems
• Gastroenterology

Background:

• Sulindac is a nonsteroidal anti-inflammatory drug (NSAID) used for pain and inflammation.
• Oral dosage forms can vary in their absorption profiles and gastrointestinal tolerability.
• Understanding absorption differences is crucial for optimizing therapeutic efficacy and patient compliance.

Purpose of the Study:

• To compare the pharmacokinetic profiles of sulindac from a novel liquid formulation (Pro-SorbTM) versus a conventional tablet form (Clinoril).
• To evaluate the absorption rate and extent of sulindac and its active metabolite.
• To assess the relationship between absorption and gastric tolerability.

Main Methods:

• A randomized crossover study involving eight healthy human volunteers.
• Administration of two 200 mg oral dosage forms: Pro-SorbTM liquid and Clinoril tablets.
• Serial blood sampling over 24 hours with sulindac and sulindac sulfide concentration analysis via High-Performance Liquid Chromatography (HPLC).
• Comparison of pharmacokinetic parameters including Cmax, AUClast, and AUC0-infinity.

Main Results:

• The Pro-SorbTM liquid formulation exhibited significantly higher maximal serum concentrations (Cmax) and area under the curve (AUC) values for sulindac compared to Clinoril tablets.
• Absorption of the active sulindac sulfide metabolite also showed differences between the two formulations.
• The enhanced absorption from the liquid form was associated with less reported gastric irritation.

Conclusions:

• Pro-SorbTM liquid offers improved bioavailability of sulindac compared to the standard Clinoril tablet.
• The liquid formulation may provide a more effective delivery of sulindac due to enhanced absorption.
• Reduced gastric irritation suggests better gastrointestinal tolerability for the Pro-SorbTM liquid formulation.