A controlled release papaverine tablet (Papacontin): a study in normal volunteers

Area of Science:

• Pharmacology
• Drug Delivery Systems
• Clinical Pharmacy

Background:

• Papaverine hydrochloride is a vasodilator.
• Optimizing papaverine hydrochloride delivery is crucial for sustained therapeutic effects.
• Existing formulations may lead to suboptimal plasma concentration profiles.

Purpose of the Study:

• To compare the in vitro release and in vivo pharmacokinetic profiles of a controlled-release papaverine hydrochloride tablet against a standard capsule formulation.
• To evaluate the therapeutic efficacy and safety of the novel controlled-release tablet.

Main Methods:

• In vitro dissolution testing of the controlled-release tablet and capsule.
• Pharmacokinetic study in human volunteers administering both formulations.
• Analysis of plasma papaverine hydrochloride concentrations over time.

Main Results:

• The controlled-release tablet demonstrated steady papaverine hydrochloride release over 10 hours in vitro.
• In vivo, the tablet achieved therapeutic plasma levels within 1 hour and maintained them for 10-12 hours.
• The capsule formulation resulted in rapid initial plasma levels followed by a quick decline.

Conclusions:

• The controlled-release tablet offers a significant improvement in papaverine hydrochloride pharmacokinetic profile compared to capsules.
• This novel formulation ensures prolonged therapeutic drug concentrations, potentially enhancing treatment efficacy and patient compliance.
• Further clinical studies are warranted to confirm the therapeutic benefits in specific patient populations.