[Studies on ethmozine sustained-release tablet remaining-floating in stomach]

Area of Science:

• Pharmacokinetics and Drug Delivery
• Gastrointestinal Drug Absorption
• Sustained-Release Formulations

Background:

• Ethmozine is an antiarrhythmic drug with a short duration of action.
• Conventional ethmozine formulations require frequent dosing, potentially leading to compliance issues.
• Developing sustained-release systems can improve therapeutic efficacy and patient convenience.

Purpose of the Study:

• To develop and characterize an oral sustained-release system for ethmozine (E-HBS).
• To evaluate the in vitro release kinetics and in vivo gastrointestinal transit of E-HBS.
• To assess the plasma concentration-time profile and in vitro-in vivo correlation of E-HBS.

Main Methods:

• Development of an oral sustained-release ethmozine formulation (E-HBS).
• In vitro drug release studies to determine release kinetics (first-order kinetics, Kr = 0.2436 h-1).
• Gamma-scintiphotographic study in humans to assess gastric residence time; plasma drug concentration monitoring.

Main Results:

• E-HBS demonstrated first-order release kinetics in vitro.
• Gamma-scintigraphy revealed E-HBS remained in the stomach for over 6 hours, significantly longer than conventional tablets (1-1.5 hours).
• Plasma concentration-time curves confirmed sustained-release characteristics, with excellent linearity between in vitro and in vivo drug release.

Conclusions:

• The developed E-HBS system provides prolonged gastric residence time and sustained ethmozine release.
• E-HBS exhibits favorable in vitro release kinetics and demonstrates good in vitro-in vivo correlation.
• This sustained-release formulation holds potential for improved therapeutic outcomes and reduced dosing frequency for ethmozine.