Development of pulsatile release tablets with swelling and rupturable layers.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Pulsatile drug delivery systems offer controlled release profiles.
• Designing systems with predictable lag times is crucial for therapeutic efficacy.
• Swelling and rupturable coatings present a viable approach for pulsatile release.

Purpose of the Study:

• To develop and evaluate a two-layered coated tablet for pulsatile drug delivery.
• To investigate the influence of formulation variables on the lag time and drug release.
• To characterize the mechanical properties of the coating layers.

Main Methods:

• Tablets with buflomedil HCl cores were prepared by direct compression.
• Cores were coated with a swelling layer (croscarmellose sodium) and a rupturable layer (ethylcellulose).
• Mechanical properties, rupture time, and dissolution profiles were evaluated.

Main Results:

• Decreased lag time with increased microcrystalline cellulose in cores.
• Increased lag time with higher levels of swelling and rupturable coatings.
• Ethylcellulose coating thickness and magnesium stearate content modulated water uptake and film strength, affecting lag time and robustness.

Conclusions:

• The developed two-layered coated tablet system effectively achieved pulsatile drug release.
• Formulation parameters, including core composition and coating levels, significantly influenced the lag time.
• This system shows promise for targeted drug delivery applications requiring a delayed release profile.