Modified release matrix prepared by compaction of spheres containing waxy material

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Development of sustained-release formulations is crucial for improving patient compliance and therapeutic efficacy.
• Waxy materials like Gelucire 50/02 offer potential for controlling drug release kinetics in oral dosage forms.
• Multiparticulate systems, such as spheres compacted into tablets, provide an alternative to conventional monolithic tablets.

Purpose of the Study:

• To prepare and characterize chlorpheniramine maleate spheres using Gelucire 50/02 and Avicel PH-101.
• To evaluate the impact of two drug incorporation methods (direct and fusion) on drug release.
• To investigate the effect of Gelucire 50/02 concentration and preparation method on drug release from compacted tablets.

Main Methods:

• Chlorpheniramine maleate spheres were prepared using an extruder/marumerizer with varying concentrations of Gelucire 50/02 (10%, 30%, 50%) and Avicel PH-101.
• Drug incorporation was achieved via direct mixing or a fusion method involving dispersion in melted wax.
• Spheres were compacted into tablets, and in vitro drug release studies were conducted.

Main Results:

• Incorporation of Gelucire 50/02 into spheres increased drug release, indicating disruption of matrix formation.
• Tablets prepared from spheres using the fusion method exhibited lower drug release compared to the direct method.
• Increasing the concentration of Gelucire 50/02 in the tablet formulation led to a decrease in drug release rate.

Conclusions:

• Gelucire 50/02 can be effectively used in preparing chlorpheniramine maleate spheres.
• The fusion method of drug incorporation and higher wax content are effective in reducing drug release from compacted multiparticulate tablets.
• This study successfully demonstrates a multiparticulate delivery system with tunable drug release characteristics.