Development and evaluation of prolonged release pellets obtained by the melt pelletization process

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Developing sustained-release dosage forms is crucial for improving patient compliance and therapeutic efficacy.
• Melt pelletization offers a solvent-free granulation method for producing pharmaceutical pellets.
• Fatty excipients like Compritol and Precirol are effective binders for controlled-release formulations.

Purpose of the Study:

• To evaluate the feasibility of producing prolonged-release matrix pellets via melt pelletization.
• To investigate the influence of process parameters on pellet characteristics.
• To assess the applicability of this method for both highly and poorly water-soluble drugs.

Main Methods:

• Melt pelletization was conducted in a laboratory high shear mixer (Mi-Pro).
• Pellet formulations utilized lactose with Compritol 888 and Precirol ATO 5 as melting binders.
• Key process parameters studied included jacket temperature, massing time (MT), and impeller speed (IS).

Main Results:

• Optimal conditions (IS: 800 rpm, chopper speed: 4000 rpm, MT: 8 min) yielded pellets with narrow size distribution.
• Increased fatty binder content (18% to 80% w/w) was investigated.
• The technique successfully produced prolonged-release pellets for phenylephrine hydrochloride and sustained-release pellets for ciprofloxacin hydrochloride, ketoprofen, and theophylline.

Conclusions:

• Melt pelletization with Compritol and Precirol mixtures is an efficient method for producing prolonged-release pellets.
• This technique is versatile, applicable to both highly water-soluble and less water-soluble drugs.
• The study demonstrates a rapid and effective approach for developing sustained-release formulations.