Development of Sinomenine Hydrochloride Sustained-release Pellet With Multiple Release Characteristics

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Rheumatology

Background:

• Clinical use of sinomenine hydrochloride (SH) for rheumatoid arthritis is limited by gastrointestinal side effects.
• Elderly patients, a primary demographic for rheumatoid arthritis, exhibit significant variations in gastric emptying.
• Individual differences in gastric emptying can affect drug efficacy and contribute to adverse gastrointestinal events.

Purpose of the Study:

• To develop innovative sinomenine hydrochloride (SH) sustained-release pellets with multiple release characteristics.
• To mitigate gastrointestinal side effects associated with SH administration.
• To reduce the impact of individual gastric emptying variations on SH drug efficacy.

Main Methods:

• Formulation optimization of drug-loaded layers using a full factorial design.
• Preparation of SH sustained-release pellets, including regular and enteric-coated types.
• In vitro dissolution testing to evaluate drug release profiles in acidic and intestinal environments.

Main Results:

• Optimal formulation yielded 96.05% pellet yield with 83.36% SH encapsulation efficiency.
• Pellets exhibited high roundness (0.971) and controlled particle size distribution (span 0.808).
• In vitro tests confirmed a 4-hour SH release in acid and a dual-phase release (4h acid resistance, then 8h intestinal release).

Conclusions:

• The developed SH sustained-release pellets demonstrate stable and compliant dissolution behavior.
• The formulation exhibits excellent physical stability and appearance.
• This research provides a valuable reference for innovative SH drug formulation strategies.