Preparation and Optimization of Sertraline Hydrochloride Tablets with Improved Dissolution Through Crystal...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Sertraline hydrochloride exhibits poor solubility and low bioavailability due to first-pass metabolism.
• Enhancing the dissolution rate is crucial for improving sertraline's therapeutic efficacy.

Purpose of the Study:

• To improve the dissolution rate and bioavailability of sertraline hydrochloride.
• To develop and characterize an optimized formulation for enhanced drug release.

Main Methods:

• Recrystallization of sertraline hydrochloride with polymers and surfactants (SLS).
• Optimization of formulation parameters including drug/polymer ratio and SLS concentration.
• Characterization of the formulation using particle size analysis, in vitro release studies, and stability testing.
• Tablet compression and evaluation of physical properties (hardness, friability) and dissolution profiles.

Main Results:

• The optimized formulation (poloxamer 407, drug/polymer ratio 1:2/3, 0.05% SLS) showed a significantly higher drug release (96%) compared to processed drug alone (56%).
• The formulation demonstrated good stability over six months, with no significant changes in drug crystallinity or interaction with excipients.
• Compressed tablets exhibited acceptable physical properties and superior dissolution profiles compared to Zoloft®.

Conclusions:

• The developed formulation effectively enhances sertraline hydrochloride dissolution and release.
• This approach offers a promising strategy for improving the bioavailability of poorly soluble drugs.
• The optimized formulation provides a viable alternative to existing commercial products.