Formulation of immediate release pellets containing famotidine solid dispersions

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Physical Pharmacy

Background:

• Famotidine (FM), an H2-receptor antagonist for peptic ulcers, exhibits low and variable bioavailability due to poor water solubility.
• Enhancing famotidine's dissolution is crucial for improving its therapeutic efficacy and patient compliance.

Purpose of the Study:

• To improve the dissolution and bioavailability of famotidine (FM) through solid dispersion technology.
• To investigate the use of hydrophilic carriers, Gelucire 50/13 and Pluronic F-127, for famotidine solid dispersion formulation.
• To evaluate the drug release characteristics of famotidine from solid dispersions and prepared pellets.

Main Methods:

• Famotidine solid dispersions were prepared using Gelucire 50/13 and Pluronic F-127 as hydrophilic carriers.
• Solid dispersions and prepared pellets were characterized using Differential Scanning Calorimetry (DSC) and Scanning Electron Microscopy (SEM).
• In vitro dissolution studies were conducted to assess drug release profiles from solid dispersions and pellets.

Main Results:

• Differential Scanning Calorimetry (DSC) confirmed no drug-carrier interactions in solid dispersions with higher carrier content (1:3 and 1:5 ratios).
• Scanning Electron Microscopy (SEM) revealed spherical pellets with sizes dependent on the carrier used.
• Dissolution studies demonstrated significantly enhanced famotidine release from solid dispersions compared to the pure drug. Pellets containing solid dispersions (1:3 ratio) achieved complete drug release within 30 minutes, whereas untreated famotidine pellets released only ~30% in 2 hours.

Conclusions:

• Solid dispersion technology effectively enhances the dissolution rate of poorly soluble famotidine using hydrophilic carriers like Gelucire 50/13 and Pluronic F-127.
• Formulation of famotidine solid dispersions into pellets further improves drug release kinetics, offering a promising approach for enhancing famotidine bioavailability.
• The optimized drug:carrier ratio of 1:3 in solid dispersions is effective for improving famotidine dissolution and release from pelletized dosage forms.