Risperidone/Randomly Methylated β-Cyclodextrin Inclusion Complex-Compatibility Study with Pharmaceutical Excipients.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery
• Supramolecular Chemistry

Background:

• Risperidone (RSP) is an atypical antipsychotic with poor water solubility and high lipophilicity.
• RSP exhibits incompatibilities with common pharmaceutical excipients like magnesium stearate and lactose.
• Improving RSP's biopharmaceutical profile is crucial for effective drug formulation.

Purpose of the Study:

• To enhance the solubility and stability of risperidone (RSP) through encapsulation.
• To investigate the formation and characteristics of RSP-RM-β-CD inclusion complexes.
• To assess the compatibility of the RSP-RM-β-CD adduct with key pharmaceutical excipients.

Main Methods:

• Formation of inclusion complexes using randomly methylated β-cyclodextrin (RM-β-CD).
• Characterization via thermal methods, PXRD, UATR-FTIR, UV spectroscopy, and solubility studies.
• Compatibility assessment using thermoanalytical tools and spectroscopic techniques.

Main Results:

• Successful formation of a 1:1 RSP-RM-β-CD inclusion complex with enhanced solubility.
• The supramolecular adduct showed no interactions with starch, magnesium stearate, and cellulose microcrystalline.
• Incompatibility was observed between the RSP-RM-β-CD adduct and anhydrous lactose.

Conclusions:

• The RSP-RM-β-CD supramolecular adduct is a promising candidate for developing stable and bioavailable formulations.
• The study identified suitable excipients (starch, magnesium stearate, cellulose microcrystalline) for solid dosage forms.
• This research facilitates informed selection of excipients for improved risperidone drug products.