Evaluation of various processes for simultaneous complexation and granulation to incorporate drug-cyclodextrin...

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Poorly soluble drugs require formulation strategies to enhance dissolution and bioavailability.
• Cyclodextrins (CDs) are common excipients used to form inclusion complexes, improving drug solubility.
• Traditional drug-CD complexation and solid dosage form production often involve multiple, complex steps.

Purpose of the Study:

• To evaluate spray granulation and fluid bed processing (FBP) as simultaneous complexation and granulation methods for poorly soluble drugs.
• To compare the efficacy of these novel granulation techniques with a standard co-evaporation-granulation process.
• To assess the dissolution profiles of drug-CD complexes produced by different methods.

Main Methods:

• Selected poorly soluble drugs: ibuprofen and glyburide.
• Standard process: Co-evaporation of drug:CD mixture followed by wet granulation.
• Alternative processes: Spray granulation and FBP using drug:CD solutions in ethanol.

Main Results:

• Tablets containing glyburide:CD complexes produced by spray granulation, FBP, and co-evaporation-granulation showed significantly improved dissolution (>70% in water, >60% in SLS) compared to plain tablets (30-34%).
• Tablets containing ibuprofen:CD complexes produced by co-evaporation-granulation and FBP exhibited superior dissolution (>90% and 100%) in acidic and buffer media compared to plain tablets (44-80%).
• Spray granulation proved effective for low-dose drugs, while FBP was suitable for moderate-dose drugs.

Conclusions:

• Spray granulation and FBP are efficient techniques for creating drug-CD complexes, simplifying the production of solid dosage forms.
• These granulation methods significantly enhance the dissolution rates of poorly soluble drugs like ibuprofen and glyburide.
• The choice between spray granulation and FBP depends on the drug's dosage and solubility characteristics.