Development of fast-dissolving tablets of flurbiprofen-cyclodextrin complexes

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Physical Chemistry

Background:

• Flurbiprofen is a practically insoluble drug, limiting its therapeutic efficacy.
• Cyclodextrins are known to enhance the solubility and dissolution of poorly soluble drugs.
• Developing effective flurbiprofen-cyclodextrin systems is crucial for improving drug delivery.

Purpose of the Study:

• To develop a tablet formulation using flurbiprofen-cyclodextrin systems for rapid and complete drug dissolution.
• To evaluate the impact of different cyclodextrins and preparation methods on drug solubility and dissolution.
• To assess the performance of these systems in direct compression tablets meeting rapid dissolving criteria.

Main Methods:

• Preparation of binary drug-cyclodextrin systems using five techniques: physical mixing, kneading, sealed-heating, coevaporation, and colyophilization.
• Characterization of systems using Differential Scanning Calorimetry, x-ray powder diffractometry, infrared spectroscopy, and optical microscopy.
• Evaluation of solubility and dissolution rates, followed by tablet formulation using chitosan and spray-dried lactose as excipients.

Main Results:

• Drug solubility improvement ranged from 2.5 to 120 times, depending on cyclodextrin type and preparation method.
• All drug-cyclodextrin formulations showed higher dissolved amounts compared to drug alone.
• Tablets with drug kneaded with methyl-beta-cyclodextrin or colyophilized with beta-cyclodextrin and spray-dried lactose met FDA rapid dissolving tablet criteria (>85% dissolved in 30 min).

Conclusions:

• Flurbiprofen-cyclodextrin systems significantly enhance drug solubility and dissolution rates.
• Formulation factors, particularly excipient choice, critically influence tablet dissolution behavior.
• Optimized formulations hold promise for improved flurbiprofen bioavailability, enabling reduced dosage and potential side effects.