Abstract

Purpose: Meloxicam is a non-steroidal anti-inflammatory drug with highly variable bioavailability due to its poor aqueous solubility and dissolution. This work aimed to improve meloxicam bioavailability by formulating it in orodispersible capsules containing a soluble complex of the drug with beta-cyclodextrin. Methods: Complexes were prepared by different methods and characterized by differential scanning calorimetry, X-ray diffraction, infrared spectroscopy and dissolution efficiency studies. Orodispersible capsule shells were prepared from conventional hard gelatin capsule shells by freeze-drying and evaluated by image analysis microscopy and moisture content estimation. Formulae containing the freeze-dried complex and different fillers were prepared and characterized for their flowability, moisture content and moisture absorption behavior. The orodispersible capsules were evaluated in-vitro and in-vivo in comparison with meloxicam commercial tablets (Mobic TM). Results: Inclusion complexes between meloxicam and beta-cyclodextrin were formed and the dissolution efficiency was greatly enhanced by the freeze-dried product. The formulations containing mannitol or anhydrous lactose as fillers were superior and disintegrated within 23 s. The dissolution efficiency after 60 min exceeded 98% for the orodispersible capsules while its value was only 79% for Mobic TM. In comparison with Mobic TM, the tested orodispersible capsules showed a 1.7-fold increase in the average C_max, a 0.5-fold decrease in the average t_max and a 1.4-fold increase in the average AUC_0-48 of meloxicam. Conclusion: Orodispersible capsules containing meloxicam/beta-cyclodextrin freeze-dried complex markedly improve meloxicam bioavailability.


Keywords:  Meloxicam   Beta-cyclodextrin   Freeze-drying   Orodispersible capsules   Dissolution efficiency   Bioavailability