Powdered self-emulsified lipid formulations of meloxicam as solid dosage forms for oral administration

Abstract

The objectives of this study were to prepare a powdered self-emulsified (SEDDS) formulation of meloxicam and to compare its oral bioavailability against commercial Mobic tablets. The SEDDS formulation was prepared by in situ salt formation of meloxicam in a blend of lipid excipients and aqueous tris (hydroxymethyl) aminomethane solution. The liquid SEDDS was subsequently adsorbed on silica powder and was tested for size, flow, and crystal growth. The flowability index of the powdered SEDDS was borderline acceptable. Absence of crystal growth with storage was confirmed by DSC and PXRD studies. Dissolution of meloxicam from the powdered SEDDS was >90% vs. <12% for powdered meloxicam and <80% for the commercial tablets. Stability of the powdered formulations after storage in gelatin and HPMC capsules was also evaluated to study the effect of water migration from the fill into capsule shells. Capsules softened to a different extent as a function of fill material with HPMC capsules showing greater resistance to water migration. Finally, oral bioavailability of the formulations was evaluated in beagle dogs. Powdered meloxicam SEDDS formulation showed a 1.3-fold increase in AUC vs. commercial Mobic® tablets. Overall, this study described a novel SEDDS formulation of meloxicam and outlined a systematic approach to adsorbing and testing the flow and stability behavior of powdered SEDDS formulations.

Formulation and in vitro evaluation of meloxicam as a self-microemulsifying drug delivery system

“…The formulations were then kept for 48 hours while being visually inspected for turbidity and phase separation before droplet size distribution tests were performed. 8 …”

Formulation and in vitro evaluation of meloxicam as a self-microemulsifying drug delivery system

“…The formulations were then kept for 48 hours while being visually inspected for turbidity and phase separation before droplet size distribution tests were performed. 8 In vitro evaluation of the prepared MLX liquid SMEDDS Thermodynamic stability studies Numerous thermodynamic stability tests (centrifugation, heating-cooling cycle, and freeze-thaw cycle) were done on all the prepared liquid SMEDDS formulations to determine the effect of centrifugation and temperature on the stability of self-microemulsions and to avoid selecting metastable formulations for further development and characterization. 9…”

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

“…Nevertheless, the release out of liquid su-SEDDS due to heat or physical stress during storage can be degrade the quality of final product; thus, the physico-chemical stability of hard capsule dosage form should be monitored during storage. Considering probability of this stability issue, the stability study of solid SEDDSs with meloxicam in gelatin and HPMC capsules were conducted [241]. It was shown that the extent of capsule deformation was dependent on the filled material and the low water and propylene glycol content affected shell deformation less.…”