Dissolution Enhancement and Formulation of Rapid-Release Lornoxicam Mini-Tablets

作者：Tawfeek Hesham M; Saleem Imran Y; Roberts Matthew^*

来源：Journal of Pharmaceutical Sciences, 2014, 103(8): 2470-2483.

DOI：10.1002/jps.24073

• bioavailability
• dissolution rate
• excipients
• formulation
• oral drug delivery
• oral absorption
• physicochemical properties
• physical stability
• tablet
• solid dispersion

The aim was to enhance the dissolution of lornoxicam (LOR) and to produce mini-tablets with an optimised system to provide a rapid-release multi-particulate formulation. LOR systems were prepared through co-evaporation with either polyethylene glycol 6000 or Pluronic((R)) F-68 (PLU) and adsorption onto Neusilin((R)) US2 alone or co-adsorption in the presence of different amounts of polysorbate 80. All systems were characterised by FT-IR, differential scanning calorimetry, X-ray diffraction, flowability and dissolution techniques. Mini-tablets were prepared using the system with the optimum dissolution profile and flowability. Tensile strengths, content uniformity and dissolution profiles of the mini-tablets were evaluated. The effects of different excipients and storage conditions on mini-tablet properties were also studied. The optimised rapid-release LOR mini-tablets were further evaluated for their in vivo pharmacokinetic profile. The co-evaporate of LOR with PLU showed significantly faster dissolution and superior flowability and was evaluated together with three directly compressible excipients (Cellactose((R)) 80, StarLac((R)) (STA) and Emcompress((R))) for mini-tablet formulation. The formulation with STA provided the optimum results in terms of tensile strength, content uniformity and rapid drug release following a 3-month stability study and was selected for further in vivo evaluation. The pharmacokinetic profile indicated the potential of the mini-tablets achieving rapid release and increased absorption of LOR.

• 出版日期2014-8