title: Dissolution enhancement and formulation of rapid-release lornoxicam mini-tablets.
abstract: 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(®) F-68 (PLU) and adsorption onto Neusilin(®) 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(®) 80, StarLac(®) (STA) and Emcompress(®)) 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.
authors.affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt; School of Pharmacy and Biomolecular Sciences, Liverpool John Moores University, Liverpool, UK.
authors.forename: Hesham M
authors.initials: HM
authors.lastname: Tawfeek
authors.forename: Imran Y
authors.initials: IY
authors.lastname: Saleem
authors.forename: Matthew
authors.initials: M
authors.lastname: Roberts
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D002152:Calorimetry, Differential Scanning; D004333:Drug Administration Routes; D005079:Excipients / Q000737:chemistry; D008297:Male; D010894:Piroxicam / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D011817:Rabbits; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013607:Tablets; D014961:X-Ray Diffraction
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D013607:Tablets; D010894:Piroxicam; C059451:lornoxicam
keywords: bioavailability; dissolution rate; excipients; formulation; oral absorption; oral drug delivery; physical stability; physicochemical properties; solid dispersion; tablet