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

Abstract

The aim was to enhance the dissolution of lornoxicam and to produce mini-tablets with an optimised system to provide a rapid release multiparticulate formulation. Lornoxicam systems were prepared through co-evaporation with either PEG or Pluronic® F-68 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, DSC, XRD, 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 lornoxicam mini-tablets were further evaluated for their in-vivo pharmacokinetic profile.The co-evaporate of lornoxicam with Pluronic® F-68 showed significantly faster dissolution and superior flowability and was evaluated together with three directly compressible excipients (Cellactose® 80, StarLac® and Emcompress®) for mini-tablet formulation. The formulation with StarLac® provided the optimum results in terms of tensile strength, content uniformity and rapid drug release following a 3 month stability study and was

Glibenclamide Mini-tablets with an Enhanced Pharmacokinetic and Pharmacodynamic Performance

“…This observation was due to the conversion of GLC from crystalline to amorphous state. Similar behavior was also recorded from other researchers [13,20,45].…”

“…Tween 80 and Pluronics were chosen as non-ionic surfactants known to enhance the solubility and dissolution of many water insoluble drugs as reported previously [13,20,22,23].…”

“…Mini-tablets with their unique size have been introduced into the field of oral delivery to address problems such as dose accuracy and swallowing difficulties [17][18][19]. Previously, Tawfeek et al [20] successfully prepared rapid-release mini-tablets containing small doses of lornoxicam compared with conventional tablets with a high dose which was more economic and suit patients with swallowing difficulties.…”

“…Generally, a reduction in drug dose will be beneficial to decrease the potential of any side effects for patients and to decrease the cost of producing and exporting expensive API for manufacturers [20,21]. In an attempt to decrease the amount of GLC contained in tablets, our study focused on enhancing the GLC dissolution.…”

A comprehensive review on pharmaceutical mini tablets

“…The drug contained in the mini-tablets gets released at different rates, depending upon composition of mini tablets. Based on the release kinetic parameters calculated, it can be concluded that minitablets containing HPMC K100M are particularly suitable to release the drug over hours of time periods 9 .…”