Studies on improvement of physicomechanical and pharmacokinetic parameters of non steroidal anti inflammatory drugs by crystal engineering

Abstract

quotBackground: There are certain key issues in the pharmaceutical newlineindustries like poor physicochemical, mechanical and processing parameters newlinerather than toxic effect or non-efficacy of the medicaments which bring less newlinethan 1% of active medicaments into the market. Among these processing newlineproblems, aqueous solubility remains a key issue. Active pharmaceuticals are newlineoften rejected during commercial production due to their poor aqueous newlinesolubility and also poor mechanical properties. newlineAim: Aim of the present study was to improve physicochemical and mechanical newlineproperties of BCS Class-II drugs, Ibuprofen and Ketoprofen, of Non-steroidal newlineAnti-inflammatory Drugs (NSAIDs) category, with poor flow, using crystal newlineengineering approach for remarkable improvement in aqueous solubility, drug newlinerelease rate, manufacturing and pharmacokinetic parameters. newlineMaterials and Methods: Influence of various excipients and method of newlinepreparations were studied separately for both drugs by changing molar ratio of drug:excipient. Treated crystals of both drugs were studied for Heckel newlineparameters showed greater plastic deformation and tensile strength with newlinenegligible elastic recovery compared to respective pure drug which enables to newlineformulate directly compressible tablets of both treated crystals without using newlineany directly compressible excipients. The molar ratio which shows greater newlineaqueous solubility, drug release rate, drug loading efficiency, and % yield was newlineselected as an optimized batch for further study. newlineResults and Discussion: SEM images of both treated crystals showed shape newlinewith an aspect ratio near to unity with improved flow, packability, compactibility newlineand compressibility parameters. FT-IR and DSC study revealed no interaction newlineoccurred between drug and excipient in their physical mixture. DSC of treated newlinecrystals depicted endothermic transition occurred which demonstrates the newlinestability of new crystal form of both drugs and indicates the absence of newlineunbound/ absorbed solvent. pXRD of treated crystals of both drugs suggested newlinethe generation of