薬学および生命科学における研究開発の国際ジャーナル

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CRYSTAL ENGINEERING OF SALBUTAMOL SULPHATEPRODUCED BY IN-SITU MICRONIZATION TECHNIQUE FOR DRY POWDER INHALATION (DPI) TO IMPROVE THERAPEUTIC EFFICIENCY: OPTIMIZATION OF PROCESS PARAMETERS

P. S. Uttekar, P. D. Chaudhari

The purpose of this study was to produce of microparticles for Dry Powder Inhalation, produced by environmentally driven In-situ Microcronization technique at different processing parameters, for inhalation therapy. Typically particle size reduction process employs jet-milling technology which can be destructive to the solid-state properties of the particles. Salbutamol Sulphate, as one of the β2-adrenoceptor stimulant commonly used in the treatment of bronchial asthmaby pulmonary delivery.The objective of the current work was to developed microcrystals by using In-situ Microcronization technique with different processing parameters. A response surface type central composite design were employed using Design-Expert 5.0 software (Stat Ease, QD Consulting, Penzance, UK) with the factors investigated werestirrer speeds investigated were 500(-1), 1000(0) and 1500 (1) rpm, addition rate of non-solvent i.e ethanol was studied at 50(-1), 100(0) and 150(1) g /min and stabilizer conc. were 0.5(-1), 1(0) and 1.5 %( 1). In the bottom up technique of micro sizing we use in-situmicronization technique which carried out using the solvent change method in presence of HPMC as stabilizing agent. The suspension wasspray dried thereafter.Optimize the process variables for less mean particle size and high Fine Particle Fraction (FPF). Spray dried crystals were subjected to XRD, FTIR, DSC and SEM analysis for stability. The PSD and FPF also depended on the balance of meso and micromixing determined by the crystallization conditions. Optimized formulation was identified and characterized to determine their suitability for pulmonary delivery by using MSLI. Optimized formulation showed the highest FPF loaded and FPF emitted of 78 (1%) and 84 ( 3%) respectively, depositing mainly on stages 3 and 4, with much lower amounts collected on the higher stages of the MSLI.