Hypromellose acetate succinate(HPMCAS) microparticles containing the poorly-water soluble drug celecoxib(CEL) were prepared by electrospraying intended for oral drug delivery. Various solvent mixtures with different s...Hypromellose acetate succinate(HPMCAS) microparticles containing the poorly-water soluble drug celecoxib(CEL) were prepared by electrospraying intended for oral drug delivery. Various solvent mixtures with different solubility for CEL and HPMCAS were used to induce changes in the polymer structural conformation of the microparticles. The performance of the prepared microparticles was evaluated by studying the solid state from, particle size and morphology, radial drug distribution and drug release. CEL was amorphous in all electrosprayed HPMCAS microparticles. The particle size and morphology was dependent on the solubility of HPMCAS in the solvent mixture used with poorer solvents resulting in smaller microparticles with rougher appearance. The CEL distribution on the particles surface was relatively homogeneous and similar for all microparticles. Drug release from the microparticles was observed at a higher rate depending on the solubility of HPMCAS in the solvent used for electrospraying, and in all cases an at least 4-fold higher rate was observed compared with the crystalline drug. Drug precipitation from the supersaturated solution was inhibited by HPMCAS for all microparticles based on its parachute effect while crystalline CEL did not reach supersaturation. This study demonstrated that electrospraying can be used to produce microparticles with tailored properties for pharmaceutical application by adjusting solvent selection.展开更多
The increasing demand for personalized medicine necessitates the production of easily customizable dosage forms. As the number of possible dosage forms may scale toward infinity, their uniqueness requires a versatile ...The increasing demand for personalized medicine necessitates the production of easily customizable dosage forms. As the number of possible dosage forms may scale toward infinity, their uniqueness requires a versatile production platform and numerical simulation in order to be manufactured efficiently. A mathematical description of these systems is the only feasible approach to manage such diverse properties of different products. However,experimental verification is still essential for evaluation of processability and related concomitant phenomena, such as possible solid state changes that may occur during production and storage.展开更多
Oral dosage forms including tablets and capsules are themost commonly used drug products. For some poorly water-soluble and poorly permeable drugs injectable dosage formscan be used to circumvent the challenges of poo...Oral dosage forms including tablets and capsules are themost commonly used drug products. For some poorly water-soluble and poorly permeable drugs injectable dosage formscan be used to circumvent the challenges of poor bioavailabil-ity.展开更多
基金the Danish Council for Inde-pendent Research(Grant No.DFF-12-131927)for financial sup-port of this project
文摘Hypromellose acetate succinate(HPMCAS) microparticles containing the poorly-water soluble drug celecoxib(CEL) were prepared by electrospraying intended for oral drug delivery. Various solvent mixtures with different solubility for CEL and HPMCAS were used to induce changes in the polymer structural conformation of the microparticles. The performance of the prepared microparticles was evaluated by studying the solid state from, particle size and morphology, radial drug distribution and drug release. CEL was amorphous in all electrosprayed HPMCAS microparticles. The particle size and morphology was dependent on the solubility of HPMCAS in the solvent mixture used with poorer solvents resulting in smaller microparticles with rougher appearance. The CEL distribution on the particles surface was relatively homogeneous and similar for all microparticles. Drug release from the microparticles was observed at a higher rate depending on the solubility of HPMCAS in the solvent used for electrospraying, and in all cases an at least 4-fold higher rate was observed compared with the crystalline drug. Drug precipitation from the supersaturated solution was inhibited by HPMCAS for all microparticles based on its parachute effect while crystalline CEL did not reach supersaturation. This study demonstrated that electrospraying can be used to produce microparticles with tailored properties for pharmaceutical application by adjusting solvent selection.
文摘The increasing demand for personalized medicine necessitates the production of easily customizable dosage forms. As the number of possible dosage forms may scale toward infinity, their uniqueness requires a versatile production platform and numerical simulation in order to be manufactured efficiently. A mathematical description of these systems is the only feasible approach to manage such diverse properties of different products. However,experimental verification is still essential for evaluation of processability and related concomitant phenomena, such as possible solid state changes that may occur during production and storage.
文摘Oral dosage forms including tablets and capsules are themost commonly used drug products. For some poorly water-soluble and poorly permeable drugs injectable dosage formscan be used to circumvent the challenges of poor bioavailabil-ity.
