Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga, Mumbai-400019 India.
Acta Pharm. 2011 Dec;61(4):435-45. doi: 10.2478/v10007-011-0036-0.
Liquid antisolvent process was explored as a solubility modulating tool. Bicalutamide, a poorly water soluble drug, was used as a candidate. Low aqueous solubility and poor dissolution of bicalutamide results into poor and variable bioavailability. Therefore, the objective of the present work was to modify the solubility of bicalutamide using the liquid antisolvent precipitation process. HPMC E5 and Poloxamer 407 were shortlisted as a hydrophilic polymer and surfactant, respectively, for the process. Process optimization was done with respect to the hydrophilic polymer, surfactant and drug loading concentration. The resultant microcrystals were characterized with various instrumental techniques for material characterization such as IR, DSC, SEM, XRD, particle size, specific surface area and dissolution kinetics.
本文探索了液-抗溶剂法作为一种调节溶解度的手段。比卡鲁胺是一种水溶性差的药物，被选为研究对象。比卡鲁胺水溶性低，溶解差，导致生物利用度差且不稳定。因此，本工作的目的是使用液-抗溶剂沉淀法来改善比卡鲁胺的溶解度。HPMC E5 和泊洛沙姆 407 分别被选为亲水性聚合物和表面活性剂用于该过程。过程优化考虑了亲水性聚合物、表面活性剂和药物负载浓度。所得的微晶体用各种仪器技术进行了材料特性表征，如红外（IR）、差示扫描量热法（DSC）、扫描电子显微镜（SEM）、X 射线衍射（XRD）、粒径、比表面积和溶解动力学。
