形成比卡鲁胺纳米分散体以提高溶解速率。

Formation of bicalutamide nanodispersion for dissolution rate enhancement.

机构信息

Key Lab for Nanomaterials, Ministry of Education, Beijing University of Chemical Technology, Beijing 100029, PR China.

出版信息

Int J Pharm. 2011 Feb 14;404(1-2):257-63. doi: 10.1016/j.ijpharm.2010.11.015. Epub 2010 Nov 18.

DOI:10.1016/j.ijpharm.2010.11.015

Abstract

Bicalutamide was loaded on hydrophilic excipients to form nanodispersions via a combination of anti-solvent precipitation and spray drying method. The particle size, BET surface area, contact angles and dissolution rate of the nanodispersions were analyzed. The results indicated that lactose was a suitable matrix to prevent the bicalutamide particles growth and aggregation. The lactose loaded particles had a mean size of 330 nm within a narrow distribution. X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) characterization indicated the nanodispersion exhibited unchanged crystalline and chemical structure. Dissolution rate of bicalutamide nanodispersion was significantly faster than that of commercial products. It increased to 94% in 10 min while both commercial formulas Casodex and bicalutamide tablets dissolved 60% and 38% respectively at the same period. It was proposed that the enhanced dissolution rate of bicalutamide nanodispersion contribute to high surface area and well-wetted state of drug particles.

摘要

比卡鲁胺通过抗溶剂沉淀和喷雾干燥法结合亲水辅料形成纳米分散体。分析了纳米分散体的粒径、BET 比表面积、接触角和溶出速率。结果表明，乳糖是防止比卡鲁胺颗粒生长和聚集的合适基质。载有乳糖的颗粒具有狭窄分布的 330nm 左右的平均粒径。X 射线衍射（XRD）、差示扫描量热法（DSC）和傅里叶变换红外（FT-IR）特性表明纳米分散体表现出不变的晶体和化学结构。比卡鲁胺纳米分散体的溶出速率明显快于商业产品。在 10 分钟内增加到 94%，而同期的两种商业配方 Casodex 和比卡鲁胺片剂分别溶解 60%和 38%。据认为，比卡鲁胺纳米分散体的增强溶出速率归因于药物颗粒的高表面积和良好润湿状态。