Sancheti P P, Vyas V M, Shah M, Karekar P, Pore Y V
Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra, India.
Pharmazie. 2008 Aug;63(8):571-5.
The objective of the present work was to improve the dissolution rate of a poorly water-soluble drug, bicalutamide, by a solid dispersion technique. The solid dispersion systems of bicalutamide were prepared with poloxamer F68 in 1:1, 1:3, and 1:5 ratios using the melting method. The interaction of drug with polymer was evaluated by TLC, FTIR, and powder XRD. The results of powder XRD showed a significant decrease in the crystallinity of drug in the binary systems of bicalutamide. All binary systems of bicalutamide showed faster dissolution than pure drug alone (p < 0.001). However, among all binary systems studied, 1:1 proportion of bicalutamide : poloxamer was found to be excellent for dissolution enhancement (DP30: 99.98% +/- 3.9) of bicalutamide. The higher ratios of poloxamer F68 (1:3 and 1:5) had retarded the release of drug from their corresponding binary systems which might be due to its gelling property in higher concentration.
本研究的目的是通过固体分散技术提高难溶性药物比卡鲁胺的溶出速率。采用熔融法，以泊洛沙姆F68为载体，按1:1、1:3和1:5的比例制备比卡鲁胺固体分散体系统。通过薄层色谱法（TLC）、傅里叶变换红外光谱法（FTIR）和粉末X射线衍射法（XRD）评估药物与聚合物之间的相互作用。粉末XRD结果显示，在比卡鲁胺二元体系中药物的结晶度显著降低。比卡鲁胺的所有二元体系的溶出速度均比单独的纯药物快（p < 0.001）。然而，在所有研究的二元体系中，发现比卡鲁胺与泊洛沙姆1:1的比例对提高比卡鲁胺的溶出效果极佳（DP30：99.98% +/- 3.9）。较高比例的泊洛沙姆F68（1:3和1:5）延缓了药物从其相应二元体系中的释放，这可能是由于其在高浓度下的胶凝特性所致。
