Maliba Pharmacy College, Bardoli Mahuva road, Dist. Surat, Gujarat, India -394 350.
Curr Drug Deliv. 2012 Jul;9(4):395-404. doi: 10.2174/156720112801323134.
The present study was carried out with a view to enhance dissolution rate of poorly water-soluble drug glipizide (GZ) (BCS class II) using polyethylene glycol (PEG) 6000, PEG 8000 and poloxamer (PXM) 188 as carriers. Solid dispersions (SDs) were prepared by melting method using different ratios of glipizide to carriers. Phase solubility study was conducted to evaluate the effect of carrier on aqueous solubility of glipizide. SD was optimized by drug content estimation and in vitro dissolution study and optimised SD was subjected to bulk characterization, Scanning electron microscopy (SEM), Fourier transformation infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC) and X-ray diffraction study (XRD). Preclinical study was performed in mice to study the decrease in blood glucose level from prepared SD compared with pure drug. Due to high solubility and drug release, PXM 188 in weight ratio of 1:2 was optimized. Decrease in blood glucose level in mice from SD was significantly higher (p < 0.05) compared to pure glipizide. Thus, solid dispersion technique can be successfully used for the improvement of the dissolution profile of GZ.
本研究旨在通过使用聚乙二醇(PEG)6000、PEG 8000 和泊洛沙姆(PXM)188 作为载体来提高难溶性药物格列吡嗪(GZ)(BCS 分类 II)的溶出速率。采用熔融法制备了不同比例的格列吡嗪与载体的固体分散体(SD)。通过相溶解度研究评估了载体对格列吡嗪水溶解度的影响。通过药物含量测定和体外溶出度研究优化了 SD,并对优化后的 SD 进行了物理性质表征、扫描电子显微镜(SEM)、傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)和 X 射线衍射研究(XRD)。在小鼠中进行了临床前研究,以研究与纯药物相比,从制备的 SD 中降低血糖水平的效果。由于高溶解度和药物释放,重量比为 1:2 的 PXM 188 被优化。与纯格列吡嗪相比,来自 SD 的小鼠血糖水平降低显著更高(p < 0.05)。因此,固体分散技术可成功用于改善 GZ 的溶出度曲线。