Design, formulation and evaluation of Azithromycin binary solid dispersions using Kolliphor series for the solubility and in vitro dissolution rate enhancement
Design, formulation and evaluation of Azithromycin binary solid dispersions using Kolliphor series for the solubility and in vitro dissolution rate enhancement
复制标题
DOI：
10.1007/s40005-013-0108-x
复制
发表时间：
2014-04-01
影响因子：
5.5
通讯作者：
Mortazavi, Seyed Alireza
中科院分区：
文献类型：
--
作者：
Adeli, Ehsan;Mortazavi, Seyed Alireza
本研究主要目的是利用固体分散技术，以Kolliphor P 237、Kolliphor P 338和Kolliphor P 407为载体，提高阿奇霉素的溶解度和溶出速率。Kolliphor（P 237、P 338和P 407），其具有各种重量性质{（1：0.5）、（1：1）、（1：1.5）和（1：2）}，利用溶剂蒸发法。根据美国药典方法，在pH 6.0的磷酸盐缓冲液中进行溶出度研究。研究了药物释放曲线，因此我们发现药物的溶出速率（通过计算溶出参数）与纯药物相比显著增加，物理混合物以及固体分散体的溶解度与完整药物相比也增加。例如，药物的溶解度从85-753 μ g/mL（-1）增加（对于Kolliphor P 237; 8倍多）。结果表明，以P237、P338、P407为最佳. IR光谱显示药物和聚合物之间没有化学不相容性。采用差示扫描量热法、粉末X射线衍射和扫描电子显微镜研究了药物-聚合物相互作用。Kolliphor可显著提高阿奇霉素固体分散体的溶出度和溶解度。另外，该方法简单有效，达到了项目目标。
The main purpose of this investigation is increasing of the solubility and dissolution rate of Azithromycin by solid dispersion technique using Kolliphor P 237, Kolliphor P 338 and Kolliphor P 407. Kolliphor (P 237, P 338 and P 407) in various properties by weight {(1:0.5), (1:1), (1:1.5) and (1:2)}, utilizing solvent evaporation method. Dissolution studies carried out in phosphate buffer with pH 6.0 according to US pharmacopoeia method. The drug release profiles were studied, so we found that the dissolution rate of the drug (by calculating the dissolution parameters) was significantly increase compared to pure drug, also solubility of physical mixtures as well as solid dispersions increased compared to the intact drug. For example solubility of the drug increased from 85-753 mu g mL(-1) (for Kolliphor P 237; 8 times more). The best results were as follows: Kolliphor P 237 > Kolliphor P 338 > Kolliphor P 407. IR spectra revealed no chemical incompatibility between drug and polymer. Drug-polymer interactions were investigated using differential scanning calorimetry, powder X-ray diffraction and scanning election microscopy. The dissolution rate and solubility of Azithromycin solid dispersions was improved significantly using Kolliphor. In addition, the simplicity of this method is very effective and have been met the project objectives.