Heng P W, Wan L S
J Pharm Sci. 1985 Mar;74(3):269-72. doi: 10.1002/jps.2600740309.
Polysorbate 80 incorporated in sulfanilamide granules was found to depress the dissolution of sulfanilamide. The largest decrease corresponded to the lowest concentration of surfactant used. Sulfanilamide granules formulated with either starch or microcrystalline cellulose also decreased the release of the drug. The effect of starch depressing sulfanilamide dissolution was greater with higher starch content in the granules. However, addition of polysorbate 80 improved the dissolution of sulfanilamide granules containing starch but not those with microcrystalline cellulose. This difference was found to be related to the ability of starch to swell and cause granule disintegration. The inclusion of polysorbate 80 in starch-containing granules produced softer and more densely packed granules which were more responsive to the swelling effect of starch.
研究发现，掺入磺胺嘧啶颗粒中的聚山梨酯80会抑制磺胺嘧啶的溶解。最大降幅对应所用表面活性剂的最低浓度。用淀粉或微晶纤维素配制的磺胺嘧啶颗粒也会降低药物的释放。颗粒中淀粉含量越高，淀粉抑制磺胺嘧啶溶解的效果越显著。然而，添加聚山梨酯80可改善含淀粉的磺胺嘧啶颗粒的溶解，但对含微晶纤维素的颗粒则无此作用。发现这种差异与淀粉膨胀并导致颗粒崩解的能力有关。在含淀粉颗粒中加入聚山梨酯80会产生更软且堆积更紧密的颗粒，这些颗粒对淀粉的膨胀作用更敏感。
