Department of Pharmaceutics and Pharmaceutical Technology, Damascus University, Syria.
Arch Pharm Res. 2010 Nov;33(11):1771-9. doi: 10.1007/s12272-010-1109-1. Epub 2010 Nov 30.
Nystatin is commonly employed to treat fungal infections in the mouth. It is not absorbed via the stomach and it will therefore not treat fungal infections in any part of the body other than the mouth. Nystatin buccoadhesive tablets release the drug very slowly due to the poor solubility of nystatin in water and also the presence of polymers with mucoadhesive properties. Therefore, the aim of the present study was to improve drug release from buccoadhesive tablets, while retaining adequate mucoadhesive properties. To this end, a solid dispersion of nystatin: lactose (1:3) was prepared and mixed with xanthan. The effects of hydrophilic surfactants such as cremophor RH40 and Tween 80 on drug release and mucoadhesive properties of nystatin tablets were also investigated as were swelling and erosion indices and strength of bioadhesion in vitro to a biological membrane. The interaction between nystatin and lactose in solid dispersion formulation was investigated by XRPD, FT-IR and DSC. The results showed that a solid dispersion formulation and mucoadhesive tablets containing surfactants led to faster drug release than their simple physical mixtures. Drug release was also faster from a solid dispersion compared to tablets containing surfactants. Swelling and erosion results showed that tablets made of a solid dispersion swelled and eroded faster than a physical mixture formulation. The presence of surfactant slightly increased the degree of swelling and erosion of buccoadhesive tablets.
制霉菌素通常用于治疗口腔真菌感染。它不会被胃吸收，因此不会治疗身体其他部位（口腔除外）的真菌感染。制霉菌素颊黏附片由于制霉菌素在水中的溶解度差以及具有黏膜黏附特性的聚合物的存在，药物释放非常缓慢。因此，本研究的目的是改善颊黏附片中药物的释放，同时保持足够的黏膜黏附特性。为此，制备了制霉菌素：乳糖（1:3）的固体分散体，并与黄原胶混合。还研究了亲水性表面活性剂如 Cremophor RH40 和吐温 80 对制霉菌素片剂的药物释放和黏膜黏附特性的影响，以及体外对生物膜的膨胀和侵蚀指数和生物黏附强度。通过 X 射线粉末衍射（XRPD）、傅里叶变换红外光谱（FT-IR）和差示扫描量热法（DSC）研究了固体分散体制剂中制霉菌素与乳糖之间的相互作用。结果表明，与简单的物理混合物相比，含有表面活性剂的固体分散体制剂和黏膜黏附片导致药物释放更快。与含有表面活性剂的片剂相比，固体分散体的药物释放也更快。膨胀和侵蚀结果表明，固体分散体片剂的膨胀和侵蚀速度快于物理混合物制剂。表面活性剂的存在略微增加了颊黏附片的溶胀和侵蚀程度。
