Ozkan Y, Atay T, Dikmen N, Işimer A, Aboul-Enein H Y
Department of Pharmaceutical Technology, Gülhane Military Medical Academy, Etlik-Ankara, Turkey.
Pharm Acta Helv. 2000 Apr;74(4):365-70. doi: 10.1016/s0031-6865(99)00063-1.
Inclusion complexes of gliclazide with beta-cyclodextrin were prepared using different two methods: neutralization and recrysstalization. Host-guest interactions were studied in the solid state by X-ray diffractometry and infrared spectroscopy. The stability constant between gliclazide and beta-cyclodextrin was calculated from the phase solubility diagram. It was found that the neutralization technique and a solid complex of gliclazide with beta-cyclodextrin in a molar ratio of 1.5:1 could be used to prepare the amorphous state of drug inclusion complexes. The dissolution rates of gliclazide from the inclusion complex made by neutralization was much faster than the pure drug, physical mixture of drug and cyclodextrin, recyristalization system and also comparable to the data reported in literature. Results of this report indicate that beta-cyclodextrin could be useful for the solid gliclazide formulations as it may results in a more rapid and uniform release of the drug.
使用两种不同方法制备了格列齐特与β-环糊精的包合物：中和法和重结晶法。通过X射线衍射法和红外光谱法对固态下的主客体相互作用进行了研究。根据相溶解度图计算了格列齐特与β-环糊精之间的稳定常数。结果发现，中和技术以及摩尔比为1.5:1的格列齐特与β-环糊精的固体复合物可用于制备药物包合物的无定形状态。由中和法制备的包合物中格列齐特的溶出速率比纯药物、药物与环糊精的物理混合物、重结晶体系快得多，并且与文献报道的数据相当。本报告结果表明，β-环糊精可用于格列齐特固体剂型，因为它可能导致药物更快速、均匀地释放。
