β-内酰胺水合物晶体药物  

Crystal drugs ofβ-lactam hydrates

作　　者：胡昌勤[1] Hu Chang-qin(National Institutes for Food and Drug Control,Beijing 102629)

机构地区：[1]中国食品药品检定研究院,北京102629

出　　处：《中国抗生素杂志》2023年第3期241-249,共9页Chinese Journal of Antibiotics

摘　　要：β-内酰胺抗生素水合物作为一类重要的晶体药物在药物研发中被广泛关注。在β-内酰胺水合物晶体药物中,结构相似的药物具有相似的分子构型,但其可以和水分子相互作用组成不同的晶胞结构,形成不同的水合物晶体。晶体中的水分子与药物分子通过氢键、配位键等形成较强的相互作用,表现为典型的化学计量特征,通常在维系晶格的稳定性中起关键作用;而与药物分子作用相对较弱的结晶水,表现为非化学计量特征,通常主要作用是维系水合物晶体的稳定性。选择适宜的结晶工艺、优化过程控制条件是得到稳定晶体药物的关键。As an important part of crystalline drugs,theβ-lactam antibiotic hydrate has drawn much attention in drug research and development.Among the crystalline drugs ofβ-lactam hydrate,theβ-lactams with similar structure may have similar molecular configurations,but they can interact with water molecules to form different crystal cells so that to form different hydrate crystals.Parts of the water molecules in crystals demonstrate strong interactions with drug molecules through hydrogen bonds and coordination bonds,which show typical stoichiometric characteristics,and usually play a major role in keeping the stability of the lattice.The other parts of the water molecules,which usually are non-stoichiometric hydrates with relatively weak interaction to drug molecules,play the role in maintaining the stability of hydrate crystals.In order to continually get stable crystalline drugs in manufacture,an appropriate crystallization process and good controlled conditions are important.

关 键 词：Β-内酰胺抗生素 晶体药物 药物水合物 特性 

分 类 号：R978.1[医药卫生—药品]