肠溶缓释型替米考星固体分散体的制备、鉴定及体外释放度评价

Preparation and identification of enteric-coated sustained-release solid dispersions of tilmicosin and evaluation of their release degree

【目的】以CMEC、Eudragit L100和HPMCP hp55s为载体,用溶剂法制备肠溶缓释型替米考星固体分散体.【方法】用X射线粉末衍射法和傅里叶变换红外光谱法对制备的3种固体分散体进行物相鉴定,并对其体外释放度进行评价.【结果】制备的3种替米考星固体分散体均为晶体结构,替米考星以无定形态分散于载体中.制备的TMC+CMEC SD、TMC+Eudragit SD和TMC+HPMCP SD 120 min时在酸中溶出量分别为8.91%、6.57%和7.04%,45 min时在缓冲液中累计溶出度分别为70.75%、75.92%和72.35%,均符合兽药典对肠溶制剂的溶出量规定.【结论】用溶剂法制备肠溶缓释型替米考星固体分散体工艺简单可行,在掩盖替米考星苦味的同时,有效解决了替米考星的胃刺激性问题.

【Objective】In this study,CMEC,Eudragit L100 and HPMCP hp55s were used as carriers to prepare the enteric-coated and sustained-release tilmicosin solid dispersion with solvent method.【Method】Three prepared tilmicosin solid dispersions were identified by the ways of XRPD and FTIR,and meanwhile their in-vitro release degree was assessed.【Result】The three prepared solid dispersions of tilmicosin were all crystal-structured,and tilmicosin was dispersed in the carrier in an amorphous form.The dissolution rates of TMC+CMEC SD,TMC+Eudragit SD and TMC+HPMCP SD are 8.91%,6.57%and 7.04%during 120 min in acidic liquid,respectively,and 70.75%,75.92%and 72.35%during 45 mins in buffer,and they all met the standards of enteric-coated preparations in veterinary pharmacopoeia.【Conclusion】The preparation of tilmicosin solid dispersions by solvent method was simple and feasible,and the preparations could cover up the bitterness of tilmicosin and effectively solve the problem of gastric irritation of tilmicosin.