泰万菌素肠溶微丸的研制及质量评价

Preparation and quality evaluation of tylvalosin enteric coated pellets

为用挤出-滚圆技术制备100g/kg泰万菌素肠溶微丸,并对其进行初步的质量评价,以泰万菌素、微晶纤维素、乳糖、羧甲基淀粉钠、氯化钠为基础配方制备素丸,以丙烯酸树脂Eudragit L30D-55水分散体作为肠溶包衣材料,单因素与正交试验筛选处方及工艺条件,制备泰万菌素肠溶微丸,采用高效液相色谱法和体外溶出试验测定该微丸的载药量和释放度。结果显示,泰万菌素、微晶纤维素、乳糖、羧甲基淀粉钠、氯化钠在合适的质量比下,包衣增重20%,制备的肠溶微丸圆整度合格,平均粒径过孔径0.350~0.701mm标准检验筛,收率达到90%以上,平均载药量9.96%,在0.1mol/L盐酸溶液中2h释放度低于10%,在pH6.8的磷酸钠缓冲液中45min释放度达到90%以上。结论：该微丸载药量稳定,体外释放度符合《中华人民共和国兽药典》肠溶型标准。

The aim of the present study was to prepare 100g/kg tylvalosin enteric pellets by extrusionspheronization method,and estimate the quality preliminary.Tylvalosin enteric pellets were prepared by basic formula including MCC,lactose,CMS-Na,NaCl,and coated by fluid-bed with polyacrylic resin Eudragit L30D-55.The formulation and technology of tylvalosin enteric pellets were selected by single-factor and orthogonal test.The content and dissolution rate of tylvalosin were determined by high performance liquid chromatography and dissolution method in vitro,respectively.The results showed that tylvalosin enteric pellets with the optimized preparation were released less than 10%in 0.1mol/L hydrochloric acid solution in the first 2hours and released more than 90%in pH6.8phosphoric buffer within 45 minutes.The pellets had smooth roundness,yield above 90%,and average drug-loading capacity was 9.96%.In conclusion,the drug-loading capacity of pellets was stable and in vitro release degree met the requirement for enteric-coated formulations set by Chinese Veterinary Pharmacopoeia.