大环内酯类抗生素苦味的掩蔽及配方研究

STUDY OF A MASKING METHOD TO DISPEL THE BITTERNESS OF MACROLIDE-ANTIBIOTICS AND ITS APPLICATION TO PRESCRIPTIONS

目的：试验鞣酸作为掩蔽剂（辅料）及其配方，以消除大环内酯类抗生素的苦味，开发新制剂。方法：按沉淀反应原理，以（1）消除苦味；（2）在胃酸中溶解为指标，评定配方。结果；找到以鞣酸作掩蔽剂时，常用大环内酯类的适宜配方。结论：掩蔽法可消除麦迪霉素、麦白霉素等大环内酯类的苦味，制成口服颗粒剂，与修饰结构的方法比较，工艺简单，成本低，尤宜大众用药。

Objective: To test tannic acid as a masking agent(assistant)and study its prescriptions in order to dispel the bitterness of macrolide-antibiotics and to develop new preparations. Methods: On the basis of the principle of precipitation making up and assessing macrolide-antibioticts' prescriptions according to: (1)how they dispel bitterness and (2) how they dissolve in the gastric juice. Results: We found an effective masking agent - tannic acid and made up many suitable macrolide-antibiotics' oral granule preparations. Conclution:The masking method is an effective way of dispe1ing the bitterness of macrolide-antibiotics such as midecamycin. melumycin and so on. It has simpler technology and lower cost than those of synthetical or embellishing structure methods. Macrolide oral granules are suitable for popular usage.