小儿清热止咳分散片的填充剂与崩解剂筛选

目的为了制备中药分散片,以小儿清热止咳糖浆方剂为模型药物筛选中药分散片的填充剂和崩解剂。方法以抗张强度、吸湿性和压缩功作为选择填充剂的依据,以吸水性实验、溶胀度实验、空白片崩解时限和加入质量分数为50%浸膏的片剂崩解时限为选择崩解剂的依据。测定发泡量和产气量作为选择泡腾崩解剂的依据。结果综合以抗张强度、吸湿性和压缩功大小,选择乳糖作为分散片的填充剂。溶胀性能优劣顺序是:CMS-Na>L-HPC(信越)>PVPP>MCC101>MCC301>L-HPC(国产)>MCC302>MCC102>滑石粉>干淀粉;吸水性能优劣顺序是:L-HPC(信越)>L-HPC(国产)>CMS-Na>PVPP>MCC302>MCC102>MCC301>MCC101>浸膏;单独使用微晶纤维素或超级崩解剂达不到分散片的质量要求,联用微晶纤维素和超级崩解剂,可以达到分散片质量要求。结论中药分散片的崩解剂可以采用超级崩解剂和微晶纤维素的混合物,泡腾崩解剂选用酒石酸和碳酸氢钠,其摩尔比为1.0∶0.8。

Screening of diluents and disintegrants of Xiao'er Qingrezhike dispersible tablets

Objective To screen the diluents and disintegrants of Xiao’er Qingrezhike medicine dispersible tablet, extract powder of Xiao’er Qingrezhike syrup formulation was used as model drug. Methods The dilutes of tablets was selected based on tensile strength, moisture absorption and compression work. Water absorption experiment, swelling capacity, blank tablet disintegration time and the tablet with 50 % extract powder were employed to select optimum disintegrants. Finally, disintegrability of the effervescence disintegrants was evaluated by effervescence capacity and aerogenesis. Results The results demonstrated that the lactose was better than other fillers in tensile strength, moisture absorption and compression work, And the sequence of swelling capacity was: CMS-Na>L-HPC(Shin-Etsu)>PVPP(ISP)>MCC101>MCC301>L-HPC(Domestic-made)>MCC302>MCC102>chalk>dried starch; the order of water absorption was: L-HPC(Shin-Etsu)>L-HPC(domestic-made)>CMS-Na>PVPP(ISP)>MCC302>MCC102>MCC301>MCC101>extract powder. However, it was shown that using MCC or super-disintegrant singlely could not meet the pharmacopoeia’s requirement for herbal dispersible tablets. The disintegration time for the herbal dispersible tablets were much shortened by the combination of super-disintegrant and MCC. The optimal ratio of acid to alkali was 1.0:0.8 for the effervescence disintegrants. Conclusions The combination of super-disintegrant and MCC should be applied during the preparation, and the optimal ratio of effervescence acid to alkali in effervescence disintegrants was 1.0:0.8 .