摘要
目的：制备阿司匹林固体分散物；选择不影响阿司匹林稳定性的ＰＥＧ 载体及其合适比例；测定阿司匹林固体分散物的体外溶出速率；分析其结构状态。方法：固体分散物的制备采用熔融法；体外溶出采用浆法；固体分散物的结构分析采用Ｘ射线衍射法。结果：ＰＥＧ 所占比例越大，熔融法制备固体分散物时，阿司匹林的水解程度越低，且ＰＥＧ２００００ 优于ＰＥＧ６０００ ；阿司匹林ＰＥＧ２００００（１∶９） 固体分散物的标示百分含量为１０４ ．６８ ％ ，水杨酸检查合格；与原料药和物理混合物相比，其溶出度显著增加（ Ｐ＜ ０ ．０１） ；该固体分散物中大部分阿司匹林以分子状态分散，只有极少部分以微晶状态分散。结论：以ＰＥＧ２００００ 为载体，按阿司匹林ＰＥＧ＝ １∶９ 的比例制备阿司匹林固体分散物是理想的，该分散物体外溶出迅速，可用于制备小规格的片剂，在不影响疗效的前提下。
OBJECTIVE:To prepare aspirin solid dispersions,select the PEG carrier and the proper weight ratio between aspirin and PEG,and determine the in vitro dissolution rate and the structural characters of the aspirin PEG20000 solid dispersion.METHODS:The aspirin solid dispersions were prepared by melting method.The oar method was used for dissolution test.The structural analysis was made by X ray diffraction.RESULTS:The higher the weight ratio of PEG in solid dispersions,the more stable aspirin was in the course of preparing solid dispersions.As a carrier,PEG20000 was superior to PEG6000.The aspirin:PEG20000(1∶9) solid dispersion was stable in which the content of aspirin was 104.68%.The dissolution rate of aspirin in the solid dispersion was markedly higher than that of chemical that in the physical mixture(P<0.01).Most of substance aspirin in the solid dispersion dispersed in a molecular form,while little existed in a tiny crystal form.CONCLUSION:The stable aspirin PEG solid dispersion was formed only at the 1∶9(drug to PEG20000,w/w).The solid dispersion dissolves more rapidly,so it is feasible to reduce gastric irritation by lowering aspirin dose without curative effect loss.
出处
《中国现代应用药学》
CAS
CSCD
1999年第5期20-22,共3页
Chinese Journal of Modern Applied Pharmacy
关键词
阿司匹林
固体分散物
溶出度
aspirin,solid dispersion,dissolution rate
