4-氨基水杨酸钠结肠定位包衣片的制备及释放度测定

目的:以多层包衣法制备4-氨基水杨酸钠口服结肠定位系统,并考察其释放度,评价包衣工艺的稳定性。方法:用渗透型和肠溶型丙烯酸树脂依次包衣,制备pH、时间双重依赖的4-氨基水杨酸钠口服结肠定位包衣片;采用紫外分光光度法测定包衣片在不同pH条件下的释放度及3批包衣片在pH=7.4介质中的累积释放度,计算并比较释放参数T50、Td、T80、m。结果:包衣片在pH=6.5介质中12h释药量小于5%,有明显时滞;在pH=7.0、pH=7.4介质中12h内释药量均大于80%,无时滞效应;3批包衣片溶出度参数之间比较均无显著性差异(P>0.05)。结论:以渗透型和肠溶型丙烯酸树脂依次包衣制备的4-氨基水杨酸钠口服结肠定位包衣片具备理想的定位与缓释功能,包衣工艺稳定,重现性好。

Preparation of 4- Paramisan Sodium Colon- specific Delivery Coated Tablets and the Determination of Its Drug- releasing Rate

OBJECTIVE:To prepare a new type of4-paramisan sodium oral colon-specific delivery system by multiˉlayer-coating method and to investigate its releasing rate as well as to evaluate the stability of the coating technology.METHODS:A double(both pH and time)dependent4-paramisan sodium oral colon-specific delivery coating tablets coated in turn with permeable and enteric soluble acrylic resin;The release rate of coating tablets under different pH conditions and the accumulative release rates of3batches of coated tablets in pH=7.4medium were also determined by ultraviolet spectrophotometry,and the releasing parameters like T 50 ,T d ,T 80 ,m were calculated and compared.RESULTS:The12h drug release of the coated tablets at pH=6.5medium was no more than5%and in which there was an obvious time lag;The12h drug releases of the coated tablets at pH=7.0and pH=7.4were all more than80%and in which no lag time effects were noted;No significant differences were noted in terms of the parameters of dissolution rates among the3batches of coated tablets(P>0.05).CONCLUSION:4-paramisan sodium oral colon-specific delivery coated tablets coated in turn with permeable and enteric soluble acrylic resin has ideal specific delivery and slow-release properties,the coating technology was stable and the reproducibility is good.