共研磨法改善氢化可的松等难溶性药物的体外溶出度

Enhancement of dissolution property of drugs from ground mixtures with pregelatinized starch

将氢化可的松、醋酸地塞米松与亲水性辅料可压性淀粉按一定比例在球磨机中研磨制备成研磨混合物。体外溶出结果表明:研磨混合物粉末中主药溶出迅速,较物理混合物及原药粉末有显著提高;采用粉末直接压片工艺,以研磨混合物制备的片剂中主药溶出较物理混合物片及市售片亦有很大程度的提高。X-射线衍射试验,扫描电镜分析结果表明:研磨混合物中主药是以非晶态存在的,且部分药物以极微小的粒子分布在可压性淀粉的表面。稳定性试验结果表明:研磨混合物粉末在37℃、相对湿度75%的条件下存放3个月,药物含量及体外溶出速度并无下降。

Ground mixtues of hydrocortisone(HC),de-xamethasone acetas(DA)with pregelatinized starch(PGS)were prepared by grinding in a ball mill.The dissolution test in vitro indicated that groundmixture powder gave a higher rate of drug dissolu-tion than physical mixture or intact drug powderand that the dissolution rate of drugs from thetablets prepared with ground mixture powder wasalso significantly greater than that from commercialtablets.The X-ray diffraction patterns and scanningelectron micrographs suggested that when the weightration of drugs with pregelatinized starch was up to1:5,drugs in ground mixture powder were in anamorphous state after 90 min of grinding.Whenground mixture powder was persevered for 3months 37℃ and RH75%,the drug content anddissolution rate in vitro showed no reduction.