熔融挤出法制备尼莫地平缓释片

Preparation of Nimodipine Sustained-release Tablets by Hot Melt Extrusion Technology

关键词:  熔融挤出  尼莫地平  固体分散体  溶出度  缓释片

Key words:  hot melt extrusion  nimodipine  solid dispersion  dissolution  sustained-release tablets

摘要:

目的 采用熔融挤出技术制备尼莫地平缓释片。方法 分别以PVP K30、PVPVA 64、PVPVA S-630、 Poloxamer188-PVP K30(2∶8)为载体，采用熔融挤出法制备不同药物-载体比的尼莫地平分散体，比较体外溶出度，并利用X-射线粉末衍射(XRD)鉴别尼莫地平在载体中的状态。选取最优固体分散体，以羟丙甲纤维素(HPMC)为骨架材料，制备尼莫地平缓释片。结果 以PVPVA 64为载体制备固体分散体，药物-载体比为1∶5时，1 h累积溶出度为98.5%。尼莫地平缓释片体外持续释药12 h以上，12 h累积释药为97.1%，体外释药行为符合零级释药方程。结论 采用熔融挤出技术可以提高药物的体外溶出度，尼莫地平缓释片处方合理，工艺稳定，具有长效的特点。

Abstract:

OBJECTIVE To prepare the nimodipine(NMP) sustained-release tablets by applying the melt extrusion technique (HME). METHODS PVP K30, PVPVA 64, PVPVA S-630, Poloxamer188-PVP K30(2∶8) were using as matrix to prepare solid dispersions of NMP by HME. The evaluation of the properties of the dispersions prepared in different ratio of matrix to drug was performed using in vitro dissolution studies. And the dispersions prepared in the matrix were evaluated using XRD. The tablets were prepared with HPMC as the material using direct compression. RESULTS The dissolution accumulative release of NMP-PVPVA 64(1∶5) solid dispersion in 60 min was 98.5%. The release of sustained-release tablets was retarded over 12 h, and the accumulative release of NMP sustained-release tablets in 12 h was 97.1%, fitted in zero-order equation. CONCLUSION Dissolution of NMP can be improved by the HME technique. The formulation of NMP sustained-release tablets was feasible, stable and long acting.