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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。
Objective To prepare nimodipine sustained release tablets by melt extrusion technology. Methods Nimodipine dispersions with different drug-carrier ratios were prepared by melt extrusion using PVP K30, PVPVA 64, PVPVA S-630 and Poloxamer 188-PVP K30 (2: 8) as carriers, respectively. The state of nimodipine in the carrier was identified by X-ray powder diffraction (XRD). The optimal solid dispersion was selected to prepare nimodipine sustained release tablets with hypromellose (HPMC) as the matrix material. Results The PVPVA 64 was used as a carrier to prepare a solid dispersion with a drug-carrier ratio of 1: 5. The cumulative dissolution rate at 1 h was 98.5%. Sustained release of nimodipine sustained-release tablets in vitro 12 h or more, 12 h accumulated release was 97.1%, in vitro release behavior in line with zero-order release equation. Conclusion Melt-extrusion technique can improve the dissolution rate of drug in vitro. Nimodipine sustained-release tablets have reasonable prescription, stable technology and long-lasting effect.