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目的:制备4-氨基吡啶(4-aminopyridine,4-AP)亲水凝胶骨架缓释片。方法:以羟丙甲纤维素的规格、处方用量及乳糖处方用量为因素设计正交试验,以体外释放度为考察指标,优化4-AP凝胶骨架片的处方,并进行批内和批间体外释放度验证试验。采用Origin软件对筛选出的最优处方释放度进行Weibull曲线拟合。考察体外释放条件对药物释放的影响。结果:优化处方为HPMC规格为K100LV,处方用量为54%,乳糖的处方用量为16%。所制得4-AP凝胶骨架片可持续释药12 h,批内释放均一性及批间重复性均良好。Weibull模型拟合方程得出药物释放符合一级速率过程。体外释放条件考察结果表明,转速对药物的释放有影响,而释放介质的种类和测定装置则无显著性影响。结论:所选4-AP凝胶骨架缓释片制备工艺可行,重复性好,有明显的缓释特性。
Objective: To prepare 4-aminopyridine (4-AP) hydrophilic gel matrix sustained-release tablets. Methods: Orthogonal test was designed with the specifications of hypromellose, prescription dosage and dosage of lactose as prescription. The in vitro release degree was taken as the index to optimize the formulation of 4-AP gel matrix tablets. In vitro release test. Origin software was used to fit Weibull curve fitting to the optimal prescription release. To investigate the release of drugs in vitro release conditions. Results: The optimal formulation was HP100 with K100LV, prescription was 54% and lactose was 16%. The prepared 4-AP gel matrix tablets sustained release of drug for 12 h, both in-batch release uniformity and batch-to-batch repeatability were good. The Weibull model fitting equation shows that drug release conforms to the first order rate process. The results of in vitro release showed that the rotational speed had an influence on the drug release, but the type of release medium and the measuring device had no significant effect. Conclusion: The preparation of 4-AP gel matrix sustained-release tablets is feasible, reproducible and has obvious sustained-release properties.