他克莫司半固体骨架缓释胶囊的制备

Studies on tacrolimus extended release semisolid matrix filled capsules

目的制备他克莫司半固体骨架缓释胶囊,考察其体外药物释放性质。方法以不同亲水亲油平衡值(HLB)和(或)熔点的骨架材料及稳定剂,通过液体灌装的方法制备他克莫司半固体骨架缓释胶囊,考察骨架材料对体外药物释放的影响,扫描电子显微镜观察药物释放后骨架的形貌。结果由亲水和疏水骨架材料制成的胶囊具有适宜的缓释特征,稳定剂羟丙基纤维素有助于增加胶囊的稳定性。结论以半固体骨架技术可方便制备他克莫司缓释胶囊。

Objective To prepare tacrolimus extended release semisolid matrix filled capsules,and evaluate the in vitro drug release properties.Methods Using the mixture of lipid materials with different HLB and melt points and stabilizer(HPC) as the matrix,the tacrolimus capsules were prepared by melting and liquid filling process.The in vitro drug release of the capsules was studied,and the morphology of the matrix after drug relese was observed with SEM.Results This semisolid matrix filled capsules composed of hydrophilic and hydrophobic lipid materials indicated suitable drug release property in vitro,and the addition of HPC in the matrix improved the stablility of the capsules.Conclusion This semisolid matrix filling is a simple method to prepare tacrolimus extended release capsules.