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苦参素微孔渗透泵片的研制

Preparation of microporous osmotic pump tablets of marine

  • 摘要: 目的: 制备苦参素微孔渗透泵片,并进行处方优化和释药机制考察。 方法: 采用湿法制粒制备苦参素微孔渗透泵片芯,然后用薄膜包衣法进行包衣,通过释放度测定来考察影响因素;采用中心复合设计优化最佳处方;并对其释药机制进行了探讨。 结果: 成功制备了苦参素微孔渗透泵片,工艺操作具有重现性;实验发现溶出介质pH、转篮转速、片芯硬度及衣膜中增塑剂用量对药物的释放均无显著性影响;片芯中氯化钠含量,包衣膜中致孔剂含量以及包衣增重对微孔渗透泵片释放速率具有显著性影响;所制备的苦参素微孔渗透泵片12 h内释药具有零级释药特征,释放机制以渗透压为主。 结论: 以渗透压为释药机制的苦参素微孔渗透泵片有望成为上市缓释制剂。

     

    Abstract: Abstract Aim: To develop marine microporous osmotic pump tablets and to investigate drug release in vitro of the optimized formulation and the release mechanism. Methods: Wet granulation and film-coating were used to develop marine micro-osmotic pump tablets. in vitro release studies were applied to evaluate the impacts of various factors on the release of the formulation.Central-composite design was exploited to aid the optimization of the formulation,and the mechanism of in vitro release was characterized. Results: There existed fairly good reproducibility in the preparation of marine micro-osmotic pump tablets.It was found that no change in the release rate of the tablets were elicited by the pH of the release media,the rotating speed selected,the hardness of the tablet core,and the amount of the plasticizer incorporated into the coating formulation.It was proved that the release of marine micro-osmotic pump tablets was closely related to the magnitudes of NaCl amount in the tablet core and the pore former in the coating formulation as well as the coating level.In addition,there existed 12-hr zero-order kinetics in the in vitro release study of the tablets.Moreover,it was shown that the osmotic pressure-controlled delivery is greatly responsible for the release of the developed tablets. Conclusion: The prepared marine microporous osmotic pump tablets are expected to be a new sustained-release medication.

     

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