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影响不同固体分散体中依泽替米贝释放的制剂因素。

Formulation factors affecting the release of ezetimibe from different liquisolid compacts.

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.

出版信息

Pharm Dev Technol. 2013 Mar-Apr;18(2):417-27. doi: 10.3109/10837450.2012.680594. Epub 2012 Apr 24.

DOI:10.3109/10837450.2012.680594
PMID:22530561
Abstract

CONTEXT

Liquisolid technique is one of the methods used to improve the dissolution rate of the poorly water soluble drugs utilizing non volatile liquids.

OBJECTIVES

Enhancement of the release of ezetimibe from different liquisolid formulations.

MATERIALS AND METHODS

Four liquid vehicles were used to prepare the liquid medications with different drug concentrations. The interaction between the drug and the excipients in liquisolid powders were characterized by DSC, X-ray, FTIR and SEM. Furthermore, the powder characteristics were evaluated by Carr's Index and powder wetting time determinations, respectively. All prepared formulations were compressed at different pressures to end with the same constant porosity and the tablets were evaluated by different tests and compared with conventional formula.

RESULTS AND DISCUSSION

No interaction had been detected in all liquisolid formulations as shown in the results of XRD, FTIR, DSC and SEM. In addition to that, all liquisolid compacts had expressed faster dissolution profiles compared with that of conventional formula.

CONCLUSION

The dissolution rate was affected by the drug concentration, solubility of the drug in the liquid vehicle and type of carrier. In addition, the presence of the liquid vehicle has been found to affect the mechanical properties of the liquisolid formulations.

摘要

背景

液质联用技术是一种利用非挥发性液体来提高难溶性药物溶出度的方法。

目的

提高不同液质联用制剂中埃扎替比的释放度。

材料与方法

采用四种液体载体制备不同药物浓度的液体制剂。通过 DSC、X 射线、FTIR 和 SEM 对液质联用粉末中药物与辅料的相互作用进行了表征。此外,通过 Carr 指数和粉末润湿时间测定分别对粉末特性进行了评价。所有制备的制剂均在不同压力下压缩,以获得相同的恒定孔隙率,并通过不同的测试对片剂进行评价,并与常规配方进行比较。

结果与讨论

如 XRD、FTIR、DSC 和 SEM 的结果所示,所有液质联用制剂中均未检测到相互作用。此外,所有液质联用压片均表现出比常规配方更快的溶出曲线。

结论

药物浓度、药物在液体载体中的溶解度和载体类型均影响溶出率。此外,液体载体的存在会影响液质联用制剂的机械性能。

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