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通过热熔挤出技术开发泊洛沙姆凝胶制剂。

Development of poloxamer gel formulations via hot-melt extrusion technology.

机构信息

Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.

Dave C. Swalm School of Chemical Engineering, Mississippi State University, Oktibbeha County, MS 39762, USA.

出版信息

Int J Pharm. 2018 Feb 15;537(1-2):122-131. doi: 10.1016/j.ijpharm.2017.12.008. Epub 2017 Dec 16.

DOI:10.1016/j.ijpharm.2017.12.008
PMID:29253585
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5798890/
Abstract

Poloxamer gels are conventionally prepared by the "hot" or the "cold" process. But these techniques have some disadvantages such as high energy consumption, requires expensive equipment and often have scale up issues. Therefore, the objective of this work was to develop poloxamer gels by hot-melt extrusion technology. The model drug selected was ketoprofen. The formulations developed were 30% and 40% poloxamer gels. Of these formulations, the 30% poloxamer gels were selected as ideal gels. DSC and XRD studies showed an amorphous nature of the drug after extrusion. It was observed from the permeation studies that with increasing poloxamer concentration, a decrease in drug permeation was obtained. Other studies conducted for the formulations included in-vitro release studies, texture analysis, rheological studies and pH measurements. In conclusion, the hot-melt extrusion technology could be successfully employed to develop poloxamer gels by overcoming the drawbacks associated with the conventional techniques.

摘要

泊洛沙姆凝胶通常通过“热”或“冷”工艺制备。但这些技术有一些缺点,例如能耗高、需要昂贵的设备,而且常常存在放大问题。因此,本工作的目的是通过热熔挤出技术开发泊洛沙姆凝胶。选择的模型药物是酮洛芬。所开发的配方为 30%和 40%泊洛沙姆凝胶。在这些配方中,选择 30%泊洛沙姆凝胶作为理想的凝胶。DSC 和 XRD 研究表明挤出后药物呈无定形状态。透过性研究表明,随着泊洛沙姆浓度的增加,药物透过性降低。对配方进行的其他研究包括体外释放研究、质地分析、流变学研究和 pH 值测量。总之,热熔挤出技术可以成功地用于开发泊洛沙姆凝胶,克服了与传统技术相关的缺点。

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