Shiyi Zhou, Yiting Wang, Zhe Li, Fei Wu, Yanlong Hong, Lan Shen, Xiao Lin
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引用次数: 0
摘要
本研究旨在确定泡腾体系中五种常用酸源的物理制造特性,以便设计此类体系的配方和工艺。研究人员调查了柠檬酸(CA)、酒石酸(TA)、苹果酸(MA)、富马酸(FA)和己二酸(AA)的吸湿性、质地特性、流变力矩、可压缩性、可压片性等,以检测其 "粉末直接压缩(DC)"和 "湿法制粒和压缩 "特性。直流能力由 SeDeM 专家系统进行评估。结果表明,所有酸粉都不符合直流电的流动性要求,压缩过程中塑性变形占主导地位。此外,CA 具有很强的吸湿性和冲孔粘连性,而 MA 的片剂性最好。TA 有较大的湿制粒空间,相对来说最适合用于 DC。AA 的吸湿性极强,随着粒度的增加,其流动性也明显改善。最后,FA 的吸湿性和喷射力最低,可压缩性和湿制粒空间大,不会出现冲孔粘连,而颗粒碎片在崩解过程中溶解缓慢。一般来说,配方或制粒方式会影响片剂的可药性,这表明与其他酸类或合适的填料搭配可能会改善其缺点。这些多维评估有效地减少了前期探索,提高了泡腾体系的开发效率。
Fingerprinting of physical manufacturing properties of different acids for effervescent systems.
The study aimed to fingerprint the physical manufacturing properties of five commonly used acid sources in effervescent systems for designing the formulation and process of such systems. The hygroscopicity, texture properties, rheological torque, compressibility, tabletability, etc., were investigated to inspect 'powder direct compression (DC)' and 'wet granulation and compression' properties of citric (CA), tartaric (TA), malic (MA), fumaric (FA), and adipic acid (AA). The DC ability was evaluated by the SeDeM expert system. The results indicated that all acid powders failed to meet flowability requirements for DC, and plastic deformation dominated during compression. Furthermore, CA exhibited strong hygroscopicity and punch sticking, while MA demonstrated the best tabletability. TA had a large wet granulation space and was relatively the most suitable for DC. AA was extremely hygroscopic, and its flowability improved significantly as particle size increased. Finally, FA displayed the lowest hygroscopicity and ejection force as well as great compressibility and wet granulation space, and did not exhibit punch sticking, while the granule fragments dissolved slowly during disintegration. Generally speaking, the formulation or granulation affected the tabletability, indicating that pairing with other acids or suitable fillers could potentially improve its disadvantages. These multidimensional assessments effectively reduce the pre-exploration and enhance the efficiency of the development of effervescent systems.
期刊介绍:
Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology.
Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as:
-Preformulation and pharmaceutical formulation studies
-Pharmaceutical materials selection and characterization
-Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation
-QbD in the form a risk assessment and DoE driven approaches
-Design of dosage forms and drug delivery systems
-Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies
-Drug delivery systems research and quality improvement
-Pharmaceutical regulatory affairs
This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.