喷雾干燥法改性紫杉醇的性能

IF 2.3 Q3 PHARMACOLOGY & PHARMACY Scientia Pharmaceutica Pub Date : 2022-10-24 DOI:10.3390/scipharm90040067
A. Taldaev, R. Terekhov, I. Selivanova, Denis I. Pankov, M. Anurova, I. Markovina, Zhaoqing Cong, Siqi Ma, Zhengqi Dong, Feifei Yang, Y. Liao
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引用次数: 2

摘要

紫杉醇因其高抗氧化活性、多种药理作用和良好的安全性而被称为活性药物成分(API)和食品补充剂。以前,taxifolin球体(TS)是从俄罗斯(RT)工业生产的原料药taxifolin中获得的。在我们的工作中,我们对这种新的taxifolin材料与rt进行了药物分析。TS是一种非晶材料;傅里叶变换红外光谱证实,在没有聚合物载体的情况下,它是稳定的。基于MDCK细胞的实验结果,RT和TS均显示出较高的安全性,并被列为生物制药分类系统的第1类。RT和TS的Hausner比值分别为1.421和1.219,Carr指数分别为29.63%和19.00%。此外,与RT相比,TS表现出片剂的缓释:RT和TS片剂的半衰期分别为14.56 min和20.63 min。因此,由于其抗炎、原虫和病毒活性,TS可能是开发具有缓释模式的口服分散片剂的有希望的对象。
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Modification of Taxifolin Properties by Spray Drying
Taxifolin is known as an active pharmaceutical ingredient (API) and food supplement due to its high antioxidant activity, multiple pharmacological effects, and good safety profile. Previously, taxifolin spheres (TS) were obtained from industrially produced API taxifolin in Russia (RT). In our work, we perform a pharmaceutical analysis of this new taxifolin material versus RT. TS is an amorphous material; however, it is stable without the polymer carrier, as confirmed by Fourier transform infrared spectroscopy. Both RT and TS demonstrate high safety profiles and are assigned to Class 1 of the Biopharmaceutical Classification System based on the results of experiments with MDCK cells. The water solubility of the new taxifolin form was 2.225 times higher compared with RT. Hausner ratios for RT and TS were 1.421 and 1.219, respectively, while Carr indices were 29.63% and 19.00%, respectively. Additionally, TS demonstrated sustained release from tablets compared with RT: the half-life values of tablets were 14.56 min and 20.63 min for RT and TS, respectively. Thus, TS may be a promising object for developing oral antiseptics in the form of orally dispersed tablets with sustained release patterns because of its anti-inflammatory, -protozoal, and -viral activities.
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来源期刊
Scientia Pharmaceutica
Scientia Pharmaceutica Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
4.60
自引率
4.00%
发文量
67
审稿时长
10 weeks
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