采用多聚物方法快速溶解 PVP-I 粉末的机理特征及其分子相互作用研究。

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pharmaceutical Development and Technology Pub Date : 2024-12-01 Epub Date: 2024-11-21 DOI:10.1080/10837450.2024.2428772
Maytawee Wutthichokmongkhonkul, Rutthapol Sritharadol, Teerapol Srichana
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引用次数: 0

摘要

聚维酮碘(PVP-I)被广泛用作医疗应用中的消毒剂。然而,它的功效受到某些缺点的限制,如在水中的溶解度低和挥发性强。因此,我们需要一种稳定的固体 PVP-I 配方。在本研究中,PVP-I 分子与聚乙二醇-聚乙烯醇共聚物(PEG-PVA 共聚物)的复合物被认为是水溶性碘剂。制备固体的方法有两种:物理混合物和捏合。使用几种光谱方法对所得固体的物理特性进行了评估。通过电位滴定法确认了碘的存在,并测试了抗菌活性。结果表明,PEG-PVA 共聚物与聚维酮的相互作用主要是通过 PEG-PVA 共聚物的羟基部分与聚维酮的酰胺部分之间的氢键,估计结合能为 3.2 kcal/mol。聚维酮中的酰胺基团极性使其更有可能与 PEG-PVA 共聚物形成氢键。此外,质子化的吡咯烷酮通过分子间氢键与三碘化阴离子结合,从而增加了 PVP-I 在水中的溶解度。与物理混合法和纯 PVP-I 相比,捏合法的溶解速度更快。碘含量在可接受的范围内(10-12%),抗菌活性对金黄色葡萄球菌、表皮葡萄球菌和变异链球菌有效。
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Mechanistic characterization of fast dissolving PVP-I powder with multipolymer approaches and investigation on their molecular interaction.

Povidone-iodine (PVP-I) is widely used as an antiseptic in medical applications. However, its effectiveness is limited by certain drawbacks, such as low solubility in water and high volatility. Therefore, a formulation of a stable solid PVP-I is desirable. In this study, complexes of molecular PVP-I with polyethylene glycol-polyvinyl alcohol copolymer (PEG-PVA copolymer) were considered water-soluble iodophors. Two different methods were used to prepare the solids: physical mixtures and kneading. The physical characteristics of the obtained solids were evaluated using several spectroscopic methods. The presence of iodine was confirmed by a potentiometric titration and antimicrobial activity was tested. The results showed that the PEG-PVA copolymer interacted with povidone primarily through hydrogen bonding between the hydroxyl part of the PEG-PVA copolymer and the amide part of povidone with an estimated binding energy of 3.2 kcal/mol. The amide groups polarity in povidone made them more likely to form hydrogen bonds with the PEG-PVA copolymer. Also, the protonated pyrrolidone bonded to the triiodide anions by intermolecular hydrogen bonds, which increased PVP-I solubility in water. The kneading method provided a faster dissolution rate than physical mixing and pure PVP-I. The iodine contents were within an acceptable range (10-12%), and the antimicrobial activity proved effective against Staphylococcus aureus, Staphylococcus epidermidis, and Streptococcus mutans.

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来源期刊
CiteScore
5.90
自引率
2.90%
发文量
82
审稿时长
1 months
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.
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