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氟化亚锡技术的最新进展:抗菌功效及对过敏症的作用机制

Recent advances in stannous fluoride technology: antibacterial efficacy and mechanism of action towards hypersensitivity.

作者信息

Miller S, Truong T, Heu R, Stranick M, Bouchard D, Gaffar A

机构信息

Colgate-Palmolive Technology Center, Piscataway, NJ 08854.

出版信息

Int Dent J. 1994 Feb;44(1 Suppl 1):83-98.

PMID:8021041
Abstract

Stannous fluoride (SnF2) is highly susceptible to oxidation and hydrolysis but both anhydrous and aqueous preparations can be well established by proper formulation. When stability in aqueous preparations is achieved by the use of certain strong complexing agents, reduced antibacterial activity is observed which may be attributed to reduced bioavailability of the stannous ion. In contrast, an anhydrous SnF2 preparation maintains stannous ion in a stable but, uncomplexed form. This preparation displays antibacterial activity in saliva and delivers stannous ion which is absorbed onto surfaces making them less susceptible to plaque formation for an extended period of time (hours). When this anhydrous preparation is brushed onto dentine in vitro or in situ, one observes a nearly complete coverage of the dentine surface and occlusion of tubules by a tin-rich surface deposit. This finding indicates that the observed clinical efficacy of this preparation at relieving hypersensitivity is due to occlusion of tubules by a mixture of low solubility complexes of tin. A water-based SnF2 preparation containing strongly complexed stannous ions does not form a surface coating on dentine in vitro suggesting that this preparation may not be optimal for treating hypersensitivity. Overall, the findings indicate that the stannous ions in a SnF2 preparation must be maintained in a stable, bioavailable form for optimal efficacy against plaque and hypersensitivity to be obtained. The results suggest that these properties are provided by stable anhydrous preparations but are difficult to achieve simultaneously in aqueous preparations. When properly formulated, stannous fluoride preparations can provide multiple oral therapeutic benefits.

摘要

氟化亚锡(SnF₂)极易氧化和水解,但通过适当的配方,无水制剂和水性制剂都能很好地制备出来。当通过使用某些强络合剂来实现水性制剂的稳定性时,会观察到抗菌活性降低,这可能归因于亚锡离子的生物利用度降低。相比之下,无水SnF₂制剂能使亚锡离子保持稳定但未络合的形式。这种制剂在唾液中显示出抗菌活性,并释放出被吸收到表面的亚锡离子,使它们在较长一段时间(数小时)内不易形成牙菌斑。当将这种无水制剂在体外或原位刷涂到牙本质上时,可以观察到牙本质表面几乎完全被覆盖,并且富含锡的表面沉积物会堵塞牙本质小管。这一发现表明,该制剂在缓解牙齿过敏方面观察到的临床疗效是由于锡的低溶解度络合物混合物堵塞了牙本质小管。含有强络合亚锡离子的水性SnF₂制剂在体外不会在牙本质上形成表面涂层,这表明该制剂可能不是治疗牙齿过敏的最佳选择。总体而言,这些发现表明,SnF₂制剂中的亚锡离子必须保持在稳定、可生物利用的形式,才能获得对牙菌斑和牙齿过敏的最佳疗效。结果表明,这些特性由稳定的无水制剂提供,但在水性制剂中难以同时实现。当配方适当时,氟化亚锡制剂可以提供多种口腔治疗益处。

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