Schwartz James R
J Drugs Dermatol. 2016 Feb;15(2):140-4.
Zinc pyrithione (ZPT) is an active material that has been used for over 50 years to effectively treat dandruff and seborrheic dermatitis (D/SD). It has become the most common material for that purpose, its use has expanded to include other skin benefits such as skin hygiene. However, there is much about ZPT that is unappreciated. It is a rationally developed molecule that was modeled after the naturally occurring antimicrobial aspergillic acid. The molecular basis for its antifungal activity has been elucidated. The efficacy of ZPT originates from two attributes. First, it has a very broad antimicrobial spectrum of activity, including fungi, gram-positive and -negative bacteria. Second, the material has very low solubility, resulting in formulation and delivery as a particulate material, which has distinct performance advantages. The particles are deposited and retained on the target skin surfaces even when delivered from rinse-off products. These particles slowly release molecularly active material to interact with the surface fungal and bacteria cells to control their population, functioning as slow-release reservoirs to provide extended and persistent benefits. This particulate nature, though, results in complex pharmaceutics to realize the full efficacy benefits; it is common to see products with the same ZPT level having widely varying levels of clinical performance. Several product matrix-determined factors directly impact resultant benefits: ZPT must be retained on the skin surface achieving uniform spatial distribution laterally as well as within hair follicles (especially on scalp); ZPT must be maintained as a physically stable dispersion in product; ZPT must be maintained in a chemically active form as there are many chemical reactions that can occur that can harm ZPT bioactivity. The benefits achievable by employing ZPT require significant pharmaceutics expertise to realize the full benefits of this active material.
吡硫翁锌(ZPT)是一种活性物质,五十多年来一直被用于有效治疗头皮屑和脂溢性皮炎(D/SD)。它已成为用于该目的最常见的物质,其用途已扩展到包括其他皮肤益处,如皮肤清洁。然而,关于ZPT仍有许多未被认识到的方面。它是一种经过合理开发的分子,是模仿天然存在的抗微生物曲酸制成的。其抗真菌活性的分子基础已经阐明。ZPT的功效源于两个特性。首先,它具有非常广泛的抗菌活性谱,包括真菌、革兰氏阳性菌和革兰氏阴性菌。其次,该物质的溶解度非常低,导致其作为颗粒物质进行制剂和递送,这具有明显的性能优势。即使从冲洗型产品中递送,这些颗粒也会沉积并保留在目标皮肤表面。这些颗粒缓慢释放分子活性物质,与表面的真菌和细菌细胞相互作用以控制它们的数量,起到缓释储存库的作用,提供持久的益处。然而,这种颗粒性质导致实现完全功效益处需要复杂的药剂学;常见的情况是,具有相同ZPT含量的产品临床性能水平差异很大。几个由产品基质决定的因素直接影响最终的益处:ZPT必须保留在皮肤表面,在横向以及毛囊内(尤其是头皮上)实现均匀的空间分布;ZPT必须在产品中保持物理稳定的分散体;ZPT必须保持化学活性形式,因为可能会发生许多损害ZPT生物活性的化学反应。采用ZPT可实现的益处需要大量药剂学专业知识才能充分发挥这种活性物质的全部益处。