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皮肤科用药载体的神秘作用。

The mystical effects of dermatological vehicles.

作者信息

Surber Christian, Smith Eric W

机构信息

Institute of Hospital Pharmacy, Department of Dermatology, University of Basel, Basel, Switzerland.

出版信息

Dermatology. 2005;210(2):157-68. doi: 10.1159/000082572.

Abstract

Topical treatment of the skin is as old as the evolution of man. Instinctively, we try to treat a skin injury or irritation with cooling or soothing substances. Even animals lick their wounds, trusting instinctively in the healing power of saliva. When did this archaic pattern of treatment take the gigantic leap from folk medicine to modern drug therapy? This text illustrates the evolution of topical dermatological vehicles, their application (guidelines) and future use. In particular, a phenomenon that has so far been ignored in product development and clinical testing is the vehicle metamorphosis. In clinical and experimental situations, most dermatological vehicles undergo considerable changes after they have been removed from the primary container and are applied to the skin. Subsequently, the initial structural matrix, and the quantitative composition of the vehicle, will most likely change during and after the mechanical shear associated with application of the product and/or evaporation of ingredients. This natural, but highly dynamic process will generate mini-environments for the active moiety that are difficult to predict and that are crucial to the fate of the active moiety. Despite the reasonable wishes of formulators, clinicians, patients and customers, there are still no universal vehicles. Each drug, at each concentration, requires a different vehicle for optimized therapy. Stability and compatibility of excipients and active moiety are crucial for any commercially available pharmaceutical or cosmetic formulation, together with local and systemic safety of all components. Nonetheless, more diverse and molecularly complex classes of new dermatological vehicles are continuously being researched and refined. The scientific progress has been remarkable when one considers the simple emulsion mixtures that were commonplace in dermatological therapy and still persist to this day in commercial products. It is to be hoped that the result of these research endeavors will be the emergence of more innovative topical formulations, applying engineered bioavailability control systems, with broader applications in topical therapeutic and cosmetic vehicles.

摘要

皮肤的局部治疗与人类的进化一样古老。出于本能,我们会尝试用清凉或舒缓的物质来治疗皮肤损伤或刺激。甚至动物也会舔舐伤口,本能地相信唾液的愈合能力。这种古老的治疗方式是何时从民间医学跃升至现代药物治疗的呢?本文阐述了局部皮肤用药载体的演变、其应用(指南)及未来用途。特别是,有一种在产品研发和临床试验中迄今被忽视的现象,即载体的变形。在临床和实验环境中,大多数皮肤用药载体从原始容器取出并应用于皮肤后,会发生相当大的变化。随后,载体的初始结构基质及其定量组成很可能在与产品应用相关的机械剪切过程中和之后以及成分蒸发过程中发生改变。这个自然但高度动态的过程会为活性成分创造难以预测且对其命运至关重要的微环境。尽管配方师、临床医生、患者和消费者有着合理的期望,但仍然没有通用的载体。每种药物在每种浓度下都需要不同的载体来实现优化治疗。辅料与活性成分的稳定性和相容性对于任何市售药品或化妆品配方都至关重要,同时所有成分的局部和全身安全性也很关键。尽管如此,更多种类且分子结构更复杂的新型皮肤用药载体仍在不断地被研究和改进。当考虑到在皮肤治疗中常见且至今仍存在于商业产品中的简单乳剂混合物时,科学进步是显著的。希望这些研究努力的结果将是出现更多创新的局部制剂,应用工程化的生物利用度控制系统,在局部治疗和化妆品载体中有更广泛的应用。

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