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瘤胃稳定递送系统

Rumen-stable delivery systems.

作者信息

Papas A, Wu SH

机构信息

Technical Service and Development Division, Eastman Chemical Company, Kingsport, USA

出版信息

Adv Drug Deliv Rev. 1997 Dec 8;28(3):323-334. doi: 10.1016/s0169-409x(97)00087-2.

Abstract

Ruminants have a distinct digestive system which serves a unique symbiotic relationship between the host animal and predominantly anaerobic rumen bacteria and protozoa. Rumen fermentation can be both beneficial by enabling utilization of cellulose and non-protein nitrogen and detrimental by reducing the nutritive value of some carbohydrates, high biological value proteins and by hydrogenating unsaturated lipids. In addition it can also result in the modification and inactivation of many pharmacologically active ingredients administered to the host animal via the oral route. The advances in ruminant nutrition and health demand a rumen-stable delivery system which can deliver the active ingredient post-ruminally while simultaneously meet efficacy, safety and cost criteria. In contrast to drug delivery systems for humans, the demand for low-cost has hindered the development of effective rumen-stable delivery systems. Historically, heat and chemical treatment of feed components, low solubility analogues or lipid-based formulations have been used to achieve some degree of rumen-stability, and products have been developed accordingly. Recently, a polymeric pH-dependent rumen-stable delivery system has been developed and commercialized. The rationale of this delivery system is based on the pH difference between ruminal and abomasal fluids. The delivery system is composed of a basic polymer, a hydrophobic substance and a pigment material. It can be applied as a coating to solid particles via a common encapsulation method such as air-suspension coating. In the future, the delivery system could be used to deliver micronutrients and pharmaceuticals post-ruminally to ruminant animals. A further possible application of the delivery system is that it could also be combined with other controlled delivery devices/systems in order to enhance slow release or to achieve targeted delivery needs for ruminants. This paper discusses the rumen protection and the abomasal release mechanism of the polymeric coating. It also reviews other rumen stable delivery systems and methods for evaluating their in vitro and in vivo performance.

摘要

反刍动物具有独特的消化系统,该系统在宿主动物与主要为厌氧的瘤胃细菌及原生动物之间形成了独特的共生关系。瘤胃发酵既有益处,因为它能使动物利用纤维素和非蛋白氮;也有坏处,因为它会降低某些碳水化合物、高生物价值蛋白质的营养价值,并使不饱和脂质氢化。此外,它还可能导致经口服途径给予宿主动物的许多药理活性成分发生改性和失活。反刍动物营养与健康方面的进展需要一种瘤胃稳定的给药系统,该系统能够在瘤胃后释放活性成分,同时满足功效、安全性和成本标准。与人类药物递送系统不同,对低成本的需求阻碍了有效的瘤胃稳定递送系统的开发。从历史上看,对饲料成分进行热处理和化学处理、使用低溶解度类似物或基于脂质的制剂来实现一定程度的瘤胃稳定性,并相应地开发了产品。最近,一种基于聚合物的pH依赖性瘤胃稳定递送系统已被开发并商业化。该递送系统的原理基于瘤胃液和皱胃液之间的pH差异。该递送系统由一种碱性聚合物、一种疏水性物质和一种色素材料组成。它可以通过常见的包封方法(如空气悬浮包衣)作为涂层应用于固体颗粒。未来,该递送系统可用于在瘤胃后向反刍动物递送微量营养素和药物。该递送系统的另一个可能应用是,它还可以与其他控释装置/系统结合,以增强缓释效果或满足反刍动物的靶向递送需求。本文讨论了聚合物涂层的瘤胃保护和皱胃释放机制。它还综述了其他瘤胃稳定递送系统以及评估其体外和体内性能的方法。

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