用于提高难溶性药物溶解度的 Liquisolid 技术--简要回顾。

Amaresh Prusty, Bikash Ranajn Jena, Vivek Barik, Piyali Khamkat, Bhakti Bhusan Barik
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引用次数: 0

摘要

新发现的候选药物大多具有亲脂性且水溶性较差,因此配制合适的给药系统成为制药行业面临的一大挑战。本综述概述了液固技术(LST),并总结了其在给药领域的各种应用进展。这种新型技术是通过将液体分散体混合或喷洒到特定的粉末载体和包衣材料上,将液态药物或液态药物(如溶液、悬浮液或乳剂)转化为干燥、不粘附、自由流动且易于压缩的粉末混合物。在 Liquisolid 系统中,液体药物被吸收到载体的内部结构中。一旦载体内部的药液达到饱和,载体颗粒表面就会形成液层,并立即被精细的涂层材料吸附。这样就形成了一种干燥、自由流动且可压缩的粉末混合物。与其他提高溶解度的技术(如微粉化、包合物络合、微囊化、纳米悬浮和自纳米乳剂)相比,LST 的制备相对简单,可为提高水溶性差的药物的溶解度提供一种具有成本效益的解决方案,从而提高其在药物制剂和给药过程中的生物利用度。
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Liquisolid Technique for Solubility Enhancement of Poorly Soluble Drug - A Brief Review.

Most of the newly discovered drug candidates are lipophilic and poorly water-soluble, making it a significant challenge for the pharmaceutical industry to formulate suitable drug delivery systems. This review gives insight into an overview of the liquisolid technique (LST) and summarizes the progress of its various applications in drug delivery. This novel technique involves converting liquid drugs or drugs in a liquid state (such as solutions, suspensions, or emulsions) into dry, nonadherent, free-flowing, and readily compressible powder mixtures by blending or spraying a liquid dispersion onto specific powder carriers and coating materials. In Liquisolid systems, the liquid medication is absorbed into the interior framework of carriers. Once the carrier's interior is saturated with liquid medication, a liquid layer forms on the surface of the carrier particles, which is instantly adsorbed by the fine coating material. As a result, a dry, free-flowing, and compressible powder mixture is formed. Compared to other solubility enhancement techniques, s.a. micronization, inclusion complexation, microencapsulation, nanosuspension, and self-nano emulsions, LST is relatively simple to prepare and may offer a cost-effective solution to enhance the solubility of poorly water-soluble drugs enhancing its bioavailability in drug formulation and delivery.

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