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纳米晶化:一种提高难溶性药物生物利用度的新兴技术。

Nanocrystalization: An Emerging Technology to Enhance the Bioavailability of Poorly Soluble Drugs.

作者信息

Joshi Kavita, Chandra Akhilesh, Jain Keerti, Talegaonkar Sushama

机构信息

Department of Pharmaceutics, Delhi Pharmaceutical Sciences and Research University, Pushp Vihar Sec III, New Delhi-110017, India.

Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi-62, India.

出版信息

Pharm Nanotechnol. 2019;7(4):259-278. doi: 10.2174/2211738507666190405182524.

Abstract

Most of the active pharmaceutical ingredient used in the management of disease have poor water solubility and offer grueling problems in drug formulation development since low solubility is generally associated with poor dissolution characteristics which leads to poor oral bioavailability. The great challenge for the development of a pharmaceutical product is to create its new formulation and drug delivery system to limit solubility problems of existing drug candidate. Limited drug-loading capacity requires a large amount of carrier material to get appropriate encapsulation of the drug, which is another major challenge in the development of pharmaceutical product which could be resolved by developing nanocrystals (NCs). A significant research in the past few years has been done to develop NCs which helps in the delivery of poorly water soluble drugs via different routes. The technology could continue to thrive as a useful tool in pharmaceutical sciences for the improvement of drug solubility, absorption and bioavailability. Many crystalline compounds have pulled in incredible consideration much of the time, due to their ability to show good physical and chemical properties when contrasted with their amorphous counterparts. Nanocrystals have been proven to show atypical properties compared to the bulk. This review article explores the principles of the important nanocrystallization techniques including NCs characterization and its application.

摘要

用于疾病治疗的大多数活性药物成分水溶性较差,在药物制剂研发中带来了棘手的问题,因为低溶解度通常与不良的溶出特性相关,进而导致口服生物利用度不佳。药品研发面临的巨大挑战是创建新的制剂和药物递送系统,以解决现有候选药物的溶解度问题。有限的载药量需要大量载体材料才能实现药物的适当包封,这是药品研发中的另一个主要挑战,而开发纳米晶体(NCs)可以解决这一问题。在过去几年中,人们开展了大量研究来开发纳米晶体,其有助于通过不同途径递送水溶性差的药物。作为药学领域用于改善药物溶解度、吸收和生物利用度的一种有用工具,该技术有望持续蓬勃发展。许多结晶化合物时常备受关注,因为与无定形对应物相比,它们能够展现出良好的物理和化学性质。与块状材料相比,纳米晶体已被证明具有非典型特性。这篇综述文章探讨了重要的纳米结晶技术原理,包括纳米晶体的表征及其应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/be90/6967137/896f09571ed4/PNT-7-259_F1.jpg

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