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首页> 外文期刊>Pharmaceutics >Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs
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Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs

机译：改善水溶性药物差和抗癌药物溶解度的固体分散技术制造方法概述

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摘要

Approximately 40% of new chemical entities (NCEs), including anticancer drugs, have been reported as poorly water-soluble compounds. Anticancer drugs are classified into biologic drugs (monoclonal antibodies) and small molecule drugs (nonbiologic anticancer drugs) based on effectiveness and safety profile. Biologic drugs are administered by intravenous (IV) injection due to their large molecular weight, while small molecule drugs are preferentially administered by gastrointestinal route. Even though IV injection is the fastest route of administration and ensures complete bioavailability, this route of administration causes patient inconvenience to visit a hospital for anticancer treatments. In addition, IV administration can cause several side effects such as severe hypersensitivity, myelosuppression, neutropenia, and neurotoxicity. Oral administration is the preferred route for drug delivery due to several advantages such as low cost, pain avoidance, and safety. The main problem of NCEs is a limited aqueous solubility, resulting in poor absorption and low bioavailability. Therefore, improving oral bioavailability of poorly water-soluble drugs is a great challenge in the development of pharmaceutical dosage forms. Several methods such as solid dispersion, complexation, lipid-based systems, micronization, nanonization, and co-crystals were developed to improve the solubility of hydrophobic drugs. Recently, solid dispersion is one of the most widely used and successful techniques in formulation development. This review mainly discusses classification, methods for preparation of solid dispersions, and use of solid dispersion for improving solubility of poorly soluble anticancer drugs.
机译：据报道，大约40％的新化学实体（NCE），包括抗癌药物，可作为水溶性差的化合物。基于有效性和安全性，抗癌药物分为生物药物（单克隆抗体）和小分子药物（非生物抗癌药物）。由于其大分子量，通过静脉注射（IV）注射施用生物药物，而小分子药物优先通过胃肠道施用。尽管IV注射是最快的给药航线，并且确保完全生物利用度，但这条局途径导致患者访问医院抗癌治疗的不便。此外，IV给药可能导致若干副作用，例如严重的超敏反应，髓抑制，中性粒细胞和神经毒性。口服给药是药物递送的首选途径，因为诸如低成本，疼痛避免和安全性等几个优点。 NCE的主要问题是有限的水溶性，导致吸收差和低生物利用度。因此，提高水溶性药物不良的口腔生物利用度是药物剂型的发展中的巨大挑战。开发了几种方法，例如固体分散，络合，基于脂质的系统，微粉化，纳米化和共晶以改善疏水药物的溶解度。最近，固体分散是制定开发中最广泛和最成功的技术之一。本综述主要讨论分类，制备固体分散体的方法，以及使用固体分散体以改善可溶性抗癌药物的溶解度。

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