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Multicomponent crystals of anti-tuberculosis drugs: a mini-review

机译：抗结核药物多组分晶体：迷你审查

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Tuberculosis (TB) is the leading cause of death from a single infectious agent globally. Some of the early research on TB treatment indicated drug resistance as one of the key challenges in fighting this disease. The discovery that administering two or more drugs simultaneously could lead to much more effective treatment, with reduced drug resistance and shorter periods of chemotherapy, was, therefore, a very significant breakthrough in TB drug research. Pursuant to this discovery, the World Health Organisation (WHO) recommended TB treatment employing fixed-dose combinations (FDCs) containing first line anti-TB drugs; rifampicin, isoniazid, pyrazinamide, streptomycin and ethambutol. Regardless, certain challenges associated with FDCs remain and these include chemical instability and reduced bioavailability of rifampicin. Therefore, some research effort has been directed towards finding ways to deal with these challenges. One such effort involves the use of pharmaceutical co-crystals of the active pharmaceutical ingredients. Consequently, several pharmaceutical co-crystals of isoniazid and pyrazinamide have been reported. This paper aims at reviewing the multicomponent crystal structures of two first-line anti-TB drugs; isoniazid and pyrazinamide. The review will first set out a brief history of the disease, milestones in TB chemotherapy and the challenges associated with current treatment regimens. This will then be followed by a brief introduction to pharmaceutical co-crystals and how they can improve the physical and chemical properties of the active pharmaceutical ingredients. Secondly, multicomponent crystals of the two active pharmaceutical ingredients will be analysed by manual inspection for common supramolecular synthons between the drug molecules as well as between drug molecules and co-formers. Lastly; stability, solubility and dissolution experiments carried out on the pharmaceutical co-crystals of pyrazinamide and isoniazid will be analysed to gain insights into progress made with regards to improving stability and solubility of the active pharmaceutical ingredients.
机译：结核病（TB）是在全球单一传染病药物中死亡的主要原因。关于TB治疗的一些早期研究表明，作为对抗这种疾病的关键挑战之一。同时施用两种或更多种药物的发现可能导致更有效的治疗，降低耐药性和化疗较短的化疗，因此是TB药物研究的非常显着的突破。根据这一发现，世界卫生组织（世卫组织）推荐使用含有第一线抗结核药物的固定剂组合（FDC）的TB治疗;利福平，异烟肼，吡嗪酰胺，链霉素和乙胺丁醇。无论如何，与FDC相关的某些挑战仍然存在，这些挑战包括化学不稳定性，降低利福平的生物利用度。因此，一些研究努力旨在寻找处理这些挑战的方法。一种这种努力涉及使用活性药物成分的药物共晶。因此，已经报道了异喹啉和吡嗪酰胺的几种药物共晶。本文旨在审查两种一线抗结核药物的多组分晶体结构;异烟肼和吡嗪酰胺。审查将首先列出疾病的简要历史，结核化疗中的里程碑和与当前治疗方案相关的挑战。然后将其简要介绍药物共晶以及它们如何改善活性药物成分的物理和化学性质。其次，将通过手动检查药物分子与药物分子与共置剂之间的常见超分子合成剂进行两种活性药物成分的多组分晶体。最后;将分析对吡唑胺和异烟肼的药物共晶体中进行的稳定性，溶解度和溶解实验，以获得关于改善活性药物成分的稳定性和溶解性的进展中的洞察。

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  • 来源
    《RSC Advances》 |2020年第61期|共8页
  • 作者

    Batisai Eustina;

  • 作者单位

    Univ Venda Dept Chem P Bag X5050 ZA-0920 Thohoyandou South Africa;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
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