两性霉素B的安全有效给药：专利综述

Safe and Effective Delivery of Amphotericin B: A Survey of Patents.

作者信息

Kaur Lakhvir, Jain Subheet K

机构信息

Department of Pharmaceutical Sciences, Guru Nanak Dev University, 143005, Amritsar, India.

出版信息

Recent Pat Nanotechnol. 2017;11(3):214-234. doi: 10.2174/1872210511666170105130210.

DOI:10.2174/1872210511666170105130210

PMID:28056751

Abstract

BACKGROUND

Amphotericin B, designated as the gold standard among antifungal drugs is the only fungicidal effective against systemic fungal infections. But this drug has various pitfalls associated with it, to bypass which various techniques have been employed and resulted in a variety of lipid based commercially available formulations, which demolished only few of the shortcomings associated with this drug. Further, improvement in the delivery systems of Amphotericin B is advancing at increasingly frenetic pace, to surmount its research and to exploit its therapeutic potency with least toxicities.

METHOD

The patent search on "Amphotericin B for its safe and effective delivery" has been carried out to present assimilated information on the patents of the universally accepted Amphotericin B formulations and technologies. Also, the area of focus was the physicochemical properties of Amphotericin B, their role in formulation development and also nanotechnology based formulations of Amphotericin B.

RESULTS

Amphotericin B possesses poor aqueous solubility and systemic toxicity rendering obstacle in its formulation development. The interest of scientists and pharmaceutical industries to make further investments in the development of Amphotericin B formulations is due to rare occurrence of resistance to this drug. To bypass these drawbacks, various techniques have been patented which resulted in a variety of commercially available formulations to overcome the limitations of high cost, limited availability, poor storage stability and poor patient compliance. In lieu to this, scientists have developed and patented many novel drug delivery system based formulations and technologies such as use of novel carriers, modification in process for production and purification of Amphotericin B, formation of salts and complexes etc. to bring in limelight the benefits of this wonder drug.

CONCLUSION

The purpose of the article is to present assimilated information regarding patents on Amphotericin B formulations and technologies.

摘要

背景

两性霉素B被视为抗真菌药物中的金标准，是唯一对系统性真菌感染有效的杀菌剂。但该药物存在各种缺陷，为克服这些缺陷，人们采用了多种技术，从而产生了多种基于脂质的市售制剂，然而这些制剂仅克服了该药物的少数缺点。此外，两性霉素B给药系统的改进正以越来越快的速度推进，以突破其研究瓶颈，并在毒性最小的情况下发挥其治疗效力。

方法

已对“用于安全有效给药的两性霉素B”进行了专利检索，以提供有关普遍认可的两性霉素B制剂和技术专利的综合信息。此外，重点关注的领域是两性霉素B的物理化学性质、它们在制剂开发中的作用以及基于纳米技术的两性霉素B制剂。

结果

两性霉素B的水溶性差且具有全身毒性，这给其制剂开发带来了障碍。科学家和制药行业之所以有兴趣进一步投资开发两性霉素B制剂，是因为对该药物耐药的情况很少见。为克服这些缺点，人们已申请了各种技术专利，从而产生了多种市售制剂，以克服高成本、供应有限、储存稳定性差和患者顺应性差等局限性。为此，科学家们已经开发并申请了许多基于新型药物递送系统的制剂和技术专利，例如使用新型载体、改进两性霉素B的生产和纯化工艺、形成盐和复合物等，以凸显这种神奇药物的益处。