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核心技术专利:CN118964589B侵权必究
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基于脂质的肌肉内长效注射剂:最新技术现状。

Lipid based intramuscular long-acting injectables: Current state of the art.

机构信息

School of Biology, University of East Anglia, Norwich Research Park, Norwich NR4 7TJ, UK; School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich NR4 7TJ, UK.

School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich NR4 7TJ, UK.

出版信息

Eur J Pharm Sci. 2022 Nov 1;178:106253. doi: 10.1016/j.ejps.2022.106253. Epub 2022 Jul 3.


DOI:10.1016/j.ejps.2022.106253
PMID:35793750
Abstract

Long acting injectables (LAI) have received increased research and commercial interest due to their potential for improving treatment effectiveness and adherence for antipsychotic, antiviral and addiction treatments. A range of materials have been used to formulate LAI products, including lipids and polymers. Classic lipid-based LAI, such as oil solutions of antipsychotic drugs, have been widely prescribed to patients. Clinical evidence has shown significantly improved key therapeutic markers such as reduction of relapses in the case of schizophrenia patients. The commercial LAI products can be given either via subcutaneous or intramuscular injection. The main types of lipid-based LAI formulations include oil solutions, lipid-based nanoparticles and lipid based liquid crystal formulations, which are currently clinically available, and oil suspensions and oleogels and which currently have no commercial products available. This review will discuss all relevant aspects related to the development of lipid-based long acting injectables with a special focus on intramuscular (IM) injectables. It aims to provide useful guidance on effective future LAI product design and development. Lipid-based nanoformulations are not discussed in this review as they are thoroughly reviewed in literature elsewhere.

摘要

长效注射剂(LAI)因其在提高抗精神病药、抗病毒和戒毒治疗的疗效和依从性方面的潜力而受到越来越多的研究和商业关注。已经使用了多种材料来制备 LAI 产品,包括脂质和聚合物。经典的基于脂质的 LAI,如抗精神病药物的油溶液,已被广泛用于患者。临床证据表明,关键治疗标志物得到了显著改善,例如精神分裂症患者的复发减少。商业 LAI 产品可以通过皮下或肌肉注射给药。基于脂质的 LAI 制剂的主要类型包括油溶液、基于脂质的纳米粒子和基于脂质的液晶制剂,这些制剂目前在临床上可用,还有油混悬剂和油凝胶,目前没有商业产品。本综述将讨论与开发基于脂质的长效注射剂相关的所有相关方面,特别关注肌肉内(IM)注射剂。它旨在为有效的未来 LAI 产品设计和开发提供有用的指导。本综述未讨论基于脂质的纳米制剂,因为它们在其他文献中有详细综述。

相似文献

[1]
Lipid based intramuscular long-acting injectables: Current state of the art.

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[2]
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[3]
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[4]
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[5]
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[6]
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[7]
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J Clin Psychopharmacol. 2012-6

[8]
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[9]
Comparison of Subjective Experiences and Effectiveness of First-Generation Long-Acting Injectable Antipsychotics and Risperidone Long-Acting Injectables in Patients With Schizophrenia.

J Clin Psychopharmacol. 2016-10

[10]
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Int J Psychiatry Clin Pract. 2020-1-14

引用本文的文献

[1]
Development of a depot formulation with an non-lamellar liquid crystal-forming system with phospholipids.

Front Drug Deliv. 2023-10-19

[2]
Unveiling the Future: Opportunities in Long-Acting Injectable Drug Development for Veterinary Care.

Pharmaceutics. 2025-5-8

[3]
Two in One: Size Characterization and Accelerated Short-Term Physical Stability of Dual-Drug Suspensions with Two Acidic Compounds (Indomethacin and Naproxen).

Pharmaceutics. 2024-11-21

[4]
Exploring the landscape of Lipid Nanoparticles (LNPs): A comprehensive review of LNPs types and biological sources of lipids.

Int J Pharm X. 2024-11-18

[5]
Long-acting parenteral formulations of hydrophilic drugs, proteins, and peptide therapeutics: mechanisms, challenges, and therapeutic benefits with a focus on technologies.

Drug Deliv Transl Res. 2025-4

[6]
The role of lipid particle-laden interfaces in regulating the co-delivery of two hydrophobic actives from o/w emulsions.

Drug Deliv. 2024-12

[7]
Patient-Centric Long-Acting Injectable and Implantable Platforms─An Industrial Perspective.

Mol Pharm. 2024-9-2

[8]
A Systematic Investigation of Process Parameters for Small-Volume Aqueous Suspension Production by the Use of Focused Ultrasonication.

AAPS PharmSciTech. 2024-8-13

[9]
Tricaprylin-based drug crystalline suspension for intramuscular long-acting delivery of entecavir with alleviated local inflammation.

Bioeng Transl Med. 2024-1-29

[10]
Forming, Enzyme-Responsive Peptoid-Peptide Hydrogels: An Advanced Long-Acting Injectable Drug Delivery System.

J Am Chem Soc. 2024-8-7

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