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布洛芬的制剂与给药策略:挑战与机遇

Formulation and delivery strategies of ibuprofen: challenges and opportunities.

作者信息

Irvine Jake, Afrose Afrina, Islam Nazrul

机构信息

a Pharmacy Discipline, School of Clinical Sciences, Faculty of Health , Queensland University of Technology , Brisbane , QLD , Australia.

b Institute of Health and Biomedical Innovation , Queensland University of Technology , Brisbane , QLD , Australia.

出版信息

Drug Dev Ind Pharm. 2018 Feb;44(2):173-183. doi: 10.1080/03639045.2017.1391838. Epub 2017 Oct 30.

Abstract

Ibuprofen, a non-steroidal anti-inflammatory drug (NSAID), is mostly administered orally and topically to relieve acute pain and fever. Due to its mode of action this drug may be useful in the treatment regimens of other, more chronic conditions, like cystic fibrosis. This drug is poorly soluble in aqueous media and thus the rate of dissolution from the currently available solid dosage forms is limited. This leads to poor bioavailability at high doses after oral administration, thereby increasing the risk of unwanted adverse effects. The poor solubility is a problem for developing injectable solution dosage forms. Because of its poor skin permeability, it is difficult to obtain an effective therapeutic concentration from topical preparations. This review aims to give a brief insight into the status of ibuprofen dosage forms and their limitations, particle/crystallization technologies for improving formulation strategies as well as suggesting its incorporation into the pulmonary drug delivery systems for achieving better therapeutic action at low dose.

摘要

布洛芬是一种非甾体抗炎药(NSAID),主要通过口服和局部给药来缓解急性疼痛和发热。由于其作用方式,这种药物可能对其他更慢性的疾病(如囊性纤维化)的治疗方案有用。该药物在水性介质中溶解度较差,因此目前可用的固体剂型的溶出速率有限。这导致口服高剂量后生物利用度不佳,从而增加了不良副作用的风险。溶解度差对于开发注射溶液剂型来说是个问题。由于其皮肤渗透性差,很难从局部制剂中获得有效的治疗浓度。本综述旨在简要介绍布洛芬剂型的现状及其局限性、用于改进制剂策略的颗粒/结晶技术,以及建议将其纳入肺部给药系统以在低剂量下实现更好的治疗效果。

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