具有胃吸收窗口的低水溶性药物肉桂嗪的给药系统和治疗方法的最新进展。

Journal of drug delivery Pub Date : 2014-01-01 Epub Date: 2014-11-13 DOI:10.1155/2014/479246
Smita Raghuvanshi, Kamla Pathak
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引用次数: 30

摘要

低溶解度导致胃肠道溶出度低是口服全身性作用药物的主要问题,如肉桂碱。肉桂碱的医药产品作为速释制剂在全球范围内商业化,其吸收低,生物利用度低且不稳定。提高生物利用度的方法在文献中被广泛引用。本文综述了难水溶性药物肉桂碱的生物利用度、并发症及临床治疗方法。本文的目的是总结药物的药代动力学局限性,特别关注如何提高生物利用度以及新剂型的有效性,以绕过这一障碍。本文提供了通过环糊精配合物和新剂型:自纳米乳化系统和浮力微粒来克服肉桂碱低和不稳定生物利用度的方法。纳米制剂需要在未来系统地探索其在预防儿童偏头痛发作中的新的临床作用。临床报告证实了肉桂碱在偏头痛预防中的作用。研究需要致力于开发有效的生物利用度和药物直接到大脑的剂型。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Recent advances in delivery systems and therapeutics of cinnarizine: a poorly water soluble drug with absorption window in stomach.

Recent advances in delivery systems and therapeutics of cinnarizine: a poorly water soluble drug with absorption window in stomach.

Recent advances in delivery systems and therapeutics of cinnarizine: a poorly water soluble drug with absorption window in stomach.

Low solubility causing low dissolution in gastrointestinal tract is the major problem for drugs meant for systemic action after oral administration, like cinnarizine. Pharmaceutical products of cinnarizine are commercialized globally as immediate release preparations presenting low absorption with low and erratic bioavailability. Approaches to enhance bioavailability are widely cited in the literature. An attempt has been made to review the bioavailability complications and clinical therapeutics of poorly water soluble drug: cinnarizine. The interest of writing this paper is to summarize the pharmacokinetic limitations of drug with special focus on strategies to improvise bioavailability along with effectiveness of novel dosage forms to circumvent the obstacle. The paper provides insight to the approaches to overcome low and erratic bioavailability of cinnarizine by cyclodextrin complexes and novel dosage forms: self-nanoemulsifying systems and buoyant microparticulates. Nanoformulations need to systematically explored in future, for their new clinical role in prophylaxis of migraine attacks in children. Clinical reports have affirmed the role of cinnarizine in migraine prophylaxis. Research needs to be dedicated to develop dosage forms for efficacious bioavailability and drug directly to brain.

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来源期刊
Journal of drug delivery
Journal of drug delivery PHARMACOLOGY & PHARMACY-
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