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Recent Advances in Delivery Systems and Therapeutics of Cinnarizine: A Poorly Water Soluble Drug with Absorption Window in Stomach

机译:桂利嗪的给药系统和治疗学的最新进展:一种水溶性差的药物,在胃中具有吸收窗口

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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.
机译:低溶解度导致在胃肠道中的低溶解度是用于口服给药后具有全身作用的药物(如肉桂那嗪)的主要问题。肉桂利嗪的医药产品已在全球范围内商业化,成为速释制剂,其吸收率低,生物利用度低且不稳定。文献中广泛引用了提高生物利用度的方法。已经尝试审查水溶性差的药物肉桂那嗪的生物利用度并发症和临床治疗方法。撰写本文的目的在于总结药物的药代动力学局限性,特别侧重于改善生物利用度的策略以及新型剂型规避障碍的有效性。本文提供了通过环糊精复合物和新型剂型(自纳米乳化系统和浮性微粒)克服肉桂酸低和不稳定生物利用度的方法的见识。纳米制剂在预防儿童偏头痛发作方面的新临床作用需要在未来进行系统地研究。临床报告已确认肉桂利嗪在预防偏头痛中的作用。需要进行专门的研究来开发有效的生物利用度和直接向大脑给药的剂型。

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