Raghuvanshi Smita, Pathak Kamla
Department of Pharmaceutics, Rajiv Academy for Pharmacy, N.H. No. 2, P.O. Chattikara, Mathura, Uttar Pradesh 281001, India.
J Drug Deliv. 2014;2014:479246. doi: 10.1155/2014/479246. Epub 2014 Nov 13.
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.
对于像桂利嗪这类口服后具有全身作用的药物而言,低溶解度导致其在胃肠道中低溶出是主要问题。桂利嗪的药品在全球作为速释制剂商业化,呈现出低吸收、生物利用度低且不稳定的特点。提高生物利用度的方法在文献中被广泛引用。已尝试对难溶性药物桂利嗪的生物利用度问题及临床治疗方法进行综述。撰写本文的目的是总结该药物的药代动力学局限性,特别关注改善生物利用度的策略以及新型剂型克服这一障碍的有效性。本文介绍了通过环糊精复合物和新型剂型(自纳米乳化系统和漂浮微粒)克服桂利嗪低且不稳定生物利用度的方法。纳米制剂在预防儿童偏头痛发作中的新临床作用有待未来系统探索。临床报告已证实桂利嗪在偏头痛预防中的作用。需要致力于开发具有有效生物利用度且能将药物直接送达脑部的剂型。