萘普生PVP纳米制剂的体外溶出度研究显示萘普生的口服生物利用度增强

P. Sandeep, D. KurdekarAditya, Chunduri La Avinash, C. Prathibha, K. Venkataramaniah
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引用次数: 6

摘要

研究了萘普生-聚乙烯吡咯烷酮纳米制剂的相溶行为、理化特性、细胞毒性、形貌和溶出增强作用。水溶性差的药物萘普生和聚合物PVP的药物-聚合物比例为1:1、1:2、1:3、1:4,通过使用常规Retsch Planetary球磨机的湿法研磨制备。与纯药物相比,在1:4的配方比下,获得了最高的溶出度提高310%。亲水表面活性剂载体加速水溶性差的药物体外溶解的能力归因于润湿、增溶和/或去絮凝。Korsmeyer-Peppas模型最适合体外溶出度数据,表明可能的药物释放机制以异常的非菲克扩散为主,从而有助于改善萘普生的物理化学特性,增强其溶出度,并可能提高药物的口服生物利用度,而不会产生任何不良的细胞毒性后果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In Vitro Dissolution Studies on Naproxen-PVP Nanoformulations Show Enhanced Oral Bioavailability of Naproxen
Phase solubility behavior, physico-chemical characteristics, cytotoxicity, morphology and dissolution enhancement of Naproxen-PVP Nanoformulations have been studied. Drug-polymer ratios of 1:1, 1:2, 1:3, 1:4 for the poorly water-soluble drug, naproxen and the polymer PVP are prepared via wet milling using a conventional Retsch Planetary ball mill. The highest dissolution enhancement over that of the pure drug, 310% was achieved for the formulation ratio of 1:4. This ability of hydrophillic surfactant carriers to accelerate the in vitro dissolution of poorly water-soluble drugs has been attributed to wetting, solubilization and/or deflocculation. The Korsmeyer-Peppas model most aptly fits the in vitro dissolution data indicating a possible drug release mechanism predominated by anomalous non-Fickian diffusion thus helping improve the physicochemical characteristics of naproxen towards its dissolution enhancement and possibly increase the oral bioavailability of the drug without any adverse cytotoxic consequences.
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