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优化后的黑胡椒纳米混悬液中胡椒碱的口服生物利用度提高。

Increased Oral Bioavailability of Piperine from an Optimized Piper nigrum Nanosuspension.

作者信息

Zafar Fatiqa, Jahan Nazish, Bhatti Haq Nawaz

机构信息

Department of Chemistry, University of Agriculture, Faisalabad, Pakistan.

出版信息

Planta Med. 2019 Feb;85(3):249-257. doi: 10.1055/a-0759-2208. Epub 2018 Oct 24.

DOI:10.1055/a-0759-2208
PMID:30357764
Abstract

The aim of the present study was to enhance the pharmaceutical potential and oral bioavailability of piperine, which is the bioactive constituent of , using the nanosuspension approach. Nanoprecipitation, which is a simple and reproducible process, was used for nanosuspension formulation. To prepare a pharmaceutical-grade nanosuspension with the required particle size, important formulation parameters (amount of plant extract, concentration of stabilizer, and antisolvent-to-solvent ratio) were optimized using the central composite design of response surface methodology. The optimized nanosuspension was characterized using scanning electron microscopy, atomic force microscopy, Fourier transform infrared spectroscopy, and dissolution testing as well as by measuring the zeta potential. pharmacokinetic studies were conducted to determine the bioavailability of the prepared nanosuspension. Results of the optimization study indicated that 0.13% plant extract, 0.25% stabilizer, and an antisolvent-to-solvent ratio of 10.0 were the best parameters to obtain a homogeneous nanosuspension with the required particle size. The optimized nanosuspension demonstrated a mean particle size, polydispersity index, and zeta potential of 172.5 nm, 0.241, and - 16.6 mV, respectively. The results of the characterization studies illustrated that the nanosuspension was in the nanometer size range and had good surface morphology. The optimized nanosuspension showed a better dissolution rate and a 3.65-fold higher oral bioavailability for the nanosuspension than its coarse suspension. The present outcomes clearly demonstrated that to obtain an effective therapeutic potential, nanoformulation of medicinal plants is a better alternative than conventional dosage forms.

摘要

本研究的目的是采用纳米混悬液方法提高胡椒碱(胡椒的生物活性成分)的药用潜力和口服生物利用度。纳米沉淀法是一种简单且可重复的过程,用于纳米混悬液的制备。为制备具有所需粒径的药用级纳米混悬液,使用响应面法的中心复合设计优化了重要的制剂参数(植物提取物用量、稳定剂浓度和抗溶剂与溶剂的比例)。通过扫描电子显微镜、原子力显微镜、傅里叶变换红外光谱、溶出度测试以及测量zeta电位对优化后的纳米混悬液进行了表征。进行了药代动力学研究以确定所制备纳米混悬液的生物利用度。优化研究结果表明,0.13%的植物提取物、0.25%的稳定剂和10.0的抗溶剂与溶剂比例是获得具有所需粒径的均匀纳米混悬液的最佳参数。优化后的纳米混悬液的平均粒径、多分散指数和zeta电位分别为172.5nm、0.241和-16.6mV。表征研究结果表明,该纳米混悬液处于纳米尺寸范围且具有良好的表面形态。优化后的纳米混悬液显示出更好的溶出速率,其纳米混悬液的口服生物利用度比其粗混悬液高3.65倍。目前的结果清楚地表明,为获得有效的治疗潜力,药用植物的纳米制剂是比传统剂型更好的选择。

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