帕利潘酮-苯甲酰胺共晶:制备、表征、体外/体内评价

Q3 Engineering

Nanoscience and Nanotechnology - Asia Pub Date : 2022-10-31 DOI:10.2174/2210681213666221031150449

E. R. Rani, G. Radha

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引用次数: 0

摘要

目前的研究有助于以苯甲酰胺(BZ)为构象的新型帕利哌酮(PPD)共晶(CCs)的开发。采用溶剂蒸发法合成了活性炭。通过饱和溶解度研究来研究其溶解度的增强。采用傅里叶变换红外光谱(FTIR)、粉末x射线衍射(PXRD)、差示扫描量热法(DSC)、扫描电镜(SEM)和质子核磁共振(1H- FT NMR)对CC的形成进行了结构表征。CCs的溶解度为2.067±0.004mg/ml，高于纯药0.473±0.012mg/ml。这表明CCs的水溶性提高了4.36倍。体外溶出度数据显示，PPD和BZ在60min内的药物释放量为96.5±1.63%，而纯药物在相同时间内的释放量为37.8±1.76%。在PPD和BZ之间形成的体内vocc为克服PPD水溶性差的溶解度障碍提供了一种新的方法。

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Paliperidone-Benzamide Cocrystals: Preparation, Characterization, In Vitro/In Vivo Evaluation

The current investigation contributes in the development of novel Paliperidone (PPD) co-crystals (CCs) using benzamide (BZ) as a conformer. The CCs were synthesized using solvent evaporation technique. The enhancement in solubility was studied by saturation solubility studies. Structural characterization of CCs was performed by Fourier Transform Infra-Red Spectroscopy (FTIR), powder X-ray diffraction (PXRD), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM) and Proton Nuclear Magnetic Resonance (1H- FT NMR) to verify CC formation. CCs exhibited higher aqueous solubility of 2.067±0.004mg/ml when compared to pure drug 0.473±0.012mg/ml. This designated aqueous solubility enhancement of CCs by 4.36 folds. In vitro dissolution data of the CCs exhibited a drug release of 96.5±1.63% in 60min, while pure drug showed a poor release of 37.8±1.76% in the same time period In vivo CCs formed between PPD and BZ present a novel approach in overcoming the hurdles in the solubility of PPD that exhibits poor aqueous solubility.

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来源期刊

Nanoscience and Nanotechnology - Asia Engineering-Engineering (all)

CiteScore

1.90

自引率

0.00%

发文量

期刊介绍： Nanoscience & Nanotechnology-Asia publishes expert reviews, original research articles, letters and guest edited issues on all the most recent advances in nanoscience and nanotechnology with an emphasis on research in Asia and Japan. All aspects of the field are represented including chemistry, physics, materials science, biology and engineering mainly covering the following; synthesis, characterization, assembly, theory, and simulation of nanostructures (nanomaterials and assemblies, nanodevices, nano-bubbles, nano-droplets, nanofluidics, and self-assembled structures), nanofabrication, nanobiotechnology, nanomedicine and methods and tools for nanoscience and nanotechnology.