Physicochemical and mechanical properties of paracetamol cocrystal with 5-nitroisophthalic acid

被引：76

作者：

Hiendrawan, Stevanus ^{[1
,2
]}

Veriansyah, Bambang ^{[1
]}

Widjojokusumo, Edward ^{[1
]}

Soewandhi, Sundani Nurono ^{[2
]}

Wikarsa, Saleh ^{[2
]}

Tjandrawinata, Raymond R. ^{[1
]}

机构：

[1] Dexa Labs Biomol Sci, Cikarang 17550, West Java, Indonesia

[2] Bandung Inst Technol, Sch Pharm, Bandung 40132, West Java, Indonesia

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2016年 / 497卷 / 1-2期

关键词：

Cocrystal; Paracetamol; 5-Nitroisophhthalic acid; Mechanical properties; Dissolution rate; HIGHLY COMPRESSIBLE PARACETAMOL; COMPACTION PROPERTIES; CO-CRYSTALS; ORTHORHOMBIC PARACETAMOL; PURE PARACETAMOL; BEHAVIOR; CRYSTALLIZATION; ACETAMINOPHEN; SALTS; NICOTINAMIDE;

D O I：

10.1016/j.ijpharm.2015.12.001

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

We report novel pharmaceutical cocrystal of a popular antipyretic drug paracetamol (PCA) with coformer 5-nitroisophhthalic acid (5NIP) to improve its tabletability. The cocrystal (PCA-5NIP at molar ratio of 1:1) was synthesized by solvent evaporation technique using methanol as solvent. The physicochemical properties of cocrystal were characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetry analysis (TGA), fourier transform infrared spectroscopy (FTIR), hot stage polarized microscopy (HSPM) and scanning electron microscopy (SEM). Stability of the cocrystal was assessed by storing them at 40 degrees C/75% RH for one month. Compared to PCA, the cocrystal displayed superior tableting performance. PCA-5NIP cocrystal showed a similar dissolution profile as compared to PCA and exhibited good stability. This study showed the utility of PCA-5NIP cocrystal for improving mechanical properties of PCA. (C) 2015 Elsevier B.V. All rights reserved.

引用

页码：106 / 113

页数：8

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