Improved dissolution and anti-inflammatory effect of ibuprofen by solid dispersion

doi:10.1007/s11684-012-0189-3

Front Med

2012, Vol. 6

Issue (2) : 195-203 https://doi.org/10.1007/s11684-012-0189-3

Research Article

Improved dissolution and anti-inflammatory effect of ibuprofen by solid dispersion

Liyuan Chen¹, Qifeng Dang¹, Chengsheng Liu¹(

), Jun Chen², Lei Song¹, Xiguang Chen¹

1. College of Marine Life Sciences, Ocean University of China, Qingdao 266003, China; 2. Department of Surgery, the Commercial Staff & Workers Hospital of Qingdao, Qingdao 266011, China

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Abstract

The purpose of this study was to improve the dissolution rate and anti-inflammatory effect of ibuprofen by a solid dispersion (SD) method. Initial screening was developed based on drug solubility in carriers in the liquid state to select a suitable water-soluble carrier system for the preparation of SDs. The dissolution of ibuprofen in urea was higher than in PEG4000 or mannitol. Thus, urea was selected as the carrier for the preparation of SDs. SDs were characterized in terms of dissolution, differential scanning calorimetry (DSC), X-ray diffraction (XRD), scanning electron microscopy (SEM), and Fourier transform infrared (FTIR) spectroscopy. Solid dispersion-based (SDBT) and conventional (CT) tablets were prepared by the wet granulation method. The anti-inflammatory effect of SDBT was evaluated using the mouse ear edema test with xylene. In vitro release results indicated that the ibuprofen dissolution rate was improved by the SD. SD characterization results suggested that ibuprofen partly precipitates in crystalline and amorphous forms after SD preparation and that ibuprofen and urea do not interact. SDBT displayed more significant anti-inflammatory effects than CT. The dissolution rate and anti-inflammatory effect of ibuprofen were significantly enhanced by the ibuprofen-urea SD.

Keywords ibuprofen solid dispersion physical mixture dissolution anti-inflammatory effect

Corresponding Author(s): Liu Chengsheng,Email:Liucs@ouc.edu.cn

Issue Date: 05 June 2012

Cite this article:

Liyuan Chen,Qifeng Dang,Chengsheng Liu, et al. Improved dissolution and anti-inflammatory effect of ibuprofen by solid dispersion[J]. Front Med, 2012, 6(2): 195-203.

URL:

https://academic.hep.com.cn/fmd/EN/10.1007/s11684-012-0189-3
https://academic.hep.com.cn/fmd/EN/Y2012/V6/I2/195

Tab.1 Conventional- and solid-dispersion-based ibuprofen tablet formulations

Fig.1 Solubility of ibuprofen in hydrophilic carriers and water mixtures.

Fig.2 The scanning spectrometer of urea (A) and ibuprofen (B).

Fig.3 dissolution of pure ibuprofen, IUSDs at 1:1, 1:2, 1:5, and 1:10 ratio, and IUPM at 1:10 ratio ( = 37 °C).

Fig.4 FTIR spectrograms of ibuprofen-urea SDs at 1: 10 ratio (A), ibuprofen-urea physical mixture at 1: 10 ratio (B), pure urea (C), and pure ibuprofen (D).

Fig.5 DSC thermograms of pure ibuprofen (A), pure urea (B), ibuprofen-urea physical mixture at 1: 10 ratio (C), and ibuprofen-urea SDs at 1:10 ratio (D).

Fig.6 X-Ray diffractograms of pure ibuprofen (A), ibuprofen-urea SDs at 1:10 ratio (B), ibuprofen-urea physical mixture at 1:10 ratio (C), and pure urea (D). Arrows indicate the characteristic diffraction peaks of ibuprofen.

Fig.7 SEM pictures of pure ibuprofen (A), pure urea (B), ibuprofen-urea physical mixture at 1:10 ratio (C), and ibuprofen-urea SDs at 1:10 ratio (D).

Tab.2 Effect of SDBT and CT on xylene-induced edema on mouse ear

Fig.8 Photomicrograph of transverse sections of mice ears sensitized with topical application of xylene (B to D) or non-inflamed (A), stained with hematoxylin-eosin and examined under a light microscope (scale bar, 50 μm). Treatments: saline (B), CT (C), and SDBT (D). Numbers 1 and 2 indicate the epidermis and dermis, respectively. Arrows indicate the inflammatory cells (polymorphonuclear neutrophils) in the dermis. The sections are representative of eight animals per group.

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