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. 2018 Apr;15(1):7-15.
doi: 10.4274/tjps.09609. Epub 2018 Apr 2.

Preparation and In Vitro Evaluation of Ibuprofen Spherical Agglomerates

Nagaraju Ravouru  1 , Subhash Chandra Bose Penjuri  2 , Saritha Damineni  3 , Raja Lakshmi Muni  1 , Srikanth Reddy Poreddy  2
Affiliations

Preparation and In Vitro Evaluation of Ibuprofen Spherical Agglomerates

Nagaraju Ravouru et al. Turk J Pharm Sci. 2018 Apr.

Abstract

Objectives: Ibuprofen, an anti-inflammatory drug, is characterized by poor water solubility, which limits its pharmacologic effects. The present work aimed to the study the effect of agglomeration on the micromeritic properties and dissolution of ibuprofen.

Materials and methods: Ibuprofen agglomerates were prepared by solvent change method using water, dichloromethane and DMSO as poor solvent, bridging liquid and good solvent respectively in the ratio of 57.5:12.5:30. Process variables such as amount of bridging liquid, mode of addition, temperature and stirring rate were optimized.

Results: SEM studies indicate that agglomerates produced were spherical and exhibit irregular shape. X-Ray Powder Diffraction spectra revealed the absence of polymorphism. DSC spectra showed no change in melting point indicating absence of crystal modification. The agglomerates exhibited improved solubility, dissolution rate and micromeritic properties compared to pure drug.

Conclusion: Anti-inflammatory studies were conducted in Wistar strain male albino rats and ibuprofen agglomerates showed more significant activity than the pure drug which may be due to better absorption. Ulcerogenic potential study was carried out for pure ibuprofen and agglomerates. Better ulcerogenic potential was observed in ibuprofen agglomerates treated rats.

Keywords: Ibuprofen; anti-inflammatory activity; spherical agglomeration; ulcerogenic potential.

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Conflict of interest statement

Conflict of Interest: No conflict of interest was declared by the authors.

Figures

Figure 1
Figure 1
Ternary phase diagram of ibuprofen-DMSO/water/DCM DMSO: Dimethyl sulfoxide
Figure 2a
Figure 2a
SEM of pure ibuprofen SEM: Scanning electron microscopy
Figure 2b
Figure 2b
SEM of agglomerates SEM: Scanning electron microscopy
Figure 3
Figure 3
Fourier transform infrared spectroscopy spectra of ibuprofen and its agglomerates
Figure 4
Figure 4
Differential scanning calorimetry thermograms of ibuprofen and its agglomerates DSC: Differential scanning calorimetry
Figure 5a
Figure 5a
X-ray diffraction spectra of ibuprofen
Figure 5b
Figure 5b
X-ray diffraction spectra of spherical agglomerates of ibuprofen
Figure 6
Figure 6
In vitro release profile of ibuprofen and its agglomerates
Figure 7
Figure 7
Photographs of isolated stomach of rats for ulcerogenic potential studies
See this image and copyright information in PMC

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