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. 2008;9(1):54-9.
doi: 10.1208/s12249-007-9019-3. Epub 2008 Jan 9.

Preparation of spherical crystal agglomerates of naproxen containing disintegrant for direct tablet making by spherical crystallization technique

A Nokhodchi  1 , M Maghsoodi
Affiliations

Preparation of spherical crystal agglomerates of naproxen containing disintegrant for direct tablet making by spherical crystallization technique

A Nokhodchi et al. AAPS PharmSciTech. 2008.

Abstract

The purpose of this research was to obtain directly compressible agglomerates of naproxen containing disintegrant by spherical crystallization technique. Acetone-water containing hydroxypropyl celloluse (HPC) and disintegrant was used as the crystallization system. In this study croscarmellose sodium (Ac-Di-Sol) was employed as disintegrant. The agglomerates were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (XRPD), and scanning electron microscopy and were evaluated for flow, packing and tableting properties and drug release. The growth of particle size and the spherical form of the agglomerates resulted in formation of products with good flow and packing properties. The improved compaction properties of the agglomerated crystals were due to their fragmentation occurred during compression. DSC and XRPD studies showed that naproxen particles, crystallized in the presence of HPC and Ac-Di-Sol did not undergo structural modifications. The dissolution rate of naproxen from tablets made of naproxen-(Ac-Di-Sol) agglomerates was enhanced significantly because of including the disintegrant in to the particles. This was attributed to an increase in the surface area of the practically water insoluble drug is exposed to the dissolution medium. In conclusion the spherical crystallization technique developed in this study is suitable for obtaining agglomerates of drug with disintegrant.

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Figures

Fig. 1
Fig. 1
Scanning electron micrographs of appearance a and surface b of naproxen particles: (1) untreated naproxen (2) naproxen agglomerates (3) naproxen–(Ac–Di–Sol) agglomerates
Fig. 2
Fig. 2
The X-ray diffraction spectra of naproxen samples
Fig. 3
Fig. 3
DSC thermograms of naproxen samples
Fig. 4
Fig. 4
The tensile strengths of the tablets made from naproxen samples
Fig. 5
Fig. 5
Dissolution profile of naproxen agglomerates, naproxen–(Ac–Di–Sol) agglomerates and physical mixture of naproxen agglomerates and Ac–Di–Sol
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References

    1. Ribardiere A., Tchoreoff P., Couarraze G., Puisieux F. Modification of ketoprofen bead structure produced by the spherical crystallization technique with a two-solvent system. Int. J. Pharm. 1996;144:195–207. doi: 10.1016/S0378-5173(96)04746-1. - DOI
    1. Paradkar A. R., Pawar A. P., Mahadik K. R., Kadam S. S. Spherical crystallization: a novel particle design technique. Indian Drugs. 1994;31(6):229–233.
    1. Kawashima Y., Lin Y., Ogawa M., Handa T., Takenaka H. Prolonged release microcapsules of indomethacin through spherical crystallization technique. J. Pharm. Sci. 1985;74:1152–1156. doi: 10.1002/jps.2600741104. - DOI - PubMed
    1. Gissing D., Stamm A. A comparative study of cross-linked carboxy-methylcellulose as a tablet disintegrant. Pharm. Ind. 1980;42:189–192.
    1. Munoz N., Ferrero C., Munoz-Ruiz A., Velasco M. V., Jimenez-Castellanos M. R. Effect of explotab on the tabletability of a poorly soluble drug. Drug Dev. Ind. Pharm. 1998;42:785–791. doi: 10.3109/03639049809082727. - DOI - PubMed

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