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63509

ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF NIMESULIDE USING SOLUBILIZATION, SOLID DISPERSION AND COMPLEXATION TECHNIQUES

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Last updated: 25 Dec 2024

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Abstract

Nimesulide is a preferential COX-2 inhibitor. It has high anti-inflammatory, antipyretic and analgesic activities. It has poor aqueous solubility (0.01mg/ml). Solubility of nimesulide was studied using different cosolvent mixtures and various classes of nonionic surfactants. Dimethylacetamide (DMA); at 10% v/v exhibited the highest solubilizing effect (10-fold) towards nimesulide as compared with other cosolvents. Among the tested nonionic surfactants at 10% w/v, brij 58 which exhibited the highest solubilization effect (39-fold). The dissolution of nimesulide from solid dispersions was also studied. Solid inclusion complexes of nimesulide with β-cyclodextrin (β-CD) and hydroxypropyl β-cyclodextrin (HP β-CD) were prepared at a molar ratio of 1:1. Eutectic mixtures were obtained at weight ratio of 1:9 binary systems as confirmed by DSC studies. The dissolution studies indicated that the highest relative amounts dissolved were obtained from solid dispersions as compared with physical mixtures or pure nimesulide. Also higher relative amounts dissolved were obtained with polyvinylpyrrolidones (PVPs) at weight ratio of nimesulide/PVP 40000 1:7. Physicochemical characterization of pure drug, PVP 40000, nimesulide/PVP 40000 solid dispersion and the physical mixture at this ratio were conducted by DSC, FTIR, X-RPD and SEM. The DSC thermograms and X-RPD patterns demonstrated that nimesulide existed in an amorphous form and there is an intermolecular hydrogen bond between the drug and the carrier as shown from FTIR analysis. SEM images confirmed the absence of the crystalline structure of nimesulide in the solid dispersion.

DOI

10.21608/bfsa.2009.63509

Authors

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S.

Last Name

Ismail

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Affiliation

Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt

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First Name

M.

Last Name

El-Mahdy

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Affiliation

Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt

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First Name

S.

Last Name

Al-Kubati

MiddleName

S.

Affiliation

Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt

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Volume

32

Article Issue

2

Related Issue

9571

Issue Date

2009-12-01

Receive Date

2009-10-16

Publish Date

2009-12-31

Page Start

321

Page End

338

Print ISSN

1110-0052

Online ISSN

3009-7703

Link

https://bpsa.journals.ekb.eg/article_63509.html

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https://bpsa.journals.ekb.eg/service?article_code=63509

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Original Article

Type Code

1,096

Publication Type

Journal

Publication Title

Bulletin of Pharmaceutical Sciences Assiut University

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https://bpsa.journals.ekb.eg/

MainTitle

ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF NIMESULIDE USING SOLUBILIZATION, SOLID DISPERSION AND COMPLEXATION TECHNIQUES

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Article

Created At

22 Jan 2023