Solubility and Dissolution Enhancement of Sulfasalazine by Solid Dispersion Technique

Shinkar, D. M.; Patil, A. N.; Saudagar, R. B.

doi:10.5958/0974-360x.2018.00237.8

Cited by 4 publications

(1 citation statement)

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“…6 Priyam and co-workers synthesized an amphiphilic derivative of SSZ to modify the solubility by conjugating it with polyethylene glycol. 7 In addition, nanocrystallization, 8 solid dispersion, 9 and noisome techniques 10 have been explored to improve the solubility and/ or dissolution performance of SSZ.…”

Section: ■ Introductionmentioning

confidence: 99%

Exploring the Crystal Structure Landscape of Sulfasalazine through Various Multicomponent Crystals

Huang

Cheemarla

Tiana

et al. 2023

Crystal Growth & Design

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Sulfasalazine is used as an anti-inflammatory drug to treat large intestine diseases and atrophic arthritis. In the solid state, two tautomers are known: an amide tautomer (triclinic polymorph) and an imide tautomer (monoclinic polymorph). Crystallization of six new multicomponent solids of sulfasalazine with three cocrystal formers and three salt formers has been achieved by slurry, liquid-assisted grinding and slow evaporation methods. All of the solid forms are characterized by X-ray diffraction techniques, thermal analysis, and Fourier transform infrared spectroscopy. The crystal structural analysis reveals that two sulfasalazine molecules or anions arrange in a head-to-head fashion involving their pyridyl, amide, and sulfonyl groups in an R 2 2(7):R 2 2(8):R 2 2(7) motif. This is the key structural unit appearing in both sulfasalazine imide polymorph and all six multicomponent crystals. In addition, sulfasalazine exists in the amide form in all unsolvated multicomponent crystals obtained in this work and adopts the imide tautomer in the solvated cocrystals and salt. Hirshfeld surface analysis and the associated two-dimensional (2D) fingerprint plots demonstrate that sulfasalazine has significant hydrogen bond donor capability when cocrystallized and is a significant hydrogen bond acceptor in the salts. The frontier molecular orbital analysis indicates that sulfasalazine cocrystals are chemically more stable than the salts.

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Section: ■ Introductionmentioning

confidence: 99%

Exploring the Crystal Structure Landscape of Sulfasalazine through Various Multicomponent Crystals

Huang

Cheemarla

Tiana

et al. 2023

Crystal Growth & Design

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Comparative Evaluation of Porous Carriers for Dissolution Improvement of BCS Class II Drug

Mahajan

Yadav

Patel

et al. 2021

RJPT

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The objective of present investigation was comparison of porous carriers to increase the dissolution properties of BCS class II drug Ziprasidone. Solvent evaporation method was used for the adsorption of ziprasidone on various porous carriers. Three different porous carriers namely Florite, Neusilin US2, Sylysia 350 were used in the study. Prepared microparticles were characterised for invitro drug release, SEM, XRD and DSC. The optimized formulation containing ziprasidone: florite microparticles had high drug release (94.88% in 45 min) than plain ziprasidone tablets (21.13% in 45 min) which is due to increase in surface area and decrease in crystallinity of drug after adsorption onto porous carrier.

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Solid Dispersions: An Effective Technology for Improving Dissolution Kinetics of Poorly Soluble Drugs

Alrouhayyah,

F. Sheshko,

N. Suslina

et al. 2023

RJPT

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Solid dispersions are one of the essential technologies for improving solubility and dissolution kinetics of drugs. They can be prepared in several ways and using different carriers. This technique is very suitable for class II BCS drugs, one of which is mefenamic acid. This paper is devoted to improving the solubility and dissolution rate of mefenamic acid by preparing solid dispersions using polyethylene glycol 4000, polyvinylpyrrolidone K30, and polysorbate 80 as carriers. Solid dispersions were prepared by kneading method, and dissolution was studied for two hours in phosphate buffer (pH=8). Experimental data of drug release from prepared solid dispersions were analysed according to different mathematical models. The results showed that the dissolution rate varied depending on the type and fraction of the carrier. However, mefenamic acid was released from all prepared formulations in accordance with the Higuchi model, and the release mechanism was better described by Fickian diffusion.

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Solubility and Dissolution Enhancement of Sulfasalazine by Solid Dispersion Technique

Cited by 4 publications

References 0 publications

Exploring the Crystal Structure Landscape of Sulfasalazine through Various Multicomponent Crystals

Exploring the Crystal Structure Landscape of Sulfasalazine through Various Multicomponent Crystals

Comparative Evaluation of Porous Carriers for Dissolution Improvement of BCS Class II Drug

Solid Dispersions: An Effective Technology for Improving Dissolution Kinetics of Poorly Soluble Drugs

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