Review Article: Solubility Enhancement by Solid Dispersion

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

doi:10.22159/ijcpr.2017.v9i3.19583

Cited by 13 publications

(19 citation statements)

References 2 publications

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“…The carrier was melted at 55 °C, and then the Cu was dispersed to molten carrier with constant stirring followed by quick cooling. The obtained dried mass was then passed through sieve # 85 and stored in a refrigerator at 4 °C until further use [18,19].…”

Section: Preparation Of Solid Dispersion By Melt Methodsmentioning

confidence: 99%

Formulation and Optimization of Curcumin Solid Dispersion Pellets for Improved Solubility

Deshkar

Satpute

2019

Int J App Pharm

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Objective: The present study was aimed at designing of solid dispersion based pellets of curcumin (Cu) for improving its solubility. Methods: Solid dispersion (SD) of Cu was prepared by the melt method using Poloxamer 407 (Pol 407) at a different weight ratio of Cu-Pol 407 (1:2, 1:3, 1:5, 1:7, 1:10). The solid dispersion was characterised by FTIR, SEM, DSC, XRD and evaluated for saturation solubility in water, drug content and in vitro dissolution. The pellets of Cu solid dispersion were prepared by extrusion spheronization technique and optimization was performed by 32full factorial design. The pellets were evaluated for size distribution, flow properties, hardness, disintegration and in vitro drug dissolution. Results: From the phase solubility analysis, Pol 407 was selected as a Solid dispersion carrier. The formation of Cu-SD by melt method using Pol 407, was confirmed from FTIR and DSC studies. XRD studies indicated a change of Cu from crystalline to amorphous form. There was a significant increase of Cu when formulated as SD compared to plain Cu. The optimization of extrusion spheronization process revealed the significant effect of Cu-Pol 407 ratio (p<0.0001) on in vitro dissolution of pellets. Higher Cu dissolution was obtained with Cu-SD pellets compared to plain Cu pellets. Conclusion: The present study demonstrated the potential of Cu-SD pellets in improving the solubility of poorly soluble Cu.

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Section: Preparation Of Solid Dispersion By Melt Methodsmentioning

confidence: 99%

Formulation and Optimization of Curcumin Solid Dispersion Pellets for Improved Solubility

Deshkar

Satpute

2019

Int J App Pharm

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“…The mixture was evaporated on 8 cm diameter china dish for 48 h at room temperature. The solid mass obtained was dried at 40 °C in the oven for 4 h, pulverized, sieved through 60 mesh and stored in an airtight container until use [6,7].…”

Section: The Solid Dispersion Of Atovaquone With Hpmc and Bio Surfactantmentioning

confidence: 99%

Formulation of Atovaquone Tablet Using Biosurfactant in a Ternary Solid Dispersion System: In Vitro and in Vivo Evaluation

Bolmal

2019

Int J App Pharm

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Objective:The goal of the present investigation was to improve the solubility and bioavailability of atovaquone tablet, using in-house biosynthesized biosurfactant in the ternary system of solid dispersion containing hydrophilic polymers with varying concentrations of biosurfactant. Atovaquone is an anti-malarial agent and belongs to biopharmaceutical classification system class IV. Methods:The solid dispersion of binary and ternary mixture was prepared using hydroxyl propyl methyl cellulose (HPMC) and biosurfactant respectively by a solvent evaporation method. All the atovaquone tablet formulations were prepared by incorporation of physical mixture, binary and ternary solid dispersed products with excipients by direct compression method. Pre-compression and post-compression parameters of atovaquone tablets were evaluated. In vivo bioavailability study was performed using female albino rabbits. Results:In vitro dissolution profile of binary and ternary system of solid dispersion products showed 8.65% and 34.64% respectively. Precompression and post-compression values of all atovaquone tablets formulations were within the specified limits. In vitro dissolution efficiency of F2 and F5 were 1.44 fold and 6.62 fold respectively, in accordance to the F1. In vivo study revealed that bioavailability of optimized formulation F5 was increased by 2.5 times and time to reach peak concentration was reduced to 1.4 h, in accordance to pure atovaquone suspension. Conclusion:Potential application of biosurfactant in the solid dosage form of atovaquone tablet was proved for enhanced dissolution rate and bioavailability of atovaquone for malaria treatment. I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s

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“…During clinical trials, the poor solubility and bioavailability of a drug substance might result in limited therapeutic potential, thereby leading to insuf icient clinical outcomes (Kawabata et al, 2011). Different factors affecting solubility, solubility enhancement techniques, its importance and applications has been reported for poorly water-soluble drugs (Savjani et al, 2012;Sikarra et al, 2012;Kadam et al, 2013;Bharti et al, 2015;Patil et al, 2017) Use of porous media like mesoporous Sylysia 350 has been investigated as a potential means to increase the solubility of poorly soluble drugs and to stabilize the amorphous drug delivery system. These materials have nano-sized capillaries, Porous and the large surface area which enable the materials to accommodate high drug loading and promote the controlled and fast release.…”

Section: Introductionmentioning

confidence: 99%

Solubility enhancement of BCS classified IV drug - Apixaban by preparation and evaluation of Mesoporous Nanomatrix

Amit¹,

S²,

J³

et al. 2020

ijrps

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Biopharmaceutics classification system (BCS) class IV compounds, exhibits low solubility, intestinal permeability and oral bioavailability among all the pharmaceutical class of drugs. Therefore, these drugs need a more compatible and efficient delivery system. Since, their solubility in various mediums will remains a limitation. Hence, the mesoporous Nanomatrix approach may prove to be a suitable solution ahead. Therefore, in the present study, the polymer-coated mesoporous material like Sylysia 350, Carbon, Tin Oxide are opted for the BCS class IV drug like Apixaban to attain higher solubility and dissolution. The prepared Nanomatrix was evaluated for its particle size, DSC, Solubility and dissolution studies. For this study, Apixaban was opted for formulating Sylysia 350, Carbon, Tin Oxide based Mesoporous Nanomatrix system. Nanomatrix was prepared by the Amorphous solid dispersion method using probe sonication. The mesoporous Nanomatrix of Apixaban showed improvement in the solubility in water by approx.7 folds when Apixaban used in combination with Sylysia 350 and Polymer HPMC K15M. From the present study, we can conclude that the optimized Apixaban mesoporous Nanomatrix may prove to be a suitable potential option for solubility enhancement, increase in-vitro drug release and effective delivery of BCS class IV drugs.

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Review Article: Solubility Enhancement by Solid Dispersion

Cited by 13 publications

References 2 publications

Formulation and Optimization of Curcumin Solid Dispersion Pellets for Improved Solubility

Formulation and Optimization of Curcumin Solid Dispersion Pellets for Improved Solubility

Formulation of Atovaquone Tablet Using Biosurfactant in a Ternary Solid Dispersion System: In Vitro and in Vivo Evaluation

Solubility enhancement of BCS classified IV drug - Apixaban by preparation and evaluation of Mesoporous Nanomatrix

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