Development of Glimepiride Solid Dispersion using The Coprocessed Excipients of Polyvinylpyrrolidone, Maltodextrin, and Polyethylene Glycol

Surini, Silvia; Evangelista, Claudia Nelrima; Iswandana, Raditya

doi:10.5530/jyp.2018.2s.9

Cited by 4 publications

(6 citation statements)

References 10 publications

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“…The solvent evaporation method previously described with a little modification was used to prepare the co-processed excipient (PECE) carrier. , Briefly, ∼100 mg of pentaerythritol and EudragitRS100 (ERS100) were separately weighed. Both ingredients were dissolved in 50 mL of ethanol and stirred well until a homogenous solution was obtained.…”

Section: Methodsmentioning

confidence: 99%

“…The solid dispersion formulation remarkably improved the solubility, permeability, dissolution, and pharmacokinetic profile of poorly aqueous soluble drugs − by reduction of drug particle size to submicron particles, changing the crystalline state to high-energy amorphous state, and improving the wettability, solubility, and dissolution rate of the drug . Previous reports have shown the use of co-processed excipients as solid dispersion carriers with an enhanced dissolution rate of glimepiride, a poorly water-soluble drug . Pentaerythritol-EudragitRS100 co-processed excipients (PECE) were investigated in the current study as potential solid dispersion carriers for improved ATV solubility, permeability, and dissolving rate.…”

Section: Introductionmentioning

confidence: 99%

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Development and Characterization of Pentaerythritol-EudragitRS100 Co-processed Excipients as Solid Dispersion Carriers for Enhanced Aqueous Solubility, In Vitro Dissolution, and Ex Vivo Permeation of Atorvastatin

Telange,

Bhaktani,

Hemke

et al. 2023

ACS Omega

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Atorvastatin (ATV), a lipid-lowering agent, has low oral bioavailability due to its poor water solubility, permeability, and low dissolution rate. Therefore, pentaerythritol-EudragitRS100 co-processed excipients (PECE) were synthesized, and their feasibility as solid dispersion carriers (ATV-PECE-SD) for improving the solubility, permeability, and dissolution rate of ATV was explored. Solid dispersions were assessed in terms of particle size and zeta potential, and solubility, in vitro dissolution, and ex vivo permeation studies were studied. Scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) were used as characterization tools. ATV-PECE-SD3 (1:4) formulations exhibited a small particle size with high stability. Physicochemical evaluation evidenced the formation of solid dispersion due to the involvement of weak electrostatic interaction between the polar functional groups of ATV and PECE carriers. ATV-PECE-SD3 (1:4) significantly enhanced the water solubility by ∼43-fold compared to pure ATV. In vitro dissolution studies showed that optimized formulation enhanced the dissolution rate of ATV compared to pure ATV. Ex vivo permeation results revealed that ATV-PECE-SD3 (1:4) enhanced the permeation rate of ATV compared to pure ATV. The optimized formulations significantly improved the dissolution rate of ATV in the fed state due to the food effect and micelle formation mechanism compared to the fasted state. The study concludes that co-processed excipients could be used as promising solid dispersion carriers to enhance the aqueous solubility, permeability, and dissolution rate of ATV.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Development and Characterization of Pentaerythritol-EudragitRS100 Co-processed Excipients as Solid Dispersion Carriers for Enhanced Aqueous Solubility, In Vitro Dissolution, and Ex Vivo Permeation of Atorvastatin

Telange,

Bhaktani,

Hemke

et al. 2023

ACS Omega

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“…The pentaerythritol-eudragit ® RS100 co-processed excipients (CE) carrier was created using a slightly modified method from one literature published in Elsevier [13,18]. Briefly, 50 ml of ethanol was used to dissolve ~ 100 mg of pentaerythritol and ~100 mg of eudragit ® RS100 (ERS).…”

Section: Preparation Of Pentaerythritol-eudragit ® Rs100 Co-processed...mentioning

confidence: 99%

“…The solid dispersion formulation significantly improved the solubility, permeability, dissolution, and pharmacokinetic profile of poorly aqueous soluble drugs [10][11][12]. Co-processed excipients have been used in prior studies to demonstrate the use of glimepiride, a BCS class II medication, as a solid dispersion carrier with an accelerated dissolution rate [13]. In this study, we investigated whether pentaerythritol-Eudragit®RS100 co-processed excipients (CE) might be used as a solid dispersion carrier to improve the solubility, permeability, and dissolution rate of ATN.…”

Section: Introductionmentioning

confidence: 99%

Enhanced Aqueous Solubility and in Vitro Dissolution of the Anti-Hyperlipidemic Agent Using Synthesized Solid Dispersion Carrier

et al. 2023

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Objective: To improve ATN's solubility, permeability, and dissolution rate of pentaerythritol-eudragit®RS100 co-processed excipients (CE) and their potential as a solid dispersion carrier (ATN-CE-SD). Methods: The ATN-CE-SD was prepared using the solvent evaporation technique. The pure ATN, physical mixture, CE carrier, and optimized ATN-CE-SD was physicochemically characterized using Scanning electron microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, powder x-ray diffractometry, solubility, and in vitro dissolution was used to evaluate solid dispersions. Results: Physical and chemical analysis showed that ATN-CE-SD formed via the involvement of weak intermolecular forces of attraction between CE carrier and ATN. The prepared solid dispersion showed the drug content around ~ 96.94 % w/w, indicating that the solvent evaporation method improved the encapsulation of ATN and, thus, enhanced its drug content. Compared to pure ATN (~ 0.11 mg/ml), ATN-CE-SD (1:2) significantly increased the aqueous solubility by around ~ 25-fold (~ 2.78 mg/ml), indicating solid dispersion improves the solubility of ATN. ATN-CE-SD enhanced the rate of dissolution of ATV (~ 65 %) compared to pure ATN (~ 25 %) and PM (~ 34 %). Likewise, ATN-CE-SD (1:2) improved the rate and extent of ATN (~ 60 %) across the biological membrane compared to pure ATN (~ 22 %) and PM (~ 32 %). The ATN-CE-SD (1:2) improved the dissolution efficiency by around ~ (57.31%) compared to pure ATN (~ 7.02%) and PM (~ 20.43%). According to the study, co-processed excipients could serve as a promising solid dispersion carrier and improve ATN's water solubility, permeability, and dissolution rate. Conclusion: Based on the results, it is possible to use synthetic solid dispersion carriers as alternatives to improve the low water solubility and permeability of ATN.

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“…Also, it has low toxicity properties and is commonly used to increase solubility and enhance drug release. 28,29 Okwuosa et al 30 did research to make immediaterelease 3D printed tablets using PVP filament matrix with theophylline and dipyridamole. Filament prepared only of PVP cannot be printed by FDM 3D printing due to the poor flow rate at the nozzle.…”

Section: Polyvinyl Pyrrolidone (Pvp)mentioning

confidence: 99%

The Application of Polymers in Fabricating 3D Printing Tablets by Fused Deposition Modeling (FDM) and The Impact on Drug Release Profile

2022

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A new chapter in the pharmaceutical industry has been created by 3D printing, particularly in the manufacturing of solid preparations. This technology can support the modification of medicine in terms of drug dosage. Furthermore, it is achieved by adjusting the volume of tablets while being designed using the software to meet the required dose. The research aims to review several polymers used in 3D printing through the fused deposition modeling technique. The polymers in filament fabrication for 3D printed tablets should be thermoplastic and have the appropriate mechanical properties for further processing steps. This review focuses on studying the characteristics of polymers such as polylacticacid, polyvinyl alcohol, polycaprolactone, polyvinyl pyrrolidone, polyethylene oxide, ethylene vinyl acetate, ethyl cellulose, hydroxypropyl methyl cellulose, and hydroxypropyl cellulose. Additionally, it discusses the effect of these polymers on the drug release profile from the 3D printed tablets.

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Development of Glimepiride Solid Dispersion using The Coprocessed Excipients of Polyvinylpyrrolidone, Maltodextrin, and Polyethylene Glycol

Cited by 4 publications

References 10 publications

Development and Characterization of Pentaerythritol-EudragitRS100 Co-processed Excipients as Solid Dispersion Carriers for Enhanced Aqueous Solubility, In Vitro Dissolution, and Ex Vivo Permeation of Atorvastatin

Development and Characterization of Pentaerythritol-EudragitRS100 Co-processed Excipients as Solid Dispersion Carriers for Enhanced Aqueous Solubility, In Vitro Dissolution, and Ex Vivo Permeation of Atorvastatin

Enhanced Aqueous Solubility and in Vitro Dissolution of the Anti-Hyperlipidemic Agent Using Synthesized Solid Dispersion Carrier

The Application of Polymers in Fabricating 3D Printing Tablets by Fused Deposition Modeling (FDM) and The Impact on Drug Release Profile

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