Optimization of formulation and process variables using central composite design for the production of nevirapine spray dried solid dispersion

Mahajan, Arpana; Surti, Naazneen; Patel, Priyal; Gheewala, Naziya; Patel, Ashwini; Shah, Dimal A.

doi:10.1080/07373937.2021.1874408

Cited by 5 publications

(3 citation statements)

References 33 publications

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“…13,14,15 The Solid dispersion is the most ISSN: 2250-1177 [24] CODEN (USA): JDDTAO convenient technique for increasing the bioavailability and solubility of poorly water-soluble drugs. 16 To improve the overall hydrophilicity of the poorly soluble drug, a water-soluble carrier or hydrophilic polymer is chosen for the solid dispersion system. 17 The most generally been used carriers includes PVP, Tween 80, Gelucire, PEG, etc.…”

Section: Introductionmentioning

confidence: 99%

Formulation, Optimization and Evaluation of Solid Dispersion of Deferasirox Using Factorial Design

Talla,

Wadher,

Umekar

et al. 2024

J. Drug Delivery Ther.

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Deferasirox, an oral iron-chelating agent, is a poorly soluble drug (Biopharmaceutical Classification System class II) having insufficient solubility in physiological fluids resulting in low bioavailability of the drug. The idea behind the present study was to explore the prospects of solid dispersion as a prolific method to enhance the dissolution rate of drug using a water soluble polymer. The solid dispersion was prepared by the solvent evaporation technique using Polyvinyl pyrrolidone with different drug to carrier and solvent ratio. Formulations were characterized through attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), Powder X-ray diffraction (XRD), and in vitro release studies. A 32 factorial design was implemented to obtain optimum solubility, % yield, and optimization of solid dispersion (SD) also quantitates the influence of PVP on the solubility and dissolution profile. Thedrug-to-carrier and solvent ratio was chosen as independent variable, while %yield, drug content, and saturation solubility were chosen as dependent variables. The results showed that the optimized formulation of SD-DFX was able to significantly enhance its solubility. The SD containing a dispersion of Deferasirox with PVP show an exceptional rise in the solubility. This study describes the development of solid dispersion that significantly improved the solubility and bioavailability of DFX. The FTIR studies indicate the interaction between the drug and polymer. The DSC and XRD analysis indicated that the drug was in an amorphous state when dispersed in the polymer. It is resolved that the SD method significantly improves the solubility and dissolution rate, which could also be exploit for other poorly water soluble drug candidates. Keywords: Deferasirox , Polyvinyl pyrrolidone, solid dispersion, Factorial design, Solubility

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Section: Introductionmentioning

confidence: 99%

Formulation, Optimization and Evaluation of Solid Dispersion of Deferasirox Using Factorial Design

Talla,

Wadher,

Umekar

et al. 2024

J. Drug Delivery Ther.

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“…This design consists of corners, central and axial points which can study the factors comprehensively, reduce the cost and process variability, and improve the quality of the product and higher yields. [15][16][17] In this study, AP extract-chitosan solid dispersion was formulated using central composite design to optimize formulation variables to enhance AGP release and study release kinetic of the optimal formulation.…”

Section: Introductionmentioning

confidence: 99%

Optimization of Formulation Variables Using Central Composite Design to Enhance Andrographolide Release from <i>Andrographis paniculata</i> Extract-Chitosan Solid Dispersion

Nontasirichayakul

Wiranidchapong

Sithithaworn

et al. 2022

Advances in Science and Technology

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Andrographolide (AGP), a major component of Andrographis paniculata (Burm.f.) Nees (AP), has several biological activities. Nevertheless, poorly water solubility and low bioavailability of AGP lead to decrease clinical benefits. Therefore, this study aims to develop of AP extract-chitosan solid dispersion using central composite design (CCD) to enhance AGP release. AP crude extract was obtained by Soxhlet extractor using 85%v/v ethanol as a solvent extraction. Then, AP extract, chitosan, and poloxamer 188 in the concentrations provided by CCD was spray dried. The in-vitro release of AP extract-chitosan spray dried powder was studied by dissolution equipped with enhancer cell in 200 ml of 50%v/v methanol at 37°C and 50 rpm of paddle speed. Samples were withdrawn at 0.25-96 hours and then determined AGP by UV spectrophotometer at 224 nm. The results of CCD indicated that %ethanol and %AGP from concentrated AP extract had significant (P < 0.05) effect on the concentration of AGP released at 5 hours. The optimum formulation composed of %ethanol of 18.25, %AGP in extract of 0.38, and %poloxamer 188 of 0.17 resulted in more AGP concentration at 5 hours than 50 μg/mL. Release kinetic study revealed that %release of the optimal formulation was best fitted to first order kinetic. In powder X-ray diffraction, intensity of AGP characteristic peaks in the optimal formulation decreased by 7.17-25.69 times compared with AGP standard. It was concluded that the optimal formulation of AP extract-chitosan solid dispersion could improve AGP release due to changing crystalline AGP to amorphous state.

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“…, el rivaroxaban(Lee et al, 2021) y 9-nitrocamptotecina(Lian et al, 2014); la fabricación mediante moldeo por solvente (en inglés, solvent casting) de DS de la resveratrol(Vasconcelos et al, 2021); los fluidos supercríticos de la simvastatina(Nandi, Ajiboye, Patel, Douroumis & Trivedi, 2021); y el secado por aspersión de arteméter, nevirapino y efavirenz (Dabhade et al, 2021;Lavra, Pereira de Santana & Ré, 2017;Mahajan et al, 2021)…”

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Evaluación de mezclas binarias para la preselección de acarreadores poliméricos

Alcántara-Fierro,

Ortiz-Reynoso,

Llera-Rojas

2024

TIP RECQB

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La selección de un polímero para mejorar la velocidad de disolución de un fármaco dentro de una fórmula farmacéutica implica el uso de múltiples pruebas que encarecen el proceso de selección, por requerir técnicas de alta especialización; lo opuesto es el uso de un método reducido basado en estudios calorimétricos y de disolución, que ayude en la selección preliminar de los materiales, sin altas inversiones monetarias o de tiempo. En este trabajo se realizó la preselección de un polímero acarreador, con potencial para ser usado en el desarrollo de dispersiones sólidas de clorhidrato de terbinafina, con base en la evaluación de mezclas binarias fármaco-polímero. Se evaluaron tres polímeros con diferentes mecanismos de solubilización, PVP-VA, PCAP-PEG y POE-POP. Los copolímeros de PVP-VA y PCAP-PEG resultaron candidatos factibles para su evaluación en el desarrollo de dispersiones sólidas por los métodos de fusión. Ambos polímeros mejoraron los valores de velocidad de disolución y el porcentaje disuelto de terbinafina, abatieron la entalpía de fusión del fármaco y mostraron termoplasticidad. Con este estudio se muestra un enfoque sencillo y de bajo costo para la preselección de polímeros útiles en la fabricación de dispersiones sólidas.

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Optimization of formulation and process variables using central composite design for the production of nevirapine spray dried solid dispersion

Cited by 5 publications

References 33 publications

Formulation, Optimization and Evaluation of Solid Dispersion of Deferasirox Using Factorial Design

Formulation, Optimization and Evaluation of Solid Dispersion of Deferasirox Using Factorial Design

Optimization of Formulation Variables Using Central Composite Design to Enhance Andrographolide Release from <i>Andrographis paniculata</i> Extract-Chitosan Solid Dispersion

Evaluación de mezclas binarias para la preselección de acarreadores poliméricos

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