Effect of screw profile and processing conditions on physical transformation and chemical degradation of gabapentin during twin-screw melt granulation

Kittikunakorn, Nada; Sun, Changquan Calvin; Zhang, Feng

doi:10.1016/j.ejps.2019.02.024

Cited by 27 publications

(8 citation statements)

References 26 publications

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“…Mixing both increases the overall diffusion of the system and decreases the diffusion layer thickness, increasing the tendency of the drug to dissolve within the molten polymer. 19,20 Conversion to the amorphous state significantly below a composition's melting point has been reported for systems that utilize mixing. Hot stage-polarized light microscopy (HS-PLM) can be used to better understand this phenomenon.…”

Section: Introductionmentioning

confidence: 99%

Selective Laser Sintering 3-Dimensional Printing as a Single Step Process to Prepare Amorphous Solid Dispersion Dosage Forms for Improved Solubility and Dissolution Rate

Davis

Thakkar

et al. 2021

Journal of Pharmaceutical Sciences

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This study reports the development of ritonavir-copovidone amorphous solid dispersions (ASDs) and dosage forms thereof using selective laser sintering (SLS) 3-dimensional (3-D) printing in a single step, circumventing the post-processing steps required in common techniques employed to make ASDs. For this study, different drug loads of ritonavir with copovidone were processed at varying processing conditions to understand the impact, range, and correlation of these parameters for successful ASD formation. Further, ASDs characterized using conventional and advanced solid-state techniques including wide-angle X-ray scattering (WAXS), solid-state nuclear magnetic resonance (ssNMR), revealed the full conversion of the crystalline drug to its amorphous form as a function of laser-assisted selective fusion in a layer-by-layer manner. It was observed that an optimum combination of the powder flow properties, surface temperature, chamber temperature, laser speed, and hatch spacing was crucial for successful ASD formation, any deviations resulted in print failures or only partial amorphous conversion. Moreover, a 21fold increase in solubility was demonstrated by the SLS 3-D printed tablets. The results confirmed that SLS 3-D printing can be used as a single-step platform for creating ASD-based pharmaceutical dosage forms with a solubility advantage.

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Section: Introductionmentioning

confidence: 99%

Selective Laser Sintering 3-Dimensional Printing as a Single Step Process to Prepare Amorphous Solid Dispersion Dosage Forms for Improved Solubility and Dissolution Rate

Davis

Thakkar

et al. 2021

Journal of Pharmaceutical Sciences

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show abstract

“…HPC granules were the most compactible, but the API in PEG 8000 and Compritol granules degraded less. API degradation in the HPC granules was linked to the higher thermal and mechanical stresses with higher required process temperature [ 49 ] and further related to mechanical energy input and API particle attrition [ 60 ].…”

Section: Binders For Granulationmentioning

confidence: 99%

“…Particle friction against the barrel, attrition, and the addition of abrasive formulation components can also cause local heating. Often overall process optimization can help avoid API degradation, but not, thermal degradation can be managed by using lower melting point binders, pre-plasticizing the binder [ 42 ], modifying the screw design [ 60 ], or adding the API later in the process.…”

Section: Tsmg Critical Process Parameters and Output Granule Propertiesmentioning

confidence: 99%

Twin-Screw Melt Granulation for Oral Solid Pharmaceutical Products

2021

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This article highlights the advantages of pharmaceutical continuous melt granulation by twin-screw extrusion. The different melt granulation process options and excipients are described and compared, and a case is made for expanded use of twin-screw melt granulation since it is a flexible and continuous process. Methods for binder selection are profiled with a focus on rheology and physical stability impacts. For twin-screw melt granulation, the mechanism of granulation and process impact on granule properties are described. Pharmaceutical applications of melt granulation ranging from immediate release of soluble and insoluble APIs, taste-masking, and sustained release formulation are reviewed, demonstrating the range of possibilities afforded by twin-screw melt granulation.

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“…The modular screw and barrel design, common among twin-screw extruders, allows for improved control of granule density and particle size. For more information, refer to recent reviews of continuous melt granulation [10,31] and process studies [33][34][35][36]. TSMG has similar process considerations to twin-screw wet granulation, which is comparatively more developed in the literature [37][38][39][40][41][42].…”

Section: Continuous Twin-screw Melt Granulation For Taste-maskingmentioning

confidence: 99%

Continuous Melt Granulation for Taste-Masking of Ibuprofen

Forster

Lebo

2021

Pharmaceutics

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Taste-masking of drugs, particularly to produce formulations for pediatric patients, can be challenging and require complex manufacturing approaches. The objective of this study was to produce taste-masked ibuprofen granules using a novel process, twin-screw melt granulation (TSMG). TSMG is an emerging, high-productivity, continuous process. Granules of ibuprofen embedded in a lipid matrix were produced across a range of process conditions, resulting in a range of output granule particle sizes. The ibuprofen appeared to be miscible with the lipid binder though it recrystallized after processing. The ibuprofen melt granules were tested in simulated saliva using a novel, small-volume dissolution technique with continuous acquisition of the ibuprofen concentration. The ibuprofen release from the granules was slower than the neat API and physical blend, beyond the expected residence time of the granules in the mouth. The ibuprofen release was inversely related to the granule size. A Noyes–Whitney dissolution model was used and the resulting dissolution rate constants correlated well with the granule size.

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Effect of screw profile and processing conditions on physical transformation and chemical degradation of gabapentin during twin-screw melt granulation

Cited by 27 publications

References 26 publications

Selective Laser Sintering 3-Dimensional Printing as a Single Step Process to Prepare Amorphous Solid Dispersion Dosage Forms for Improved Solubility and Dissolution Rate

Selective Laser Sintering 3-Dimensional Printing as a Single Step Process to Prepare Amorphous Solid Dispersion Dosage Forms for Improved Solubility and Dissolution Rate

Twin-Screw Melt Granulation for Oral Solid Pharmaceutical Products

Continuous Melt Granulation for Taste-Masking of Ibuprofen

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