Application of mechanism-based modeling to predict drug quality during the pharmaceutical unit operations of granulation and compression: a review

seo, Park mi; Duhyung, Choi

doi:10.1007/s40005-020-00489-6

Cited by 8 publications

(4 citation statements)

References 97 publications

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“…If there is no uniform and continuous flow or if the granule sheet from the roller system is not in a complete ribbon shape due to insufficient pressure, numerous fines may be included through the milling process, causing capping, chipping, lining, and mass deviation in the tableting process. However, if an excessive pressure is applied to the input powder, the dissolution may be delayed due to over-compressed granules [ 19 ]. Therefore, it is important to find the optimum conditions in which the feeding speed is synchronized, and the appropriate pressure is applied.…”

Section: Resultsmentioning

confidence: 99%

Improved Manufacturability and In Vivo Comparative Pharmacokinetics of Dapagliflozin Cocrystals in Beagle Dogs and Human Volunteers

et al. 2021

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Dapagliflozin (DAP), which improves glycemic control in patients with type 2 diabetes mellitus, has poor physical properties against heat and moisture, thus hindering its manufacturing potential. The superior physicochemical properties of a recently developed cocrystal of DAP and citric acid (DAP cocrystal) in comparison with those of DAP and Forxiga®, a patented solvate form with propandiol monohydrate, were identified via structural analysis and moisture sorption isotherm. For the first time, the formulation, manufacturability, and in vivo bioavailability of DAP cocrystals were successfully investigated to develop oral dosage forms that substitute Forxiga®. The intrinsic dissolution rate of DAP cocrystal was controlled by varying particle size distribution. Unlike the direct compression (DC), roller compaction (RC) was more preferable to obtain good flowability of dry granules for a continuous manufacturing system. The cocrystal structure was maintained throughout the stability assessment period. In Vitro dissolution pattern differences of the optimized DAP cocrystal tablet with RC and the reference tablet, Forxiga® 10 mg, were pharmaceutically equivalent within 5% in four different media. Furthermore, comparative pharmacokinetic analysis confirmed that a 10 mg DAP cocrystal tablet with RC was bioequivalent to a 10 mg Forxiga® tablet, as assessed in beagle dogs and human volunteers.

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Section: Resultsmentioning

confidence: 99%

Improved Manufacturability and In Vivo Comparative Pharmacokinetics of Dapagliflozin Cocrystals in Beagle Dogs and Human Volunteers

et al. 2021

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“…Computational and mathematical models can be used to improve the mechanistic understanding of tablet coating processes and help to optimize the process [ 101 ]. Modeling approaches are useful to determine optimal process time, minimize the number of experiments, and reduce process failures, leading to lower development cost [ 102 ].…”

Section: Recent Technology and Tools Used To Characterize Coated Tmentioning

confidence: 99%

“…They can be used to examine the coating processes with the variation of operating conditions. These models require one or more parameters to be measured experimentally [ 100 , 101 , 102 , 103 ]. On the other hand, first-principle models are exemplified by computational fluid dynamics (CFD) and discrete element method (DEM) [ 100 , 103 ].…”

Section: Recent Technology and Tools Used To Characterize Coated Tmentioning

confidence: 99%

Pharmaceutical Application of Tablet Film Coating

et al. 2020

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Tablet film coating is a common but critical process providing various functionalities to tablets, thereby meeting diverse clinical needs and increasing the value of oral solid dosage forms. Tablet film coating is a technology-driven process and the evolution of coated dosage forms relies on advancements in coating technology, equipment, analytical techniques, and coating materials. Although multiple coating techniques are developed for solvent-based or solvent-free coating processes, each method has advantages and disadvantages that may require continuous technical refinement. In the film coating process, intra- and inter-batch coating uniformity of tablets is critical to ensure the quality of the final product, especially for active film coating containing active pharmaceutical ingredients in the coating layer. In addition to experimental evaluation, computational modeling is also actively pursued to predict the influence of operation parameters on the quality of the final product and optimize process variables of tablet film coating. The concerted efforts of experiments and computational modeling can save time and cost in optimizing the tablet coating process. This review provides a brief overview of tablet film coating technology and modeling approaches with a focus on recent advancements in pharmaceutical applications.

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“…Physics-based models include the discrete element model, computational fluid dynamics, the finite element method, and hybrid models [ 5 ]. Engineering principles-based models include the dimensionless number, thermodynamic model, and heat and mass transfer model [ 7 ].…”

Section: Introductionmentioning

confidence: 99%

Control Strategy for Process Development of High-Shear Wet Granulation and Roller Compaction to Prepare a Combination Drug Using Integrated Quality by Design

2021

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In this study, we developed a control strategy for a drug product prepared by high-shear wet granulation and roller compaction using integrated quality by design (QbD). During the first and second stages, we optimized the process parameters through the design of experiments and identified the intermediate quality attributes (IQAs) and critical quality attributes (CQAs) relationship, respectively. In the first stage, we conducted an initial risk assessment by selecting critical process parameters with high impact on IQAs and CQAs and confirmed the correlation between control and response factors. Additionally, we performed Monte Carlo simulations by optimizing the process parameters to deriving and building a robust design space. In the second stage, we identified the IQAs and CQAs relationship for the control strategy, using multivariate analysis (MVA). Based on MVA, in the metformin layer, dissolution at 1 h was significantly correlated with intrinsic dissolution rate and granule size, and dissolution at 3 h was significantly correlated with bulk density and granule size. In dapagliflozin layer, dissolution at 10 min and 15 min was significantly correlated with granule size. Our results suggest that the desired drug quality may result through IQAs monitoring during the process and that the integrated QbD approach utilizing MVA can be used to develop a control strategy for producing high-quality drug products.

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Application of mechanism-based modeling to predict drug quality during the pharmaceutical unit operations of granulation and compression: a review

Cited by 8 publications

References 97 publications

Improved Manufacturability and In Vivo Comparative Pharmacokinetics of Dapagliflozin Cocrystals in Beagle Dogs and Human Volunteers

Improved Manufacturability and In Vivo Comparative Pharmacokinetics of Dapagliflozin Cocrystals in Beagle Dogs and Human Volunteers

Pharmaceutical Application of Tablet Film Coating

Control Strategy for Process Development of High-Shear Wet Granulation and Roller Compaction to Prepare a Combination Drug Using Integrated Quality by Design

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