Novel approach for overcoming the stability challenges of lipid-based excipients. Part 1: Screening of solid-state and physical properties of polyglycerol esters of fatty acids as advanced pharmaceutical excipients

Corzo, Carolina; Lopes, Diogo Gomes; Lochmann, Dirk; Reyer, Sebastian; Stehr, Michael; Salar-Behzadi, Sharareh

doi:10.1016/j.ejpb.2020.01.012

Cited by 16 publications

(2 citation statements)

References 35 publications

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“…Therefore, CPE usually require additional lubricating aids. Compritol ® (glyceryl behenate) and Precirol ® (glyceryl palmitostearate) are well-known lipophilic glycerides with low HLB (hydrophilic-lipophilic balance) values that can be used as lubricants or matrix-forming agents in the conventional solid oral dosage forms [ 34 ] and are also suitable for several melting-based processing methods [ 35 ]. Melt-granulation has already been recognized as a suitable CP method for directly compressible CPEs [ 9 ].…”

Section: Introductionmentioning

confidence: 99%

Application of Machine-Learning Algorithms for Better Understanding of Tableting Properties of Lactose Co-Processed with Lipid Excipients

Djuriš

Cirin-Varadjan²,

Aleksić

et al. 2021

Pharmaceutics

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Co-processing (CP) provides superior properties to excipients and has become a reliable option to facilitated formulation and manufacturing of variety of solid dosage forms. Development of directly compressible formulations with high doses of poorly flowing/compressible active pharmaceutical ingredients, such as paracetamol, remains a great challenge for the pharmaceutical industry due to the lack of understanding of the interplay between the formulation properties, process of compaction, and stages of tablets’ detachment and ejection. The aim of this study was to analyze the influence of the compression load, excipients’ co-processing and the addition of paracetamol on the obtained tablets’ tensile strength and the specific parameters of the tableting process, such as (net) compression work, elastic recovery, detachment, and ejection work, as well as the ejection force. Two types of neural networks were used to analyze the data: classification (Kohonen network) and regression networks (multilayer perceptron and radial basis function), to build prediction models and identify the variables that are predominantly affecting the tableting process and the obtained tablets’ tensile strength. It has been demonstrated that sophisticated data-mining methods are necessary to interpret complex phenomena regarding the effect of co-processing on tableting properties of directly compressible excipients.

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Section: Introductionmentioning

confidence: 99%

Application of Machine-Learning Algorithms for Better Understanding of Tableting Properties of Lactose Co-Processed with Lipid Excipients

Djuriš

Cirin-Varadjan²,

Aleksić

et al. 2021

Pharmaceutics

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“…The challenge of lipid-based formulations is, however, their instability during storage [3]. During the last decades, a large body of investigations showed the correlation between the monotropic polymorphism of lipids and the instability of their pharmaceutical products [3][4][5][6][7][8][9][10]. Beyond this, the relationship between alteration in the microstructure level, including crystal growth and phase separation, and the unstable product performance was investigated in our group [3,6].…”

Section: Introductionmentioning

confidence: 99%

Impact of Surface Properties of Core Material on the Stability of Hot Melt-Coated Multiparticulate Systems

2021

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Hot melt coating (HMC) of an active pharmaceutical ingredient (API) powder with lipid-based excipients is an innovative method for manufacturing patient-convenient dosage forms. However, drug release instability is still its main industrial challenge. The correlation between the unstable pharmaceutical product performance with the solid-state alteration of lipids is currently well-investigated. The remaining problem is the inconsistent release alteration of different APIs coated with the same lipid after storage, such as faster release in some cases and slower release in others. The interaction between API surface and lipid-based coating and its alteration during storage were investigated in this work. The surface properties of five different APIs and the coating composition of tripalmitin and polysorbate 65 were screened via Washburn and pendant drop methods, respectively. Metformin hydrochloride and hydrochlorothiazide particles were each coated with the coating composition. The water sorption alteration of coated particles and the crystal growth of tripalmitin in the coating after storage were measured via tensiometry and X-ray diffraction. The cleavage work necessary to overcome the adhesion of coating composition on the core surface was calculated for each API. The accelerated release of the polar core (metformin) after storage was correlated with a low cleavage work and a distinctive phase separation. In contrast, a decelerated release of the hydrophobic core (hydrochlorothiazide) was favored by the crystal growth of the lipid-based coating. The gained knowledge can be used to design the product stability during the formulation development.

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Personalization of lipid-based oral dosage forms via filament-based 3D-printing

Abdelhamid,

Corzo,

Afonso Urich

et al. 2024

Applied Materials Today

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Novel approach for overcoming the stability challenges of lipid-based excipients. Part 1: Screening of solid-state and physical properties of polyglycerol esters of fatty acids as advanced pharmaceutical excipients

Cited by 16 publications

References 35 publications

Application of Machine-Learning Algorithms for Better Understanding of Tableting Properties of Lactose Co-Processed with Lipid Excipients

Application of Machine-Learning Algorithms for Better Understanding of Tableting Properties of Lactose Co-Processed with Lipid Excipients

Impact of Surface Properties of Core Material on the Stability of Hot Melt-Coated Multiparticulate Systems

Personalization of lipid-based oral dosage forms via filament-based 3D-printing

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