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4 pages, 193 KiB

Open AccessEditorial

Special Issue on “Particulate Processes in the Formulation of Pharmaceuticals, Nutraceuticals and Bioactive Compounds”

by Ioannis Nikolakakis

Processes 2023, 11(2), 308; https://doi.org/10.3390/pr11020308 - 17 Jan 2023

Viewed by 1284

Abstract

Introduction [...] Full article

(This article belongs to the Special Issue Particulate Processes in the Formulation of Pharmaceuticals, Nutraceuticals and Bioactive Compounds)

Research

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15 pages, 4994 KiB

Open AccessFeature PaperEditor’s ChoiceArticle

A Continuous Conical-Mill Operation for Dry Coating of Pharmaceutical Powders: The Role of Processing Time

by William Roy, Inès Esma Achouri, Sophie Hudon, Jean-Sébastien Simard and Nicolas Abatzoglou

Processes 2022, 10(3), 540; https://doi.org/10.3390/pr10030540 - 9 Mar 2022

Cited by 3 | Viewed by 2618

Abstract

Over the last decade, the conical mill has emerged as a potential piece of equipment to use for continuous dry coating pharmaceutical powders. In this work, silicon dioxide was used as a guest particle on two excipients, fast flow lactose (FFL) and grade [...] Read more.

Over the last decade, the conical mill has emerged as a potential piece of equipment to use for continuous dry coating pharmaceutical powders. In this work, silicon dioxide was used as a guest particle on two excipients, fast flow lactose (FFL) and grade PH200 microcrystalline cellulose (MCC), for dry coating by a conical mill with a modified screen that permitted batch and continuous mode operation. Samples were pre-processed in a V-blender. SEM images, particle size distribution, and EDS mapping were used to characterise the treated powders. Pre-processed samples showed some discrete coating of the host particle. After batch processing, the samples were covered with a complete coating. When processed at high impeller speed, coating of FFL was a mix of A200P and FFL fines generated by attrition. Continuous mode processed samples, which had a lower processing time, were coated discretely and showed a better coating than the pre-processed samples. Increasing guest/host mass ratio with FFL host particle had a positive impact on the quality of the coating. These results help to build the case that the processing time of the conical mill is a key parameter to the success of the conical mill as dry coating equipment in the pharmaceutical industry. Full article

(This article belongs to the Special Issue Particulate Processes in the Formulation of Pharmaceuticals, Nutraceuticals and Bioactive Compounds)

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25 pages, 6699 KiB

Open AccessFeature PaperArticle

Moisture Transport Coefficients Determination on a Model Pharmaceutical Tablet

by Komlan Koumbogle, François Gitzhofer and Nicolas Abatzoglou

Processes 2022, 10(2), 254; https://doi.org/10.3390/pr10020254 - 27 Jan 2022

Cited by 5 | Viewed by 3301

Abstract

In this work, a novel methodology to determine moisture transport coefficients for MMC PH101 tablets is presented. Absolute permeability, moisture diffusion, moisture transfer, and water vapor permeability coefficients were estimated on compressed powder tablets produced with different compression pressures (20 MPa to 200 [...] Read more.

In this work, a novel methodology to determine moisture transport coefficients for MMC PH101 tablets is presented. Absolute permeability, moisture diffusion, moisture transfer, and water vapor permeability coefficients were estimated on compressed powder tablets produced with different compression pressures (20 MPa to 200 MPa with an interval of 20 MPa). The ASTM D6539 standard test was used to measure the absolute permeability. The moisture transfer coefficient was determined from measured absolute permeability. The moisture diffusion coefficient was obtained with the tablet average pore radius, which was determined with the water droplet penetration method. Descriptive and phenomenological models derived from the measurements were confronted with existing and adopted models, and a good agreement was found. The obtained models are of the function of the microstructural properties of the tablet (average pore radius and average porosity). The tablet average porosity was found to be the principal parameter that governs the behavior of the moisture transport coefficients. The findings of this study might be applicable to obtain a series of input parameters for modelling software, such as COMSOL Multiphysics^®, to infer delamination, sticking, and failure propensity from the effect of moisture. Full article

(This article belongs to the Special Issue Particulate Processes in the Formulation of Pharmaceuticals, Nutraceuticals and Bioactive Compounds)

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15 pages, 4862 KiB

Open AccessArticle

Cumulative Production of Bioactive Rg3, Rg5, Rk1, and CK from Fermented Black Ginseng Using Novel Aspergillus niger KHNT-1 Strain Isolated from Korean Traditional Food

by Jin Kyu Park, Dong Uk Yang, Lakshminarayanan Arunkumar, Yaxi Han, Seung Jin Lee, Muhammad Huzaifa Arif, Jin Feng Li, Yue Huo, Jong Pyo Kang, Van An Hoang, Jong Chan Ahn, Deok Chun Yang and Se Chan Kang

Processes 2021, 9(2), 227; https://doi.org/10.3390/pr9020227 - 26 Jan 2021

Cited by 10 | Viewed by 3824

Abstract

Ginseng is an ancient herb widely consumed due to its healing property of active ginsenosides. Recent researchers were explored to increase its absorption and bioavailability of ginsenosides at the metabolic sites, due to its pharmacological activity. The purpose of this study was to [...] Read more.

Ginseng is an ancient herb widely consumed due to its healing property of active ginsenosides. Recent researchers were explored to increase its absorption and bioavailability of ginsenosides at the metabolic sites, due to its pharmacological activity. The purpose of this study was to investigate the isolation and characteristics of components obtained by a shorter steaming cycle (seven cycles) of white ginseng to fermented black ginseng, using a novel strain of Aspergillus niger KHNT-1 isolated from fermented soybean. The degree of bioactive of Rg3 increased effectively during the steaming process, and biotransformation converted the color towards black along active ginsenosides. Glycol moiety associated with C-3, C-6, or C-20 underwent rapid biotransformation and hydrolysis, such as Rb1, Rb2, Rc, Rd → Rg3, F2, and was converted to CK. Dehydration produces Rg3 → Rk1, Rg5. Rh2 → Rk2; thus, converted fermented black ginseng was solvent-extracted, and the isolated components were identified by TLC, HPLC, and quantification by LCMS. The unique composition obtained during this process with Rk1, Rg3, Rg5, and CK is nontoxic to HaCaT cell line up to 200 ug/mL for 24 h and was found to be effective in B16BL6 cell lines, in a dose- and time-dependent manner. Thus, it is a suitable candidate for nutraceuticals and cosmeceuticals. Full article

(This article belongs to the Special Issue Particulate Processes in the Formulation of Pharmaceuticals, Nutraceuticals and Bioactive Compounds)

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16 pages, 3907 KiB

Open AccessFeature PaperArticle

Fabrication of Biopolymer Based Nanoparticles for the Entrapment of Chromium and Iron Supplements

by Nishay Patel, Mohammed Gulrez Zariwala and Hisham Al-Obaidi

Processes 2020, 8(6), 707; https://doi.org/10.3390/pr8060707 - 19 Jun 2020

Cited by 3 | Viewed by 3792

Abstract

The objective of this study was to encapsulate iron and chromium into novel nanoparticles formulated using chitosan (CS), dextran sulfate (DS) and whey protein isolate (WPI) for oral drug delivery. Empty and loaded CS-DS nanoparticles were prepared via complex coacervation whilst whey protein [...] Read more.

The objective of this study was to encapsulate iron and chromium into novel nanoparticles formulated using chitosan (CS), dextran sulfate (DS) and whey protein isolate (WPI) for oral drug delivery. Empty and loaded CS-DS nanoparticles were prepared via complex coacervation whilst whey protein nanocarriers were produced by a modified thermal processing method using chitosan. The physiochemical properties of the particles were characterized to determine the effects of formulation variables, including biopolymer ratio on particle size and zeta potential. Permeability studies were also undertaken on the most stable whey protein–iron nanoparticles by measuring Caco-2 ferritin formation. A particle size analysis revealed that the majority of samples were sub-micron sized, ranging from 420–2400 nm for CS-DS particles and 220–1000 nm for WPI-CS samples. As expected, a higher chitosan concentration conferred a 17% more positive zeta potential on chromium-entrapped WPI nanoparticles, whilst a higher dextran volume decreased the size of CS-DS nanoparticles by 32%. The addition of iron also caused a significant increase in size for all samples, as seen where the loaded WPI samples were 296 nm larger than the empty particles. Caco-2 iron absorption revealed that one formulation, which had the lowest particle size (226 ± 10 nm), caused a 64% greater iron absorption compared to the ferrous sulfate standard. This study describes, for the first time, the novel design of chromium- and iron-entrapped nanoparticles, which could act as novel systems for oral drug delivery. Full article

(This article belongs to the Special Issue Particulate Processes in the Formulation of Pharmaceuticals, Nutraceuticals and Bioactive Compounds)

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26 pages, 5715 KiB

Open AccessArticle

DEM Investigation of the Influence of Particulate Properties and Operating Conditions on the Mixing Process in Rotary Drums: Part 1—Determination of the DEM Parameters and Calibration Process

by Jakub Hlosta, Lucie Jezerská, Jiří Rozbroj, David Žurovec, Jan Nečas and Jiří Zegzulka

Processes 2020, 8(2), 222; https://doi.org/10.3390/pr8020222 - 14 Feb 2020

Cited by 58 | Viewed by 8814

Abstract

This paper’s goal was to select methods and a calibration procedure which would lead to the determination of relevant parameters of a discrete element method (DEM) and virtual material creation. Seven particulates were selected with respect to their shape (spherical and non-spherical), size [...] Read more.

This paper’s goal was to select methods and a calibration procedure which would lead to the determination of relevant parameters of a discrete element method (DEM) and virtual material creation. Seven particulates were selected with respect to their shape (spherical and non-spherical), size and density. The first calibration experiment involved “packing test” to determine the shape accuracy and bulk density of virtual packed particulates. The series of simulations were compared with real experiments, and the size, shape and density of virtual particles were optimized. Using three apparatuses, the input parameter values were experimentally determined for a contact model that defines the behavior of particulates in DEM simulations. The research part of the paper examines the influence of factors such as particle number; pile formation method; and the method of evaluation of the angle of repose on the process of the calibration of virtual material. The most reproducible results were achieved by the “pilling” method and by the rotating drum—both evaluated by the geometric method. However, it is always advisable to make an overall visual comparison of the slope shape between the calibration simulation and the experimental curves. The bowl’s diameter to particle size ratio should be greater than 25, and the calibration experiment should contain approximately 4000 particles to ensure representative results during angle of repose calibration experiment. Full article

(This article belongs to the Special Issue Particulate Processes in the Formulation of Pharmaceuticals, Nutraceuticals and Bioactive Compounds)

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18 pages, 8170 KiB

Open AccessArticle

DEM Investigation of the Influence of Particulate Properties and Operating Conditions on the Mixing Process in Rotary Drums: Part 2—Process Validation and Experimental Study

by Jakub Hlosta, Lucie Jezerská, Jiří Rozbroj, David Žurovec, Jan Nečas and Jiří Zegzulka

Processes 2020, 8(2), 184; https://doi.org/10.3390/pr8020184 - 5 Feb 2020

Cited by 33 | Viewed by 6756

Abstract

The process of homogenization of particulates is an indispensable part of many industrial processes, and, therefore, it is necessary to pay a special attention to this area and develop it. This paper deals with a complex study of homogenization of particulate matters in [...] Read more.

The process of homogenization of particulates is an indispensable part of many industrial processes, and, therefore, it is necessary to pay a special attention to this area and develop it. This paper deals with a complex study of homogenization of particulate matters in a rotary drum in terms of shape, size, and density of particles. In addition, the influence of operating parameters, such as drum filling capacity, rotational speed, and drum filling pattern are also investigated. Studies of reproducibility of discrete element method simulations, effects of rotary drum sizes or effects of drum volumetric filling to the mixture homogeneity index were also carried out. In general, the least satisfactory values of the homogeneity index resulted from the mixing of particles with different densities. The dominating factor of homogenization was the drum filling-up degree. The course of the homogeneity index in 140, 280, and 420 mm drums was very similar and after five revolutions of the drum, identical values of the homogeneity index were achieved for all the drum diameters. The optimal drum filling-up degree is at 40–50% for the spherical particles and 30–40% for the sharp-edged particles. The repeatability of simulations showed the maximum relative standard deviation of the homogeneity index at 0.6% from ten simulation repetitions with the same parametric conditions. Full article

(This article belongs to the Special Issue Particulate Processes in the Formulation of Pharmaceuticals, Nutraceuticals and Bioactive Compounds)

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13 pages, 2748 KiB

Open AccessArticle

Taste Masking of Nizatidine Using Ion-Exchange Resins

by Pattaraporn Panraksa, Kasidech Boonsermsukcharoen, Kyu-Mok Hwang, Eun-Seok Park and Pensak Jantrawut

Processes 2019, 7(11), 779; https://doi.org/10.3390/pr7110779 - 30 Oct 2019

Cited by 12 | Viewed by 5240

Abstract

The purpose of this study was to mask the bitter taste of nizatidine (NZD) using cation-exchange resins. Amberlite IRP-69 and Dowex-50 containing cross-linked polystyrene backbones were used. The drug resin complexes were prepared by batch process using drug: resin ratios of 1:1, 1:3, [...] Read more.

The purpose of this study was to mask the bitter taste of nizatidine (NZD) using cation-exchange resins. Amberlite IRP-69 and Dowex-50 containing cross-linked polystyrene backbones were used. The drug resin complexes were prepared by batch process using drug: resin ratios of 1:1, 1:3, and 1:5. The optimum drug: resin ratio and the time required for maximum percentage drug loading into the complexes were determined. The selected drug-resin complexes were evaluated for morphology, drug release, and taste. The NZD-Dowex complex was obtained at a drug: resin ratio of 1:5 using a stirring time of 1 h in order to get 100% loading of NZD. The NZD-Dowex complex had a spherical shape and smooth texture similar to Dowex resin. The NZD-Dowex complex with a ratio of 1:5 showed that in vitro drug release of 4.27% at 5 min in simulated salivary fluid of pH 6.8 and 99.67% at 1 h in simulated gastric fluid of pH 1.2. NZD’s bitter taste was effectively masked when it formed a complex with Dowex at a ratio of 1:5. This was proved by an electronic tongue and human test panel. Full article

(This article belongs to the Special Issue Particulate Processes in the Formulation of Pharmaceuticals, Nutraceuticals and Bioactive Compounds)

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