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1.
Food Res Int ; 191: 114713, 2024 Sep.
Article in English | MEDLINE | ID: mdl-39059913

ABSTRACT

This study aimed to explore the effects of various lipids on the structure, cooking quality, and in vitro starch digestibility of extruded buckwheat noodles (EBNs) with and without 20% high-amylose corn starch (HACS). Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction revealed that lauric acid bound more strongly to starch than did stearic acid and oleic acid, and the binding capacity of fatty acids with starch was stronger than that of glycerides. The presence of HACS during extrusion facilitated increased formation of starch-lipid complexes. Evaluations of cooking quality and digestion characteristics showed that EBNs containing 20% HACS and 0.5% glycerol monooleate demonstrated the lowest cooking loss (7.28%), and that with 20% HACS and 0.5% oleic acid displayed the lowest predicted glycemic index (pGI) (63.54) and highest resistant starch (RS) content (51.64%). However, excessive starch-lipid complexes were detrimental to EBNs cooking quality and the resistance of starch to digestive enzymes because of the damage to the continuity of the starch gel network. This study establishes a fundamental basis for the development of EBNs with superior cooking quality and a relatively lower GI.


Subject(s)
Cooking , Digestion , Fagopyrum , Fatty Acids , Starch , Fagopyrum/chemistry , Fatty Acids/chemistry , Starch/chemistry , Glycerides/chemistry , Glycemic Index , Spectroscopy, Fourier Transform Infrared , Amylose/chemistry , X-Ray Diffraction , Calorimetry, Differential Scanning , Stearic Acids/chemistry , Oleic Acid/chemistry , Lauric Acids/chemistry
2.
Carbohydr Polym ; 342: 122400, 2024 Oct 15.
Article in English | MEDLINE | ID: mdl-39048199

ABSTRACT

Previous RS5 (type 5 resistant starch) research has significantly broadened starch use and benefited society, yet the effects of the molecular weight of amylose on RS5 remain underexplored. In this study, amyloses with different molecular weights were complexed with caproic acid (C6), lauric acid (C12), and stearic acid (C18) to observe the effects of the molecular weight of amylose on the structure and in vitro digestive properties of RS5. Gel permeation chromatography revealed that the peak average molecular weight (Mp) values of high-amylose cornstarch NF-CGK (CGK), high-amylose cornstarch obtained via cornstarch via autoclave (high temperature and high pressure)-cooling combined pullulanase enzymatic hydrolysis (CTE), and high-amylose cornstarch NF-G370 (HCK) were 21,282, 171,537, and 188,084 before fatty acid complexation, respectively. Additionally, their weight average molecular weight (Mw) values of 32,429, 327,344, and 410,610 and hydrolysis rates of 58.12 %, 86.77 %, and 64.58 %, respectively. The hydrolysis rate of low-Mw amylose (GCK) complexes with fatty acids was lower than that of HCK and CTE starch-lipid complexes. However, HCK and CTE having similar molecular weights, there was no significant difference in the hydrolysis rate of starch-lipid complexes. X-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy and complexing index analyses confirmed the formation of these complexes. This study proposed the mechanism of RS5 formation and provided guidance for its future development.


Subject(s)
Amylose , Lauric Acids , Molecular Weight , Amylose/chemistry , Lauric Acids/chemistry , Hydrolysis , Starch/chemistry , Starch/metabolism , Digestion , Stearic Acids/chemistry , Lipids/chemistry , Caprylates
3.
Chem Pharm Bull (Tokyo) ; 72(6): 584-595, 2024.
Article in English | MEDLINE | ID: mdl-38945947

ABSTRACT

In order to introduce a cost-effective strategy method for commercial scale dry granulation at the early clinical stage of drug product development, we developed dry granulation process using formulation without API, fitted and optimized the process parameters adopted Design of Experiment (DOE). Then, the process parameters were confirmed using one formulation containing active pharmaceutical ingredient (API). The results showed that the roller pressure had significant effect on particle ratio (retained up to #60 mesh screen), bulk density and tapped density. The roller gap had significant influence on particle ratio and specific energy. The particle ratio was significantly affected by the mill speed (second level). The tabletability of the powder decreased after dry granulation. The effect of magnesium stearate on the tabletability was significant. In the process validation study, the properties of the prepared granules met the requirements for each response studied in the DOE. The prepared tablets showed higher tensile strength, good content uniformity of filled capsules, and the dissolution profiles of which were consistent with that of clinical products. This drug product process development and research strategies could be used as a preliminary experiment for the dry granulation process in the early clinical stage.


Subject(s)
Tablets , Tablets/chemistry , Particle Size , Drug Compounding , Powders/chemistry , Stearic Acids/chemistry , Tensile Strength , Excipients/chemistry , Solubility
4.
Int J Pharm ; 660: 124370, 2024 Jul 20.
Article in English | MEDLINE | ID: mdl-38906498

ABSTRACT

Limited attempts have been made previously to develop high-loading CBD inhalable powders, which are essential for high dose delivery. Therefore, this study aimed to develop and characterise inhalable powders with ≥ 95 % w/w CBD by wet ball milling. The effects of magnesium stearate (2 % and 5 %) and inhaler resistance (low-resistance and high-resistance RS01 inhalers) on aerosol performance were also compared. Wet ball milling produced CBD powders with > 50 % production yield. The milled particles showed irregular shapes. The powders were crystalline with minimal amorphous content, low residual solvent level (<1%), and low moisture sorption (<4%). Magnesium stearate improved both the emitted and fine particle fractions. The aerodynamic particle size distribution of the formulations differed between the low-resistance and high-resistance RS01 inhalers. The latter decreased throat deposition but increased inhaler retention. The dissolution profiles showed that all three formulations released CBD steadily and plateaued at 30 min. The best scenario was CBD with 5 % magnesium stearate dispersed from the high resistance RS01 inhaler, showing the highest FPF with the lowest throat deposition. This combination may be tested in vivo in the future to investigate its pharmacokinetic profile.


Subject(s)
Cannabidiol , Particle Size , Powders , Stearic Acids , Administration, Inhalation , Stearic Acids/chemistry , Cannabidiol/administration & dosage , Cannabidiol/chemistry , Cannabidiol/pharmacokinetics , Aerosols , Dry Powder Inhalers , Excipients/chemistry , Chemistry, Pharmaceutical/methods , Drug Liberation , Nebulizers and Vaporizers , Drug Compounding/methods , Solubility
5.
Int J Pharm ; 660: 124315, 2024 Jul 20.
Article in English | MEDLINE | ID: mdl-38852747

ABSTRACT

The compendial USP〈701〉 disintegration test method offers a crucial pass/fail assessment for immediate release tablet disintegration. However, its single end-point approach provides limited insight into underlying mechanisms. This study introduces a novel calorimetric approach, aimed at providing comprehensive process profiles beyond binary outcomes. We developed a novel disintegration reaction calorimeter to monitor the heat release throughout the disintegration process and successfully obtained enthalpy change profiles of placebo tablets with various porosities. The formulation comprised microcrystalline cellulose (MCC), anhydrous lactose, croscarmellose sodium (CCS), and magnesium stearate (MgSt). An abrupt temperature rise was observed after introducing the disintegration medium to tablets, and the relationship between the heat rise time and the tablet's porosity was investigated. The calorimeter's sensitivity was sufficient to discern distinct heat changes among individual tablets, and the analysis revealed a direct correlation between the two. Higher porosity corresponded to shorter heat rise time, indicating faster disintegration rates. Additionally, the analysis identified a concurrent endothermic process alongside the anticipated exothermic phenomenon, potentially associated with the dissolution of anhydrous lactose. Since lactose is the only soluble excipient within the blend composition, the endothermic process can be attributed to the absorption of heat as lactose molecules dissolve in water. The findings from this study underscore the potential of utilising calorimetric methods to quantify the wettability of complex compounds and, ultimately, optimise tablet formulations.


Subject(s)
Calorimetry , Cellulose , Excipients , Hot Temperature , Lactose , Stearic Acids , Tablets , Lactose/chemistry , Cellulose/chemistry , Excipients/chemistry , Porosity , Stearic Acids/chemistry , Calorimetry/methods , Solubility , Carboxymethylcellulose Sodium/chemistry , Chemistry, Pharmaceutical/methods , Drug Liberation , Drug Compounding/methods
6.
AAPS PharmSciTech ; 25(5): 113, 2024 May 15.
Article in English | MEDLINE | ID: mdl-38750336

ABSTRACT

Transport of oral nanocarriers across the GI epithelium necessitates transport across hydrophilic mucus layer and the hydrophobic epithelium. Based on hydrophobic-hydrophilic balance, Curcumin-Lipomer (lipid-polymer hybrid nanoparticles) comprising hydrophobic stearic acid and hydrophilic Gantrez™ AN 119 (Gantrez) were developed, by a radical in-situ approach, to successfully traverse both barriers. A monophasic preconcentrate (Cur-Pre) comprising Cur (Curcumin), stearic acid, Gantrez and stabilizers, prepared by simple solution, was added to an aqueous phase to instantaneously generate Curcumin-Lipomer (Cur-Lipo) of nanosize and high entrapment efficiency (EE). Cur-Lipo size and EE was optimized by Box-Behnken Design. Cur-Lipomers of varying hydrophobic-hydrophilic property obtained by varying the stearic acid: Gantrez ratio exhibited size in the range 200-400 nm, EE > 95% and spherical morphology as seen in the TEM. A decrease in contact angle and in mucus interaction, evident with increase in Gantrez concentration, indicated an inverse corelation with hydrophilicity, while a linear corelation was observed for mucopenetration and hydrophilicity. Cur-SLN (solid lipid nanoparticles) which served as the hydrophobic reference revealed contact angle > 90°, maximum interaction with mucus and minimal mucopenetration. The ex-vivo permeation study through chicken ileum, revealed maximum permeation with Cur-Lipo1 and comparable and significantly lower permeation of Cur-Lipo1-D and Cur-SLN proposing the importance of balancing the hydrophobic-hydrophilic property of the nanoparticles. A 1.78-fold enhancement in flux of hydrophobic Cur-SLN, with no significant change in permeation of the hydrophilic Cur-Lipomers (p > 0.05) following stripping off the mucosal layer was observed. This reiterated the significance of hydrophobic-hydrophilic balance as a promising strategy to design nanoformulations with superior permeation across the GI barrier.


Subject(s)
Curcumin , Drug Carriers , Hydrophobic and Hydrophilic Interactions , Intestinal Mucosa , Nanoparticles , Stearic Acids , Nanoparticles/chemistry , Administration, Oral , Animals , Stearic Acids/chemistry , Curcumin/administration & dosage , Curcumin/pharmacokinetics , Curcumin/chemistry , Intestinal Mucosa/metabolism , Drug Carriers/chemistry , Particle Size , Lipids/chemistry , Polymers/chemistry , Biological Transport/physiology , Polyvinyls/chemistry
7.
Int J Pharm ; 657: 124190, 2024 May 25.
Article in English | MEDLINE | ID: mdl-38701910

ABSTRACT

Lubricants are essential for most tablet formulations as they assist powder flow, prevent adhesion to tableting tools and facilitate tablet ejection. Magnesium stearate (MgSt) is an effective lubricant but may compromise tablet strength and disintegratability. In the design of orodispersible tablets, tablet strength and disintegratability are critical attributes of the dosage form. Hence, this study aimed to conduct an in-depth comparative study of MgSt with alternative lubricants, namely sodium lauryl sulphate (SLS), stearic acid (SA) and hydrogenated castor oil (HCO), for their effects on the tableting process as well as tablet properties. Powder blends were prepared with lactose, sodium starch glycolate or crospovidone as the disintegrant, and a lubricant at different concentrations. Angle of repose was determined for the mixtures. Comparative evaluation was carried out based on the ejection force, tensile strength, liquid penetration and disintegratability of the tablets produced. As the lubricant concentration increased, powder flow and tablet ejection improved. The lubrication efficiency generally decreased as follows: MgSt > HCO > SA > SLS. Despite its superior lubrication efficacy, MgSt is the only lubricant of four evaluated that reduced tablet tensile strength. Tablet disintegration time was strongly determined by tensile strength and liquid penetration, which were in turn affected by the lubricant type and concentration. All the above factors should be taken into consideration when deciding the type and concentration of lubricant for an orodispersible tablet formulation.


Subject(s)
Excipients , Lubricants , Stearic Acids , Tablets , Tensile Strength , Lubricants/chemistry , Stearic Acids/chemistry , Excipients/chemistry , Drug Compounding/methods , Powders/chemistry , Sodium Dodecyl Sulfate/chemistry , Castor Oil/chemistry , Povidone/chemistry , Starch/chemistry , Starch/analogs & derivatives , Lactose/chemistry , Administration, Oral , Solubility , Chemistry, Pharmaceutical/methods
8.
Food Res Int ; 186: 114355, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38729701

ABSTRACT

In this study, five C18 fatty acids (FA) with different numbers of double bonds and configurations including stearic acid (SA), oleic acid (OA), elaidic acid (EA), linoleic acid (LA), and α-linolenic acid (ALA), were selected to prepare highland barely starch (HBS)-FA complexes to modulate digestibility and elaborate the underlying mechanism. The results showed that HBS-SA had the highest complex index (34.18 %), relative crystallinity (17.62 %) and single helix content (25.78 %). Furthermore, the HBS-C18 FA complexes were formed by EA (C18 FA with monounsaturated bonds) that had the highest R1047/1022 (1.0509) and lowest full width at half-maximum (FWHM, 20.85), suggesting good short-range ordered structure. Moreover, all C18 FAs could form two kinds of V-type complexes with HBS, which can be confirmed by the results of CLSM and DSC measurements, and all of them showed significantly lower digestibility. HBS-EA possessed the highest resistant starch content (20.17 %), while HBS-SA had the highest slowly digestible starch content (26.61 %). In addition, the inhibition of HBS retrogradation by fatty acid addition was further proven, where HBS-SA gel firmness (37.80 g) and aging enthalpy value were the lowest, indicating the most effective. Overall, compounding with fatty acids, especially SA, could be used as a novel way to make functional foods based on HBS.


Subject(s)
Digestion , Fatty Acids , Hordeum , Oleic Acid , Starch , Starch/chemistry , Fatty Acids/analysis , Fatty Acids/chemistry , Hordeum/chemistry , Oleic Acid/chemistry , Stearic Acids/chemistry , Linoleic Acid/chemistry , alpha-Linolenic Acid/chemistry , Oleic Acids
9.
J Mater Chem B ; 12(23): 5661-5677, 2024 Jun 12.
Article in English | MEDLINE | ID: mdl-38747312

ABSTRACT

Magnesium alloy is currently regarded as the most favourable biodegradable metal; however, obstacles remain to be overcome in terms of managing its corrosion and ensuring its biocompatibility. In this study, a metal-organic complex comprising Ca ions incorporated in tannic acid (TA) was prepared and used to coat magnesium alloy by chemical conversion and dipping processes, followed by modification with stearic acid (SA). This metal-organic complex coating was demonstrated to be homogeneous and compact, and it significantly improved the electrochemical corrosion resistance and long-term degradation behaviour of the coated samples. Consequently, the well-controlled release of Mg and Ca ions, as well as the osteo-compatible TA and SA molecules, promoted the proliferation of osteoblast cells. This metal-organic complex coating offers a promising modifying strategy for magnesium-based orthopaedic implants.


Subject(s)
Alloys , Coated Materials, Biocompatible , Magnesium , Magnesium/chemistry , Alloys/chemistry , Alloys/pharmacology , Corrosion , Coated Materials, Biocompatible/chemistry , Coated Materials, Biocompatible/pharmacology , Materials Testing , Tannins/chemistry , Tannins/pharmacology , Cell Proliferation/drug effects , Surface Properties , Osteoblasts/drug effects , Osteoblasts/cytology , Absorbable Implants , Humans , Stearic Acids/chemistry , Animals , Calcium/chemistry , Calcium/metabolism , Cell Line
10.
Spectrochim Acta A Mol Biomol Spectrosc ; 318: 124517, 2024 Oct 05.
Article in English | MEDLINE | ID: mdl-38801790

ABSTRACT

The effects of common migration substances in milk packaging on digestive protease were studied. We choose the common migrants found in eight types of multi-layer composite milk packaging. Enzyme activity experiments revealed that pepsin activity decreased by approximately 18 % at 500 µg/mL of stearic acid and stearamide treatment, while trypsin activity decreased by approximately 18 % only by stearic acid treatment (500 µg/mL). Subsequently, fluorescence spectroscopy, circular dichroism spectroscopy, and molecular docking technology were employed to investigate the inhibition mechanism of protease activity by migrating substances in three systems: stearic acid-trypsin, stearic acid-pepsin, and stearamide-pepsin. Results showed that the inhibitory effect of stearic acid on trypsin is a reversible mixed inhibition, whereas the inhibitory effects of stearic acid and stearamide on pepsin are non-competitive. In all three systems, ΔH < 0, ΔS < 0, and ΔG < 0, indicating the binding process between the migrant and the protease is a spontaneous exothermic process primarily driven by hydrogen bonding and van der Waals forces. In addition, their binding constants are all around 104 L/moL, indicating that there are moderate binding affinities exist between migrants and proteases. The binding process results in the quenching of the protease's endogenous fluorescence and induces alterations in the enzyme's secondary structure. Synchronized fluorescence spectroscopy showed that stearic acid enhanced the hydrophobicity near the Tyr residue of trypsin. The molecular docking results indicated that the binding affinity of stearic acid-trypsin, stearic acid-pepsin, and stearamide-pepsin was -22.51 kJ/mol, -12.35 kJ/mol, -19.28 kJ/mol respectively, which consistent with the trend in the enzyme activity results. This study can provide references for the selection of milk packaging materials and the use of processing additives, ensuring food health and safety.


Subject(s)
Food Packaging , Milk , Molecular Docking Simulation , Spectrometry, Fluorescence , Trypsin , Animals , Milk/chemistry , Trypsin/metabolism , Trypsin/chemistry , Stearic Acids/chemistry , Stearic Acids/metabolism , Pepsin A/metabolism , Pepsin A/chemistry , Circular Dichroism , Peptide Hydrolases/metabolism , Peptide Hydrolases/chemistry , Thermodynamics
11.
ACS Nano ; 18(18): 11813-11827, 2024 May 07.
Article in English | MEDLINE | ID: mdl-38657165

ABSTRACT

Nanoenabled strategies have recently attracted attention as a sustainable platform for agricultural applications. Here, we present a mechanistic understanding of nanobiointeraction through an orthogonal investigation. Pristine (nS) and stearic acid surface-modified (cS) sulfur nanoparticles (NPs) as a multifunctional nanofertilizer were applied to tomato (Solanum lycopersicumL.) through soil. Both nS and cS increased root mass by 73% and 81% and increased shoot weight by 35% and 50%, respectively, compared to the untreated controls. Bulk sulfur (bS) and ionic sulfate (iS) had no such stimulatory effect. Notably, surface modification of S NPs had a positive impact, as cS yielded 38% and 51% greater shoot weight compared to nS at 100 and 200 mg/L, respectively. Moreover, nS and cS significantly improved leaf photosynthesis by promoting the linear electron flow, quantum yield of photosystem II, and relative chlorophyll content. The time-dependent gene expression related to two S bioassimilation and signaling pathways showed a specific role of NP surface physicochemical properties. Additionally, a time-dependent Global Test and machine learning strategy applied to understand the NP surface modification domain metabolomic profiling showed that cS increased the contents of IA, tryptophan, tomatidine, and scopoletin in plant leaves compared to the other treatments. These findings provide critical mechanistic insights into the use of nanoscale sulfur as a multifunctional soil amendment to enhance plant performance as part of nanoenabled agriculture.


Subject(s)
Nanoparticles , Solanum lycopersicum , Sulfur , Solanum lycopersicum/metabolism , Solanum lycopersicum/drug effects , Sulfur/metabolism , Sulfur/chemistry , Nanoparticles/chemistry , Nanoparticles/metabolism , Photosynthesis , Surface Properties , Time Factors , Fertilizers , Stearic Acids/metabolism , Stearic Acids/chemistry , Plant Leaves/metabolism
12.
Recent Adv Drug Deliv Formul ; 18(1): 61-76, 2024.
Article in English | MEDLINE | ID: mdl-38362679

ABSTRACT

PURPOSE: The primary objective of this study was to optimize formulation variables and investigate the in vitro characteristics of fluticasone propionate (FP)-loaded mixed polymeric micelles, which were composed of depolymerized chitosan-stearic acid copolymer (DC-SA) in combination with either tocopheryl polyethylene glycol succinate or dipalmitoylphosphatidylcholine for pulmonary drug delivery. METHODS: A D-optimal design was employed for the optimization procedure, considering lipid/ polymer ratio, polymer concentration, drug/ polymer ratio, and lipid type as independent variables. Dependent variables included particle size, polydispersion index, zeta potential, drug encapsulation efficiency, and loading efficiency of the polymeric micelles. Additionally, the nebulization efficacy and cell viability of the optimal FP-loaded DC-SA micellar formulations were evaluated. RESULTS: The mixed polymeric micelles were successfully prepared with properties falling within the desired ranges, resulting in four optimized formulations. The release of FP from the optimal systems exhibited a sustained release profile over 72 hours, with 70% of the drug still retained within the core of the micelles. The nebulization efficiency of these optimal formulations reached up to 63%, and the fine particle fraction (FPF) ranged from 41% to 48%. Cellular viability assays demonstrated that FP-loaded DC-SA polymeric micelles exhibited lower cytotoxicity than the free drug but were slightly more cytotoxic than empty mixed micelles. CONCLUSION: In conclusion, this study suggests that DC-SA/ lipid mixed micelles have the potential to serve as effective carriers for nebulizing poorly soluble FP.


Subject(s)
Cell Survival , Chitosan , Fluticasone , Micelles , Stearic Acids , Chitosan/chemistry , Stearic Acids/chemistry , Humans , Fluticasone/administration & dosage , Fluticasone/pharmacology , Fluticasone/chemistry , Cell Survival/drug effects , Particle Size , Administration, Inhalation , Drug Carriers/chemistry , Drug Delivery Systems/methods , Drug Liberation , Nebulizers and Vaporizers , Bronchodilator Agents/administration & dosage , Bronchodilator Agents/pharmacology , Bronchodilator Agents/chemistry
13.
Int J Pharm ; 651: 123792, 2024 Feb 15.
Article in English | MEDLINE | ID: mdl-38190952

ABSTRACT

The majority of tablets manufactured contain lubricants to reduce friction during ejection. However, especially for plastically deforming materials, e.g., microcrystalline cellulose (MCC), the internal addition of lubricants is known to reduce tablet tensile strength. This reduction is caused by the surface coverage by lubricant particles, the extent of which depends on both process and formulation parameters. Previously published models to predict the lubrication effect on mechanical strength do not account for changes in the excipient particle size. In this study, the impact of both lubricant concentration and mixing time on the tensile strength of tablets consisting of three different grades of MCC and four grades of magnesium stearate (MgSt) was evaluated. By taking into account the particle size of the applied excipients, a unifying relationship between the theoretically estimated surface coverage and compactibility reduction was identified. Evaluating the dispersion kinetics of MgSt as a function of time reveals a substantial impact of the initial surface coverage on the dispersion rate, while the minimal tensile strength was found to be comparable for the majority of formulations. In summary, the presented work extends the knowledge of lubricant dispersion and facilitates the reduction of necessary experiments during the development of new tablet formulations.


Subject(s)
Cellulose , Excipients , Stearic Acids , Particle Size , Excipients/chemistry , Stearic Acids/chemistry , Tablets/chemistry , Lubricants/chemistry , Tensile Strength
14.
Eur J Pharm Biopharm ; 193: 262-273, 2023 Dec.
Article in English | MEDLINE | ID: mdl-37944711

ABSTRACT

This study discusses the lubricant properties of magnesium stearate solid lipid nanoparticles (MgSt-SLN) and their effect on the tabletability, mechanical properties, disintegration, and acetaminophen-model dissolution time of microcrystalline cellulose (MCC) tablets prepared by direct compression. The behavior of MgSt-SLN was compared to reference material (RM) to identify advantages and drawbacks. The nanoprecipitation/ion exchange method was employed to prepare the MgSt-SLN. Particle size, zeta potential, specific surface area, morphology, and true density were measured to characterize the nanosystem. The MgSt-SLN particle sizes obtained were 240 ± 5 nm with a specific surface area of 12.2 m2/g. The MCC tablets with MgSt-SLN presented a reduction greater than 20 % in their ejection force, good tabletability, higher tensile strength, lower disintegration delay, and marked differences in acetaminophen dissolution when compared to the RM. The reduced particle size of the magnesium stearate seems to offer a promising technological advantage as an efficient lubricant process that does not affect the properties of tablets.


Subject(s)
Acetaminophen , Lubricants , Lubricants/chemistry , Stearic Acids/chemistry , Excipients/chemistry , Tablets/chemistry , Tensile Strength
15.
Pharm Dev Technol ; 28(10): 992-999, 2023 Dec.
Article in English | MEDLINE | ID: mdl-37938090

ABSTRACT

Punch sticking is a recurrent problem during the pharmaceutical tableting process. Powder moisture content plays a key role in the buildup of sticking; it evaporates due to increased tablet temperature, accumulates at the punch-tablet interface, and causes sticking through capillary force. This study investigated the effects of compaction pressure (CP), compaction speed (CS), and lubrication level (magnesium stearate (MgSt) ratio) on tablet surface temperature (TST) and tablet surface moisture content (TSMC). TST and TSMC were measured with an infrared thermal camera and near-infrared sensor, respectively. Microcrystalline cellulose was used as the tableting powder and MgSt as the lubricant. The low range of CS values (16-32 mm/s) considered in this study did not have significant effects on TST and TSMC. MgSt ratio had a significant positive effect on TST; this may be explained by the increase in powder blend effusivity with the addition of MgSt. However, MgSt ratio did not have a significant effect on TSMC. CP had a significant positive effect on both TST and TSMC. Increased CP induced higher heat generation through particle deformation and friction during the compaction phase, leading to increased TST. Furthermore, the water vapor diffusion rate through the powder bed might have increased due to the rise in thermal energy and led to further moisture accumulation at the tablet-punch interface, causing the significant positive effect of CP on TSMC. This result may explain the occurrence of sticking regardless of the CP applied during the tableting process.


Subject(s)
Lubricants , Stearic Acids , Lubrication , Powders/chemistry , Temperature , Lubricants/chemistry , Tablets/chemistry , Stearic Acids/chemistry
16.
J Oleo Sci ; 72(8): 733-743, 2023 Aug 01.
Article in English | MEDLINE | ID: mdl-37468274

ABSTRACT

Lycopene is a natural bioactive compound possessing higher antioxidant and anti-inflammatory properties, which are known to efficiently eliminate the risk of cancer, cardiac complications, and oxidative stress. Food manufacturers are keen on producing lycopene-fortified food products owing to their numerous health benefits and higher nutritional value. The incorporation of lycopene is limited to food products due to its hydrophobic nature and low chemical stability. This study aims to understand the incorporation of lycopene in Oleogel as a new delivery system. Briefly, lycopene and stearic acid (gelator) were combined at ratios of 0, 25, 50, 75, and 100% (w/w) and added to coconut oil (20 g (w/w) ) for the preparation of edible oleogel combinations. These combinations were characterized for oil binding capacity, swelling capacity, color analysis, and texture profile analysis. Further, the formulations were characterized by FTIR (Fourier Transform Infrared Spectroscopy) and DSC (Differential scanning calorimetry). It was observed that samples prepared with a combination of 50% lycopene and stearic acid were found to possess a firm texture and good stability. Conversely, samples with no gelator produced oleogels with less stability. Further, the FTIR spectra helped determine the network formation in the oleogels, which was stabilized by the hydrogen bond. Furthermore, the results of DSC exhibited that the oleogel combinations with gelator and lycopene were not in the crystalline state, and the oleogels held superior internal structure till 45°C. Overall, oleogel-based carrier systems can be used as an alternative method to encapsulate various bioactive compounds having possible potential applications in the bakery and confectionery industries.


Subject(s)
Stearic Acids , Coconut Oil , Lycopene , Stearic Acids/chemistry
17.
Int J Pharm ; 643: 123265, 2023 Aug 25.
Article in English | MEDLINE | ID: mdl-37482231

ABSTRACT

Lubricants are excipients used in tablet formulations to reduce friction and adhesion forces within the die or on the punches surface during the manufacturing process. Despite these excipients are always required for the tablets production, their amount must be carefully evaluated since lubricants can negatively impact on mechanical strength, disintegration and dissolution behavior of solid dosage forms. Alternative compounds have been suggested to overcome the issues of conventional lubricants and sodium lauryl sulfate (SDS) is one of the most promising one. Despite SDS has been object of several investigations, a definitive conclusion on its effectiveness cannot still be drawn. Particularly, its efficacy on tablets disaggregation and API dissolution is still unclear. Here, the effect of SDS on all the relevant features of tablets and tableting process has been evaluated on immediate release hydrophobic tablets formulations in comparison with conventional lubricants. The results of this investigation are quite outspoken: SDS has a low lubricant power while it determines only a limited improvement on tablets hardness. It greatly improves the tablets wettability but only on model formulations, the presence of superdisintegrants resets its effectiveness and any possible effect on tablets disaggregation. None of the tested formulations showed improvement on the API dissolution rate.


Subject(s)
Excipients , Lubricants , Sodium Dodecyl Sulfate/chemistry , Lubricants/chemistry , Excipients/chemistry , Stearic Acids/chemistry , Drug Compounding
18.
Molecules ; 28(11)2023 May 25.
Article in English | MEDLINE | ID: mdl-37298812

ABSTRACT

Here, we describe the behavior of mixtures of stearic acid (SA) and its hydroxylated counterpart 12-hydroxystearic acid (12-HSA) in aqueous mixtures at room temperature as a function of the 12-HSA/SA mole ratio R. The morphologies of the self-assembled aggregates are obtained through a multi-structural approach that combines confocal and cryo-TEM microscopies with small-angle neutron scattering (SANS) and wide-angle X-ray scattering (WAXS) measurements, coupled with rheology measurements. Fatty acids are solubilized by an excess of ethanolamine counterions, so that their heads are negatively charged. A clear trend towards partitioning between the two types of fatty acids is observed, presumably driven by the favorable formation of a H-bond network between hydroxyl OH function on the 12th carbon. For all R, the self-assembled structures are locally lamellar, with bilayers composed of crystallized and strongly interdigitated fatty acids. At high R, multilamellar tubes are formed. The doping via a low amount of SA molecules slightly modifies the dimensions of the tubes and decreases the bilayer rigidity. The solutions have a gel-like behavior. At intermediate R, tubes coexist in solution with helical ribbons. At low R, local partitioning also occurs, and the architecture of the self-assemblies associates the two morphologies of the pure fatty acids systems: they are faceted objects with planar domains enriched in SA molecules, capped with curved domains enriched in 12-HSA molecules. The rigidity of the bilayers is strongly increased, as well their storage modulus. The solutions remain, however, viscous fluids in this regime.


Subject(s)
Fatty Acids , Stearic Acids , Temperature , Stearic Acids/chemistry , Fatty Acids/chemistry , Microscopy , Micelles
19.
Int J Pharm ; 630: 122422, 2023 Jan 05.
Article in English | MEDLINE | ID: mdl-36410668

ABSTRACT

Scanning electron microscopy-based energy dispersive X-ray spectroscopy (SEM-EDS) is proposed as a versatile tool for quantifying surface area coverage (SAC) by magnesium stearate (MgSt) on pharmaceutical tablets and particles. Our approach involved fast elemental mapping and subsequent SAC quantitation by image analysis. The study was conducted using a multi-component system, but the particle-level mapping was limited to active pharmaceutical ingredient (API) crystals. For both tablets and API particles, the calculated SAC against MgSt loading afforded a positive linear correlation over the range of MgSt levels examined in this work. On the tablet surface, MgSt was found to be preferentially concentrated at or in the close vicinity of grain boundaries, supporting the idea of compression-driven migration and relocation of MgSt within the tablet. On the particle surface, only discrete aggregates of MgSt were observed, as opposed to the widely accepted phenomenon of the formation of a thin lubricant film around host particles. The selection of proper SEM-EDS operating conditions and the challenges confronted in particle surface mapping are discussed in detail.


Subject(s)
Excipients , Stearic Acids , Tablets/chemistry , Stearic Acids/chemistry , Excipients/chemistry , Lubricants/chemistry
20.
Food Chem ; 404(Pt A): 134176, 2023 Mar 15.
Article in English | MEDLINE | ID: mdl-36242964

ABSTRACT

To provide a theoretical basis for the quality improvement of plant protein-based meat substitutes with lipids, the interactions between pea protein and fatty acids (stearic, oleic and linoleic acids) and the effect on protein conformational changes during high-moisture extrusion (HME) processing were investigated using a dead-stop operation. The surface hydrophobicity analysis and Fourier transform infrared spectroscopy results revealed that the fatty acids induced the exposure of hydrophobic groups in the pea proteins, weakened hydrogen bonds, affected the aggregation of legumin subunits and promoted the conversion of α-helix and ß-sheet structures to ß-turn and random coil during HME processing. In the die, unsaturated fatty acids limited the refolding of protein chains and covalent interactions between proteins. Micromorphology analysis indicated that the coalescence of oleic and linoleic acids in the cooling zone hindered the formation of anisotropic structures while stearic acid promoted the formation of fibrous structures by enhanced disulfide bonds.


Subject(s)
Fabaceae , Pea Proteins , Fatty Acids/metabolism , Stearic Acids/chemistry , Linoleic Acids , Fabaceae/metabolism , Hydrogen Bonding
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