scholarly journals Homogenization of Amorphous Solid Dispersions Prepared by Electrospinning in Low-Dose Tablet Formulation

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 114 ◽  
Author(s):  
Gergő Fülöp ◽  
Attila Balogh ◽  
Balazs Farkas ◽  
Attila Farkas ◽  
Bence Szabó ◽  
...  
Keyword(s):  
Low Dose ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Electrospun Fibers ◽  
Sieve Analysis ◽  
High Shear ◽  
Plastic Bags ◽  
Shear Mixing ◽  
Model Drug ◽  
Dose Tablet

Low-dose tablet formulations were produced with excellent homogeneity based on drug-loaded electrospun fibers prepared by single-needle as well as scaled-up electrospinning (SNES and HSES). Carvedilol (CAR), a BCS II class compound, served as the model drug while poly (vinylpyrrolidone-co-vinyl acetate) (PVPVA64) was adopted as the fiber-forming polymer. Scanning electron microscopy (SEM) imaging was used to study the morphology of HSES and SNES samples. Different homogenization techniques were compared to maximize homogeneity: mixing in plastic bags and in a high-shear granulator resulting in low-shear mixing (LSM) and high-shear mixing (HSM). Drug content and homogeneity of the tablets were measured by UV-Vis spectrometry, the results revealed acceptably low-dose fluctuations especially with formulations homogenized with HSM. Sieve analysis was used on the final LSM and HSM powder mixtures in order to elucidate the observed differences between tablet homogeneity. Tablets containing drug-loaded electrospun fibers were also studied by Raman mapping demonstrating evenly distributed CAR within the corpus.

scholarly journals Particle Forming Amorphous Solid Dispersions: A Mechanistic Randomized Pharmacokinetic Study in Humans

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 401
Author(s):  
Andreas Schittny ◽  
Samuel Waldner ◽  
Urs Duthaler ◽  
Alexander Vorobyev ◽  
Rimma Abramovich ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Aqueous Solubility ◽  
Ambulatory Setting ◽  
Pharmacokinetic Parameters ◽  
Supersaturated Solution ◽  
Open Label ◽  
Amorphous Solid Dispersions ◽  
Model Drug

Amorphous solid dispersions (ASDs) are a promising drug-delivery strategy to overcome poor solubility through formulation. Currently, the understanding of drug absorption mechanisms from ASDs in humans is incomplete. Aiming to gain insights in this matter, we conducted a randomized cross-over design open-label clinical study (NCT03886766) with 16 healthy male volunteers in an ambulatory setting, using micro-dosed efavirenz as a model drug. In three phases, subjects were administered (1) solid ASD of efavirenz 50 mg or (2) dissolved ASD of efavirenz 50 mg or (3) a molecular solution of efavirenz 3 mg (non-ASD) as a control in block-randomized order. Endpoints were the pharmacokinetic profiles (efavirenz plasma concentration vs. time curves) and derived pharmacokinetic parameters thereof (AUC0–t, Cmax, tmax, and ka). Results showed that the dissolved ASD (intervention 2) exhibited properties of a supersaturated solution (compared to aqueous solubility) with rapid and complete absorption of the drug from the drug-rich particles. All interventions showed similar AUC0–t and were well tolerated by subjects. The findings highlight the potential of particle forming ASDs as an advanced drug-delivery system for poorly soluble drugs and provide essential insights into underlying mechanisms of ASD functioning in humans, partially validating current conceptual models.

Development of novel darunavir amorphous solid dispersions with mesoporous carriers

2021 ◽  
Vol 159 ◽  
pp. 105700
Author(s):  
Sergey A. Zolotov ◽  
Natalia B. Demina ◽  
Anna S. Zolotova ◽  
Natalia V. Shevlyagina ◽  
Grigorii A. Buzanov ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersions

Effect of Carrier Type and Tween® 80 Concentration on the Release of Silymarin from Amorphous Solid Dispersions

2021 ◽  
pp. 102416
Author(s):  
Valentyn Mohylyuk ◽  
Thomas Pauly ◽  
Oleksandr Dobrovolnyi ◽  
Nathan Scott ◽  
David S. Jones ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersions

scholarly journals Enhanced Oral Bioavailability of Resveratrol by Using Neutralized Eudragit E Solid Dispersion Prepared via Spray Drying

Antioxidants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 90
Author(s):  
Eun-Sol Ha ◽  
Du Hyung Choi ◽  
In-hwan Baek ◽  
Heejun Park ◽  
Min-Soo Kim
Keyword(s):  
Spray Drying ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Pharmaceutical Products ◽  
In Vitro Dissolution ◽  
Dependent Manner ◽  
Amorphous Solid Dispersions ◽  
Eudragit E

In this study, we designed amorphous solid dispersions based on Eudragit E/HCl (neutralized Eudragit E using hydrochloric acid) to maximize the dissolution of trans-resveratrol. Solid-state characterization of amorphous solid dispersions of trans-resveratrol was performed using powder X-ray diffraction, scanning electron microscopy, and particle size measurements. In addition, an in vitro dissolution study and an in vivo pharmacokinetic study in rats were carried out. Among the tested polymers, Eudragit E/HCl was the most effective solid dispersion for the solubilization of trans-resveratrol. Eudragit E/HCl significantly inhibited the precipitation of trans-resveratrol in a pH 1.2 dissolution medium in a dose-dependent manner. The amorphous Eudragit E/HCl solid dispersion at a trans-resveratrol/polymer ratio of 10/90 exhibited a high degree of supersaturation without trans-resveratrol precipitation for at least 48 h by the formation of Eudragit E/HCl micelles. In rats, the absolute oral bioavailability (F%) of trans-resveratrol from Eudragit E/HCl solid dispersion (10/90) was estimated to be 40%. Therefore, trans-resveratrol-loaded Eudragit E/HCl solid dispersions prepared by spray drying offer a promising formulation strategy with high oral bioavailability for developing high-quality health supplements, nutraceutical, and pharmaceutical products.

Expanded vermiculite-filled flexible polymer composites

2021 ◽  
pp. 009524432110290
Author(s):  
Mukaddes Sevval Cetin ◽  
Ozan Toprakci ◽  
Omer Suat Taskin ◽  
Abdullah Aksu ◽  
Hatice Aylin Karahan Toprakci
Keyword(s):  
Mechanical Properties ◽  
Thermal Stability ◽  
Contact Angle ◽  
Polymer Composites ◽  
Flame Retardancy ◽  
Composite Films ◽  
Filler Concentration ◽  
High Shear ◽  
Flexible Polymer ◽  
Shear Mixing

This study focuses on the fabrication and characterization of vermiculite-filled flexible polymer composites. Exfoliated vermiculite was incorporated into triblock thermoplastic elastomer copolymer, styrene- b-(ethylene- co-butylene)- b-styrene (SEBS), at various levels from 1 to 15 wt% by a high shear mixer. The composite films were obtained by the combination of solvent casting and compression molding. The morphological, structural, thermal, and mechanical properties and contact angle of the composites were determined. Some micro-morphological differences were observed between the samples and the difference was assumed to be caused by high shear mixing and filler concentration. High shear mixing was found effective in terms of the detachment of vermiculite layers at all concentrations. However, at low filler loading, that behavior was more obvious. At 1 wt% filler concentration, mechanical properties increased that was probably caused by good filler-matrix interaction stemmed from smaller particle size. At higher vermiculite concentrations, fillers found to show agglomerations that led to a decrease in mechanical strength and strain at break. Elastic and secant modulus showed an increasing trend. Contact angle measurements were carried out to determine the oleophilic character of the samples. An increase in the vermiculite content resulted in higher oleophilic character and the lowest contact angle was obtained at 15 wt% VMT loading. In addition to these, thermal stability, thermal dimensional stability and flame retardancy were improved by the incorporation of VMT. 15 wt% vermiculite-filled sample showed the best performance in terms of thermal stability and flame retardancy.

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