scholarly journals Combinations of Freeze-Dried Amorphous Vardenafil Hydrochloride with Saccharides as A Way to Enhance Dissolution Rate and Permeability

2021 ◽  
Vol 14 (5) ◽  
pp. 453
Author(s):  
Gabriela Wiergowska ◽  
Dominika Ludowicz ◽  
Kamil Wdowiak ◽  
Andrzej Miklaszewski ◽  
Kornelia Lewandowska ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Density Functional ◽  
Hydroxypropyl Methylcellulose ◽  
Fold Increase ◽  
Crystalline Form ◽  
Amorphous Form ◽  
Freeze Dried ◽  
Apparent Solubility ◽  
Gastrointestinal Epithelium ◽  
The Impact

To improve physicochemical properties of vardenafil hydrochloride (VAR), its amorphous form and combinations with excipients—hydroxypropyl methylcellulose (HPMC) and β-cyclodextrin (β-CD)—were prepared. The impact of the modification on physicochemical properties was estimated by comparing amorphous mixtures of VAR to their crystalline form. The amorphous form of VAR was obtained as a result of the freeze-drying process. Confirmation of the identity of the amorphous dispersion of VAR was obtained through the use of comprehensive analysis techniques—X-ray powder diffraction (PXRD) and differential scanning calorimetry (DSC), supported by FT-IR (Fourier-transform infrared spectroscopy) coupled with density functional theory (DFT) calculations. The amorphous mixtures of VAR increased its apparent solubility compared to the crystalline form. Moreover, a nearly 1.3-fold increase of amorphous VAR permeability through membranes simulating gastrointestinal epithelium as a consequence of the changes of apparent solubility (Papp crystalline VAR = 6.83 × 10−6 cm/s vs. Papp amorphous VAR = 8.75 × 10−6 cm/s) was observed, especially for its combinations with β-CD in the ratio of 1:5—more than 1.5-fold increase (Papp amorphous VAR = 8.75 × 10−6 cm/s vs. Papp amorphous VAR:β-CD 1:5 = 13.43 × 10−6 cm/s). The stability of the amorphous VAR was confirmed for 7 months. The HPMC and β-CD are effective modifiers of its apparent solubility and permeation through membranes simulating gastrointestinal epithelium, suggesting a possibility of a stronger pharmacological effect.

scholarly journals Pyr1,xTFSI Ionic Liquids (x = 1–8): A Computational Chemistry Study

2020 ◽  
Vol 10 (23) ◽  
pp. 8552
Author(s):  
Sergio Brutti
Keyword(s):  
Ionic Liquids ◽  
Physicochemical Properties ◽  
Density Functional ◽  
Ion Pairs ◽  
Molecular Size ◽  
Molecular Structures ◽  
Safety Standards ◽  
Oxidation Reduction ◽  
Reduction Stability ◽  
The Impact

Pyrrolidinium-based (Pyr) ionic liquids are a very wide family of molecular species. Pyrrolidinium cations are electrochemically stable in a large potential interval and their molecular size hinders their transport properties. The corresponding ionic liquids with trifluoromethyl sulphonyl imide anions are excellent solvents for lithium/sodium salts and have been demonstrated as electrolytes in aprotic batteries with enhanced safety standards. In this study, the analysis of the physicochemical properties of a homologous series of pyrrolidinium-based ionic liquids with general formula Pyr1,xTFSI (x = 1–8) have been tackled by first principles calculations based on the density functional theory. The molecular structures of isolated ions and ion pairs have been predicted by electronic structure calculations at B3LYP level of theory in vacuum or in simulated solvents. Thermodynamic properties have been calculated to evaluate the ion pairs dissociation and oxidation/reduction stability. This is the first systematic computational analysis of this series of molecules with a specific focus on the impact of the length of the alkyl chain on the pyrrolidinium cation on the overall physicochemical properties of the ion pairs.

Effect of Biopolymer on the Dissolution and Stability of Itraconazole

2013 ◽  
Vol 747 ◽  
pp. 115-118 ◽  
Author(s):  
Benchawan Chamsai ◽  
Pornsak Sriamornsak
Keyword(s):  
Polyethylene Glycol ◽  
Drug Release ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
Crystalline Form ◽  
Dissolution Time ◽  
Polyethylene Glycol 4000 ◽  
Melting Method ◽  
Amorphous Form ◽  
X Ray

traconazole (ITZ) polyethylene glycol 4000 (PEG) solid dispersions (SDs) containing hydroxypropyl methylcellulose (HPMC) and/or low methoxy pectin (LMP) were prepared by melting method at a ratio of drug to carrier of 1:9. ITZPEG formulations showed the highest drug release (83.51%) when compared to the formulations containing HPMC and/or pectin (i.e., 43.02%, 40.64% and 59.94% for those containing HPMC, LMP and HPMC+LMP, respectively). Powder X-ray diffractograms of all formulations revealed that the drug was present in an amorphous form while a crystalline form was observed only in ITZ or its physical mixture. After storage at accelerated condition (40°C, 75%RH) for 2 and 12 months, the crystalline of ITZ was clearly not observed in all SDs. All formulations showed an increase in mean dissolution time (MDT) but the formulations containing biopolymer showed the lower MDT than that containing no biopolymer. The results suggested that either HPMC or LMP in SDs can help to inhibit the recrystallization of amorphous ITZ in SD, probably by a polymer anti-plasticizing effect.

A Systems Approach to ER Stress Pathway Dynamics Reveals the Impact of Freeze-Dried Broccoli Extract to Mitigate Inflammation in Human Adipocytes through the Mevalonate Pathway

Diabetes ◽  
2018 ◽  
Vol 67 (Supplement 1) ◽  
pp. 2076-P
Author(s):  
ALICE MURPHY ◽  
SAHAR AZHARIAN ◽  
GYANENDRA TRIPATHI ◽  
GUY BARKER ◽  
MICHAEL J. CHAPPELL ◽  
...  
Keyword(s):  
Er Stress ◽  
Systems Approach ◽  
Mevalonate Pathway ◽  
Human Adipocytes ◽  
Freeze Dried ◽  
The Impact ◽  
Stress Pathway

Novel Applications of Nanotechnology in Controlling HIV and HSV Infections

2020 ◽  
Vol 12 ◽  
Author(s):  
Sai Akilesh M ◽  
Ashish Wadhwani
Keyword(s):  
Drug Delivery ◽  
Viral Infections ◽  
Polymeric Nanoparticles ◽  
Volume Ratio ◽  
Fold Increase ◽  
Multi Drug Resistance ◽  
Health Crisis ◽  
Pharmaceutical Properties ◽  
Simplex Virus ◽  
The Impact

: Infectious diseases have been prevalent since many decades and viral pathogens have caused global health crisis and economic meltdown on a devastating scale. High occurrence of newer viral infections in the recent years, in spite of the progress achieved in the field of pharmaceutical sciences defines the critical need for newer and more effective antiviral therapies and diagnostics. The incidence of multi-drug resistance and adverse effects due to the prolonged use of anti-viral therapy is also a major concern. Nanotechnology offers a cutting edge platform for the development of novel compounds and formulations for biomedical applications. The unique properties of nano-based materials can be attributed to the multi-fold increase in the surface to volume ratio at the nano-scale, tunable surface properties of charge and chemical moieties. Idealistic pharmaceutical properties such as increased bioavailability and retention times, lower toxicity profiles, sustained release formulations, lower dosage forms and most importantly, targeted drug delivery can be achieved through the approach of nanotechnology. The extensively researched nano-based materials are metal and polymeric nanoparticles, dendrimers and micelles, nano-drug delivery vesicles, liposomes and lipid based nanoparticles. In this review article, the impact of nanotechnology on the treatment of Human Immunodeficiency Virus (HIV) and Herpes Simplex Virus (HSV) viral infections during the last decade are outlined.

scholarly journals Effect of Freeze Drying and Simulated Gastrointestinal Digestion on Phenolic Metabolites and Antioxidant Property of the Natal Plum (Carissa macrocarpa)

Foods ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1420
Author(s):  
Faith Seke ◽  
Vimbainashe E. Manhivi ◽  
Tinotenda Shoko ◽  
Retha M. Slabbert ◽  
Yasmina Sultanbawa ◽  
...  
Keyword(s):  
Freeze Drying ◽  
Array Detector ◽  
Gastrointestinal Digestion ◽  
Liquid Chromatograph ◽  
Antioxidant Power ◽  
Intestinal Phase ◽  
Glucosidase Activity ◽  
Freeze Dried ◽  
Small Intestinal ◽  
The Impact

Natal plums (Carissa macrocarpa) are a natural source of bioactive compounds, particularly anthocyanins, and can be consumed as a snack. This study characterized the impact of freeze drying and in vitro gastrointestinal digestion on the phenolic profile, antioxidant capacity, and α-glucosidase activity of the Natal plum (Carissa macrocarpa). The phenolic compounds were quantified using high performance liquid chromatography coupled to a diode-array detector HPLC-DAD and an ultra-performance liquid chromatograph (UPLC) with a Waters Acquity photodiode array detector (PDA) coupled to a Synapt G2 quadrupole time-of-flight (QTOF) mass spectrometer. Cyanidin-3-O-β-sambubioside (Cy-3-Sa) and cyanidin-3-O-glucoside (Cy-3-G) were the dominant anthocyanins in the fresh and freeze-dried Natal plum powder. Freeze drying did not affect the concentrations of both cyanidin compounds compared to the fresh fruit. Both cyanidin compounds, ellagic acid, catechin, epicatechin syringic acid, caffeic acid, luteolin, and quercetin O-glycoside from the ingested freeze-dried Natal plum powder was quite stable in the gastric phase compared to the small intestinal phase. Cyanidin-3-O-β-sambubioside from the ingested Natal plum powder showed bioaccessibility of 32.2% compared to cyanidin-3-O-glucoside (16.3%). The degradation of anthocyanins increased the bioaccessibility of gallic acid, protocatechuic acid, coumaric acid, and ferulic acid significantly, in the small intestinal digesta. The ferric reducing antioxidant power (FRAP), 2,2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) activities, and inhibitory effect of α-glucosidase activity decreased in the small intestinal phase. Indigenous fruits or freeze-dried powders with Cy-3-Sa can be a better source of anthocyanin than Cy-3-G due to higher bioaccessibility in the small intestinal phase.

scholarly journals Administrative Coding Methods Impact Surgical Site Infection Rates

2020 ◽  
Vol 41 (S1) ◽  
pp. s111-s112
Author(s):  
Mohammed Alsuhaibani ◽  
Mohammed Alzunitan ◽  
Kyle Jenn ◽  
Daniel Diekema ◽  
Michael Edmond ◽  
...  
Keyword(s):  
Cesarean Section ◽  
Surgical Procedures ◽  
Hip Prosthesis ◽  
Knee Prosthesis ◽  
Surgical Site Infections ◽  
Fold Increase ◽  
Abdominal Hysterectomy ◽  
Absolute Difference ◽  
Coding Method ◽  
The Impact

Background: Surveillance for surgical site infections (SSI) is recommended by the CDC. Currently, colon and abdominal hysterectomy SSI rates are publicly available and impact hospital reimbursement. However, the CDC NHSN allows surgical procedures to be abstracted based on International Classification of Diseases, Tenth Revision (ICD-10) or current procedural terminology (CPT) codes. We assessed the impact of using ICD and/or CPT codes on the number of cases abstracted and SSI rates. Methods: We retrieved administrative codes (ICD and/or CPT) for procedures performed at the University of Iowa Hospitals & Clinics over 1 year: October 2018–September 2019. We included 10 procedure types: colon, hysterectomy, cesarean section, breast, cardiac, craniotomy, spinal fusion, laminectomy, hip prosthesis, and knee prosthesis surgeries. We then calculated the number of procedures that would be abstracted if we used different permutations in administration codes: (1) ICD codes only, (2) CPT codes only, (3) both ICD and CPT codes, and (4) at least 1 code from either ICD or CPT. We then calculated the impact on SSI rates based on any of the 4 coding permutations. Results: In total, 9,583 surgical procedures and 180 SSIs were detected during the study period using the fourth method (ICD or CPT codes). Denominators varied according to procedure type and coding method used. The number of procedures abstracted for breast surgery had a >10-fold difference if reported based on ICD only versus ICD or CPT codes (104 vs 1,109). Hip prosthesis had the lowest variation (638 vs 767). For SSI rates, cesarean section showed almost a 3-fold increment (2.6% when using ICD only to 7.32% with both ICD & CPT), whereas abdominal hysterectomy showed nearly a 2-fold increase (1.14% when using CPT only to 2.22% with both ICD & CPT codes). However, SSI rates remained fairly similar for craniotomy (0.14% absolute difference), hip prosthesis (0.24% absolute difference), and colon (0.09% absolute difference) despite differences in the number of abstracted procedures and coding methods. Conclusions: Denominators and SSI rates vary depending on the coding method used. Variations in the number of procedures abstracted and their subsequent impact on SSI rates were not predictable. Variations in coding methods used by hospitals could impact interhospital comparisons and benchmarking, potentially leading to disparities in public reporting and hospital penalties.Funding: NoneDisclosures: None

scholarly journals Ethanol/Gasoline Blends as Alternative Fuel in Last Generation Spark-Ignition Engines: A Review on CO and HC Engine Out Emissions

Energies ◽  
2021 ◽  
Vol 14 (13) ◽  
pp. 4034
Author(s):  
Paolo Iodice ◽  
Massimo Cardone
Keyword(s):  
Physicochemical Properties ◽  
Alternative Fuels ◽  
Experimental Studies ◽  
Alternative Fuel ◽  
Exhaust Emissions ◽  
Spark Ignition ◽  
Operating Conditions ◽  
Spark Ignition Engine ◽  
Spark Ignition Engines ◽  
The Impact

Among the alternative fuels existing for spark-ignition engines, ethanol is considered worldwide as an important renewable fuel when mixed with pure gasoline because of its favorable physicochemical properties. An in-depth and updated investigation on the issue of CO and HC engine out emissions related to use of ethanol/gasoline fuels in spark-ignition engines is therefore necessary. Starting from our experimental studies on engine out emissions of a last generation spark-ignition engine fueled with ethanol/gasoline fuels, the aim of this new investigation is to offer a complete literature review on the present state of ethanol combustion in last generation spark-ignition engines under real working conditions to clarify the possible change in CO and HC emissions. In the first section of this paper, a comparison between physicochemical properties of ethanol and gasoline is examined to assess the practicability of using ethanol as an alternative fuel for spark-ignition engines and to investigate the effect on engine out emissions and combustion efficiency. In the next section, this article focuses on the impact of ethanol/gasoline fuels on CO and HC formation. Many studies related to combustion characteristics and exhaust emissions in spark-ignition engines fueled with ethanol/gasoline fuels are thus discussed in detail. Most of these experimental investigations conclude that the addition of ethanol with gasoline fuel mixtures can really decrease the CO and HC exhaust emissions of last generation spark-ignition engines in several operating conditions.

scholarly journals Grill Workers Exposure to Polycyclic Aromatic Hydrocarbons: Levels and Excretion Profiles of the Urinary Biomarkers

2020 ◽  
Vol 18 (1) ◽  
pp. 230
Author(s):  
Marta Oliveira ◽  
Sílvia Capelas ◽  
Cristina Delerue-Matos ◽  
Simone Morais
Keyword(s):  
Polycyclic Aromatic Hydrocarbons ◽  
Aromatic Hydrocarbons ◽  
High Performance ◽  
Principal Component ◽  
Fold Increase ◽  
Urinary Biomarkers ◽  
Analysis Model ◽  
Exposed Workers ◽  
Polycyclic Aromatic ◽  
The Impact

Grilling activities release large amounts of hazardous pollutants, but information on restaurant grill workers’ exposure to polycyclic aromatic hydrocarbons (PAHs) is almost inexistent. This study assessed the impact of grilling emissions on total workers’ exposure to PAHs by evaluating the concentrations of six urinary biomarkers of exposure (OHPAHs): naphthalene, acenaphthene, fluorene, phenanthrene, pyrene, and benzo(a)pyrene. Individual levels and excretion profiles of urinary OHPAHs were determined during working and nonworking periods. Urinary OHPAHs were quantified by high-performance liquid-chromatography with fluorescence detection. Levels of total OHPAHs (∑OHPAHs) were significantly increased (about nine times; p ≤ 0.001) during working comparatively with nonworking days. Urinary 1-hydroxynaphthalene + 1-hydroxyacenapthene and 2-hydroxyfluorene presented the highest increments (ca. 23- and 6-fold increase, respectively), followed by 1-hydroxyphenanthrene (ca. 2.3 times) and 1-hydroxypyrene (ca. 1.8 times). Additionally, 1-hydroxypyrene levels were higher than the benchmark, 0.5 µmol/mol creatinine, in 5% of exposed workers. Moreover, 3-hydroxybenzo(a)pyrene, biomarker of exposure to carcinogenic PAHs, was detected in 13% of exposed workers. Individual excretion profiles showed a cumulative increase in ∑OHPAHs during consecutive working days. A principal component analysis model partially discriminated workers’ exposure during working and nonworking periods showing the impact of grilling activities. Urinary OHPAHs were increased in grill workers during working days.

scholarly journals An Evaluation of the Impact of the Amount of Potassium Hydroxide on the Porous Structure Development of Activated Carbons

Materials ◽  
2021 ◽  
Vol 14 (8) ◽  
pp. 2045
Author(s):  
Mirosław Kwiatkowski ◽  
Elżbieta Broniek ◽  
Vanessa Fierro ◽  
Alain Celzard
Keyword(s):  
Density Functional Theory ◽  
Porous Structure ◽  
Potassium Hydroxide ◽  
Density Functional ◽  
Activated Carbons ◽  
Chemical Activation ◽  
Appropriate Technology ◽  
Functional Theory ◽  
Homogeneous Surface ◽  
The Impact

This paper presents the results of an evaluation of the impact of the amount of potassium hydroxide on the obtained porous structure of the activated carbons derived from the shells of pistachios, hazelnuts, and pecans by carbonization and subsequent chemical activation with potassium hydroxide by different adsorption methods: Brunauer–Emmett–Teller, Dubinin–Raduskevich, the new numerical clustering-based adsorption analysis, Quenched Solid Density Functional Theory, and 2D-Non-linear Density Functional Theory for Heterogeneous Surfaces, applied to nitrogen adsorption isotherms at −196 °C. Based on the conducted research, a significant potential for the production of activated carbons from waste materials, such as nut shells, has been demonstrated. All the activated carbons obtained in the present study at the activator/char mass ratio R = 4 exhibited the most developed porous structure, and thus very good adsorption properties. However, activated carbons obtained from pecan shells deserve special attention, as they were characterized by the most homogeneous surface among all the samples analyzed, i.e., by a very desirable feature in most adsorption processes. The paper demonstrates the necessity of using different methods to analyze the porous structure of activated carbons in order to obtain a complete picture of the studied texture. This is because only a full spectrum of information allows for correctly selecting the appropriate technology and conditions for the production of activated carbons dedicated to specific industrial applications. As shown in this work, relying only on the simplest methods of adsorption isotherm analysis can lead to erroneous conclusions due to lack of complete information on the analyzed porous structure. This work thus also explains how and why the usual characterizations of the porous structure of activated carbons derived from lignocellulosic biomass should not be taken at face value. On the contrary, it is advisable to cross reference several models to get a precise idea of the adsorbent properties of these materials, and therefore to propose the most suitable production technology, as well as the conditions of the preparation process.

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