scholarly journals Directly Compressed Tablets of Free Acid Ibuprofen with Nanocellulose Featuring Enhanced Dissolution: A Side-by-Side Comparison with Commercial Oral Dosage Forms

Pharmaceutics ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 71 ◽  
Author(s):  
Athanasios Mantas ◽  
Marie-Amélie Petit ◽  
Albert Mihranyan
Keyword(s):  
Surface Area ◽  
Free Acid ◽  
High Surface ◽  
High Surface Area ◽  
Oral Dosage ◽  
Simulated Gastric Fluid ◽  
Intestinal Fluid ◽  
Biorelevant Media ◽  
Simulated Intestinal Fluid ◽  
Enhanced Dissolution

We have previously reported that heated powder mixtures of ibuprofen (IBU) and high surface area nanocellulose exhibit an enhanced dissolution and solubility of the drug due to IBU amorphization. The goal of the present work was to further elaborate the concept and conduct side-by-side in vitro drug release comparisons with commercial formulations, including film-coated tablets, soft gel liquid capsules, and IBU-lysine conjugate tablets, in biorelevant media. Directly compressed tablets were produced from heated mixtures of 20% w/w IBU and high surface area Cladophora cellulose (CLAD), with 5% w/w sodium croscarmelose (AcDiSol) as superdisintegrant. The side-by side studies in simulated gastric fluid, fasted-state simulated intestinal fluid, and fed-state simulated intestinal fluid corroborate that the IBU-CLAD tablets show more rapid and less variable release in various media compared to three commercial IBU formulations. On the sidelines of the main work, a possibility of the presence of a new meta-crystalline form of IBU in mixture with nanocellulose is discussed.

scholarly journals Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate

Pharmaceutics ◽  
2019 ◽  
Vol 11 (1) ◽  
pp. 37 ◽  
Author(s):  
Athanasios Mantas ◽  
Albert Mihranyan
Keyword(s):  
Dissolution Rate ◽  
Surface Area ◽  
Channel Blocker ◽  
High Surface ◽  
High Surface Area ◽  
Intestinal Fluid ◽  
Dry Powder ◽  
Biorelevant Media ◽  
Simulated Intestinal Fluid ◽  
Powder Mixtures

Nifedipine (NIF) is a 1,4-dihydropyridine-based calcium channel blocker with poor solubility, whose bioavailability is highly dependent on the type of formulation. Dry powder mixtures of 20% w/w NIF with microcrystalline cellulose (MCC) and its high surface area nanocellulose analogue, which is namely Cladophora (CLAD) cellulose, were produced by heating at the melting temperature of the drug for 1 h. Non-heated samples were used as a reference. The solid-state properties of the mixtures were characterized by scanning electron microscopy, differential scanning calorimetry and X-ray diffraction. The drug release was studied in biorelevant media, including simulated gastric fluid (SGF), fasted-state simulated intestinal fluid (FaSIF) and fed-state simulated intestinal fluid (FeSIF). An enhanced apparent solubility and faster dissolution rate of NIF were observed in the heated mixture of NIF with CLAD-H in all tested biorelevant media (i.e., SGF, FaSIF and FeSIF), which was due to NIF amorphization in the high surface area nanocellulose powder. Ordinary MCC, which is essentially non-porous, did not produce an enhancement of a similar magnitude. The results of the study suggest that dry powder formulation using high surface area nanocellulose is a facile new strategy for formulating calcium channel blocker drugs, which could potentially be a viable alternative to currently used soft gel liquid capsules.

scholarly journals Dissolution Behavior of Flufenamic Acid in Heated Mixtures with Nanocellulose

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1277 ◽  
Author(s):  
Athanasios Mantas ◽  
Albert Mihranyan
Keyword(s):  
Surface Area ◽  
Flufenamic Acid ◽  
Simulated Gastric Fluid ◽  
Great Promise ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Fed State ◽  
Fasted State

Flufenamic acid (FFA) is a problem drug that has up to eight different polymorphs and shows poor solubility. Variability in bioavailability has been reported in the past resulting in limited use of FFA in the oral solid dosage form. The goal of this article was to investigate the polymorphism and amorphization behavior of FFA in non-heated and heated mixtures with high surface area nanocellulose, i.e., Cladophora cellulose (CLAD). As a benchmark, low surface area microcrystalline cellulose (MCC) was used. The solid-state properties of mixtures were characterized with X-ray diffraction, Fourier-transform infrared spectroscopy, and differential scanning calorimetry. The dissolution behavior of mixtures was studied in three biorelevant media, i.e., fasted state simulated gastric fluid, fasted state simulated intestinal fluid, and fed state simulated intestinal fluid. Additional thermal analysis and dissolution tests were carried out following 4 months of storage at 75% RH and room temperature. Heated mixtures of FFA with CLAD resulted in complete amorphization of the drug, whereas that with MCC produced a mixture of up to four different polymorphs. The amorphous FFA mixture with CLAD exhibited rapid and invariable fasted/fed state dissolution in simulated intestinal fluids, whereas that of MCC mixtures was highly dependent on the biorelevant medium. The storage of the heated FFA-CLAD mixture did not result in recrystallization or changes in dissolution profile, whereas heated FFA-MCC mixture showed polymorphic changes. The straightforward dry powder formulation strategy presented here bears great promise for reformulating a number of problem drugs to enhance their dissolution properties and reduce the fasted/fed state variability.

scholarly journals Dissolution Testing of Single- and Dual-Component Thyroid Hormone Supplements

Separations ◽  
2019 ◽  
Vol 6 (1) ◽  
pp. 18
Author(s):  
Samantha Bowerbank ◽  
Michelle Carlin ◽  
John Dean
Keyword(s):  
Thyroid Hormone ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Dissolution Testing ◽  
Liquid Chromatography Mass Spectrometry ◽  
Intestinal Fluid ◽  
Biorelevant Media ◽  
Simulated Intestinal Fluid ◽  
Biorelevant Dissolution ◽  
Fasted State

A method for the analysis of thyroid hormones by liquid chromatography-mass spectrometry was used for the dissolution testing of single- and dual-component thyroid hormone supplements via a two-stage biorelevant dissolution procedure. The biorelevant media consisted of fasted-state simulated gastric fluid and fasted state simulated intestinal fluid at 37 °C, and was investigated using an internationally recognized protocol. The dissolution profiles showed consistent solubilization for both single- and dual-component batches at pH 6.5 in the fasted-state simulated intestinal fluid.

scholarly journals Amorphisation of Free Acid Ibuprofen and Other Profens in Mixtures with Nanocellulose: Dry Powder Formulation Strategy for Enhanced Solubility

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 68 ◽  
Author(s):  
Athanasios Mantas ◽  
Valentine Labbe ◽  
Irena Loryan ◽  
Albert Mihranyan
Keyword(s):  
Surface Area ◽  
Free Acid ◽  
High Surface ◽  
In Vitro Dissolution ◽  
Pharmacokinetic Analysis ◽  
Strong Impact ◽  
Scanning Calorimetry ◽  
Biorelevant Media ◽  
Enhanced Solubility

The formulation of arylpropionic acid derivatives (profens), which are poorly soluble Biopharmaceutical Classification System (BCS) Type II drugs, has a strong impact on their therapeutic action. This article shows that heat-treated powder mixtures of free acid profens with high surface area Cladophora cellulose induces drug amorphization and results in enhanced solubility and bioavailability. Similar mixtures produced using conventional low surface area cellulose, i.e., microcrystalline cellulose, does not produce the same effect. The concept is thoroughly described and links the solid-state characterization data, such as differential scanning calorimetry, X-ray powder diffraction, and Fourier-transform infra-red spectroscopy, with in vitro dissolution in biorelevant media and in vivo pharmacokinetic analysis in rats. The concept is demonstrated for several substances from the profens group, including ibuprofen (main model drug), ketoprofen, flurbiprofen, and naproxen. The presented approach opens new ways to produce solid dosage forms of profen drugs in their free acidic form as alternatives to existing analogues, e.g., drug-salt conjugates or soft gel liquid capsules.

Tenacious Mass Transfer Limitations Drive Catalytic Selectivity during Electrochemical Carbon Dioxide Reduction

2019 ◽  
Author(s):  
Kailun Yang ◽  
Recep Kas ◽  
Wilson A. Smith
Keyword(s):  
Surface Area ◽  
High Surface ◽  
High Surface Area ◽  
Catalyst Layer ◽  
Active Surface ◽  
Active Surface Area ◽  
High Concentration ◽  
Copper Electrodes ◽  
Surface Enhanced ◽  
Local Current

<p>This study evaluated the performance of the commonly used strong buffer electrolytes, i.e. phosphate buffers, during CO<sub>2</sub> electroreduction in neutral pH conditions by using in-situ surface enhanced infrared absorption spectroscopy (SEIRAS). Unfortunately, the buffers break down a lot faster than anticipated which has serious implications on many studies in the literature such as selectivity and kinetic analysis of the electrocatalysts. Increasing electrolyte concentration, surprisingly, did not extend the potential window of the phosphate buffers due to dramatic increase in hydrogen evolution reaction. Even high concentration phosphate buffers (1 M) break down within the potentials (-1 V vs RHE) where hydrocarbons are formed on copper electrodes. We have extended the discussion to high surface area electrodes by evaluating electrodes composed of copper nanowires. We would like highlight that it is not possible to cope with high local current densities on these high surface area electrodes by using high buffer capacity solutions and the CO<sub>2</sub> electrocatalysts are needed to be evaluated by casting thin nanoparticle films onto inert substrates as commonly employed in fuel cell reactions and up to now scarcely employed in CO<sub>2</sub> electroreduction. In addition, we underscore that normalization of the electrocatalytic activity to the electrochemical active surface area is not the ultimate solution due to concentration gradient along the catalyst layer.This will “underestimate” the activity of high surface electrocatalyst and the degree of underestimation will depend on the thickness, porosity and morphology of the catalyst layer. </p> <p> </p>

scholarly journals Rugae-like FeP nanocrystal assembly on a carbon cloth: an exceptionally efficient and stable cathode for hydrogen evolution

Nanoscale ◽  
2015 ◽  
Vol 7 (25) ◽  
pp. 10974-10981 ◽  
Author(s):  
Xiulin Yang ◽  
Ang-Yu Lu ◽  
Yihan Zhu ◽  
Shixiong Min ◽  
Mohamed Nejib Hedhili ◽  
...  
Keyword(s):  
Gas Phase ◽  
Surface Area ◽  
Hydrogen Evolution ◽  
Hydrogen Generation ◽  
High Surface ◽  
High Surface Area ◽  
Catalytic Efficiency ◽  
Carbon Cloth ◽  
Nanocrystal Assembly

High surface area FeP nanosheets on a carbon cloth were prepared by gas phase phosphidation of electroplated FeOOH, which exhibit exceptionally high catalytic efficiency and stability for hydrogen generation.

High Surface Area NiCoP Nanostructure as Efficient Water Splitting Electrocatalyst for the Oxygen Evolution Reaction

2021 ◽  
pp. 111312
Author(s):  
Sisir Maity ◽  
Dheeraj Kumar Singh ◽  
Divya Bhutani ◽  
Suchitra Prasad ◽  
Umesh V. Waghmare ◽  
...  
Keyword(s):  
Surface Area ◽  
Water Splitting ◽  
Oxygen Evolution ◽  
Oxygen Evolution Reaction ◽  
High Surface ◽  
High Surface Area

scholarly journals Fast synthesis of high surface area bio-based porous carbons for p-nitrophenol removal

MethodsX ◽  
2021 ◽  
pp. 101464
Author(s):  
Yichen Wu ◽  
Nan Zhang ◽  
Charles-François de Lannoy
Keyword(s):  
Surface Area ◽  
High Surface ◽  
High Surface Area ◽  
Porous Carbons ◽  
Fast Synthesis

Synthesis of high surface area and functionalized nanoporous biocarbons and their efficiency for CO2 capture and supercapacitors

2021 ◽  
Author(s):  
Gurwinder Singh ◽  
Rohan Bahadur ◽  
Ajanya Maria Ruban ◽  
Jefrin Marykala Davidraj ◽  
Dawei Su ◽  
...  
Keyword(s):  
Energy Storage ◽  
Surface Area ◽  
Co2 Capture ◽  
Water Purification ◽  
High Surface ◽  
High Surface Area ◽  
Energy Storage And Conversion ◽  
Waste Biomass ◽  
Fabrication Technology ◽  
Significant Attention

Nanoporous biocarbons derived from waste biomass have created significant attention owing to their great potential for energy storage and conversion and water purification. However, the fabrication technology for these materials...

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