scholarly journals Clozapine-carboxylic acid plasticized co-amorphous dispersions: Preparation, characterization and solution stability evaluation

2015 ◽  
Vol 65 (2) ◽  
pp. 133-146 ◽  
Author(s):  
Ahmed Mahmoud Abdelhaleem Ali ◽  
Adel Ahmed Ali ◽  
Ibrahim Abdullah Maghrabi
Keyword(s):  
Carboxylic Acid ◽  
Tartaric Acid ◽  
Molar Ratio ◽  
Sublingual Administration ◽  
Solution Stability ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Great Chance ◽  
Amorphous Dispersions ◽  
Pass Metabolism

Abstract This study addressed the possibility of forming of co-amorphous systems between clozapine (CZ) and various carboxylic acid plasticizers (CAPs). The aim was to improve the solubility and oral bioavailability of clozapine. Co-amorphous dispersions were prepared using modified solvent evaporation methodology at drug/plasticizer stoichiometric ratios of 1:1, 1:1.5 and 1:2. Solid state characterization was performed using differential scanning calorimetry, X-ray diffraction and infra red spectroscopy. Highly soluble homogeneous co-amorphous dispersions were formed between clozapine and CAPs via hydrogen bonding. The co-amorphous dispersions formed with tartaric acid (1:2) showed the highest dissolution percentage (> 95 % in 20 minutes) compared to pure crystalline CZ (56 %). Highly stable solutions were obtained from co-amorphous CZ-citric and CZ-tartaric acid at 1:1.5 molar ratio. The prepared dispersions suggest the possibility of peroral or sublingual administration of highly soluble clozapine at a reduced dose with the great chance to bypass the first pass metabolism.

scholarly journals Microstructure Evolution and Performance Improvement of Hypereutectic Al–Mg2Si Metallic Composite with Ca or Sb

Materials ◽  
2020 ◽  
Vol 13 (12) ◽  
pp. 2714
Author(s):  
Min Zuo ◽  
Boda Ren ◽  
Zihan Xia ◽  
Wenwen Ma ◽  
Yidan Lv ◽  
...  
Keyword(s):  
Heat Treatment ◽  
Molar Ratio ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Nucleation Behavior ◽  
X Ray ◽  
Primary Mg2si ◽  
Before And After ◽  
And Performance ◽  
Hardness Values

In this article, the modification effects on Al–Mg2Si before and after heat treatment were investigated with Ca, Sb, and (Ca + Sb). In comparison with single Ca or Sb, the samples with composition modifiers (Ca + Sb) had the optimal microstructure. The sample with a molar ratio for Ca-to-Sb of 1:1 obtained relatively higher properties, for which the Brinell hardness values before and after heat treatment were remarkably increased by 31.74% and 28.93% in comparison with bare alloy. According to differential scanning calorimetry analysis (DSC), it was found that the nucleation behavior of the primary Mg2Si phase could be significantly improved by using chemical modifiers. Some white particles were found to be embedded in the center of Mg2Si phases, which were deduced to be Ca5Sb3 through X-ray diffraction (XRD) and field-emission scanning electron microscope (FESEM) analyses. Furthermore, Ca5Sb3 articles possess a rather low mismatch degree with Mg2Si particles based on Phase Transformation Crystallography Lab software (PTCLab) calculation, meaning that the efficient nucleation capability of Ca5Sb3 for Mg2Si particles could be estimated.

scholarly journals Alumina Extraction from Coal Fly Ash via Low-Temperature Potassium Bisulfate Calcination

Minerals ◽  
2019 ◽  
Vol 9 (10) ◽  
pp. 585 ◽  
Author(s):  
Chunbin Guo ◽  
Jingjing Zou ◽  
Shuhua Ma ◽  
Jianlin Yang ◽  
Kehan Wang
Keyword(s):  
Fly Ash ◽  
Low Temperature ◽  
Extraction Efficiency ◽  
Coal Fly Ash ◽  
Molar Ratio ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Increasing Demand ◽  
Technology Effects ◽  
Best Fit

Owing to the depletion of bauxite and increasing demand for alumina, calcination methods for extracting alumina from coal fly ash (CFA) were developed. However, these methods have disadvantages such as the need for high temperatures and the emission of toxic gases. Hence, in this study, Al2O3 was extracted from CFA via low-temperature potassium bisulfate calcination technology. Effects of the potassium bisulfate amount, calcination temperature, and calcination time on the alumina extraction efficiency were investigated using X-ray diffraction, thermal gravimetry, scanning electron microscopy, differential scanning calorimetry, and energy-dispersive spectroscopy. It was found that this technique could recover alumina efficiently, and potassium bisulfate significantly contributed to the degradation of mullite and corundum phases. Al2O3 in CFA was converted into soluble K3Al(SO4)3. With a KHSO4/Al2O3 molar ratio of 7:1, calcining temperature of 230 °C, and calcining time of 3 h, the alumina extraction efficiency reached a maximum of 92.8%. The Avrami–Erofeev equation showed the best fit with the kinetic data for the low-temperature calcination of CFA with KHSO4. The activation energy was 28.36 kJ/mol.

Iron and Iron-oxide on Silica Nanocomposites Prepared by the Sol-gel Method

2002 ◽  
Vol 17 (3) ◽  
pp. 590-596 ◽  
Author(s):  
G. Ennas ◽  
M. F. Casula ◽  
G. Piccaluga ◽  
S. Solinas ◽  
M. P. Morales ◽  
...  
Keyword(s):  
Sol Gel ◽  
Silica Matrix ◽  
Molar Ratio ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Gel Method ◽  
Sol Gel Method ◽  
Silica Nanocomposites ◽  
Transmission Electron ◽  
Nanometric Particles

γ–Fe2O3/SiO2 and Fe/SiO2 nanocomposites, with a Fe/Si molar ratio of 0.25, were prepared by the sol-gel method starting from ethanolic solutions of tetraethoxysilane and iron (III) nitrate. After gelation the xerogels were oxidated or reduced. Samples were investigated by transmission electron microscopy, x-ray diffraction, differential scanning calorimetry, and thermogravimetry. Magnetic properties of the samples were investigated at room temperature (RT) and at 77 K. Nanometric particles supported in the silica matrix were obtained in all cases. Bigger particles (10 nm) were obtained in the case of Fe/SiO2 nanocomposites with respect to the γ–Fe2O3/SiO2 samples (5–8 nm). A slight effect of sol dilution on particle size was observed only in the case of γ–Fe2O3/SiO2 nanocomposites. A superparamagnetic behavior was shown at RT only by γ–Fe2O3/SiO2 nanocomposites. Iron-based composites exhibited coercivity values higher than 700 Oe at RT.

Reactive phase formation in sputter-deposited Ni/Al multilayer thin films

1997 ◽  
Vol 12 (1) ◽  
pp. 133-146 ◽  
Author(s):  
K. Barmak ◽  
C. Michaelsen ◽  
G. Lucadamo
Keyword(s):  
Phase Formation ◽  
Molar Ratio ◽  
X Ray Diffraction ◽  
Nucleation Kinetics ◽  
Scanning Calorimetry ◽  
Calorimetric Analysis ◽  
Transmission Electron ◽  
Nial Phase ◽  
Magnetron Sputter ◽  
Sputter Deposited

We have investigated reactive phase formation in magnetron sputter-deposited NiyAl multilayer films with a 1 : 3 molar ratio and various periodicities, L, ranging from 320 nm down to a codeposited film with zero effective periodicity. The films were studied by x-ray diffraction, differential scanning calorimetry, electrical resistance measurements, and transmission electron microscopy. We find that Ni and Al have reacted during deposition to form the B2 NiAl phase and an amorphous phase. The formation of these phases substantially reduces the driving force for subsequent reactions and explains why nucleation kinetics become important for these reactions. Depending on the periodicity, these reactions result in the formation of NiAl3 or Ni2Al9 followed by NiAl3. Detailed calorimetric analysis reveals differences in the nucleation and growth behavior of NiAl3 compared with other studies.

Crystallization Kinetics of β-Spodumene/Cordierite-Based Glass-Ceramics

2016 ◽  
Vol 881 ◽  
pp. 83-88 ◽  
Author(s):  
Rafael Bianchini Nuernberg ◽  
Oscar Rubem Klegues Montedo
Keyword(s):  
Crystallization Kinetics ◽  
Glass Ceramics ◽  
Molar Ratio ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Kinetics Parameters ◽  
Crystalline Phases ◽  
Cordierite Glass ◽  
Thermal And Electrical Properties ◽  
Kinetics Of

This work aims to investigate the crystallization kinetics of β-spodumene/cordierite glass-ceramics. Thus, three glasses with compositions based predominantly on cordierite (C), β-spodumene (L) and in a molar ratio 1:1 of both phases (CL) were prepared. The kinetics parameters such as activation energy for crystallization (ranging from 160 to 358 kJ/mol) and Avrami exponent (ranging from 1.4 to 10.7) were determined by means of non-isothermal methods using differential scanning calorimetry (DSC). Additionally, the samples were crystalized according to DSC analyses and characterized by using x-ray diffraction (XRD). The main detected crystalline phases were β-spodumene to the glass L, cordierite to the glass C and β-quartz, mulite and spinel to the glass CL. Considering the thermal and electrical properties of these crystalline phases, these glass-ceramics have potential use for LTCC (Low Thermal Co-fired Ceramics) applications.

scholarly journals Physical Mixture Interaction of Acetaminophenol with Naringenin

2018 ◽  
Vol 18 (1) ◽  
pp. 18 ◽  
Author(s):  
Normyzatul Akmal Abd Malek ◽  
Hamizah Mohd Zaki ◽  
Mohammad Noor Jalil
Keyword(s):  
Interaction Strength ◽  
Active Pharmaceutical Ingredient ◽  
Binary Interaction ◽  
Molar Ratio ◽  
Attenuated Total Reflectance ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Mixture Ratio ◽  
X Ray ◽  
New Phase

The interaction of Active Pharmaceutical Ingredient (API) with other compounds will affect drugs stability, toxicity, modified dissolution profiles or may form a new compound with the different crystal structure. Acetaminophenol (APAP), the most common drug used widely (also known as Panadol) was mixed with Naringenin (NR) to glance for a new phase of interactions leading to new compound phase. The amide-acid supramolecular heterosynthon; N-H…O interaction between acid and the respective base were observed in the APAP-NR mixture blends. The interaction was prepared by the binary interaction from neat grinding and liquid-assisted grinding techniques at a different stoichiometry of binary mixture ratio of APAP-NR which were 1:1, 1:2 and 2:1 molar ratio. The interaction was estimated using Group Contribution Method (GCM) and physicochemical properties were characterized by Attenuated Total Reflectance Fourier Transform Infrared (ATR-FTIR), powder X-ray diffraction (PXRD) and Differential Scanning Calorimetry (DSC) analysis. The GCM calculation gave good interaction strength at 212.93 MPa1/2. The ATR-FTIR, DSC and PXRD results obtained revealed an interaction with new phase formed.

scholarly journals Synthesis of Glibenclamide-Oxalic Acid Cocrystal using ThermalSolvent-Free Method

2020 ◽  
Vol 11 (03) ◽  
pp. 404-408
Author(s):  
Arif Budiman ◽  
Sandra Megantara ◽  
Rifaa’tush Sholihah ◽  
Saeful Amin
Keyword(s):  
Oxalic Acid ◽  
In Silico ◽  
Active Pharmaceutical Ingredient ◽  
Molar Ratio ◽  
Dissolution Profile ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Dissolution Tests ◽  
Ir Spectrophotometry ◽  
Crystalline Component

Solubility is an important parameter affecting the bioavailability of drugs. The solubility of an active pharmaceutical ingredient (API) could be improved through the formation of cocrystal, which is a crystalline complex composed of two or more different molecules. Glibenclamide (GCM) is an API with poor solubility in water, which belongs to class II, characterized as highly permeable with low solubility. Therefore, this study aimed to synthesize and characterize the cocrystal of GCM-oxalic acid (OA) using the melting method. The interaction between GCM-OA complexes was predicted using the in silico method. Also, the cocrystal complexes were characterized by differential scanning calorimetry (DSC), infrared (IR) spectrophotometry, and powder X-ray diffraction (PXRD), as well as, through solubility and dissolution tests. The result showed that GCM and OA have the potential of forming cocrystal through the in silico method. Also, the cocrystal of GCM-OA with a molar ratio 1:2, significantly improved the solubility and dissolution profile of GCM. In addition, the spectrum IR of cocrystal exhibited a shifting peak at 1,700 cm-1 indicating the presence of intermolecular interaction between GCM and OA. Furthermore, the DSC and PXRD analyses showed a new single endothermic peak and new diffraction peak pattern, respectively, indicating the formation of a new crystalline component.

Solvates of the antifungal drug griseofulvin: structural, thermochemical and conformational analysis

2013 ◽  
Vol 70 (1) ◽  
pp. 54-62 ◽  
Author(s):  
Srinivasulu Aitipamula ◽  
Pui Shan Chow ◽  
Reginald B. H. Tan
Keyword(s):  
Melting Point ◽  
Solvent Free ◽  
Antifungal Drug ◽  
Free Form ◽  
Solution Stability ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Solvent Molecules ◽  
Solid Form

Four solvates of an antifungal drug, griseofulvin (GF), were discovered. All the solvates were characterized by differential scanning calorimetry, thermogravimetric analysis, and their crystal structures were determined by single-crystal X-ray diffraction. The solvents that form the solvates are acetonitrile, nitromethane and nitroethane (2:1 and 1:1). It was found that all the solvates lose the solvent molecules from the crystal lattice between 343 and 383 K, and that the melting point of the desolvated materials matched the melting point of the solvent-free GF (493 K). The conformation of the GF molecule in solvent-free form was found to be significantly different from the conformations found in the solvates. Solution stability studies revealed that the GF–acetonitrile solvate transforms to GF and that GF–nitroethane (1:1) solvate transforms to GF–nitroethane (2:1) solvate. On the other hand, GF–nitromethane and GF–nitroethane (2:1) solvates were found to be stable in solution. Our results highlight the importance of the co-crystallization technique in the pharmaceutical drug development; it not only expands the solid form diversity but also creates new avenues for unraveling novel solvates.

scholarly journals Fluconazole-tartaric acid co-crystal formation and its mechanical properties

2021 ◽  
pp. 116-122
Author(s):  
Fikri Alatas ◽  
Nia Suwartiningsih ◽  
Hestiary Ratih ◽  
Titta Hartyana Sutarna
Keyword(s):  
Mechanical Properties ◽  
Tartaric Acid ◽  
Crystal Morphology ◽  
Active Pharmaceutical Ingredient ◽  
Raw Material ◽  
Molar Ratio ◽  
Crystal Formation ◽  
Polarization Microscopy ◽  
Scanning Calorimetry ◽  
Pxrd Pattern

Introduction: The formation of co-crystal is widely studied to obtain more favourable physicochemical properties than the pure active pharmaceutical ingredient (API). The co-crystal formation between an anti-fungal drug, fluconazole (FLU), and tartaric acid (TAR) has been investigated and its impact on mechanical properties has also been studied. Methods: The co-crystal of FLU-TAR (1:1) molar ratio was prepared by ultrasound-assisted solution co-crystallization (USSC) method with ethanol as the solvent. Polarization microscopy was used to observe the crystal morphology. Meanwhile, powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC) methods were used to characterise the co-crystal formation. The mechanical properties of the co-crystal, such as flowability and tablet-ability, were compared with pure FLU. Results: Photomicroscopes revealed the unique crystal morphology of the USSC product was different from the two starting components. The typical PXRD pattern was shown by the USSC product, which indicated the formation of FLU-TAR co-crystal. In addition, the DSC thermogram revealed 169.2°C as the melting point of the FLU-TAR co-crystal, which is between the melting points of FLU and TAR. It indicates that FLU-TAR co-crystal has better flowability and tablet-ability than pure FLU. Conclusion: FLU-TAR co-crystal is one of the alternative solid forms for a raw material in pharmaceutical tablet preparation because it has better mechanical properties than pure fluconazole.

Development and Characterization of Aspirin-Phospholipid Complex for Improved Drug Delivery

2010 ◽  
Vol 3 (2) ◽  
pp. 940-947 ◽  
Author(s):  
A Semalty ◽  
M Semalty ◽  
D Singh ◽  
M S M Rawat
Keyword(s):  
In Vitro Dissolution ◽  
Molar Ratio ◽  
X Ray Diffraction ◽  
Phospholipid Complex ◽  
Scanning Calorimetry ◽  
Dissolution Study ◽  
Drug Content ◽  
Poorly Soluble ◽  
Gi Toxicity

Aspirin (acetylsalicylic acid) is one of the most widely used analgesic.  Aspirin is poorly soluble in water and causes gastrointestinal (GI) irritation. To improve the solubility (and hence the bioavailability) and minimize the GI irritation, its complexes with soya-phospholipid-80 % (in  1: 1 molar ratio) were prepared in an organic solvent and evaluated for solubility, drug content, scanning electron microscopy (SEM), FT-IR spectra, X ray diffraction, differential scanning calorimetry (DSC) and in vitro dissolution study. Aspirin-phospholipid complex were found to be disc shaped with rough surface in SEM. Drug content in the complex was found to be 95.6 %. DSC thermograms, XRD and FTIR confirmed the formation of phospholipid complex. Solubility of the prepared complex was found to be improved. Aspirin complex and aspirin showed 90.93 % and 69.42 % of drug release at the end of 10 h in dissolution study in pH 1.2 acid buffer. It was concluded that the phospholipid complex of aspirin may be of potential use for improving the solubility of aspirin and hence its bioavailability. The complexes may also reduce GI toxicity of the drug.  

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