scholarly journals Mechanochemical Synthesis and Physicochemical Characterization of Previously Unreported Praziquantel Solvates with 2-Pyrrolidone and Acetic Acid

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1606
Author(s):  
Debora Zanolla ◽  
Lara Gigli ◽  
Dritan Hasa ◽  
Michele R. Chierotti ◽  
Mihails Arhangelskis ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Water Solubility ◽  
Physicochemical Characterization ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Pxrd Pattern ◽  
Intrinsic Dissolution ◽  
Ft Ir ◽  
Biopharmaceutical Properties

Two new solvates of the widely used anthelminthic Praziquantel (PZQ) were obtained through mechanochemical screening with different liquid additives. Specifically, 2-pyrrolidone and acetic acid gave solvates with 1:1 stoichiometry (PZQ-AA and PZQ-2P, respectively). A wide-ranging characterization of the new solid forms was carried out by means of powder X-ray diffraction, differential scanning calorimetry, FT-IR, solid-state NMR and biopharmaceutical analyses (solubility and intrinsic dissolution studies). Besides, the crystal structures of the two new solvates were solved from their Synchrotron-PXRD pattern: the solvates are isostructural, with equivalent triclinic packing. In both structures acetic acid and 2-pyrrolidone showed a strong interaction with the PZQ molecule via hydrogen bond. Even though previous studies have shown that PZQ is conformationally flexible, the same syn conformation as the PZQ Form A of the C=O groups of the piperazinone-cyclohexylcarbonyl segment is involved in these two new solid forms. In terms of biopharmaceutical properties, PZQ-AA and PZQ-2P exhibited water solubility and intrinsic dissolution rate much greater than those of anhydrous Form A.

scholarly journals THE PHYSICOCHEMICAL CHARACTERISTICS OF RECYCLED-PLASTIC PELLETS OBTAINED FROM DISPOSABLE FACE MASK WASTES

2021 ◽  
Vol 23 (1) ◽  
pp. 16
Author(s):  
Vienna Saraswaty ◽  
Rossy Choerun Nissa ◽  
Bonita Firdiana ◽  
Akbar Hanif Dawam Abdullah
Keyword(s):  
Tensile Strength ◽  
Physicochemical Characterization ◽  
Face Mask ◽  
Physicochemical Characteristics ◽  
Scanning Calorimetry ◽  
Elongation At Break ◽  
Ft Ir ◽  
The Government ◽  
Plastic Pellets

THE PHYSICOCHEMICAL CHARACTERISTICS OF RECYCLED-PLASTIC PELLETS OBTAINED FROM DISPOSABLE FACE MASK WASTES. The government policy to wear a face mask during the COVID-19 pandemic has increased disposable face mask wastes. Thus, to reduce such wastes, it is necessary to evaluate the physicochemical characteristics of disposable face masks wastes before the recycling process and the recycled products. In this study, physicochemical characterization of the 3-ply disposable face masks and the recycled plastic pellets after disinfection using 0.5% v/v sodium hypochlorite were evaluated. A set of parameters including the characterization of surface morphology by a scanning electron microscope (SEM), functional groups properties by a fourier transform infra-red spectroscopy (FT-IR), thermal behavior by a differential scanning calorimetry (DSC), tensile strength and elongation at break were evaluated. The surface morphological of each layer 3-ply disposable face mask showed that the layers were composed of non-woven fibers. The FT-IR evaluation revealed that 3-ply disposable face mask was made from a polypropylene. At the same time, the DSC analysis found that the polypropylene was in the form of homopolymer. The SEM analysis showed that the recycled plastic pellets showed a rough and uneven surface. The FT-IR, tensile strength and elongation at break of the recycled plastic pellets showed similarity with a virgin PP type CP442XP and a recycled PP from secondary recycling PP (COPLAST COMPANY). In summary, recycling 3-ply disposable face mask wastes to become plastic pellets is recommended for handling disposable face mask wastes problem.

Preparation and characterization of titanium—segmented polyurethane composites for bone tissue engineering

2018 ◽  
Vol 33 (1) ◽  
pp. 11-22 ◽  
Author(s):  
Fernando Javier Aguilar-Perez ◽  
Rossana Vargas-Coronado ◽  
Jose Manuel Cervantes-Uc ◽  
Juan Valerio Cauich-Rodriguez ◽  
Raul Rosales-Ibañez ◽  
...  
Keyword(s):  
Stem Cells ◽  
Dental Pulp ◽  
Soft Segment ◽  
Physicochemical Characterization ◽  
Dental Pulp Stem Cells ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Human Dental Pulp ◽  
Polyurethane Composites

Segmented polyurethanes were prepared with polycaprolactone diol as soft segment and 4,4-methylene-bis cyclohexyl diisocyanate and l-glutamine as the rigid segment. These polyurethanes were filled with 1 wt.% to 5 wt.% titanium particles (Ti), physicochemically characterized and their biocompatibility assessed using human dental pulp stem cells and mice osteoblasts. Physicochemical characterization showed that composites retained the properties of the semicrystalline polyurethane as they exhibited a glass transition temperature (Tg) between −35°C and −45°C, melting temperature (Tm) at 52°C and crystallinity close to 40% as determined by differential scanning calorimetry. In agreement with this, X-ray diffraction showed reflections at 21.3° and 23.6° for polycaprolactone diol and reflections at 35.1°, 38.4°, and 40.2° for Ti particles suggesting that these particles are not acting as nucleating sites. The addition of up to 5 wt.% of Ti reduced both, tensile strength and maximum strain from 1.9 MPa to 1.2 MPa, and from 670% to 172% for pristine and filled polyurethane, respectively. Although there were differences between composites at low strain rates, no significant differences in mechanical behavior were observed at higher strain rate where a tensile stress of 8.5 MPa and strain of 223% were observed for 5 wt.% composites. The addition to titanium particles had a beneficial effect on both human dental pulp stem cells and osteoblasts viability, as it increased with the amount of titanium in composites up to 10 days of incubation.

Structures and physicochemical properties of vortioxetine salts

2016 ◽  
Vol 72 (5) ◽  
pp. 723-732 ◽  
Author(s):  
Xinbo Zhou ◽  
Xiurong Hu ◽  
Suxiang Wu ◽  
Jiali Ye ◽  
Mengying Sun ◽  
...  
Keyword(s):  
Antidepressant Drug ◽  
Drug Candidate ◽  
X Ray Diffraction ◽  
High Solubility ◽  
Scanning Calorimetry ◽  
Intrinsic Dissolution ◽  
X Ray ◽  
Acidic Proton ◽  
Water Ph ◽  
Ft Ir

In the present work, novel salts of the multimodal antidepressant drug vortioxetine (VT) were crystallized with pharmaceutically acceptable acids, aiming to improve the solubility of VT. The acids for VT were selected based on ΔpKabeing greater than 2 or 3. Salts of hydrobromic acid (HBr), hydrochloric acid (HCl),p-hydroxybenzoic acid (PHBA), saccharin (SAC) and L-aspartic acid (ASP) were reported. All salts were characterized by single-crystal X-ray diffraction, FT–IR, powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC). The acidic proton is transferred to the secondary N atom on the piperazine ring of VT, forming the charge-assisted hydrogen bond N+—H...X−(X= Cl, Br, O). Solubility and intrinsic dissolution rate (IDR) experiments were carried out in distilled water (pH = 7.0) to compare the solubilities of the salts with that of VT. The VT–ASP–H2O (1:1:2) salt showed 414 times higher solubility and 1722 times faster IDR compared with VT. VT–ASP–H2O (1:1:2) is a high solubility salt that is stable in a slurry experiment at 298 K in 95% ethanol. The experimental data for the VT–ASP–H2O (1:1:2) salt identify it as a promising drug candidate.

scholarly journals Development, Fabrication, and Characterization of Composite Polycaprolactone Membranes Reinforced with TiO2 Nanoparticles

Polymers ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 1955 ◽  
Author(s):  
Karina del Ángel-Sánchez ◽  
César I. Borbolla-Torres ◽  
Luis M. Palacios-Pineda ◽  
Nicolás A. Ulloa-Castillo ◽  
Alex Elías-Zúñiga
Keyword(s):  
Acetic Acid ◽  
Titanium Dioxide Nanoparticles ◽  
Sol Gel ◽  
Tensile Tests ◽  
Experimental Characterization ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
The One

This paper focuses on developing, fabricating, and characterizing composite polycaprolactone (PCL) membranes reinforced with titanium dioxide nanoparticles (NPs) elaborated by using two solvents; acetic acid and a mixture of chloroform and N,N-dimethylformamide (DMF). The resulting physical, chemical, and mechanical properties of the composite materials are studied by using experimental characterization techniques such as scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier-transform infrared (FTIR) analysis, contact angle (CA), uniaxial and biaxial tensile tests, and surface roughness measurements. Experimental results show that the composite material synthesized by sol-gel and chloroform-DMF has a better performance than the one obtained by using acetic acid as a solvent.

Preparation and characterization of pure and copper-doped PVC films

2017 ◽  
Vol 37 (1) ◽  
pp. 83-92 ◽  
Author(s):  
K. Bhagya Sree ◽  
Y. Madhava Kumar ◽  
N.O. Gopal ◽  
Ch. Ramu
Keyword(s):  
Polymer Film ◽  
Polymer Films ◽  
Dopant Concentration ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Bending Vibrations ◽  
Paramagnetic Resonance ◽  
Solution Cast ◽  
Ft Ir

Abstract Pure and Cu2+-doped polyvinyl chloride (PVC) polymer films were prepared using the solution cast technique. Investigations were conducted using DSC, TGA, XRD, FT-IR, UV–Vis, SEM and EPR. Differential scanning calorimetry studies suggested that the Cu2+ samples have higher values of the glass transition (Tg) temperature, and thermo gravimetric studies show that weight loss of polymer film indicates the improved thermal stability of the polymer film. The features of the complexation of the polymer films were studied by X-ray diffraction. FT-IR spectra exhibits the bands in three regions, which are attributed to C–Cl, C–C and numerous CH groups of stretching and bending vibrations. The absorption spectra have been recorded in the wavelength range 200–900 nm. The absorption edge, direct bandgap, indirect bandgap and urbach energy have been evaluated. Film morphology was examined by scanning electron microscopy. XRD, DSC and SEM reveal the amorphous nature and surface morphology of polymer films, respectively. Electron paramagnetic resonance studies were used to calculate the number of spins and paramagnetic susceptibility as a function of dopant concentration, all the Cu2+-doped PVC samples exhibit signal with g values g⊥=2.176 and g||=2.254. The observed variation in the EPR signal intensity is due to variation in the dopant concentration.

scholarly journals Two Novel Palbociclib-Resorcinol and Palbociclib-Orcinol Cocrystals with Enhanced Solubility and Dissolution Rate

Pharmaceutics ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 23
Author(s):  
Chenxin Duan ◽  
Wenwen Liu ◽  
Yunwen Tao ◽  
Feifei Liang ◽  
Yanming Chen ◽  
...  
Keyword(s):  
Water Solubility ◽  
Cancer Drug ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Dissolution Rates ◽  
Intrinsic Dissolution ◽  
X Ray ◽  
Enhanced Solubility

Palbociclib (PAL) is an effective anti-breast cancer drug, but its use has been partly restricted due to poor bioavailability (resulting from extremely low water solubility) and serious adverse reactions. In this study, two cocrystals of PAL with resorcinol (RES) or orcinol (ORC) were prepared by evaporation crystallization to enhance their solubility. The cocrystals were characterized by single crystal X-ray diffraction, Hirshfeld surface analysis, powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared and scanning electron microscopy. The intrinsic dissolution rates of the PAL cocrystals were determined in three different dissolution media (pH 1.0, pH 4.5 and pH 6.8), and both cocrystals showed improved dissolution rates at pH 1.0 and pH 6.8 in comparison to the parent drug. In addition, the cocrystals increased the solubility of PAL at pH 6.8 by 2–3 times and showed good stabilities in both the accelerated stability testing and stress testing. The PAL-RES cocrystal also exhibited an improved relative bioavailability (1.24 times) than PAL in vivo pharmacokinetics in rats. Moreover, the in vitro cytotoxicity assay of PAL-RES showed an increased IC50 value for normal cells, suggesting a better biosafety profile than PAL. Co-crystallization may represent a promising strategy for improving the physicochemical properties of PAL with better pharmacokinetics.

scholarly journals DEVELOPMENT OF AMORPHOUS BINARY AND TERNARY SOLID DISPERSIONS OF NATEGLINIDE FOR IMPROVED SOLUBILITY AND DISSOLUTION

2020 ◽  
pp. 106-112
Author(s):  
SHRADHA S. TIWARI ◽  
SHAILESH J. WADHER ◽  
SURENDRA G. GATTANI
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Dissolution Behavior ◽  
Enhanced Solubility ◽  
Ft Ir ◽  
Ternary Solid Dispersion ◽  
Ternary Solid Dispersions

Objective: Nateglinide is a commonly used oral hypoglycemic, biopharmaceutical classification system Class II drug, which shows relatively poor water solubility and variable bioavailability. The objective of the present investigation was to develop the binary and ternary solid dispersions of nateglinide for improved solubility and dissolution. Methods: Nateglinide solid dispersions were prepared by a common solvent evaporation method. Polymers like soluplus, kolliphor P188, sylloid 244FP, gelucire 48/16, affinisol (HPMCAS), HPβCD, βCD were used in different combinations. The physicochemical characterization of the optimized ternary dispersion was studied by using FT-IR, DSC, and PXRD. Solubility and dissolution behavior of all dispersions were studied. Result: From all prepared ternary solid dispersions, nateglinide dissolution was significantly faster than pure nateglinide. With ternary solid dispersion of NTG, soluplus and kolliphor P188 there was a big improvement in solubility and dissolution. This combination enhanced the solubility of NTG by 23 folds. Another ternary dispersion of NTG with soluplus and gelucire 48/16 enhanced solubility by 25 fold. Conclusion: Ternary solid dispersion found superior over binary dispersions. For the ternary dispersions, showing the best solubility, tablets were prepared. Dissolution and drug release from the formulated tablet was as good as a marketed product.

Preparation and Physicochemical Characterization of Magnetic Composite: CuFe2O4 / Layered Double Hydroxide

2014 ◽  
Vol 955-959 ◽  
pp. 47-50
Author(s):  
Dan Chen ◽  
Xiao Long Ma
Keyword(s):  
Layered Double Hydroxide ◽  
Spinel Ferrite ◽  
Sol Gel ◽  
Physicochemical Characterization ◽  
Magnetic Composite ◽  
X Ray Diffraction ◽  
Microwave Hydrothermal ◽  
Ft Ir ◽  
Double Hydroxide

We fabricated new magnetic material CuFe2O4/Zn2Cr-LDH by the combination of CuFe2O4 and layered double hydroxide (LDH) through two steps. CuFe2O4 was prepared by sol-gel method with the assistant of citric acid, which was used in synthesis of the composite via microwave hydrothermal method subsequently. The physicochemical properties of the composite was characterized by several techniques, such as X-ray diffraction (XRD), Fourier transform infrared (FT-IR) spectroscopy, Vibrating sample magnetometer (VSM) and Thermogravimetry-differential thermal analysis (TG-DTA). The magnetic composite reveals several advantage of LDH structure and spinel ferrite oxide and is potential for the application of heterogeneous catalysis.

scholarly journals CHARACTERIZATION OF DRUGS ENCAPSULATED INTO MESOPOROUS SILICA

2019 ◽  
pp. 7-11
Author(s):  
ARIF BUDIMAN
Keyword(s):  
Water Solubility ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Molecular State ◽  
Water Soluble ◽  
Crystal Nucleation ◽  
Formulation Development ◽  
Scanning Calorimetry

Solubility of the drug has a strong influence to achieve higher bioavailability of the drug in systemic circulation. More than 70% NCEs (new chemical entities) are hydrophobic, and practically difficult into solid formulation due to their poor water solubility. Mesoporous silicas (MSP) have been used for drug delivery system, especially for poorly water-soluble drugs. Encapsulation and interaction of drugs in MSP can enhance the delivery and maintain the stability of the drug. However, the characterization of the drug in MSP is necessary to confirm its molecular state. In this review, we present an overview of reports related to the characterization of drug encapsulated into MSP. Encapsulation of drugs in MSP can prevent recrystallization of drugs due to its inhibition of crystal nucleation. A porous material in MSP can maintain the drug in a physically stable amorphous state. The preventing of drug crystallization in MSP can enhance the solubility and the dissolution rate of drug. Therefore, in this work, attempts have been made to understand the molecular state of the drug in MSP. The physicochemical characterization of drug by transmission electron microscopy (TEM), scanning electron microscope (SEM), differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FTIR), powder x-ray diffraction (PXRD) and thermogravimetric analysis (TGA) were discussed. The effect of solvent and methods of drug loading and the effect of the shape of MSP on release profiles are also presented. Overall, this review provides information about the characterization of drug encapsulated into MSP which will be useful in pharmaceutical formulation development.

scholarly journals ENHANCEMENT OF GLIBENCLAMIDE DISSOLUTION RATE BY SOLID DISPERSION METHOD USING HPMC AND PVP

2019 ◽  
pp. 19-24 ◽  
Author(s):  
ARIF BUDIMAN ◽  
IYAN SOPYAN ◽  
DENIA SEPTY RIYANDI
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Rate Test ◽  
Ft Ir

Objective: The aim of this study was to investigate the effects of changing in the proportions of the solid dispersion formula on the dissolution rate of glibenclamide. Methods: Solid dispersions were prepared by solvent evaporation method by using methanol as solvent, hydroxypropyl methylcellulose (HPMC) and polyvinyl pyrrolidone (PVP) as polymers. The prepared product was evaluated by the saturated solubility test and the dissolution rate test. The prepared product was characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) and Scanning Electron Microscopy (SEM). Results: The result showed solid dispersion with a ratio of glibenclamide: PVP: HPMC (1: 3: 6) has the highest increase in solubility (20 fold) compared to pure glibenclamide. This formula also showed an improvement in dissolution rate from 19.9±1.19% (pure glibenclamide) to 99±1.60% in 60 min. Characterization of FT-IR showed that no chemical reaction occurred in solid dispersion of glibenclamide. The results of X-ray diffraction analysis showed an amorphous form in all solid dispersion formulas. The results of DSC analysis showed that endothermic peak melting point of solid dispersion occurred, and the morphology of solid dispersion was more irregular than pure glibenclamide based on SEM characterization Conclusion: The solid dispersion of glibenclamide using PVP: HPMC as carriers can increase the solubility and dissolution rate compared to pure glibenclamide.

Sign in / Sign up

Export Citation Format

Share Document