scholarly journals Study of Different Crystal Habits of Aprepitant: Dissolution and Material Attributes

2021 ◽  
Vol 11 (12) ◽  
pp. 5604
Author(s):  
Satyajit R. Datir ◽  
Dinesh Kumar ◽  
Pradeep Kumar ◽  
Sanyog Jain ◽  
Arvind Kumar Bansal ◽  
...  
Keyword(s):  
Flow Property ◽  
Crystal Habit ◽  
Dissolution Profile ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Tabular Crystal ◽  
Characterization Studies ◽  
Strength And Plasticity ◽  
Habit Modification ◽  
Better Than

In the present study, aprepitant (APT) was selected to find its suitable crystal habit, which can improve its existing poor dissolution and manufacturing processability. Solvents were screened out for solubility analysis of APT and further crystal habit modification. Solid-state characterization studies like powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and Fourier infrared spectroscopy (FTIR) distinguished that tabular crystal habit was generated from acetone (APT-AC) and long tabular crystal habit was generated from ethyl acetate (APT-EA). Kawakita analysis and powder flow property studies showed that APT-EA is cohesive, has poor flow property and low bulk density compared to APT-AC (p < 0.05). Heckel plots reflected that APT-EA shows higher fragmentation and particle rearrangement during the initial stages as indicated by the higher intercept values. Higher slopes in APT-EA and APT-AC confirmed better plasticity but lower yield pressure in APT-AC proved good plastic deformation compared to APT-EA (p < 0.05). The dissolution profile of the APT-EA was found to be better than that of APT-AC. Overall, it can be concluded that APT-AC crystal habit has a better flow rate, tensile strength, and plasticity whereas APT-EA has better dissolution.

scholarly journals Tuning the Crystal Habits of Organic Explosives by Antisolvent Crystallization: The Case Study of 2,6-dimaino-3,5-dinitropyrazine-1-oxid (LLM-105)

Crystals ◽  
2019 ◽  
Vol 9 (8) ◽  
pp. 392 ◽  
Author(s):  
Xiaoqing Zhou ◽  
Junhui Shan ◽  
Dong Chen ◽  
Hongzhen Li
Keyword(s):  
Methylene Chloride ◽  
Crystal Habit ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Crystallization Experiments ◽  
Antisolvent Crystallization ◽  
Ft Ir ◽  
Habit Modification

Crystallization is one of the most important methods in the crystal habit control of explosive products. For this study, the antisolvent crystallization experiments were carried out to tune the crystal habits of 2,6-dimaino-3,5-dinitropyrazine-1-oxid (LLM-105). Dimethyl sulphoxide (DMSO) was used as an organic solvent. Water, methanol, acetic acid, nitromethane, acetone, ethanol, methylene chloride, o-dichlorobenzene, and toluene were selected as antisolvents. The X-shaped, spherical cluster-like, rod-like, needle-like, and dendritic crystals were successfully produced by varying the kind of the antisolvent. These results manifested that the polarity and functional groups of antisolvent molecules played important roles in the crystal habits of LLM-105 explosive. The powder X-ray diffraction (PXRD) and Fourier transform infrared (FT-IR) measurements indicated that these antisolvents just tuned the crystal habit of LLM-105 but did not change the crystal structure. The differential scanning calorimetry (DSC) and thermogravimetry (TG) results of the obtained crystals showed that the crystal habits significantly affected the thermal properties. This study can contribute to the investigation of the mechanism of antisolvent-induced crystal habit modification and screen out the efficient antisolvents.

Glibenclamide-Nicotinamide Cocrystals Synthesized by The Solvent Evaporation Method to Enhance Solubility and Dissolution Rate of Glibenclamide

2019 ◽  
Vol 9 (01) ◽  
pp. 21-26
Author(s):  
Arif Budiman ◽  
Ayu Apriliani ◽  
Tazyinul Qoriah ◽  
Sandra Megantara
Keyword(s):  
Solvent Evaporation ◽  
Physical Mixture ◽  
Dissolution Profile ◽  
Solvent Evaporation Method ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Evaporation Method ◽  
Dissolution Properties ◽  
Mixture Characterization

Purpose: To develop glibenclamide-nicotinamide cocrystals with the solvent evaporation method and evaluate their solubility and dissolution properties. Methods: Cocrystals of glibenclamide-nicotinamide (1:2) were prepared with the solvent evaporation method. The prediction of interactive cocrystals was observed using in silico method. The solubility and dissolution were performed as evaluation of cocrystals. The cocrystals also were characterized by differential scanning calorimetry (DSC), infrared spectrophotometry, and powder X-ray diffraction (PXRD). Result: The solubility and dissolution profile of glibenclamide-nicotinamide cocrystal (1:2) increased significantly compared to pure glibenclamide as well as its physical mixture. Characterization of cocrystal glibenclamide-nicotinamide (1:2) including infrared Fourier transform, DSC, and PXRD, indicated the formation of a new solid crystal phase differing from glibenclamide and nicotinamide. Conclusion: The confirmation of cocrystal glibenclamide-nicotinamide (1:2) indicated the formation of new solid crystalline phases that differ from pure glibenclamide and its physical mixture

scholarly journals Development of a Solid Dispersion of Nystatin with Maltodextrin as a Carrier Agent: Improvements in Antifungal Efficacy against Candida spp. Biofilm Infections

2021 ◽  
Vol 14 (5) ◽  
pp. 397
Author(s):  
Carlos Benavent ◽  
Carlos Torrado-Salmerón ◽  
Santiago Torrado-Santiago
Keyword(s):  
Antifungal Activity ◽  
Solid Dispersions ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Candida Spp ◽  
Microbiological Techniques ◽  
Characterization Studies ◽  
Candida Albicans Biofilms

The aim of this study was to improve the treatment of Candida albicans biofilms through the use of nystatin solid dispersions developed using maltodextrins as a hyperosmotic carrier. Characterization studies by differential scanning calorimetry, X-ray diffraction, dissolution studies, and particle size analysis were performed to evaluate changes in nystatin crystallinity. Antifungal activity and anti-biofilm efficacy were assessed by microbiological techniques. The results for nystatin solid dispersions showed that the enhancement of antifungal activity may be related to the high proportions of maltodextrins. Anti-biofilm assays showed a significant reduction (more than 80%) on biofilm formation with SD-N:MD [1:6] compared to the nystatin reference suspension. The elaboration process and physicochemical properties of SD-N:MD [1:6] could be a promising strategy for treatment of Candida biofilms.

scholarly journals EFFECT OF SELECTED POLYMERS ON DISSOLUTION AND STABILIZATION OF AMORPHOUS FORM OF MELOXICAM

2017 ◽  
Vol 9 (9) ◽  
pp. 33
Author(s):  
Rana Obaidat ◽  
Bashar Al-taani ◽  
Hanan Al-quraan
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersions ◽  
Dissolution Profile ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Polyethylene Glycol 4000 ◽  
Amorphous Form ◽  
Molecular Weights ◽  
Low Solubility ◽  
Reproducible Manner

Objective: Meloxicam is classified as class II corresponding to its high permeability and low solubility (12μg/ml). This study aims to compare the effect of selected polymers on stabilization of amorphous form, and dissolution of meloxicam by preparation of different solid dispersions using selected polymers (chitosan oligomers, polyvinylpyrrolidone K30, and polyethylene glycols).Methods: These solid dispersions were prepared using two different methods; solvent evaporation method for the two molecular weights chitosan carriers (16 and 11KDa) and polyvinylpyrrolidone-K30 and melting method for the two different molecular weights polyethylene glycol (4000 and 6000). The physicochemical properties of solid dispersions were analyzed using differential scanning calorimetry, Fourier transform infra-red analysis, Powder X-ray diffraction, and scanning electron microscopy. Selected dispersions were then compared to two selected marketed drugs (Mobic® and Moven®).Results: Best dissolution rates were obtained for both polyvinylpyrrolidone-K30 and polyethylene glycol 6000, followed by chitosan 16 kDa, chitosan 11 kDa, and polyethylene glycol 4000. Increasing polymeric ratio increased dissolution rate except for chitosan. Precipitation of the drug as amorphous form occurred in chitosan and polyvinylpyrrolidone-K30 dispersions, while no change in crystallinity obtained for polyethylene glycol dispersions. Failure of polyvinylpyrrolidone-K30 in the maintenance of stability during storage time was observed while re-crystallization occurred in chitosan-based dispersions, which ends with preferences to polyethylene glycol dispersions. After comparing the release of selected dispersions with the two selected polymers; all dispersions got a higher release than that of the two marketed drugs release.Conclusion: The dissolution profile of meloxicam has been increased successfully in a reproducible manner.

scholarly journals Structure, Optical, and Thermal Properties of 9, 10-diphenylanthracene Crystals

Crystals ◽  
2019 ◽  
Vol 9 (10) ◽  
pp. 512 ◽  
Author(s):  
Liu ◽  
Zhu ◽  
Hu ◽  
Dong ◽  
Tan
Keyword(s):  
Single Crystal ◽  
Emission Wavelength ◽  
Molecular Formula ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Cell Parameters ◽  
Lattice Constants ◽  
Solution Methods ◽  
Fast Neutron Detection ◽  
Better Than

9,10-diphenylanthracene (DPA) single crystal is a promising scintillator material for fast-neutron detection. Two centimetre-sized polymorph crystals of DPA were grown by melting and solution methods (DPA-Melt and DPA-Solution, respectively), and characterised by single-crystal X-ray diffraction, Raman spectroscopy, Fourier-transform infrared spectroscopy, fluorescence spectroscopy, UV-Vis absorbance spectroscopy, and thermogravimetric/differential scanning calorimetry. The DPA-Melt crystal possessed a P21/n structure, with excitation bands at approximately 331, 348, 367, and 387 nm, and the strongest emission wavelength at approximately 454 nm. On the other hand, the DPA-Solution crystal possessed a C2/c structure, with excitation bands at approximately 335, 353, 372, and 396 nm, and the strongest emission wavelength at approximately 468 nm. The two kinds of DPA crystals have the same molecular formula but different crystal structures, crystal lattice constants, and cell parameters. The theoretical density of the DPA-Solution crystal was 1.239 g/cm3, while that of the DPA-Melt crystal was 1.211 g/cm3. The two types of crystals exhibited the same melting point, but the thermal stability of the DPA-Solution crystal is better than that of the DPA-Melt crystal.

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.

Development of Pediatric Orodispersible Tablets Based on Efavirenz as a New Therapeutic Alternative

2020 ◽  
Vol 18 (5) ◽  
pp. 342-353
Author(s):  
José Lourenço de Freitas Neto ◽  
Ilka do Nascimento Gomes Barbosa ◽  
Camila Gomes de Melo ◽  
Matheus Alves Ângelos ◽  
Larissa Morgana dos Santos Mendes ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Aqueous Solubility ◽  
Dissolution Profile ◽  
Multicomponent Systems ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
Immunodeficiency Syndrome

Background: Efavirenz is the most used medication in the treatment of Acquired Immunodeficiency Syndrome (AIDS). The limited number of pediatric antiretroviral formulations approved by regulatory agencies is the most significant obstacle to adequate and efficient pharmacotherapy for this group of patients. The efavirenz has excellent therapeutic potential, but has low aqueous solubility/bioavailability. Methods: To minimize these limitations, multicomponent systems with β-cyclodextrin and polyvinylpyrrolidone K-30 were obtained. Due to the limited number of pediatric antiretroviral formulations, the development of a pediatric orodispersible tablet is an alternative that is thought easy to administer, since it disintegrates rapidly in the oral cavity. The multicomponent systems were obtained by the method of kneading and characterized by solubility test, X-ray diffraction, differential scanning calorimetry and infrared absorption spectroscopy by Fourier transform. The orodispersible tablets were prepared by direct compression. The quality control of hardness, friability, disintegration, and dissolution was performed. The influence of the components of the formulation on the characteristics of the tablets was evaluated through a 22 factorial design added with three central points, to compare the effect of the dependent variables on the responses. Results: An increase in drug solubility was observed, with a decrease in crystallinity. Besides that, an excellent dissolution profile presented with more than 83% of the drug's content dissolved in less than 15 minutes. Satisfactory disintegration time and friability were observed. Conclusion: It was observed that reduced concentrations of mannitol decreased the hardness and disintegration time of the formulations. The orodispersible tablet composed of efavirenz: β- cyclodextrin: polyvinylpyrrolidone, favors greater absorption and bioavailability. It has several advantages for pediatric patients, as the dosage form disintegrates quickly in the mouth and does not require water for administration, thereby improving patient compliance with the treatment.

scholarly journals Development, characterization and evaluation of the dissolution profile of sulfasalazine suspensions

2015 ◽  
Vol 51 (2) ◽  
pp. 449-459 ◽  
Author(s):  
Mayre Aparecida Borges da Costa ◽  
Ana Lucia Vazquez Villa ◽  
Rita de Cássia da Silva Ascenção Barros ◽  
Eduardo Ricci-Júnior ◽  
Elisabete Pereira dos Santos
Keyword(s):  
Particle Size ◽  
Size Distribution ◽  
Inflammatory Diseases ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Neutral Media ◽  
Sedimentation Volume

<p>This paper reports the development, characterization and <italic>in vitro</italic>dissolution behavior of sulfasalazine suspensions for treatment of chronic intestinal inflammatory diseases. Three formulations were developed, from powdered sulfasalazine obtained from different suppliers. The sulfasalazine was characterized regarding concentration, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), particle size distribution, polydispersion and solubility. The suspensions were developed and characterized regarding pH, viscosity, density, particle size, sedimentation volume, concentration and dissolution. The pH values were slightly acidic. The method of preparing the suspensions reduced the particle sizes and made the size distribution more homogeneous. The dissolution studies showed that the sulfasalazine suspensions had low solubility in acidic media, but dissolve quickly, reaching levels of 85%, in neutral media or media containing 0.5% of surfactants such as polysorbate 80. Besides this, the sulfasalazine suspensions were classified as having immediate dissolution because they reached dissolution levels near 100% in 20 minutes.</p>

Effect of Montmorillonite Content on Nucleation of Polypropylene

2013 ◽  
Vol 664 ◽  
pp. 538-542 ◽  
Author(s):  
Onusa Saravari ◽  
Phanitnan Srisuwan ◽  
Noppadon Kerddonfag ◽  
Wannee Chinsirikul
Keyword(s):  
Crystal Structure ◽  
Wide Angle ◽  
Melt Blending ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Nucleation Effect ◽  
Blending Process ◽  
Internal Mixer ◽  
Better Than

In this article, the effect of montmorillonite (MMT) concentration on the nucleation of polypropylene (PP) was investigated. The PP/MMT nanocomposites containing various content of MMT (0.075-3.0 wt%) were prepared by a melt blending process using an internal mixer, followed by compression molding into sheets. The nucleation effect of MMT was characterized by X-ray diffraction (XRD), wide angle X-ray diffraction (WAXD) and differential scanning calorimetry (DSC) techniques. XRD results indicated that the PP nanocomposites loaded with less than 1.5 wt% of MMT formed an exfoliated structure. DSC results showed that the crystallization temperature (Tc) of PP/MMT nanocomposites were higher than that of neat PP. Tc also increased with increasing MMT content, indicating that MMT was effective in nucleating PP crystal. WAXD patterns revealed that the addition of MMT did not affect the crystal structure of PP. Mechanical property tests showed that the tensile and impact strengths of the PP/MMT nanocomposites were better than those of neat PP when the MMT content was lower than 1.5 wt%.

scholarly journals Co-crystallization of quercetin and isonicotinamide using solvent evaporation method

2021 ◽  
Vol 18 (4) ◽  
pp. 697-702
Author(s):  
Budipratiwi Wisudyaningsih ◽  
Dwi Setyawan ◽  
Siswandono
Keyword(s):  
Minimum Energy ◽  
Solvent Evaporation ◽  
Crystal Habit ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Dissolution Profile ◽  
Solvent Evaporation Method ◽  
Scanning Calorimetry ◽  
Evaporation Method

Purpose: To obtain quercetin-isonicotinamide co-crystal (CQINA) with improved physicochemical and in-vitro dissolution characteristics. Methods: Co-crystallization of quercetin (Q) and isonicotinamide (INA) in molar ratio of 1:1 was performed using solvent evaporation method with the addition of 50 mL of ethanol (99.9%, v/v). The resultant solution was thoroughly mixed and stirred at room temperature for 48 h to slowly evaporate the solvent until CQINA was obtained. The co-crystal phase was characterized using differential scanning calorimetry (DSC), powder x-ray diffractometry (PXRD), scanning electron microscopy (SEM), and fourier transform infrared (FTIR) spectroscopy. In-vitro dissolution was performed by USP method II in 900 mL citrate buffer (pH 5.0 ± 0.05), with stirring at 100 rpm and at 37 ± 0.5 °C. Results: Computational approach predicted the formation of hydrogen bonds between Q and coformers used, and the interaction involved minimum energy. In CQINA thermogram, a new endothermic peak was formed with a melting point of 255.26 °C, while Q (314.85 °C) and INA (156.62 °C). Images from DSC, PXRD, SEM and FTIR showed that the crystal habits and morphologies of the CQINA differed from those of the original components. There was an improvement in the dissolution profile of CQINA, when compared with those of the original components. Conclusion: Q and INA subjected to solvent evaporation result in the formation of a CQINA with different crystal habit, which possess physicochemical characteristics different from those of its constituents. Modification of Q crystals in CQINA increases its in vitro dissolution, making it a potential pharmaceutical agent.

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