Browse
Submit Data
Databases
API
Help

Dataset Information

20 Views

0 Connections

0 Citations

0 Reanalyses

0 Downloads

Omics score: 0

Synthesis of Celecoxib-Eutectic Mixture Particles via Supercritical CO₂ Process and Celecoxib Immediate Release Tablet Formulation by Quality by Design Approach.

ABSTRACT: Significant improvements in the wettability and dissolution rate of celecoxib (CEL), a poorly soluble selective cyclooxygenase-2 (COX-2) inhibitor, have been shown by Huyn et al., 2019 by combining the binary pharmaceutical compositions including CEL and one of the two co-formers, adipic acid (ADI) and saccharin (SAC), into eutectic mixtures (EM). Purpose: In this study, we developed a therapeutic eutectic system for CEL which is a promising approach for oral delivery to enhance bioavailability. CEL EM were synthesized by novel techniques including supercritical CO₂ techniques and new tablet formulations were purposed. Methods: CEL EM were synthesized by evaporation crystallization method, spray drying, supercritical fluid (SCF) techniques. The CEL EM particles were then characterized by differential scanning calorimetry, powder X-ray diffraction, Fourier-transform infrared spectroscopy, scanning electron microscope, and particle size analysis. Dissolution studies were carried out. With a quality by design approach, a statistical method through design of experiment and data analysis by JMP^® (SAS institute) was applied to CEL EM immediate release tablet formulation development. Results: CEL EM produced by spray drying technique, supercritical fluid (SCF) techniques were identified and characterized. The enhancement of dissolution was observed for SCF processed samples. The design space for CEL-ADI EM IR tablet and control limits for individual parameters were determined.

SUBMITTER: Hong SH

PROVIDER: S-EPMC9331714 | biostudies-literature |

REPOSITORIES: biostudies-literature

ACCESS DATA

Json Xml

Similar Datasets

Pseudo-Binary Phase Diagram of LiNH2-MH (M = Na, K) Eutectic Mixture.

Project description:The hunt for a cleaner energy carrier leads us to consider a source that produces no toxic byproducts. One of the targeted alternatives in this approach is hydrogen energy, which, unfortunately, suffers from a lack of efficient storage media. Solid-state hydrogen absorption systems, such as lithium amide (LiNH2) systems, may store up to 6.5 weight percent hydrogen. However, the temperature of hydrogenation and dehydrogenation is too high for practical use. Various molar ratios of LiNH2 with sodium hydride (NaH) and potassium hydride (KH) have been explored in this paper. The temperature of hydrogenation for LiNH2 combined with KH and NaH was found to be substantially lower than the temperature of individual LiNH2. This lower temperature operation of both LiNH2-NaH and LiNH2-KH systems was investigated in depth, and the eutectic melting phenomenon was observed. Systematic thermal studies of this amide-hydride system in different compositions were carried out, which enabled the plotting of a pseudo-binary phase diagram. The occurrence of eutectic interaction increased atomic mobility, which resulted in the kinetic modification followed by an increase in the reactivity of two materials. For these eutectic compositions, i.e., 0.15LiNH2-0.85NaH and 0.25LiNH2-0.75KH, the lowest melting temperature was found to be 307 °C and 235 °C, respectively. Morphological studies were used to investigate and present the detailed mechanism linked with this phenomenon.

| S-EPMC9268627 | biostudies-literature

Formation of Fine Particles from Curcumin/PVP by the Supercritical Antisolvent Process with a Coaxial Nozzle.

Project description:The production of fine particles via the supercritical carbon dioxide (SC-CO2) antisolvent process was carried out. The experiments were conducted at temperatures of 40-60 °C and pressures of 8-12 MPa with a 15 mL min-1 carbon dioxide (CO2) and 0.5 mL min-1 feed solution flow rate. As a feed solution, the curcumin and the polyvinylpyrrolidone (PVP) powder were dissolved in acetone and ethanol at concentrations of 1.0 mg mL-1 and 2.0-4.0% in weight, respectively. Scanning electron microscopy (SEM) images described that most of the precipitated particle products have spherical morphologies with a size of less than 1 ?m. The Fourier transform infrared spectroscopy (FT-IR) spectra exhibited that the curcumin structural properties did not shift after the SC-CO2 antisolvent process. Moreover, the PVP addition in the curcumin particle products can enhance the curcumin dissolution in distilled water significantly.

| S-EPMC7114885 | biostudies-literature

Optimization of process parameters for preparation of polystyrene PM2.5 particles by supercritical antisolvent method using BBD-RSM.

Project description:The objective of this study is to optimize the process parameters for preparing polystyrene (PS) PM2.5 particles by supercritical antisolvent (SAS) method. Toluene was selected as the solvent and supercritical carbon dioxide (SC-CO2) was used as the antisolvent. The Box-Behnken design-response surface method was applied to investigate the effect of crystallizer pressure, PS massic concentration, flow ratio of CO2/solution and crystallizer temperature on the size and the distribution of PS particles, systematically. It is found that crystallizer temperature is the most significant variable on the size and the distribution of PS particles, followed by flow ratio of CO2/solution and PS massic concentration, and crystallizer pressure is the slightest significant factor. The particle size increases with the increase of crystallizer temperature. The optimum conditions are obtained as crystallizer pressure 9.8 MPa, PS massic concentration 1.6 wt%, flow ratio of CO2/solution 140 g/g and crystallizer temperature 309 K. Under these conditions, the PS particle with the size of 2.78 μm and a narrow size distribution has been prepared, meeting PM2.5 standard aerosols. The results suggest that it is feasible to produce PM2.5 standard aerosols by SAS.

| S-EPMC7341738 | biostudies-literature

Design of Deep Eutectic Systems: A Simple Approach for Preselecting Eutectic Mixture Constituents.

Project description:Eutectic systems offer a wide range of new (green) designer solvents for diverse applications. However, due to the large pool of possible compounds, selecting compounds that form eutectic systems is not straightforward. In this study, a simple approach for preselecting possible candidates from a pool of substances sharing the same chemical functionality was presented. First, the melting entropy of single compounds was correlated with their molecular structure to calculate their melting enthalpy. Subsequently, the eutectic temperature of the screened binary systems was qualitatively predicted, and the systems were ordered according to the depth of the eutectic temperature. The approach was demonstrated for six hydrophobic eutectic systems composed of L-menthol and monocarboxylic acids with linear and cyclic structures. It was found that the melting entropy of compounds sharing the same functionality could be well correlated with their molecular structures. As a result, when the two acids had a similar melting temperature, the melting enthalpy of a rigid acid was found to be lower than that of a flexible acid. It was demonstrated that compounds with more rigid molecular structures could form deeper eutectics. The proposed approach could decrease the experimental efforts required to design deep eutectic solvents, particularly when the melting enthalpy of pure components is not available.

| S-EPMC7179121 | biostudies-literature

Characterization and stabilization in process development and product formulation for super large proteinaceous particles.

Project description:Super large proteinaceous particles (SLPPs) such as virus, virus like particles, and extracellular vesicles have successful and promising applications in vaccination, gene therapy, and cancer treatment. The unstable nature, the complex particulate structure and composition are challenges for their manufacturing and applications. Rational design of the processing should be built on the basis of fully understanding the characteristics of these bio-particles. This review highlights useful analytical techniques for characterization and stabilization of SLPPs in the process development and product formulations, including high performance size exclusion chromatography, multi-angle laser light scattering, asymmetrical flow field-flow fractionation, nanoparticle tracking analysis, CZE, differential scanning calorimetry, differential scanning fluorescence, isothermal titration calorimetry , and dual polarization interferometry. These advanced analytical techniques will be helpful in obtaining deep insight into the mechanism related to denaturation of SLPPs, and more importantly, in seeking solutions to preserve their biological functions against deactivation or denaturation. Combination of different physicochemical techniques, and correlation with in vitro or in vivo biological activity analyses, are considered to be the future trend of development in order to guarantee a high quality, safety, and efficacy of SLPPs.

| S-EPMC7645648 | biostudies-literature

Generation of Highly Antioxidant Submicron Particles from Myrtus communis Leaf Extract by Supercritical Antisolvent Extraction Process.

Project description:Submicron particles have been produced from an ethanolic extract of Myrtus communnis leaves using supercritical carbon dioxide technology, hereinafter referred to as Supercritical Antisolvent Extraction (SAE). The influence of pressure (9-20 MPa), temperature (308 and 328 K) and injection rate (3 and 8 mL/min) on the particles' precipitation has been investigated, and it has been confirmed that increases in pressure and temperature led to smaller particle sizes. The obtained particles had a quasi-spherical shape with sizes ranging from 0.42 to 1.32 μm. Moreover, the bioactivity of the generated particles was assessed and large contents of phenolic compounds with a high antioxidant activity were measured. The particles were also subjected to in vitro studies against oxidative stress. The myrtle particles demonstrated cytoprotective properties when applied at low concentrations (1 μM) to macrophage cell lines.

| S-EPMC9951993 | biostudies-literature

Mesalazine granule formulation improves clinical data in Crohn's disease compared with tablet formulation.

Project description:The efficacy of sustained-release preparations of mesalazine as a remission maintenance treatment for Crohn's disease remains to be established. We aimed to examine the changes in compliance rate and clinical data 2 years after switching from mesalazine tablet to granule formulation at our facility among patients with Crohn's disease in remission. We investigated the rate of continuous treatment of mesalazine granules and examined the changes in Crohn's Disease Activity Index (CDAI) and serum C-reactive protein (CRP), albumin, and hemoglobin (Hb) levels 2 years after the switch. Compliance rate (continuous treatment vs. additional treatment) and continuous treatment rate [good (rate of ≥ 70%) vs. poor (rate < 70%)] were investigated. Of 46 patients, 12 (27.3%) received additional treatment and 32 (72.7%) did not require additional treatment in 2 years. No significant change in CDAI after switching to granule modification was noted in 32 patients in the continuous treatment group. Nevertheless, clinical remission was maintained for 2 years, and serum CRP levels decreased significantly (P = 0.023) and Hb levels increased significantly (P = 0.002). No change in the compliance rate was found. Our results suggest that mesalazine granule formulation may have a remission maintenance effect that is superior to that of mesalazine tablets.

| S-EPMC7721736 | biostudies-literature

Exfoliated MoS2 and MoSe2 Nanosheets by a Supercritical Fluid Process for a Hybrid Mg-Li-Ion Battery.

Project description:The ultrathin two-dimensional nanosheets of layered transition-metal dichalcogenides (TMDs) have attracted great interest as an important class of materials for fundamental research and technological applications. Solution-phase processes are highly desirable to produce a large amount of TMD nanosheets for applications in energy conversion and energy storage such as catalysis, electronics, rechargeable batteries, and capacitors. Here, we report a rapid exfoliation by supercritical fluid processing for the production of MoS2 and MoSe2 nanosheets. Atomic-resolution high-angle annular dark-field imaging reveals high-quality exfoliated MoS2 and MoSe2 nanosheets with hexagonal structures, which retain their 2H stacking sequence. The obtained nanosheets were tested for their electrochemical performance in a hybrid Mg-Li-ion battery as a proof of functionality. The MoS2 and MoSe2 nanosheets exhibited the specific capacities of 81 and 55 mA h g-1, respectively, at a current rate of 20 mA g-1.

| S-EPMC6640930 | biostudies-literature

A Novel Supercritical CO2 Foam System Stabilized With a Mixture of Zwitterionic Surfactant and Silica Nanoparticles for Enhanced Oil Recovery.

Project description:In order to improve the CO2 foam stability at high temperature and salinity, hydrophilic silica nanoparticles (NPs) were added into a dilute zwitterionic surfactant solution to stabilize supercritical CO2 (SC-CO2) foam. In the present paper, the foaming capacity and stability of SC-CO2 foam were investigated as a function of NP concentration at elevated temperatures and pressures. It was observed that the drainage rate of SC-CO2 foam was initially fast and then became slower with NPs adsorption at the gas-liquid interface. The improved foam stability at high temperature was attributed to the enhanced disjoining pressure with addition of NPs. Furthermore, an obvious increase in the foam stability was noticed with the increasing salinity due to the screening of NP charges at the interface. The rheological characteristics including apparent viscosity and surface elasticity, resistance factor, and microstructures of SC-CO2 foam were also analyzed at high temperature and pressure. With addition of 0.7% NPs, SC-CO2 foam was stabilized with apparent viscosity increased up to 80 mPa·s and resistance factor up to 200. Based on the stochastic bubble population (SBP) model, the resistance factor of SC-CO2 foam was simulated by considering the foam generation rate and maximum bubble density. The microstructural characteristics of SC-CO2 foam were detected by optical microscopy. It was found that the effluent bubble size ranged between 20 and 30 μm and the coalescence rate of SC-CO2 foam became slow with the increasing NP concentration. Oscillation measurements revealed that the NPs enhanced surface elasticity between CO2 and foam agents for resisting external disturbances, thus resulting in enhanced film stability and excellent rheological properties.

| S-EPMC6828982 | biostudies-literature

Development of a Scalable Process of Film-Coated bi-Layer Tablet Containing Sustained-Release Metoprolol Succinate and Immediate-Release Amlodipine Besylate.

Project description:The development of new drugs that combine active ingredients for the treatment hypertension is critically essential owing to its offering advantages for both patients and manufacturers. In this study, for the first time, detailed development of a scalable process of film-coated bi-layer tablets containing sustained-release metoprolol succinate and immediate-release amlodipine besylate in a batch size of 10,000 tablets is reported. The processing parameters of the manufacturing process during dry mixing-, drying-, dry mixing- completion stages were systematically investigated, and the evaluation of the film-coated bi-layer tablet properties was well established. The optimal preparation conditions for metoprolol succinate layer were 6 min- dry mixing with a high-speed mixer (120 rpm and 1400 rpm), 30-min drying with a fluid bed dryer, and 5-min- mixing completion at 25 rpm. For the preparation of amlodipine besylate layer, the optimal dry-mixing time using a cube mixer (25 rpm) was found to be 5 min. The average weight of metoprolol succinate layers and bi-layer tablets were controlled at 240-260 mg and 384-416 mg, respectively. Shewhart R chart and X¯ charts of all three sampling lots were satisfactory, confirming that the present scalable process was stable and successful. This study confirms that the manufacturing process is reproducible, robust; and it yields a consistent product that meets specifications.

| S-EPMC8618854 | biostudies-literature