scholarly journals Preparation of Solid Dispersions of Simvastatin and Soluplus Using a Single-Step Organic Solvent-Free Supercritical Fluid Process for the Drug Solubility and Dissolution Rate Enhancement

2021 ◽  
Vol 14 (9) ◽  
pp. 846
Author(s):  
Uttom Nandi ◽  
Adejumoke Lara Ajiboye ◽  
Preksha Patel ◽  
Dennis Douroumis ◽  
Vivek Trivedi
Keyword(s):  
Dissolution Rate ◽  
Supercritical Fluid ◽  
Solid Dispersions ◽  
Single Step ◽  
Solvent Free ◽  
Drug Dissolution ◽  
Scanning Calorimetry ◽  
Fluid Process ◽  
Physicochemical Characterisation ◽  
Polymer Ratio

The study was designed to investigate the feasibility of supercritical carbon dioxide (scCO2) processing for the preparation of simvastatin (SIM) solid dispersions (SDs) in Soluplus® (SOL) at temperatures below polymer’s glass transition. The SIM content in the SDs experimental design was kept at 10, 20 and 30% to study the effect of the drug–polymer ratio on the successful preparation of SDs. The SIM–SOL formulations, physical mixtures (PMs) and SDs were evaluated using X-ray diffraction (XRD), differential scanning calorimetry (DSC), attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), scanning electron microscopy (SEM), and dissolution studies. The scCO2 processing conditions and drug–polymer ratio were found to influence the physicochemical properties of the drug in formulated SDs. SIM is a highly crystalline drug; however, physicochemical characterisation carried out by SEM, DSC, and XRD demonstrated the presence of SIM in amorphous nature within the SDs. The SIM–SOL SDs showed enhanced drug dissolution rates, with 100% being released within 45 min. Moreover, the drug dissolution from SDs was faster and higher in comparison to PMs. In conclusion, this study shows that SIM–SOL dispersions can be successfully prepared using a solvent-free supercritical fluid process to enhance dissolution rate of the drug.

Fusion as an Approach to Enhance Dissolution Rate of a Poorly Water-Soluble Drug (Curcurmin)

2011 ◽  
Vol 393-395 ◽  
pp. 119-122
Author(s):  
Dong Hua Wan ◽  
Fen Lin ◽  
Qu Xiang Liao
Keyword(s):  
Dissolution Rate ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Gastric Fluid ◽  
Molecular State ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Simulated Gastric Fluid ◽  
Scanning Calorimetry ◽  
Rate Improvement

It’s well known that curcumin is practically insoluble in water. Therefore, to improve the drug dissolution rate, fusion approach was employed to prepare curcumin solid dispersions (SDs) in the carrier Pluronic F68 with three different drug loads. The dissolution rate of curcumin from the SDs was measured at simulated gastric fluid. The concentration of the dissolved drug in the medium was determined by HPLC. The dissolution rates of the formulations were dependent on the drug loading in SDs. 92.2% CUR was dissolved in 10 min from the SDs with 8.97% drug load, whereas the amounts of drug released were 65.8% and 84.2% within 120 min from the SDs with 18.9% and 29.0% drug loads, respectively. The Fourier transform infrared spectra indicated hydrogen bond between the drug and carrier. Furthermore, their physicochemical properties were well investigated using differential scanning calorimetry and X-ray diffraction. In the dispersions containing 8.97% CUR, the drug was in the molecular state. At a composition of approximately 18.9%, CUR was dispersed as micro-fine crystals. These interesting results indicate that the physical states of the drug in the carrier, which are governed by the drug loading, can affect the dissolution rate improvement.

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

Improvement of the dissolution rate of artemisinin by means of supercritical fluid technology and solid dispersions

2003 ◽  
Vol 254 (2) ◽  
pp. 173-181 ◽  
Author(s):  
T Van Nijlen ◽  
K Brennan ◽  
G Van den Mooter ◽  
N Blaton ◽  
R Kinget ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Supercritical Fluid ◽  
Solid Dispersions ◽  
Supercritical Fluid Technology

COMPLEX OF ELUXADOLINE WITH SODIUM CAPRYLATE FOR IMPROVED SOLUBILITY AND DISSOLUTION RATE

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 22-26
Author(s):  
Manisha Dhere ◽  
◽  
Arti Majumdar ◽  
Neelesh Malviya
Keyword(s):  
Dissolution Rate ◽  
Solvent Evaporation ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Solvent Evaporation Method ◽  
Scanning Calorimetry ◽  
Evaporation Method ◽  
Solubility Study ◽  
Sodium Caprylate

In the present research, newly developed complex with sodium caprylate was investigated for solubility and dissolution enhancement of eluxadoline. Complexes were prepared in different ratios by solvent evaporation method and characterised solubility study, Infrared spectroscopy (IR), Diffrential scanning calorimetry (DSC), X-Ray Diffraction (XRD), drug content analysis and in vitro Drug release. The solubility and dissolution rate revealed most suitable ratio of eluxadoline and sodium caprylate (1:4). The IR, DSC and X-RD data also confirmed the results. It was concluded that complex prepared with (1:4 drug:sodium caprylate ratio) using solvent evaporation method showed significant improvement in solubility and drug dissolution.

scholarly journals Solvent-Free and Scalable Procedure to Prepare PYR13TFSI/LiTFSI/PVDF–HFP Thermoplastic Electrolytes with Controlled Phase Separation and Enhanced Li Ion Diffusion

Membranes ◽  
2019 ◽  
Vol 9 (4) ◽  
pp. 50 ◽  
Author(s):  
Víctor Gregorio ◽  
Nuria García ◽  
Pilar Tiemblo
Keyword(s):  
Ionic Conductivity ◽  
Polyvinylidene Fluoride ◽  
Ionic Conductivities ◽  
Single Step ◽  
Solvent Free ◽  
High Concentration ◽  
Scanning Calorimetry ◽  
Melt Compounding ◽  
Li Ion ◽  
Pfg Nmr

Solid electrolytes for Li transport have been prepared by melt-compounding in one single step. Electrolytes are composed of polyvinylidene fluoride–hexafluoropropylene (PVDF–HFP) with PYR13TFSI on its own or with varying concentration of LiTFSI. While the extrusion of PVDF–HFP with PYR13TFSI is possible up to relatively high liquid fractions, the compatibility of PVDF–HFP with LiTFSI/PYR13TFSI solutions is much lower. An organo-modified sepiolite with D-α-tocopherol polyethylene glycol 1000 succinate (TPGS-S) can be used to enhance the compatibility of these blends and allows to prepare homogeneous PYR13TFSI/LiTFSI/PVDF–HFP electrolytes with controlled microphase separations by melt-compounding. The structure and morphology of the electrolytes has been studied by FTIR, differential scanning calorimetry (DSC), SEM, and AFM. Their mechanical properties have been studied by classical strain–stress experiments. Finally, ionic conductivity has been studied in the −50 to 90 °C temperature range and in diffusivity at 25 °C by PFG-NMR. These electrolytes prove to have a microphase-separated morphology and ionic conductivity which depends mainly on their composition, and a mechanical behavior typical of common thermoplastic polymers, which makes them very easy to handle. Then, in this solvent-free and scalable fashion, it is possible to prepare electrolytes like those prepared by solvent casting, but in few minutes instead of several hours or days, without solvent evaporation steps, and with ionic conductivities, which are very similar for the same compositions, above 0.1 mS·cm−1 at 25 °C. In addition, some of the electrolytes have been prepared with high concentration of Li ion, what has allowed the anion exchange Li transport mechanism to contribute significantly to the overall Li diffusivity, making DLi become similar and even clearly greater than DTFSI.

scholarly journals The Role of Functional Excipients in Solid Oral Dosage Forms to Overcome Poor Drug Dissolution and Bioavailability

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 393 ◽  
Author(s):  
Jannes van der Merwe ◽  
Jan Steenekamp ◽  
Dewald Steyn ◽  
Josias Hamman
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Drug Dissolution ◽  
Specific Reference ◽  
Dissolution Rates ◽  
Bioavailability Enhancement ◽  
Poor Solubility

Many active pharmaceutical ingredients (APIs) exhibit poor solubility and low dissolution rates in aqueous environments such as the luminal fluids of the gastrointestinal tract. The oral bioavailability of these compounds is usually very low as a result of their poor solubility properties. In order to improve the bioavailability of these poorly soluble drugs, formulation strategies have been applied as a means to improve their aqueous solubility and dissolution rates. With respect to formulation approaches, excipients can be incorporated in the formulation to assist in the dissolution process of the drug, or specialized dosage forms can be formulated that improve dissolution rate through various mechanisms. This paper provides an overview of selected excipients (e.g., alkalinizing agents, surfactants and sugars) that can be used in formulations to increase the dissolution rate as well as specialized dosage forms such as self-emulsifying delivery systems and formulation techniques such as inclusion complexes and solid dispersions. These formulation approaches are discussed with available examples with specific reference to positive outcomes in terms of drug solubility and bioavailability enhancement.

scholarly journals Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate

2016 ◽  
Vol 52 (1) ◽  
pp. 1-13 ◽  
Author(s):  
Ehsan Adeli
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Polyethylene Glycols ◽  
X Ray Diffraction ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Peg 4000 ◽  
Poorly Soluble

ABSTRACT Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical mixtures of azithromycin were made using PEG 4000, 6000, 8000, 12000 and 20000 in various ratios, based on the solvent evaporation method. From the studied drug release profile, it was discovered that the dissolution rate of the physical mixture, as the well as the solid dispersions, were higher than those of the drug alone. There was no chemical incompatibility between the drug and polymer from the observed Infrared (IR) spectra. Drug-polymer interactions were also investigated using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Election Microscopy (SEM). In conclusion, the dissolution rate and solubility of azithromycin were found to improve significantly, using hydrophilic carriers, especially PEG 6000.

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