scholarly journals Aprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing

Sci ◽  
2019 ◽  
Vol 1 (1) ◽  
pp. 29 ◽  
Author(s):  
Stavroula Nanaki ◽  
Rodanthi Maria Eleftheriou ◽  
Panagiotis Barmpalexis ◽  
Margaritis Kostoglou ◽  
Evangelos Karavas ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Polarized Light ◽  
Release Mechanism ◽  
Mechanism Analysis ◽  
Scanning Calorimetry ◽  
Melt Mixing ◽  
Element Analysis ◽  
Poloxamer 188 ◽  
Enhanced Dissolution ◽  
Spectroscopy Studies

In the present study Aprepitant (APT) ternary solid dispersions (SDs) were developed and evaluated for the first time. Specifically, ternary SDs of APT with Poloxamer 188 and Soluplus® (SOL) were prepared via melt mixing and compared to binary APT/Poloxamer 188 and APT/SOL SDs. Initially, combined thermo-gravimetric and hot-stage polarized light microscopy studies indicated that all tested compounds were thermally stable up to 280 °C, while Poloxamer 188 acted as a plasticizer to SOL by significantly reducing the temperature required to fully solubilize the API during SD preparation. Differential scanning calorimetry combined with wide angle X-ray diffraction studies showed that crystalline API was dispersed in both binary and ternary SDs, while Fourier transformation-infrared spectroscopy studies revealed no molecular interactions among the components. Scanning electron microscopy combined with EDAX element analysis showed that the API was dispersed in nano-scale within the polymer matrices, while increasing APT content led to increasing API nano-crystals within the SDs. Finally, dissolution studies showed that the prepared formulations enhanced dissolution of Aprepitant and its mechanism analysis was further studied. A mathematical model was also investigated to evaluate the drug release mechanism

scholarly journals Evaluation of Dissolution Enhancement of Aprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing

Sci ◽  
2019 ◽  
Vol 1 (2) ◽  
pp. 48
Author(s):  
Stavroula Nanaki ◽  
Rodanthi Maria Eleftheriou ◽  
Panagiotis Barmpalexis ◽  
Margaritis Kostoglou ◽  
Evangelos Karavas ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Polarized Light ◽  
Dissolution Enhancement ◽  
Release Mechanism ◽  
Mechanism Analysis ◽  
Scanning Calorimetry ◽  
Melt Mixing ◽  
Element Analysis ◽  
Poloxamer 188 ◽  
Enhanced Dissolution

In the present study Aprepitant (APT) ternary solid dispersions (SDs) were developed and evaluated for the first time. Specifically, ternary SDs of APT with Poloxamer 188 and Soluplus® (SOL) were prepared via melt mixing and compared to binary APT/Poloxamer 188 and APT/SOL SDs. Initially, combined thermo-gravimetric and hot-stage polarized light microscopy studies indicated that all tested compounds were thermally stable up to 280 °C, while Poloxamer 188 acted as a plasticizer to SOL by significantly reducing the temperature required to fully solubilize the API during SD preparation. Differential scanning calorimetry combined with wide angle X-ray diffraction studies showed that crystalline API was dispersed in both binary and ternary SDs, while Fourier transformation-infrared spectroscopy studies revealed no molecular interactions among the components. Scanning electron microscopy combined with EDAX element analysis showed that the API was dispersed in nano-scale within the polymer matrices, while increasing APT content led to increasing API nano-crystals within the SDs. Finally, dissolution studies showed that the prepared formulations enhanced dissolution of Aprepitant and its mechanism analysis was further studied. A mathematical model was also investigated to evaluate the drug release mechanism.

Evaluation of Dissolution Enhancement of Aprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing

Sci ◽  
2019 ◽  
Vol 1 (1) ◽  
pp. 11 ◽  
Author(s):  
Stavroula Nanaki ◽  
Rodanthi Maria Eleftheriou ◽  
Panagiotis Barmpalexis ◽  
Margaritis Kostoglou ◽  
Evangelos Karavas ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Polarized Light ◽  
Dissolution Enhancement ◽  
Release Mechanism ◽  
Mechanism Analysis ◽  
Scanning Calorimetry ◽  
Melt Mixing ◽  
Element Analysis ◽  
Poloxamer 188 ◽  
Enhanced Dissolution

In the present study Aprepitant (APT) ternary solid dispersions (SDs) were developed and evaluated for the first time. Specifically, ternary SDs of APT with Poloxamer 188 and Soluplus® (SOL) were prepared via melt mixing and compared to binary APT/Poloxamer 188 and APT/SOL SDs. Initially, combined thermo-gravimetric and hot-stage polarized light microscopy studies indicated that all tested compounds were thermally stable up to 280 °C, while Poloxamer 188 acted as a plasticizer to SOL by significantly reducing the temperature required to fully solubilize the API during SD preparation. Differential scanning calorimetry combined with wide angle X-ray diffraction studies showed that crystalline API was dispersed in both binary and ternary SDs, while Fourier transformation-infrared spectroscopy studies revealed no molecular interactions among the components. Scanning electron microscopy combined with EDAX element analysis showed that the API was dispersed in nano-scale within the polymer matrices, while increasing APT content led to increasing API nano-crystals within the SDs. Finally, dissolution studies showed that the prepared formulations enhanced dissolution of Aprepitant and its mechanism analysis was further studied. A mathematical model was also investigated to evaluate the drug release mechanism.

scholarly journals KARAKTERISASI FISIKOKIMIA DAN LAJU DISOLUSI DISPERSI PADAT IBUPROFEN DENGAN PEMBAWA POLIETILENGLIKOL 6000

2015 ◽  
Vol 4 (1) ◽  
pp. 25
Author(s):  
Erizal Zaini ◽  
Rahmi x Rahmi Nofita ◽  
Salman ◽  
Irna Kurniati
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Polarized Light ◽  
Water Soluble ◽  
Dissolution Rates ◽  
Hot Stage Microscopy ◽  
Enhanced Dissolution ◽  
Water Soluble Compound ◽  
Polyethylene Glycol 6000

 Solid dispersions of the antiinflamation drug ibuprofen and polyethylene glycol 6000 (PEG 6000) were prepared by the melting method in order to increase the dissolution rates of this poorly water-soluble compound. The temperature/composition phase diagram of binary system was analyzed by termal analysis hot-stage microscopy, showing an eutectic formation. Polarized light hot stage microscopy and X-ray-powder diffraction confirmed, that solid dispersion technique decrease the crystalliny of ibuprofen after melting and solidifying of a 4/6 (w/w) mixture of ibuprofen and polyethylene glycol 6000 respectively, which the results enhanced dissolution rates compared to the physical mixtures and ibuprofen intact. However, no such chemical interactions in the solid state were confirmed by FTIR spectra which showed the presence of ibuprofen crystalline in solid dispersion.   

scholarly journals PREPARATION AND EVALUATION OF DOLUTEGRAVIR SOLID DISPERSIONS

2021 ◽  
pp. 193-198
Author(s):  
SUNDEEP MUPPARAJU ◽  
VIDYADHARA SURYADEVARA ◽  
SANDEEP DOPPALAPUDI
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Content Uniformity ◽  
Fusion Method ◽  
Scanning Calorimetry ◽  
Poloxamer 188

Objective: The current work mainly focuses on solubility enhancement of dolutegravir which is a BCS (Biopharmaceutical Classification System) class-II drug using various excipients. Methods: Solid dispersions of dolutegravir were prepared by solvent evaporation and fusion methods using carriers like poloxamer-188 and plasdone K-29/32 in different ratios (1:0.5 to 1:3.0). The amount of dolutegravir used was kept constant and the polymer concentrations were increased. Various physical parameters like angle of repose, carr’s index, Hausner’s ratio were calculated for the prepared solid dispersions. They were also evaluated for particle size and drug content uniformity along with in vitro drug release. Characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM) and X-Ray Diffraction (XRD) were also done. Results: Dolutegravir solid dispersions showed good to excellent flow properties. From in vitro dissolution studies, it was observed that the solid dispersion formulation DF3 containing dolutegravir and poloxamer-188 in 1:1.5 ratios prepared by fusion method showed better dissolution rate when compared with other formulations. The dissolution parameters were also evaluated. DF3 showed a higher drug release of 86.33% in 60 min. FTIR and DSC studies revealed that there were no major interactions between drug and excipients. XRD studies revealed the nature of formulations. Conclusion: The solid dispersions prepared using poloxamer-188 by fusion method has enhanced the solubility of dolutegravir.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design

2018 ◽  
Vol 11 (6) ◽  
pp. 4337-4348
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas I
Keyword(s):  
Central Composite Design ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Release Mechanism ◽  
Solvent Evaporation Method ◽  
Onset Of Action ◽  
Evaporation Method ◽  
Central Composite

Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.

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

The Development of Pemetrexed Diacid-Loaded Gelatin-Cloisite 30B (MMT) Nanocomposite for Improved Oral Efficacy Against Cancer: Characterization, In-Vitro and Ex-Vivo Assessment

2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Confocal Laser ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Cloisite 30B ◽  
Ft Ir

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.

scholarly journals The Effect of Surface Treatment with Isocyanate and Aromatic Carbodiimide of Thermally Expanded Vermiculite Used as a Functional Filler for Polylactide-Based Composites

Polymers ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 890
Author(s):  
Mateusz Barczewski ◽  
Olga Mysiukiewicz ◽  
Aleksander Hejna ◽  
Radosław Biskup ◽  
Joanna Szulc ◽  
...  
Keyword(s):  
Impact Strength ◽  
Mechanical Stability ◽  
Thermomechanical Analysis ◽  
Thermomechanical Properties ◽  
Phenyl Isocyanate ◽  
Sem Analysis ◽  
Scanning Calorimetry ◽  
Melt Mixing ◽  
Expanded Vermiculite ◽  
Chain Extenders

In this work, thermally expanded vermiculite (TE-VMT) was surface modified and used as a filler for composites with a polylactide (PLA) matrix. Modification of vermiculite was realized by simultaneous ball milling with the presence of two PLA chain extenders, aromatic carbodiimide (KI), and 4,4’-methylenebis(phenyl isocyanate) (MDI). In addition to analyzing the particle size of the filler subjected to processing, the efficiency of mechanochemical modification was evaluated by Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The composites of PLA with three vermiculite types were prepared by melt mixing and subjected to mechanical, thermomechanical, thermal, and structural evaluation. The structure of composites containing a constant amount of the filler (20 wt%) was assessed using FTIR spectroscopy and SEM analysis supplemented by evaluating the final injection-molded samples’ physicochemical properties. Mechanical behavior of the composites was assessed by static tensile test and impact strength hardness measurements. Heat deflection temperature (HDT) test and dynamic thermomechanical analysis (DMTA) were applied to evaluate the influence of the filler addition and its functionalization on thermomechanical properties of PLA-based composites. Thermal properties were assessed by differential scanning calorimetry (DSC), pyrolysis combustion flow calorimetry (PCFC), and thermogravimetric analysis (TGA). The use of filler-reactive chain extenders (CE) made it possible to change the vermiculite structure and obtain an improvement in interfacial adhesion and more favorable filler dispersions in the matrix. This translated into an improvement in impact strength and an increase in thermo-mechanical stability and heat release capacity of composites containing modified vermiculites.

scholarly journals Development of Controlled-Release Carbamide Peroxide Loaded Nanoemulgel for Tooth Bleaching: In Vitro and Ex Vivo Studies

2021 ◽  
Vol 14 (2) ◽  
pp. 132
Author(s):  
Siriporn Okonogi ◽  
Adchareeya Kaewpinta ◽  
Sakornrat Khongkhunthian ◽  
Pisaisit Chaijareenont
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Tooth Bleaching ◽  
Polymer Mixture ◽  
Release Mechanism ◽  
Burst Release ◽  
Order Kinetic ◽  
Carbamide Peroxide ◽  
Periodontal Tissues

Burst release of carbamide peroxide (CP) from traditional hydrogels causes severe inflammation to periodontal tissues. The present study explores the development of a novel CP nanoemulgel (CP-NG), an oil-in-water nanoemulsion-based gel in which CP was loaded with a view to controlling CP release. CP solid dispersions were prepared, using white soft paraffin or polyvinylpyrrolidone-white soft paraffin mixture as a carrier, prior to formulating nanoemulsions. It was found that carrier type and the ratio of CP to carrier affected drug crystallinity. Nanoemulsions formulated from the optimized CP solid dispersions were used to prepare CP-NG. It was found that the ratio of drug to carrier in CP solid dispersions affected the particle size and zeta potential of the nanoemulsions as well as drug release behavior and tooth bleaching efficacy of CP-NG. Drug release from CP-NG followed a first-order kinetic reaction and the release mechanism was an anomalous transport. Drug release rate decreased with an increase in solid dispersion carriers. CP-NG obtained from the solid dispersion with a 1:1 ratio of CP to the polymer mixture is suitable for sustaining drug release with high tooth bleaching efficacy and without reduction of enamel microhardness. The developed CP-NG is a promising potential tooth bleaching formulation.

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