scholarly journals Valuing Best Poloxamer Carrier for Meloxicam Solid Dispersions by novel microwave fusion: Designing and Characterization

2019 ◽  
pp. 1-15
Keyword(s):  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Poloxamer 407 ◽  
Research Activity ◽  
Fusion Technique ◽  
Poloxamer 188 ◽  
Tablet Compression ◽  
Tablet Formulations

Present research activity is to establish the best Poloxamer carriers for making solid dispersions (SD) with Meloxicam. The main aim of this investigation is to find the best among the better Poloxamer carriers viz., Poloxamer-108, Poloxamer-188, Poloxamer-237, Poloxamer-338 and Poloxamer-407 for making SD by novel microwave fusion technique. Four portions of Meloxicam: Poloxamer in various ratios (1:1, 1:2, 1:4 and 1:6) are used for making SD by microwave fusion technique later compressed using 8 station tablet compression machine. The SD and tablet formulations are evaluated for physicochemical characterization. All the prepared batches found to have satisfactory specifications as per pharmacopoeia. The authors concluded that Poloxamer-188 is found to be the best carrier among the Poloxamer carriers used for making Meloxicam SD. Keywords: Meloxicam, Poloxamer, microwave, solid dispersions, tablets

scholarly journals STUDIES ON SOLID DISPERSIONS OF LEFLUNOMIDE

2020 ◽  
pp. 187-190
Author(s):  
MAHAPARALE PR ◽  
THORAT VP
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Poloxamer 188 ◽  
Evaporation Method ◽  
Enhanced Solubility

Objective: Leflunomide is Non steroidal Anti-Inflammatory drug, which is poorly water soluble. In present study attempt has been made to prepare and characterize solid dispersions of leflunomide to increase solubility of drug.Method:  In Preparation of solid dispersion of leflunomide different polymer like PEG 4000, PEG 6000, Poloxamer 188 and Poloxamer 407 were used.  Effects of several variables such as type of carrier used, drug: carrier ratios, method of preparation were studied. The evaluation of solid dispersions was done by solubility study, dissolution study and X-ray diffractometry. Result: Improvement in dissolution of drug was observed in all solid dispersions as compared to pure drug alone. Solid dispersions prepared using Poloxamer 188 showed fastest in vitro drug release. Solid dispersions prepared using solvent evaporation method showed relatively faster drug release than melt evaporation method. XRD patterns indicated reduced crystallinity of drug particles, which suggests mechanism of enhanced solubility and dissolution of drug in solid dispersion systems.Conclusion:  A significant result obtained with the study indicated that solid dispersion by solvent evaporation can successfully be further explored and employed to improve solubility and dissolution characteristics of poorly soluble drugs.Keywords: Leflunomide, Solid dispersion, Carrier

scholarly journals Effect of Hydrophilic Carriers for Solubility and Dissolution Enhancement of Sulfamerazine by Solid Dispersions Technique

2021 ◽  
pp. 313-326
Author(s):  
Jitendra Gupta ◽  
Reena Gupta
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Dissolution Enhancement ◽  
Infrared Spectrometry ◽  
Antibacterial Drug ◽  
Dissolution Profile ◽  
Fusion Technique ◽  
Pure Drug

Aims: The present research was carried out to investigate the effect of hydrophilic carriers in enhancing the solubility and dissolution rate of Sulfamerazine (SMZ) employing the fusion technique of solid dispersions (SD). Methodology: SMZ is an oral antibacterial drug exhibiting a poor dissolution profile and water solubility. SD of SMZ was prepared using poloxamer 407 (PX407) and Polyethylene glycol 6000 (PEG6000) as a hydrophilic carrier by employing the fusion technique. Results: The powder SDs were subjected for solubility, Fourier transform infrared spectrometry (FTIR), Differential scanning calorimetry (DSC), in-vitro dissolution profile, Scanning electron microscopy (SEM), and X-ray diffraction (XRD) study. The FTIR spectral analysis showed no significant incompatibility between drug and carriers and confirmed the presence of SMZ. From XRD and DSC, SMZ indicated the amorphous form in solid dispersion with larger specific surface area, resulting in a better in-vitro rate of dissolution of the drug from solid dispersions than pure drug. However, SD of PX407 (SDSMFF8) indicated higher aqueous solubility than pure SMZ. Further, SDSMFF7 showed higher in-vitro drug release 96.45±0.3% within 60 minutes, and pure drug (18.54±0.8%). Conclusion: In conclusion, enhancing thesolubility and dissolution of SMZ using hydrophilic carriers by solid dispersion technique provides new strategies for broadening its potential clinical application.

Solid Dispersions: A Review

2014 ◽  
Vol 4 (2) ◽  
Author(s):  
Sumant Saini ◽  
Yashwant .
Keyword(s):  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Water Soluble ◽  
Absolute Minimum ◽  
Technology Transfers ◽  
Molecular Arrangement ◽  
Water Soluble Drugs ◽  
Carrier Solvent ◽  
Preparation Techniques ◽  
Selection Of

Solid dispersions are one of the most promising strategies to improve the oral bioavailability of poorly water soluble drugs. By reducing drug particle size to the absolute minimum, and hence improving drug wettability, bioavailability may be significantly improved. This article reviews the various preparation techniques for solid dispersion and compiles some of the recent technology transfers. The different types of solid dispersions based on the molecular arrangement have been highlighted. Some of the practical aspects to be considered for the preparation of solid dispersions, such as selection of carrier, solvent and methods of physicochemical characterization, along with an insight into the molecular arrangement of drugs in solid dispersions are also discussed. In this review, it is intended to discuss the recent advances related on the area of solid dispersions.

Preparation and Evaluation of Glipizide Tablets Containing both Enhanced and Sustained Release Solid Dispersions

1970 ◽  
Vol 2 (4) ◽  
pp. 714-725
Author(s):  
Adel M. Aly ◽  
Ahmed S. Ali
Keyword(s):  
Blood Glucose ◽  
Blood Glucose Level ◽  
Glucose Level ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
In Vivo Studies ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Tablet Formulations

: Glipizide (GZ) is an oral blood-glucose-lowering drug of the sulfonylurea class characterized by its poor aqueous solubility. Aiming for the production of GZ tablets with rapid onset of action followed by prolonged effect; GZ-Polyethylene glycol (PEG 4000 and 6000) solid dispersions with different ratios, (using melting and solvent evaporation method), as well as, coprecipitate containing GZ with polymethyl-methacrylate (PMMA) were prepared. Four tablet formulations were prepared containing; a) GZ alone, b) GZ: PEG6000, 1:10, c) GZ:PMMA 1:3, and, d)both GZ:PEG6000 1:10 and GZ:PMMA 1:3. The solvent evaporation method showed more enhancement of GZ solubility than the melting one, and this solubilizing effect increased with PEG increment. Generally, PEG6000 showed more enhancement of dissolution than PEG4000 especially at 1:10 drug: polymer ratio (the most enhancing formula). Also, the prepared tablet formulations showed acceptable physical properties according to USP/NF requirements. The dissolution results revealed that tablets containing PEG6000 (1:10) have the most rapid release rate, followed by the formula containing both PEG6000 and PMMA, while that including PMMA alone showed the slowest dissolution rate. Moreover, In-vivo studies for each of the above four formulations, were performed using four mice groups. The most effective formula in decreasing the blood glucose level, through the first 6 hours, was that containing GZ and PEG6000, 1:10. However, formula containing the combination of enhanced and sustained GZ was the most effective in decreasing the blood glucose level through 16 hours. Successful in-vitro in-vivo correlations could be detected between the percent released and the percent decreasing of blood glucose level after 0.5 hours.

Physicochemical Characterization of Solid Dispersions of Cefdinir with PVP K-30 and PEG 4000

2010 ◽  
Vol 3 (2) ◽  
pp. 948-956
Author(s):  
Kumar P ◽  
S Kumar ◽  
A Kumar ◽  
M Chander
Keyword(s):  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Drug Carriers ◽  
Dissolution Properties ◽  
Rate Of Dissolution ◽  
Peg 4000 ◽  
Release Studies ◽  
Crystalline Nature ◽  
Physical Mixtures

The purpose of this study was to prepare and characterize solid dispersions of the antibacterial agent Cefdinir with PEG 4000 and PVP K-30 with a view to improve its dissolution properties. Investigations of the properties of the dispersions were performed using release studies, X-ray powder diffraction (XRD) and Fourier transform infrared (FTIR). The results obtained showed that the rate of dissolution of Cefdinir was considerably improved when formulated in solid dispersions with PVP K-30 and PEG 4000 as compared with pure drug and physical mixtures. The results from XRD studies showed the transition of crystalline nature of drug to amorphous form, while FTIR studies demonstrated the absence of drug-carriers interaction.

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

scholarly journals Preparation, characterization and evaluation of the in vivo trypanocidal activity of ursolic acid-loaded solid dispersion with poloxamer 407 and sodium caprate

2015 ◽  
Vol 51 (1) ◽  
pp. 101-109 ◽  
Author(s):  
Josimar Oliveira Eloy ◽  
Juliana Saraiva ◽  
Sérgio de Albuquerque ◽  
Juliana Maldonado Marchetti
Keyword(s):  
Ursolic Acid ◽  
Solid Dispersion ◽  
Oral Absorption ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Drug Dissolution ◽  
Limiting Factors ◽  
Sodium Caprate ◽  
Trypanocidal Activity

Ursolic acid is a promising candidate for treatment of Chagas disease; however it has low aqueous solubility and intestinal absorption, which are both limiting factors for bioavailability. Among the strategies to enhance the solubility and dissolution of lipophilic drugs, solid dispersions are growing in popularity. In this study, we employed a mixture of the surfactants poloxamer 407 with sodium caprate to produce a solid dispersion containing ursolic acid aimed at enhancing both drug dissolution and in vivo trypanocidal activity. Compared to the physical mixture, the solid dispersion presented higher bulk density and smaller particle size. Fourier Transform Infrared Spectroscopy results showed hydrogen bonding intermolecular interactions between drug and poloxamer 407. X-ray diffractometry experiments revealed the conversion of the drug from its crystalline form to a more soluble amorphous structure. Consequently, the solubility of ursolic acid in the solid dispersion was increased and the drug dissolved in a fast and complete manner. Taken together with the oral absorption-enhancing property of sodium caprate, these results explained the increase of the in vivo trypanocidal activity of ursolic acid in solid dispersion, which also proved to be safe by cytotoxicity evaluation using the LLC-MK2 cell line.

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

scholarly journals Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique

2019 ◽  
Vol 28 (2) ◽  
pp. 105-114
Author(s):  
Samer K. Ali ◽  
Eman B. H. Al-Khedairy
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Dissolution Enhancement ◽  
Drug Solubility ◽  
Scanning Calorimetry ◽  
Poorly Soluble

            Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs.           The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents.            All solid dispersion adsorbate (SDA) formulas  were prepared in ratios of 1:1:1  (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content,  , dissolution, crystal structure using  X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC)  studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction.                The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38  fold increase in solubility compared to  solubility of pure ATR and  solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility  and  dissolution .

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