scholarly journals EFFECT OF SOLID DISPERSIONS ON THE SOLUBILITY OF METRONIDAZOLE

2021 ◽  
Vol 9 (3) ◽  
pp. 195-204
Author(s):  
I. I. Krasnyuk (Jr.) ◽  
S. R. Naryshkin ◽  
I. I. Krasnyuk ◽  
A. V. Belyatskaya ◽  
O. I. Stepanova ◽  
...  
Keyword(s):  
Optical Properties ◽  
Solid Dispersion ◽  
Active Substance ◽  
Solid Phase ◽  
Solid Dispersions ◽  
Dosage Forms ◽  
Polyethylene Glycols ◽  
Uv Spectrophotometry ◽  
Colloidal Solutions ◽  
Constant Weight

The aim of the work is to study the effect of solid dispersions using polyethylene glycols of various molecular weights on the solubility of metronidazole in water. Metronidazole is an antimicrobial and antiprotozoal drug. Its low solubility in water limits the use of metronidazole, causing technological difficulties and reducing its bioavailability. The solubility and release of the active substance from dosage forms can be increased using the solid dispersion methods. Solid dispersions are bi- or multicomponent systems consisting of an active substance and a carrier (a highly dispersed solid phase of the active substance or molecular-dispersed solid solutions) with a partial formation of complexes of variable compositions with the carrier material.Materials and methods. The substance of metronidazole used in the experiment, was manufactured by Hubei Hongyuan Pharmaceutical Technology Co., Ltd. (China). To obtain solid dispersions, polyethylene glycols of various molar masses – 1500, 2000 and 3000 g/mol – were used. The solid dispersions were prepared by “the solvent removal method”: metronidazole and the polymer were dissolved in a minimum volume of 96% ethyl alcohol (puriss. p.a./analytical grade) at 65±2°C, and then the solvent was evaporated under vacuum to the constant weight. A vacuum pump and a water bath were used at the temperature of 40±2°C. The dissolution of the samples was studied using a magnetic stirrer with heating, and a thermostatting device. The concentration of metronidazole was determined on a spectrophotometer using quartz cuvettes at the wavelength of 318±2 nm. To filter the solutions, syringe nozzles were used, the pores were 0.45 μm, the filter was nylon. Microcrystalloscopy was performed using a microscope with a digital camera. The optical properties of the solutions were investigated using a quartz cuvette and a mirror camera (the image exposure – 20 sec).Results. Obtaining solid dispersions increases the completeness and rate of the metronidazole dissolution. The solubility of metronidazole from solid dispersions increases by 14–17% in comparison with the original substance. The complex of physical-chemical methods of the analysis, including UV spectrophotometry, microcrystalloscopy and the study of the optical properties of the obtained solutions, makes it possible to suggest the following. The increase in the solubility of metronidazole from solid dispersions is explained by the loss of crystallinity and the formation of a solid solution of the active substance and the solubilizing effect of the polymer with the formation of colloidal solutions of metronidazole at subsequent dissolution of the solid dispersion in water.Conclusion. The preparation of solid dispersions with polyethylene glycols improves the dissolution of metronidazole in water. The results obtained are planned to be used in the development of rapidly dissolving solid dosage forms of metronidazole with an accelerated release and an increased bioavailability.

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.

scholarly journals FAST DISSOLVING TABLET USING SOLID DISPERSION TECHNIQUE: A REVIEW

2017 ◽  
Vol 9 (6) ◽  
pp. 1
Author(s):  
Pratik Swarup Das ◽  
Sushma Verma ◽  
Puja Saha
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Dosage Forms ◽  
Water Soluble ◽  
Solvent Method ◽  
Agglomeration Process ◽  
Water Soluble Drugs ◽  
And Performance ◽  
Dispersion Technique ◽  
Industrial Level

Fast dissolving tablets are also called as mouth-dissolving tablets, melt-in mouth tablets, orodispersible tablets, quick dissolving etc. Fast dissolving tablets are those when put on tongue disintegrate instantaneously releasing the drug, which dissolve or disperses in the saliva. The faster the drug dissolved into solution, quicker the absorption and onset of clinical effect. Oral routes of drug administration have wide acceptance up to 50-60% of total dosage forms. Fast dissolving tablet containing solid dispersion was developed to improve the dissolution of drug and stability of solid dispersion. They are disintegrating and/or dissolve rapidly in the saliva without the need for water. Thus it is regarded as the safest, most convenient and most economical method of drug delivery having the highest patient compliance. The later part of the article focus on the progress in methods of manufacturing, evaluation and various latest technologies involved in the development of Fast dissolving tablets. Solid dispersion is basically a drug–polymer two-component system; the drug–polymer interaction is the determining factor in its design and performance. It also discusses about modern characterization technique to characterize solid dispersion. In this review, it is intended to discuss the recent advances related on the area of solid dispersion technology. Different methods are also been used for preparation of solid dispersions such as Melting method, Solvent method, Melting solvent method, Melt extrusion method, lyophilisation Technique, Melt Agglomeration Process, The Use Of Surfactant, Electro spinning and Super Critical Fluid Technology. The introduction of fast dissolving dosage forms has solved some of the problems encountered in administration of drugs to the pediatric and elderly patient, which constitutes a large proportion of the world's population. Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bio availability of a range of poorly water-soluble drugs. The focus of one part of the review article is based on solid dispersion mainly advantages, disadvantages, types, the method of preparation, and characterization of the solid dispersion at laboratory and industrial level.

scholarly journals Development and Validation of Dimeric Macrocyclic Tannin Assay Method in Dosage Forms

2020 ◽  
Vol 9 (4) ◽  
pp. 93-98
Author(s):  
E. V. Ignаteva ◽  
I. V. Yartseva ◽  
Z. S. Shprakh ◽  
I. R. Prosalkova ◽  
S. A. Sasov ◽  
...  
Keyword(s):  
Active Substance ◽  
Quantitative Assessment ◽  
Dosage Forms ◽  
Assay Method ◽  
Uv Spectrophotometry ◽  
Drug Form ◽  
Development And Validation ◽  
Antiangiogenic Drug ◽  
Drug Quality Control

Introduction. Quantitative assessment of the active substance is necessary and perhaps the most significant part of the drug quality control. Validation of the analytical methods of quantitative assessment ensures their compliance with high requirements. The present study describes the development and validation of a spectrophotometry method for the quantitative evaluation of the active substance in the drug form of the national antitumor and antiangiogenic drug «Dimeric macrocyclic tannin (DMT) lyophilizate for solution for injection, 100 mg».Aim. The development and validation of the assay method for the standardization of «DMT lyophilizate for solution for injection, 100 mg».Materials and metods. The study used «DMT lyophilizate for solution for injection, 100 mg» and the active substance DMT. Method – spectrophotometry.Results and discussion. The methodof the quantitative assessment of the active substance in the DMT lyophilized drug by direct UV spectrophotometry was developed and the validation characteristics of the method were defined as a result of the study.Conclusion. The validation results showed that the assay method of DMT in the drug form has the appropriate accuracy, precision and linearity. The obtained results correspond to the approved criteria that allow the use of the developed methodology for evaluating the quality of the drug.

scholarly journals Solid Dispersion to Improve Dissolution of Drug Product

2013 ◽  
Vol 2 (1) ◽  
pp. 42-58
Author(s):  
Asma Huq
Keyword(s):  
Solid Dispersion ◽  
Drug Product ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Dosage Forms ◽  
Water Soluble ◽  
Inert Matrix ◽  
Inert Carrier

The term ‘solid dispersion’ has been utilized to describe a family of dosage forms whereby the drug is dispersed in a biologically inert matrix, usually with a view to enhancing oral bioavailability. It may be defined as the dispersion of one or more active ingredients in an inert carrier matrix at solid-state prepared by the melting (fusion), solvent or melting-solvent method. In practice, these dosage forms have been traditionally regarded as being synonymous with systems whereby the in vitro release of the drug is enhanced compared to conventional dosage forms, with concomitant implications for in vivo release. Furthermore, the carrier used has, again traditionally, been a water-soluble or water-miscible polymer such as polyethylene glycol (PEG) or polyvinylpyrrolidone (PVP) or low molecular weight materials such as sugars. However, the proliferation of publications in the area since the first solid dispersions were described1 has led to a broadening of these definitions to include water insoluble matrices such as Gelucires and Eudragits that may yield either slow or rapid release or absorption.DOI: http://dx.doi.org/10.3329/ijpls.v2i1.15134 International Journal of Pharmaceutical and Life Sciences Vol.2(1) 2013: 42-58

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.

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.

scholarly journals Enhanced Oral Bioavailability of Resveratrol by Using Neutralized Eudragit E Solid Dispersion Prepared via Spray Drying

Antioxidants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 90
Author(s):  
Eun-Sol Ha ◽  
Du Hyung Choi ◽  
In-hwan Baek ◽  
Heejun Park ◽  
Min-Soo Kim
Keyword(s):  
Spray Drying ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Pharmaceutical Products ◽  
In Vitro Dissolution ◽  
Dependent Manner ◽  
Amorphous Solid Dispersions ◽  
Eudragit E

In this study, we designed amorphous solid dispersions based on Eudragit E/HCl (neutralized Eudragit E using hydrochloric acid) to maximize the dissolution of trans-resveratrol. Solid-state characterization of amorphous solid dispersions of trans-resveratrol was performed using powder X-ray diffraction, scanning electron microscopy, and particle size measurements. In addition, an in vitro dissolution study and an in vivo pharmacokinetic study in rats were carried out. Among the tested polymers, Eudragit E/HCl was the most effective solid dispersion for the solubilization of trans-resveratrol. Eudragit E/HCl significantly inhibited the precipitation of trans-resveratrol in a pH 1.2 dissolution medium in a dose-dependent manner. The amorphous Eudragit E/HCl solid dispersion at a trans-resveratrol/polymer ratio of 10/90 exhibited a high degree of supersaturation without trans-resveratrol precipitation for at least 48 h by the formation of Eudragit E/HCl micelles. In rats, the absolute oral bioavailability (F%) of trans-resveratrol from Eudragit E/HCl solid dispersion (10/90) was estimated to be 40%. Therefore, trans-resveratrol-loaded Eudragit E/HCl solid dispersions prepared by spray drying offer a promising formulation strategy with high oral bioavailability for developing high-quality health supplements, nutraceutical, and pharmaceutical products.

Characterization of Novel Solid Dispersions of Moringa oleifera Leaf Powder Using Thermo-Analytical Techniques

Processes ◽  
2021 ◽  
Vol 9 (12) ◽  
pp. 2230
Author(s):  
Nontsikelelo Noxolo Tafu ◽  
Victoria A. Jideani
Keyword(s):  
Solid Dispersion ◽  
Moringa Oleifera ◽  
Solid Dispersions ◽  
Intermolecular Hydrogen Bond ◽  
Thermo Gravimetric Analysis ◽  
Analytical Techniques ◽  
Gravimetric Analysis ◽  
Scanning Calorimetry ◽  
Hydrogen Bond Interactions ◽  
Leaf Powder

Moringa oleifera leaf powder (MOLP) has been identified as the most important functional ingredient owing to its rich nutritional profile and healthy effects. The solubility and functional properties of this ingredient can be enhanced through solid dispersion technology. This study aimed to investigate the effects of polyethylene glycols (PEGs) 4000 and 6000 as hydrophilic carriers and solid dispersion techniques (freeze-drying, melting, solvent evaporation, and microwave irradiation) on the crystallinity and thermal stability of solid-dispersed Moringa oleifera leaf powders (SDMOLPs). SDMOLPs were dully characterized using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermo-gravimetric analysis (TGA), and Fourier transform infrared spectroscopy (FTIR). The PXRD results revealed that the solid dispersions were partially amorphous with strong diffraction peaks at 2θ values of 19° and 23°. The calorimetric and thermogravimetric curves showed that PEGs conferred greater stability on the dispersions. The FTIR studyrevealed the existence of strong intermolecular hydrogen bond interactions between MOLP and PEG functional groups. MOLP solid dispersions may be useful in functional foods and beverages and nutraceutical formulations.

ENHANCED DISSOLUTION OF A POORLY WATER-SOLUBLE DRUG BY SOLID DISPERSIONS (SOLVENT EVAPORATION) TECHNIQUE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 13-19
Author(s):  
R. O Sonawane ◽  
◽  
S. Nayak ◽  
M. D. Chaudhari ◽  
V. V. Pande
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Differential Scanning Calorimetric ◽  
Maximum Enhancement ◽  
Enhanced Dissolution ◽  
Water Soluble Drugs ◽  
Fusion Methods ◽  
Poorly Water Soluble

The poorly water soluble drugs tend to have low bioavailability and this can be improved by several methods. Solid dispersion is a promising formulation approach to improve solubility and dissolution and ultimately oral bioavailability of these drugs. The aim of this study was to prepare and characterize solid dispersion of anti-diabetic glimepiride, a BCS class II drug, with the hydrophilic carrier PVP K30 by solvent evaporation and microwave induced fusion methods. Scanning electron microscopy (SEM), X–ray powder diffractometry (XRD) and differential scanning calorimetric (DSC) were used to evaluate the physical state of the drug. The solid dispersions were also evaluated for drug content, solubility and dissolution studies. Solid dispersions prepared by solvent evaporation method were showed maximum enhancement of solubility and dissolution in comparison to that prepared by other method.

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