scholarly journals Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

2020 ◽  
Vol 21 (8) ◽  
Author(s):  
Athira R. Nair ◽  
Yarlagadda Dani Lakshman ◽  
Vullendula Sai Krishna Anand ◽  
K. S. Navya Sree ◽  
Krishnamurthy Bhat ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Informed Choice ◽  
Complete Classification ◽  
Subject Area ◽  
Polymeric Carrier ◽  
Polymeric Carriers ◽  
Scientific Papers ◽  
The Stability ◽  
Preparation Techniques

AbstractSolid dispersion is the preferred technology to prepare efficacious forms of BCS class-II/IV APIs. To prepare solid dispersions, there exist a wide variety of polymeric carriers with interesting physicochemical and thermochemical characteristics available at the disposal of a formulation scientist. Since the advent of the solid dispersion technology in the early 1960s, there have been more than 5000 scientific papers published in the subject area. This review discusses the polymeric carrier properties of most extensively used polymers PVP, Copovidone, PEG, HPMC, HPMCAS, and Soluplus® in the solid dispersion technology. The literature trends about preparation techniques, dissolution, and stability improvement are analyzed from the Scopus® database to enable a formulator to make an informed choice of polymeric carrier. The stability and extent of dissolution improvement are largely dependent upon the type of polymeric carrier employed to formulate solid dispersions. With the increasing acceptance of transfer dissolution setup in the research community, it is required to evaluate the crystallization/precipitation inhibition potential of polymers under dynamic pH shift conditions. Further, there is a need to develop a regulatory framework which provides definition and complete classification along with necessarily recommended studies to characterize and evaluate solid dispersions.

scholarly journals Formulation of Mouth Dissolving Tablets Using Solid Dispersion Technique: A Review

2018 ◽  
Vol 6 (03) ◽  
pp. 66-72
Author(s):  
Gurpreet Singh ◽  
Jayesh Dwivedi ◽  
Jeyabalan Govindasamy ◽  
Naresh Kalra ◽  
Rajesh Sharma
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Two Component System ◽  
Solvent Method ◽  
Agglomeration Process ◽  
Process Use ◽  
Dispersion Technique ◽  
The Stability ◽  
Industrial Level ◽  
Drug Polymer Interaction

Mouth-dissolving tablets are also called as fast disintegrating tablets, melt-in mouth tablets, orodispersible tablets, quick dissolving etc. Mouth dissolving tablets are those when put on tongue disintegrate rapidly thereby releasing the drug, which dissolve or disperses in the saliva. The faster the drug dissolved into solution, quick will be the absorption and onset of clinical effect. Mouth dissolving tablet containing solid dispersion was developed to improve the solubility of drug and stability of solid dispersion. Such tablets are disintegrate and/or dissolve rapidly in the saliva without the need for water. Hence it is regarded as the safest, most convenient and most economical method of drug delivery having the highest patient compliance. The later portion of the article focus on the progress in methods of manufacturing, evaluation and various latest technologies involved in the development of Mouth dissolving tablets. Solid dispersion is basically a drug with polymer two-component system; hence the drug–polymer interaction should be determined first in order to ensure the stability of the formulation. This review is intended to discuss the recent advances related on the area of solid dispersion technology. Since different methods are used for the preparation of solid dispersions such as fusion method, solvent method, melting solvent method, melt extrusion method, lyophilisation technique, melt agglomeration process, use of surfactant, electro spinning and super Critical Fluid Technology, of them which method is good and suitable for which type of drug. The use of Mouth dissolving dosage forms has solved various problems noted in administration of drugs to the pediatric and elderly patient, which constitutes a large proportion of the world's population. The initial focus of this 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 An attempt to improve the solubility and stability of Ocimum tenuiflorum aqueous leaves extract

Food Research ◽  
2021 ◽  
Vol 5 (1) ◽  
pp. 357-365
Author(s):  
Rohini J. ◽  
Muhammad Ezzudin R. ◽  
Rabeta M.S.
Keyword(s):  
Medicinal Plants ◽  
Bioactive Compounds ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Health Benefits ◽  
Active Compounds ◽  
Different Types ◽  
Ocimum Tenuiflorum ◽  
The Stability

Medicinal plants have gained attention in recent years due to the presence of various bioactive compounds which promote distinct health benefits and is less toxic. However, the plants face common and serious problems due to their active compounds which are the solubility and stability. Ocimum tenuiflorum, one of the ancient medicinal plants were its medicinal values have been widely studies. Yet, study to improve its quality still lacking. Thus, an effort was taken to study and improve the solubility and stability of the plant. Solid dispersions were prepared with extract and different types of surfactants at different ratio have used to improve the stability. Lecithin (1:1 ratio) have improved the solubility significantly (p<0.05) when compared to extract. Enhancement in solubility, hence improved the stability when stored at 4°C of the solid dispersion of extract. Overall, the study has successfully improved the quality of the extract with lecithin complex whereby the solubility and increases stability.

scholarly journals Characterization Methods of Amorphous Form Stability in Solid Dispersion : A Review

2020 ◽  
Vol 2 (2) ◽  
pp. 55
Author(s):  
Maria Elvina Tresia Butarbutar ◽  
Nasrul Wathoni ◽  
Yoga Windu Wardhana
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Amorphous Solid ◽  
Stable Form ◽  
Characterization Methods ◽  
Amorphous Form ◽  
Pharmaceutical Ingredients ◽  
The Stability ◽  
Form Stability

Solubility as a cause of ineffective active pharmaceutical ingredients (API) needs to be a concern. One of the solutions to increase the solubility by choosing active ingredients in the amorphous form. However, the amorphous form tends to be unstable because it has high Gibbs free energy and molecular mobility. To overcome those properties solid dispersion methods can be an answer. The dispersion of the amorphous form in the polymer is expected to prevent the transformation of API to crystal stable form. The solid dispersion (SD) resulted needs for physicochemical characterization to prove the ability of SD to maintain the amorphous form. Therefore, the physicochemical properties of the amorphous solid dispersions (ASDs) have to analyze there in any interactions that are able to occur between the drug and the polymer. Also for evaluate the stability of the ASDs within a certain period. In the article presents, some articles related with ASDs and its characterization will studying, include several product on the market as example. The number of literature used in this article is 69 articles.Keywords: Solubility, amorphous for, solid dispersion, characterization ASDs.

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.

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.

scholarly journals Solid Dispersions of Anthelmintics and Plant Protection Preparations

Solids ◽  
2021 ◽  
Vol 2 (1) ◽  
pp. 60-75
Author(s):  
Salavat S. Khalikov
Keyword(s):  
Plant Protection ◽  
Rapid Development ◽  
Solid Dispersions ◽  
Animal Health ◽  
Water Soluble ◽  
Biologically Active ◽  
Cultivated Plants ◽  
Industrial Complex ◽  
Scientific Papers ◽  
Poorly Soluble

Because of the rapid development of nanotechnologies, materials, in particular, solid dispersions (SDs), which are actively introduced into the life of modern man, have been obtained. Special progress in this area is observed in industry and medicine. The use of SDs in agriculture is lagging far behind, despite the growing number of scientific papers on this topic. At the same time, the prospects for the introduction of SDs in the agro-industrial complex are obvious. The review presents the results of research on the development of innovative preparations based on SD to protect plants from diseases and pests of cultivated plants, as well as parasiticides to protect animal health based on modern achievements of nanotechnology. One of these technologies is the methods of mechanochemistry, which improve the properties of poorly soluble biologically active substances by their joint mechanical treatment with water-soluble polymers and auxiliary substances.

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.

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