Formulation and Evaluation of Atorvastatin Solid Dispersions using Entada scandens seed starch as Superdisintegrant

2021 ◽  
pp. 5141-5149
Author(s):  
Sandeep Doppalapudi ◽  
Vidyadhara Suryadevara ◽  
Sailaja Yallam ◽  
Sowjanya Lakshmi Battula ◽  
Vanya Nayudu
Keyword(s):  
Solid Dispersions ◽  
Pharmaceutical Research ◽  
Surface Characteristics ◽  
Water Soluble ◽  
Physical Parameters ◽  
Poorly Soluble Drugs ◽  
Scanning Calorimetry ◽  
Dsc Studies ◽  
Poorly Soluble ◽  
Evaporation Technique

The present work mainly focuses on solubility enhancement of poorly soluble drugs using superdisintegrants. One of such poorly soluble drugs is Atorvastatin, which belongs to the category of statins. Atorvastatin belongs to BCS class – II, which is poorly water soluble and highly permeable. Natural sources are now-a-days playing a key role in pharmaceutical research. They have several pharmaceutical applications. Starches obtained from plants are pharmaceutically useful as binders, diluents, disintegrants and lubricants. Various physical parameters were evaluated. Solid dispersions were prepared using solvent evaporation technique. Where as in solid dispersions, formulations F2 and F5 showed better dissolution rate compared with other formulations. Fourier Transform Infra red spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) studies for optimized formulations revealed that there were no major interactions between the drug and excipients. X-Ray Diffraction (XRD) studies revealed the crystalline and amorphous nature of formulations. Scanning Electron Microscopy (SEM) revealed the surface characteristics. Thus from the present study, it was concluded that Entada scandens seed starch posses superdisintegrant property.

scholarly journals ENHANCEMENT OF THE SOLUBILITY OF FAMOTIDINE SOLID DISPERSION USING NATURAL POLYMER BY SOLVENT EVAPORATION

2021 ◽  
pp. 193-198
Author(s):  
HUSSEIN K. ALKUFI ◽  
ASMAA M. RASHID
Keyword(s):  
Hyaluronic Acid ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Natural Polymer ◽  
Solubility Study ◽  
Poorly Soluble ◽  
Pure Drug

Objective: The aims of the study to enhance solubility and dissolution of famotidine using natural polymer. Solubility study of a drug is one of the contributing factors of its oral bioavailability. The formulation of poorly soluble drugs for oral delivery presents a challenge to the formulation technologists. Methods: The present study has shown that it is possible to raise the solubility for poorly soluble drugs like famotidine, by preparing solid dispersion using natural water-soluble polymer (xyloglucan and hyaluronic acid) as solubilizer through solvent evaporation method. Physical mixture and solid dispersion of famotidine with xyloglucan (XG) or hyaluronic acid in a ratio of 1:1, 1:2, 1:3 were prepared. Solubility study, drug content, dissolution profile and compatibility study were performed for famotidine in solid dispersions XS1, XS2, XS3, HS4, HS5, HS6 as well as in physical mixtures at a ratio 1:1 for both polymer (XG and hyaluronic acid). Results: It was observed that solid dispersions of each drugs showed an increase in dissolution rate in comparison with its pure drug in the ratio of 1:1 (Drug: carrier). It can be concluded that with the care and proper use of xyloglucan, the solubility of drugs poorly soluble can be improved. The prepared solid dispersion showed improvement of drug solubility in all prepared formulas. The best result was obtained with formula XS1 (famotidine: xyloglucan at ratio 1:1) that showed 26 fold increase in solubility compared to the solubility of pure drug. Conclusion: The natural solid dispersion, increased wettability and reduced crystallinity of the drug which leads to improving solubility and dissolution.

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 Carboxymethyl Cellulose Acetate Butyrate: A Review of the Preparations, Properties, and Applications

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Mohamed El-Sakhawy ◽  
Samir Kamel ◽  
Ahmed Salama ◽  
Hebat-Allah Sarhan
Keyword(s):  
Cellulose Acetate ◽  
Carboxymethyl Cellulose ◽  
Solid Dispersions ◽  
Pharmaceutical Research ◽  
Amorphous Solid ◽  
Water Soluble ◽  
Cellulose Acetate Butyrate ◽  
Wide Range ◽  
Poorly Soluble ◽  
Acetate Butyrate

Carboxymethyl cellulose acetate butyrate (CMCAB) has gained increasing importance in several fields, particularly in coating technologies and pharmaceutical research. CMCAB is synthesized by esterification of CMC sodium salt with acetic and butyric anhydrides. CMCAB mixed esters are relatively high molecular weight (MW) thermoplastic polymers with high glass transition temperatures (Tg). CMCAB ester is dispersible in water and soluble in a wide range of organic solvents, allowing varied opportunity to the solvent choice. It makes application of coatings more consistent and defect-free. Its ability to slow down the release rate of highly water-soluble compounds and to increase the dissolution of poorly soluble compounds makes CMCAB a unique and potentially valuable tool in pharmaceutical and amorphous solid dispersions (ASD) formulations.

Formulation and Evaluation of Gliclazide Tablets Containing PVP-K30 and Hydroxypropyl-β-cyclodextrin Solid Dispersion

2012 ◽  
Vol 5 (2) ◽  
pp. 1706-1719
Author(s):  
Mohan M Varma ◽  
Satish Kumar P
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Drug Polymer Interaction ◽  
Pvp K30

Gliclazide is an anti-diabetic drug. It is a BCS class-II (poorly water soluble) drug and its bioavailability is dissolution rate limited. The dissolution rate of the drug was enhanced by using the solid dispersion technique. Solid dispersions were prepared using PVP-K30 (polyvinylpyrrolidone) and hydroxypropyl-β-cyclodextrin (HP BCD) as the hydrophilic carriers. The solid dispersions were characterized by using DSC (Differential scanning calorimetry), XRD (X-ray diffractometry) and FTIR (Fourier transform infrared spectroscopy). Solid dispersions were formulated into tablets. The formulated tablets were evaluated for the quality control parameters and dissolution rates. The solid-dispersion tablets enhanced the dissolution rate of the poorly soluble drug. The optimized formulation showed a 3 fold faster drug release compared to the branded tablet. The XRD studies demonstrated the remarkable reduction in the crystallinity of the drug in the solid dispersion. The faster dissolution rate of the drug from the solid dispersion is attributed to the marked reduction in the crystallinity of the drug. The DSC and FTIR studies demonstrated the absence of the drug-polymer interaction.

scholarly journals Solid Dispersion: Solubility Enhancement Technique of Poorly Water Soluble Drug

2020 ◽  
Vol 10 (1) ◽  
pp. 173-177 ◽  
Author(s):  
, Ikram ◽  
Kapil Kumar
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Inert Carrier ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersion is a technique which is widely and successfully applied to improve the solubility, dissolution rates and consequently the bioavailability of poorly soluble drugs. Dispersion of one or more active ingredients (hydrophobic) is done with an inert carrier (hydrophilic) at solid-state prepared by fusion method, solvent, and melting solvent method. In this review article, we have focused on the methods of preparation, advantages, disadvantages and characterization of the solid dispersions. Keywords: Solid dispersion; dissolution; solubility.

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.

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 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.

scholarly journals Relative Contributions of Solubility and Mobility to the Stability of Amorphous Solid Dispersions of Poorly Soluble Drugs: A Molecular Dynamics Simulation Study

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 101 ◽  
Author(s):  
Michael Brunsteiner ◽  
Johannes Khinast ◽  
Amrit Paudel
Keyword(s):  
Molecular Dynamics ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Dynamics Simulation ◽  
Limiting Factor ◽  
Poorly Soluble Drugs ◽  
Formulation Development ◽  
Amorphous Solid Dispersions ◽  
Poorly Soluble

Amorphous solid dispersions are considered a promising formulation strategy for the oral delivery of poorly soluble drugs. The limiting factor for the applicability of this approach is the physical (in)stability of the amorphous phase in solid samples. Minimizing the risk of reduced shelf life for a new drug by establishing a suitable excipient/polymer-type from first principles would be desirable to accelerate formulation development. Here, we perform Molecular Dynamics simulations to determine properties of blends of eight different polymer–small molecule drug combinations for which stability data are available from a consistent set of literature data. We calculate thermodynamic factors (mixing energies) as well as mobilities (diffusion rates and roto-vibrational fluctuations). We find that either of the two factors, mobility and energetics, can determine the relative stability of the amorphous form for a given drug. Which factor is rate limiting depends on physico-chemical properties of the drug and the excipients/polymers. The methods outlined here can be readily employed for an in silico pre-screening of different excipients for a given drug to establish a qualitative ranking of the expected relative stabilities, thereby accelerating and streamlining formulation development.

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