scholarly journals SOLID DISPERSION FOR INCREASING DISSOLUTION RATE OF SODIUM DICLOFENAC WITH VARIATIONS OF POLYVINYL PYRROLIDONE K30

2021 ◽  
Vol 3 (2) ◽  
pp. 86-98
Author(s):  
Noval Noval ◽  
◽  
Rosyifa Rosyifa ◽  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Diclofenac Sodium ◽  
Sodium Diclofenac ◽  
Significant Difference ◽  
Moisture Percentage ◽  
Inert Carrier ◽  
Low Solubility ◽  
Pvp K30

Diclofenac sodium is included in class II category based on biopharmaceutics classification system (BCS), sodium diclofenac has low solubility and high permeability. Low solubility will affect absorption of drugs in body because rate of dissolution will decrease. PVP K30 is inert carrier that dissolves easily in water and can affect solubility of an active drug substance. To know solid dispersion system increasing dissolution rate of sodium diclofenac by adding variations concentration of PVP K30. Solid dispersion uses solvent method with variations concentration of PVP K30 1:3, 1:5, 1:7 and 1:9. Test physical properties of solid dispersions using a moisture test and compressibility. Solid dispersion dissolution test using type 2 dissolutions test and determination of concentration using UV-VIS spectrophotometry. Test results were analyzed using One Way ANOVA and continued test. Solid dispersion has a good physical whit moisture percentage not >5% and compressibility not >20%. Solid dispersion of sodium diclofenac with addition of PVP K30 can increase dissolution rate compared to pure sodium diclofenac (p<0,05) with highest at ratio 1:7. Each comparison has significant difference (p<0,05) expect in ratio 1:9. Solid dispersion of sodium diclofenac with PVP K30 can increase dissolution rate of pure sodium diclofenac.

scholarly journals Dispersi Padat untuk Peningkatan Laju Disolusi Natrium Diklofenak dengan Variasi Konsentrasi Polivinil Pirolidon K30

2021 ◽  
Vol 6 (2) ◽  
pp. 94-101
Author(s):  
Noval Noval ◽  
Rosyifa Rosyifa
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Diclofenac Sodium ◽  
The Body ◽  
Sodium Diclofenac ◽  
Significant Difference ◽  
Moisture Percentage ◽  
Low Solubility ◽  
Pvp K30

Diclofenac sodium is included in the class II category based on the biopharmaceutics classification system (BCS), sodium diclofenac has low solubility and high permeability. Low solubility will affect the absorption of drugs in the body because the rate of dissolution will decrease. Polyvinyl Pyrrolidone (PVP) K30 is an inert carrier that dissolves easily in water and can affect the solubility of an active drug substance. To know solid dispersion system increasing dissolution rate of sodium diclofenac by adding variations concentration of PVP K30. Solid dispersion uses a solvent method with variations concentration of PVP K30 1:3, 1:5, 1:7, and 1:9. Test physical properties of solid dispersions using a moisture test and compressibility. Solid dispersion dissolution test using type 2 dissolutions test and determination of concentration using UV-VIS spectrophotometry. Test results were analyzed using One Way ANOVA and continued test. Solid dispersion has a good physical whit moisture percentage not >5% and compressibility not >20%. Solid dispersion of sodium diclofenac with the addition of PVP K30 can increase dissolution rate compared to pure sodium diclofenac (p<0,05) with the highest ratio 1:7. Each comparison has a significant difference (p<0,05) except in ratio 1:9. Solid dispersion of sodium diclofenac with PVP K30 can increase the dissolution rate of pure sodium diclofenac.

scholarly journals Solid Dispersions : An Approach to Enhance the Bioavailability of Poorly Water-Soluble Drugs

2013 ◽  
pp. 37-46
Author(s):  
Sanjoy Kumar Das
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Historical Background ◽  
Solid Dosage ◽  
Advantages And Disadvantages ◽  
Water Soluble Drugs ◽  
Inert Carrier ◽  
Dispersion Technique

Improving oral bioavailability of drugs those given as solid dosage forms remains a challenge for the formulation scientists due to solubility problems. The dissolution rate could be the rate-limiting process in the absorption of a drug from a solid dosage form of relatively insoluble drugs. Therefore increase in dissolution of poorly soluble drugs by solid dispersion technique presents a challenge to the formulation scientists. Solid dispersion techniques have attracted considerable interest of improving the dissolution rate of highly lipophilic drugs thereby improving their bioavailability by reducing drug particle size, improving wettability and forming amorphous particles. The term solid dispersion refers to a group of solid products consisting of at least two different components, generally a hydrophilic inert carrier or matrix and a hydrophobic drug. This article reviews historical background of solid dispersion technology, limitations, classification, and various preparation techniques with its advantages and disadvantages. This review also discusses the recent advances in the field of solid dispersion technology. Based on the existing results and authors’ reflection, this review give rise to reasoning and suggested choices of carrier or matrix and solid dispersion procedure.

scholarly journals Review: Solid Dispersion of Fenofibrate Using Poly Ethylene Glycol 6000

2021 ◽  
Vol 6 (6) ◽  
pp. 42-51
Author(s):  
Nelvia Helsinta ◽  
Auzal Halim ◽  
Maria Dona Octavia ◽  
Harrizul Rivai
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Literature Search ◽  
Solid Dispersions ◽  
Poly Ethylene Glycol ◽  
Peg 6000 ◽  
Poly Ethylene ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

This review aimed to find information about the solubility of the fenofibrate solid dispersion system using PEG 6000. Fenofibrate is an antihyperlipidemic drug that belongs to the Biopharmaceutical Classification System Class II (BCS II) with low solubility. To find information was by conducting a literature search in national and international journals in the last ten years (2010-2020) through websites, namely Google Scholar, Science Direct, NCBI, ResearchGate, and other trusted journals. Several keywords were used as follows: fenofibrate, solid dispersion, PEG 6000, and dissolution rate. The results of several research journals showed that the solid dispersion of fenofibrate using PEG 6000 made by various methods causes a reduction in particle size to increase the solubility and dissolution rate of fenofibrate. The solid dispersions system was made using several methods, namely fusion (melting), solvent evaporation, dropping, and co-grinding, which is a technique used to increase the solubility of a drug. PEG 6000 was chosen as the carrier because it has high hydrophilicity, is non-toxic, inert, economical, has a low melting point, and is dense at melting temperature to withstand crystallization. Thus it can be concluded that the manufacture of solid dispersion of fenofibrate using PEG 6000 and several methods showed the same results, namely an increase in solubility and dissolution rate.

scholarly journals FORMULATION OF SOLID DISPERSIONS FOR ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF SIMVASTATIN

2021 ◽  
pp. 94-100
Author(s):  
PAYAL D. BORAWAKE ◽  
KAUSLYA ARUMUGAM ◽  
JITENDRA V. SHINDE
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Fourier Transforms ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Drug Content ◽  
Pvp K30

Objective: The objective of the present work was to formulate the solid dispersions of simvastatin for enhancement of its aqueous solubility and dissolution rate. Methods: In the present study, solid dispersions of simvastatin were prepared by Kneading and Solvent evaporation methods. The polymeric carriers like Polyethylene glycol (PEG) 6000 and Polyvinyl Pyrrolidone (PVP) K30 were used in different ratios (ratio of drug: carrier was 1:1, 1:2) to formulate solid dispersions. The prepared solid dispersions were characterized by differential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FTIR), and evaluated for drug content, percentage yield, saturation solubility, in vitro dissolution studies. The best formula of the solid dispersion was selected according to the solubility and dissolution data. Results: The F7 formulation was found to be an optimized formulation containing PVP K30 in the ratio 1:1 prepared by solvent evaporation technique. The Drug content was found to be higher i.e. 94.89 in the F7 batch. The FT-IR spectra revealed that there was no interaction between drugs and carriers. DSC thermogram indicated entrapment of simvastatin in PVP K30 and the conversion of crystalline simvastatin into an amorphous form. The F7 formulation showed maximum drug release i.e. 98.60% in 60 min which is 2 times greater than pure drug making it an optimized formulation. Conclusion: The solubility of simvastatin was successfully enhanced through the solid dispersion technique. Solid dispersions prepared with solvent evaporation method were more soluble than solid dispersions prepared with kneading method with carrier PVP K30.

Enhancement of Dissolution Rate of Daidzein in Ternary Solid Dispersions

2012 ◽  
Vol 550-553 ◽  
pp. 1000-1004 ◽  
Author(s):  
Hui Wang ◽  
Hong Xin Xu ◽  
Na Zhang ◽  
Lian Dong Hu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
X Ray Diffraction ◽  
Positive Role ◽  
X Ray ◽  
Dissolution Tests ◽  
Ternary Solid Dispersions ◽  
Pvp K30

The purpose of this study was to enhance the dissolution rate of daidzein (DZ) by solid dispersions. DZ solid dispersion was prepared by solvent method, with PVP K30 and surfactant as carriers. The influences of drug-carrier proportion, the kind of surfactant and the amount of surfactant on the dissolution of DZ were examined. Solid dispersions were characterized by infrared spectroscopy (IR), X-ray diffraction spectroscopy, and dissolution tests. When appropriate amount of poloxamer was added into the solid dispersion, the dissolution of DZ could be improved obviously. The data of IR showed that the absence of well-defined drug-polymer interactions. The data of X-ray diffraction showed that the drug might exist in the form of amorphism or molecule in solid dispersions. Both the binary and ternary solid dispersions enhanced the dissolution of DZ. Moreover, poloxamer played an important positive role in improving the dissolution rate of DZ in the solid dispersion.

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 Enhancement of Dissolution Rate of Gliclazide Using Solid Dispersions: Characterization and Dissolution Rate Comparison

2013 ◽  
Vol 16 (1) ◽  
pp. 45-52 ◽  
Author(s):  
Sharmi Islam ◽  
Laboni Rani Dey ◽  
Mohammad Shahriar ◽  
Irin Dewan ◽  
SM Ashraful Islam
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Poloxamer 407 ◽  
Dissolution Behavior ◽  
Significant Difference ◽  
Xrd Studies

In this study solid dispersion (SDs) of gliclazide were prepared by solvent evaporation technique using poloxamer 407 as carrier. Drug carrier weight ratio were 1:1, 1:3 and 1:5. Physical mixtures of the same ratio were also prepared for comparison. The solid dispersions were investigated for drug loading and dissolution behavior and were found effective to enhance the solubility of gliclazide in dissolution medium significantly. Evaluation of the properties of the SDs was also performed by using Fourier-transform infrared (FTIR) spectroscopy and X-ray diffraction (XRD) studies. The FTIR spectroscopic studies showed the stability of gliclazide and absence of interaction between gliclazide and poloxomer 407. The XRD studies indicated the amorphous state of gliclazide in SDs. Dissolution data of SDs were compared by using both model dependant and model independent techniques. No significant difference in % DE (dissolution efficiency) was found among the SDs. But the drug release rate from SDs differs from that of physical mixture. So, solid dispersion technique may be an effective way to enhance dissolution rate of gliclazide. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14490 Bangladesh Pharmaceutical Journal 16(1): 45-52, 2013

Solubility Enhancement of Poorly Soluble Drug Simvastatin by Solid Dispersion Technique

2016 ◽  
Vol 2 (2) ◽  
pp. 91-95
Author(s):  
Neelima Rani T ◽  
Pavani A ◽  
Sobhita Rani P ◽  
Srilakshmi N
Keyword(s):  
Dissolution Rate ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Onset Of Action ◽  
Kneading Method ◽  
Wetting Property ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Low Solubility

This study aims to formulate solid dispersions (SDs) of Simvastatin (SIM) to improve the aqueous solubility, dissolution rate and to facilitate faster onset of action. Simvastatin is a BCS class II drug having low solubility & therefore low oral bioavailability. In the present study, SDs of simvastatin different drug-carrier ratios were prepared by kneading method. The results showed that simvastatin solubility & dissolution rate enhanced with polymer SSG in the ratio 1:7 due to increase in wetting property or possibly may be due to change in crystallinity of the drug.

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 Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

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