scholarly journals Enhancement of Dissolution Profile of Poorly Water Soluble Loratadine by Solid Dispersion Technique

2017 ◽  
Vol 15 (2) ◽  
pp. 195-201
Author(s):  
Md Zahir Uddin ◽  
Jakir Ahmed Chowdhury ◽  
Ikramul Hasan ◽  
Md Selim Reza
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Release Mechanism ◽  
Dissolution Profile ◽  
X Ray Diffraction ◽  
Dissolution Properties ◽  
Poorly Water Soluble ◽  
Dispersion Technique ◽  
Physical Mixtures

This study was carried out to improve the dissolution properties of loratadine by solid dispersion technique. A series of solid dispersions of loratadine in PVP K-30 (1:1, 1:3 and 1:5) were prepared by kneading technique. The prepared solid dispersions were characterized by various physicochemical properties (fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy) and the dissolution characteristics were compared with loratadine and the physical mixtures of loratadine. It was revealed from the physicochemical analyses that there was a good compatibility between drug and carrier. On the other hand, the drug release from the prepared binary solid dispersions was significantly enhanced in comparison to both drug alone and the physical mixtures. Finally solid dispersion of loratadine: PVP K-30 prepared as 1:5 ratio was found to be described by non-Fickian release mechanism and was selected as the best formulation in this study.Dhaka Univ. J. Pharm. Sci. 15(2): 195-201, 2016 (December)

scholarly journals Enhancing dissolution profile of diazepam using hydrophilic polymers by solid dispersion technique

2012 ◽  
Vol 1 (12) ◽  
pp. 423-430 ◽  
Author(s):  
Md. Sariful Islam Howlader ◽  
Jayanta Kishor Chakrabarty ◽  
Khandokar Sadique Faisal ◽  
Uttom Kumar ◽  
Md. Raihan Sarkar ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Distilled Water ◽  
Dissolution Profile ◽  
Peg 6000 ◽  
Solvent Method ◽  
Pure Drug ◽  
Dispersion Technique

The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug by a solid dispersion technique, in order to investigate the effect of these polymers on release mechanism from solid dispersions. Diazepam was used as a model drug to evaluate its release characteristics from different matrices. Solid dispersions were prepared by using polyethylene glycol 6000 (PEG-6000), HPMC, HPC and Poloxamer in different drug-to-carrier ratios (1:2, 1:4, 1:6, 1:8, 1:10). The solid dispersions were prepared by solvent method. The pure drug and solid dispersions were characterized by in vitro dissolution study. Distilled water was used as dissolution media, 1000 ml of distilled water was used as dissolution medium in each dissolution basket at a temperature of 37°C and a paddle speed of 100 rpm. The very slow dissolution rate was observed for pure Diazepam and the dispersion of the drug in the polymers considerably enhanced the dissolution rate. This can be attributed to improved wettability and dispersibility, as well as decrease of the crystalline and increase of the amorphous fraction of the drug. SEM (Scanning Electron microscope) studies shows that the solid dispersion having a uniform dispersion. Solid dispersions prepared with PEG-6000, Poloxamer showed the highest improvement in wettability and dissolution rate of Diazepam. Solid dispersion containing polymer prepared with solvent method showed significant improvement in the release profile as compared to pure drug, Diazepam.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12453 International Current Pharmaceutical Journal 2012, 1(12): 423-430

scholarly journals Dissolution study of Spironolactone by using solid dispersion technique

2012 ◽  
Vol 4 (2) ◽  
pp. 42-47
Author(s):  
Irwin Dewan ◽  
SM Ashraful Islam ◽  
Mohammad Shahriar
Keyword(s):  
Drug Delivery ◽  
Solid Dispersion ◽  
Release Rate ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Dispersion Technique

The main objective of the current study was to formulate poorly water soluble drug Spirinolactone by using solid dispersion technique in order to achieve a better dissolution rate which would further help in enhancing oral bioavailability. Solid dispersions were prepared using two methods; solvent method and fusion method. Solid dispersion was prepared by using polymers, such as Hydroxy propylymethyl cellulose (HPMC 6cp), Hydroxy propyl cellulose (HPC), Sodium carboxymethylcellulose (Na-CMC), Povidone K12, Povidone K30, Poloxamer 407. Solid dispersions containing Spironolactone with HPC (96.81%), HPMC 6cp (93.05%), Poloxamer 407 (90.84%) and Na-CMC (89.93%) provided higher release rate than the release rate of solid dispersion containing only Spironolactone (35.27%), and Spironolactone with Povidone K12 (76.17%), Povidone K30 (67.92%). So the present study revealed that the solid dispersion may be an ideal means of drug delivery system for poorly water soluble drugs. Further study in this field was required to establish these drug delivery systems so that in future it can be used effectively in commercial basis.DOI: http://dx.doi.org/10.3329/sjps.v4i2.7776S. J. Pharm. Sci. 4(2) 2011: 42-47

scholarly journals Enhancement of Solubility and Dissolution Characteristics of Ibuprofen by Solid Dispersion Technique

2012 ◽  
Vol 11 (1) ◽  
pp. 1-6 ◽  
Author(s):  
Md Abdullah Al Masum ◽  
Florida Sharmin ◽  
S M Ashraful Islam ◽  
Md Selim Reza
Keyword(s):  
Solid Dispersion ◽  
Phosphate Buffer ◽  
Drug Carrier ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
Saturation Solubility ◽  
Dispersion Technique ◽  
Physical Mixtures

In this study solid dispersions (SDs) of ibuprofen were prepared by melt dispersion technique using macrogol 4000 and macrogol 6000 as carrier. Physical mixtures (PMs) of ibuprofen were also prepared with the same carrier and in the same drug-carrier ratio (1:0.5, 1:1 and 1:1.5) to compare the dissolution profile. The solid dispersions and physical mixtures were investigated for drug loading, saturation solubility and dissolution behavior. Saturation solubility study was carried out in phosphate buffer (pH 7.2), 0.1 N HCl solution and distilled water. Solid dispersions were found effective to enhance the solubility of ibuprofen significantly in all the media. Dissolution test was carried out in two different media, phosphate buffer (pH 7.2) and 0.1 N HCl. Solid dispersion containing macrogol 6000 at the ratio of 1:1.5 (drug: carrier) showed faster and higher drug release and was found to be most effective among all the solid dispersions. Drug carrier interactions were studied by comparing Fourier Transform Infrared Spectroscopy (FT-IR) of solid dispersions with pure drug which revealed that the SDs were stable. So, solid dispersion may be an effective technique to enhance dissolution rate of ibuprofen. DOI: http://dx.doi.org/10.3329/dujps.v11i1.12480 Dhaka Univ. J. Pharm. Sci. 11(1): 1-6, 2012 (June)

scholarly journals Enhancement of Solubility Ibuprofen by Solid Dispersion Technique on Natural Mucilage

2021 ◽  
Vol 04 (10) ◽  
Author(s):  
Mr. Shikalgar S. S. ◽  
Keyword(s):  
Solid Dispersion ◽  
Phosphate Buffer ◽  
Drug Carrier ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
Saturation Solubility ◽  
Dispersion Technique ◽  
Physical Mixtures

In this study generally solid dispersions (SDs) of ibuprofen were prepared by for all intents and purposes melt dispersion technique using natural mucilage of Lemon seed as carrier, which really is quite significant. Physical mixtures (PMs) of ibuprofen literally were also prepared with the same carrier and in the same drug-carrier ratio (1:0.5, 1:1 and 1:1.5) to compare the dissolution profile, which generally is fairly significant. The solid dispersions and kind of physical mixtures for all intents and purposes were investigated for drug loading, saturation solubility and dissolution behavior in a subtle way. Saturation solubility study really actually was basically carried out in phosphate buffer (pH 7.4), 0.1 N HCL solution and distilled water, which kind of literally is quite significant. Solid dispersions for all intents and purposes particularly were mostly really found definitely fairly effective to literally kind of enhance the solubility of ibuprofen significantly in all the media, which actually is quite significant. Dissolution test specifically was mostly carried out in two different media, phosphate buffer (pH 7.4) and 0.1 N HCL. Solid dispersion containing Lemon seed mucilage at the ratio of 1:1.5 (drug: carrier) basically showed faster and sort of definitely higher drug release and basically was specifically really found to for the most part actually be most sort of effective among all the very actually solid dispersions in a generally big way, which kind of is fairly significant. Drug carrier interactions specifically specifically were studied by comparing Fourier definitely mostly Transform generally Infrared Spectroscopy (FT-IR) of particularly solid dispersions with pure drug which essentially revealed that the SDs specifically were kind of really stable in a pretty big way, which is fairly significant. So, fairly very solid dispersion may particularly be an definitely really effective technique to specifically enhance dissolution rate of ibuprofen, which kind of literally is fairly significant in a fairly big way.

scholarly journals Solid Dispersion (Kneading) Technique: A Platform for Enhancement Dissolution Rate of Valsartan Poorly Water Soluble Drug

2020 ◽  
Vol 11 (01) ◽  
pp. 20-24
Author(s):  
Vinod T. Wagh ◽  
Ritu M. Gilhotra ◽  
Rajendra D. Wagh
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
X Ray Diffraction ◽  
Water Soluble Drug ◽  
Kneading Method ◽  
Differential Scanning Colorimetry ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The objective of this study was to the enhancement of dissolution rate of Valsartan. Using a solid dispersion (kneading) method with Kollidon and Povidone K30 as a carrier. Eight different drugs: Carrier ratios were prepared. Using factorial design taking 3 factors i.e., the concentration of Valsartan (x1), Kollidon (x2), and Povidone K30(x3). The enhancement of dissolution depends on the amount of carrier and an increase in the concentration of carrier. Enhancement of dissolution rate depends on reduce particle size of drug place on the surface of carrier and increased wettability of drug particle by carrier. Solid Dispersions prepared with Kollidon as a carrier in ratio 1:4 shows the enhancing dissolution in 30 mins to drug and Physical Mixture. Formulation evaluated by fourier-transform infrared spectroscopy, differential scanning colorimetry, X-ray diffraction, Scanning Electron Microscopy.

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.

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 Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Polymers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 1679
Author(s):  
Thao T.D. Tran ◽  
Phuong H.L. Tran
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Insoluble Polymers

In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

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 Development and Biopharmaceutical Evaluation of Tablets Based on the Poorly Water-soluble Substance 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil

2020 ◽  
Vol 9 (4) ◽  
pp. 79-87
Author(s):  
D. V. Demchenko ◽  
E. A. Jain (Korsakova) ◽  
V. Yu. Balabanyan ◽  
M. N. Makarova ◽  
V. G. Makarov
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Active Pharmaceutical Ingredient ◽  
Oral Route ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Technological Properties ◽  
Enhanced Dissolution ◽  
Dispersion Technique

Introduction. 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil is a substance of scientific interest intended for the treatment of HIV-infection. However, its low bioavailability is a major limitation in successful drug delivery by oral route. Therefore, the objective of the present work was to enhance itssolubility by using solid dispersion technique followed by the development of a solid dosage form.Aim. Development of the composition and technology of tablets based on 1- [2-(2-benzoylphenoxy)ethyl]-6-methyluracil with the appropriate technological properties providing the most complete release of the active pharmaceutical ingredient (API) in vitro.Materials and methods. The pharmaceutical substance 1-[2-(2-benzoylphenoxy) ethyl]-6-methyluracil is a crystalline powder with poor solubility. Solid dispersions were prepared using Lactose, Kollidon® 17PF, Kollidon® 30, Kollidon® VA64, Kollidon 90F, and PEG-6000 as a carrier mostly in 1:4 ratio by two methods – co-melting and solvent evaporation. The technological properties of substance, tablet masses and tablet quality were determined according to the methods described in the State Pharmacopoeia of the Russian Federation (14th edition).Results and discussion. Article shows the results of development of the composition and technology of a medicine in the form of tablets based on the substance 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil. Solid dispersion technique was used to improve the biopharmaceutical properties of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil.Conclusion. In vitro dissolution studies showed enhanced dissolution rate of the drug-loaded solid dispersion with Kollidon 17PF as a carrier as compared to pure drug.

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