scholarly journals Optimizing surfactant ratio for the production of capsules containing glicazide using solid dispersion technique

2017 ◽  
Vol 2 (1) ◽  
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Flow Property ◽  
Angle Of Repose ◽  
Dispersion Method ◽  
Peg 6000 ◽  
Comparison Results ◽  
Model Drug ◽  
Dispersion Technique

The objective of this study was to formulate and prepare gliclazide capsule by solid dispersion method using different surfactants and their in vitro evaluation. Solubilising capacity of polyethylene glycol (PEG 6000, PEG 20000) and polyvinylpyrrolidone (PVP K 30) was determined at 2% concentration where gliclazide was used as a model drug and water was used as control for comparison. Results showed that PVP K 30 exhibited maximum solubilising capacity. Fusion method of solid dispersion was adopted for preparation of capsules using PEG 6000 & PEG 20000 in different ratios. Although these agents are claimed to be good surfactants but our results showed that, the highest cumulative drug release was 1.81 % for gliclazide and PEG 6000 in a ratio of 1:6. The flow property of capsule granules was determined by angle of repose. The capsules were also subjected to weight uniformity test, disintegration test and moisture permeation test and the chemical analysis of solid dispersions were done by FTIR. From this study, it can be concluded that it is possible to formulate and prepare gliclazide capsule by using solid dispersion method.

scholarly journals DEVELOPMENT AND EVALUATION OF MONOLITHIC OSMOTIC TABLET OF KETOPROFEN: USING SOLID DISPERSION TECHNIQUE

2016 ◽  
Vol 8 (12) ◽  
pp. 41
Author(s):  
S. Kaushik ◽  
Kamla Pathak
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Immediate Release ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 6000 ◽  
Environmental Media ◽  
Dispersion Technique

<p><strong>Objective: </strong>The aim of the present study was to develop and evaluate the monolithic osmotic tablet (MOT) composed of the solid dispersion of ketoprofen (KETO), a poorly water-soluble drug. Solid dispersion technique is generally used for immediate release, as this maximizes the amount of drug absorbed. Sustained release may be obtained by combining solid dispersion technique with MOT so as to increase the therapy efficacy and patient compliance.</p><p><strong>Methods: </strong>Solid dispersion of KETO was prepared by using solvent melt method with polyethylene glycol (PEG) 6000, a hydrophilic carrier. The ratio of KETO to PEG 6000 were 1:1, 1:3 and 1:5 (%w/w). These solid dispersions were characterized by differential scanning calorimetry (DSC), Thermogravimetric analysis (TGA) and powder X-ray diffraction (PXRD) to ascertain whether there were any physicochemical interactions between drug and carrier.</p><p>The tablet core was prepared by using Polyox N80 (a suspending agent), sodium chloride (an osmotic agent), a solid dispersion consisting of PEG 6000 and KETO followed by a coating of cellulose acetate to make the monolithic osmotic tablet.</p><p><strong>Results: </strong>The results of DSC and PXRD indicated that the drug was in the amorphous state in solid dispersion when PEG 6000 was used as a carrier. The dissolution rate of the solid dispersion was much faster than those for the corresponding physical mixture and pure drug. The optimized MOT formulations were able to deliver KETO at the constant zero order release, above 95% <em>in vitro</em>, independent to environmental media and stirring rate. The release rate of KETO in the MOT is controlled by osmotic pressure, suspending agent and drug solubility in solid dispersion.</p><p><strong>Conclusion: </strong>The monolithic osmotic tablet containing solid dispersion has great potential in the controlled delivery of ketoprofen, a water-insoluble drug.</p><p><strong>Keywords: </strong>Ketoprofen, Monolithic osmotic tablet, Solid dispersion, Water insoluble</p>

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 DEVELOPMENT AND IN VITRO DISSOLUTION STUDY OF BINARY AND TERNARY SOLID DISPERSIONS OF ACECLOFENAC

2019 ◽  
Author(s):  
Md. Shahidul Islam ◽  
Rasheda Akter Lucky
Keyword(s):  
Polyethylene Glycol ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Peg 6000

The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.

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.

scholarly journals Enhancement of dissolution rate of Olmesartan medoxomil using urea as carrier by different solid dispersion techniques

2018 ◽  
Vol 1 (1) ◽  
pp. 36-42
Author(s):  
B Sangameswaran ◽  
M Gomathi
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Olmesartan Medoxomil ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Poor Solubility ◽  
Co Precipitation

The poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T fluid often leads to insufficient bioavailability. As per Biopharmaceutical Classification System (BCS), Olmesartan belongs to the class-II category having poor solubility and high permeability. Since only dissolved drug can pass the gastrointestinal membrane, the proper solubility of the drug is ultimately desired. Its oral bioavailability is 26%. Hence, an attempt was made to enhance its solubility by formulating solid dispersions using different techniques viz., Melting, Kneading, Co-precipitation, Solvent evaporation and Physical mixing etc., Drug and carrier (Urea) in different ratios like 1: 1, 1: 2, 1: 3 and 1:4 were used for formulating solid dispersions. The compatibility of the drug with the carrier was checked by FTIR studies, these results revealed that there was no interaction between them. The angle of repose, bulk density, tapped density; Carr’s index and Hausner ratio were calculated for the micrometric characterization of all the solid dispersions. The drug content was found to be high and uniform in all formulations. The prepared Solid dispersion SEM4 (1:4) showed minimal wetting time of 13 seconds compared with the other formulations. In vitro dissolution, release studies in Phosphate buffer pH of 6.8 revealed that the prepared solid dispersions showed faster drug release compared with the pure drug.  The in vitro dissolution profile showed ascendency on increasing the carrier concentration

scholarly journals EVALUATING THE BEST POLYETHYLENE GLYCOL AS SOLID DISPERSION CARRIER BY TAKING ETORICOXIB AS A MODEL DRUG

2019 ◽  
pp. 250-255
Author(s):  
HEMANTH A ◽  
HINDUSTAN ABDUL AHAD ◽  
DEVANNA N
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Physicochemical Characteristics ◽  
Peg 6000 ◽  
Good Solubility ◽  
Peg 4000 ◽  
Tablet Compression ◽  
Model Drug ◽  
Peg 8000

Objective: The main objective of the current research is focused in discovering the best polyethylene glycol (PEG) as solid dispersion carrier using etoricoxib (ECB) as a model drug. Methods: Varieties of PEG, namely PEG - 3350, PEG - 4000, PEG - 6000, PEG - 8000, and PEG - 20000, were evaluated as a carrier for making ECB solid dispersions. ECB:PEG was taken in the ratios of 1:1, 1:2, 1:4, and 1:6. The solid dispersions were prepared by microwave fusion method and compressed using 8 station tablet compression machine. The fabricated solid dispersion tablets were tested for physicochemical characteristics and drug release rates. The release of ECB from the prepared solid dispersions was further analyzed kinetically using the first order and Hixson-Crowell’s plots. Results: All the solid dispersion batches were shown satisfactory physicochemical characteristics. ECB solid dispersion batches with PEG - 6000 showed good solubility in distilled water (up to 2.29±0.01 μg/ml) and in 0.1 N HCl (up to 2.18±0.01 μg/ml) when compared with ECB alone (0.21±0.01 μg/ml and 0.32±0.01 μg/ml). The prepared solid dispersions with PEG 6000 are shown good ECB release. Conclusion: Among PEG carriers, PEG - 6000 was found to be the best carrier for increasing the solubility and release rate of ECB form the solid dispersions compared to PEG - 3350, PEG - 4000, PEG - 8000, and PEG - 20000.

Formulation and Characterization of Solid Dispersion Containing Capsaicin for the Treatment of Diabetes

2020 ◽  
Vol 15 (3) ◽  
pp. 219-225
Author(s):  
Tapan Kumar Giri ◽  
Payel Roy ◽  
Subhasis Maity
Keyword(s):  
Thermal Analysis ◽  
Differential Thermal Analysis ◽  
Animal Study ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Peg 6000 ◽  
X Ray

Background: Chili peppers are widely used in many cuisines as a spice, and capsaicin is the main component. It has been reported that capsaicin acts as an antihyperglycemic agent. However, it shows poor aqueous solubility and bioavailability. Objective: The is to enhance the aqueous solubility and antihyperglycemic activity of capsaicin through solid dispersion formulation. Methods: Solid dispersions were prepared by the solvent evaporation method using polyethylene glycol 6000 (PEG 6000) as a hydrophilic carrier. Polymer-drug miscibility and drug crystallinity were characterized through the differential thermal analysis and X-ray powder patterns analysis. Solid dispersions were evaluated for solubility, in vitro drug dissolution and in vivo animal study in rats. Results: Results of x-ray powder patterns analysis showed a considerable reduction of drug crystallinity in solid dispersion. Differential thermal analysis result revealed a complete disappearance of capsaicin melting onset temperature in solid dispersion. From the phase solubility data, it was observed that the aqueous solubility of capsaicin was increased with increasing concentration of PEG 6000. Solid dispersion formulation showed considerable enhancement of in vitro release of drugs in comparison to pure capsaicin. In vivo animal study in rats shows that the solid dispersion containing capsaicin significantly reduced the blood glucose level in comparison to the free capsaicin. Conclusion: Higher anti-hyperglycemic effect of capsaicin loaded solid dispersion in comparison to the pure drug may be due to the enhancement of aqueous solubility of capsaicin. Thus, the solid dispersion of capsaicin showed a simple approach for capsaicin delivery with improved antidiabetic activity.

scholarly journals Enhancement of Solubility and Dissolution Rate of Curcumin Using Porous Starch by Solid Dispersion Technique

2021 ◽  
Vol 23 (2) ◽  
Author(s):  
Indrayani D.Raut ◽  
◽  
Nikita D. Gidde D. Gidde ◽  
Priyanka V. Desai ◽  
Priyanka V. Bagade V. Bagade ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
In Vitro Dissolution ◽  
Hydrophilic Matrix ◽  
Novel Method ◽  
Improved Performance ◽  
Dispersion Technique ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

The poor dissolution characteristics of biopharmaceutical class II drugs are a major concern for scientists in thepharmaceutical industry. Solid dispersion is introduced as a novel method for enhancement of solubility. Class IIdrugs are low solubility and high permeability according to the biopharmaceutical classification system and arepromising candidates for improving solubility and bioavailability through solid dispersion. The purpose of the present attempt is to prepare a solid dispersion of curcumin and porous starch in order to increase the solubility and dissolution of drugs that are poorlysoluble. Solid dispersions (SDs) of BCS-II drugs were prepared by ball milling in ratio of drug: polymer i.e. curcumin: porous starch (1:0.5, 1:1, 1:2 and 1:3). Further, SDs were investigated by solubility, FTIR, XRD, DSC, micromeritics, and in-vitro dissolution. . Conclusively, porous starch offers a hydrophilic matrix to deliver poorwater soluble drugs and Solid dispersion system have demonstrated an improved performance. Solid dispersionsystem have demonstrated an improved performance

scholarly journals SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF EZETIMIBE BY SOLID DISPERSION AND PELLETIZATION TECHNIQUES USING SOLUPLUS AS CARRIER

2019 ◽  
pp. 57-64
Author(s):  
Viswanadh Kunam ◽  
Vidyadhara Suryadevara ◽  
Devala Rao Garikapati ◽  
Venkata Basaveswara Rao Mandava ◽  
RLC Sasidhar
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Physicochemical Parameters ◽  
Solid Dispersions ◽  
Surface Characteristics ◽  
Sem Analysis ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Pure Drug

Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the nonpareil sugar beads as pellets. Methods: Ezetimibe solid dispersions were prepared by kneading method using soluplus. Crospovidone was added as a disintegrant in pellets. Ezetimibe pellets were prepared by dissolving soluplus and crospovidone in ethanol in different ratios and coated on nonpareil sugar beads as a drug layer by pan coating technique. Various physicochemical parameters like particle size, friability, angle of repose and drug content were evaluated for the prepared solid dispersions and pellet formulations. In vitro dissolution studies were carried out in 1% SLS using USP apparatus II. FTIR and SEM analysis were performed for solid dispersions, pellet formulations and its polymers to determine the interactions and surface characteristics. Results: The physicochemical parameters were within the specified I. P limits. It was observed that the solid dispersion formulation ED5 showed better dissolution rate to the extent of 1.07 folds and 1.95 folds when compared to a marketed formulation and the pure drug, respectively. Similarly, pellet formulation EP5 containing 1:5 ratio of ezetimibe to soluplus showed an improved dissolution rate to the extent of 1.173 folds and 2.136 folds when compared to the marketed formulation and the pure drug, respectively. FTIR analysis revealed that there was no major interaction between the drug and the excipients.  Conclusion: From the present study, it was observed that the solubility of ezetimibe was enhanced by soluplus in pellet formulations when compared to solid dispersions.

scholarly journals Preparation, Physicochemical Characterization and In-Vitro Dissolution Studies of Ketoprofen Solid Dispersion with PEG 6000 and HPMC 6 cps

2020 ◽  
Vol 23 (1) ◽  
pp. 44-53
Author(s):  
Sharmin Akhter ◽  
AKM Saif Uddin ◽  
Aninda Kumar Nath ◽  
Md Salahuddin ◽  
Mohammad Fahim Kadir ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Oral Absorption ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Fixed Amount ◽  
Peg 6000

Ketoprofen [2-(3-benzoylphenyl)-propionic acid], a non-steroidal anti-inflammatory drug exhibits poor dissolution pattern. Solid dispersion (SD) techniques were used because it is particularly promising to improve the oral absorption and bioavailability of BCS Class II drugs. This investigation entails solid dispersion of ketoprofen which was formulated and characterized for better release profile and immediate action of the drug. Melting method was applied to prepare solid dispersion by using two immediate release (IR) polymer PEG 6000 and HPMC 6 cps at different weight ratios. In the formulation, a fixed amount of lactose was used as adsorbent. The solid dispersions were investigated for drug entrapment efficiency and dissolution behavior. In vitro dissolution study was performed in phosphate buffer (pH 7.4) medium for one hour. Percent cumulative drug release from solid dispersion was found to be minimum 92.19% and maximum 98.95% within one hour, which showed a better dissolution compared to the active drugs. Evaluation of the properties of the solid dispersion was also performed by using Scanning Electron Microscopy (SEM) study and Differential Thermal Analysis (DTA). SEM results indicated that ketoprofen crystallinity in SDs was significantly reduced, and that the majority of ketoprofen was in amorphous form. No interaction was found between drug and polymers from DTA and Fourier-transform infrared (FTIR) spectroscopy analysis. So, solid dispersion technique may be an effective technique to enhance dissolution rate of ketoprofen. Bangladesh Pharmaceutical Journal 23(1): 44-53, 2020

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