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

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 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 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 Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique

2019 ◽  
Vol 28 (2) ◽  
pp. 105-114
Author(s):  
Samer K. Ali ◽  
Eman B. H. Al-Khedairy
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Dissolution Enhancement ◽  
Drug Solubility ◽  
Scanning Calorimetry ◽  
Poorly Soluble

            Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs.           The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents.            All solid dispersion adsorbate (SDA) formulas  were prepared in ratios of 1:1:1  (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content,  , dissolution, crystal structure using  X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC)  studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction.                The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38  fold increase in solubility compared to  solubility of pure ATR and  solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility  and  dissolution .

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 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.

scholarly journals STUDIES ON SOLID DISPERSIONS OF LEFLUNOMIDE

2020 ◽  
pp. 187-190
Author(s):  
MAHAPARALE PR ◽  
THORAT VP
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Poloxamer 188 ◽  
Evaporation Method ◽  
Enhanced Solubility

Objective: Leflunomide is Non steroidal Anti-Inflammatory drug, which is poorly water soluble. In present study attempt has been made to prepare and characterize solid dispersions of leflunomide to increase solubility of drug.Method:  In Preparation of solid dispersion of leflunomide different polymer like PEG 4000, PEG 6000, Poloxamer 188 and Poloxamer 407 were used.  Effects of several variables such as type of carrier used, drug: carrier ratios, method of preparation were studied. The evaluation of solid dispersions was done by solubility study, dissolution study and X-ray diffractometry. Result: Improvement in dissolution of drug was observed in all solid dispersions as compared to pure drug alone. Solid dispersions prepared using Poloxamer 188 showed fastest in vitro drug release. Solid dispersions prepared using solvent evaporation method showed relatively faster drug release than melt evaporation method. XRD patterns indicated reduced crystallinity of drug particles, which suggests mechanism of enhanced solubility and dissolution of drug in solid dispersion systems.Conclusion:  A significant result obtained with the study indicated that solid dispersion by solvent evaporation can successfully be further explored and employed to improve solubility and dissolution characteristics of poorly soluble drugs.Keywords: Leflunomide, Solid dispersion, Carrier

scholarly journals Comparative Evaluation of Amorphous Polymers in Solubility and Bioavailability Enhancement of Famotidine Through Solid Dispersion

2021 ◽  
Author(s):  
Ankit Mishra ◽  
Priyanka Chaturvedi ◽  
Pranali Mishra ◽  
MS Sudheesh
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Milk Powder ◽  
Amorphous Polymers ◽  
Dissolution Enhancement ◽  
Study Results ◽  
Xrd Studies

The present study aimed to enhance the dissolution rate, therefore bioavailability, of famotidine (FMT) using its solid dispersions (SDs) with polyvinyl pyrrolidone (PVP)-K 30, milk powder, and inulin, both in-vitro and in-vivo. The study was also aimed to compare the effect of different amorphous polymers in enhancing the dissolution rate of FMT. The SDs were prepared with a 1:4 weight ratio by a solvent evaporation technique. Evaluation of the properties of the SDs was performed using dissolution, Fourier-transform infrared (FTIR) spectroscopy, and X-ray diffraction (XRD) studies. The SDs of FMT exhibited an enhanced dissolution rate. The FTIR spectroscopic studies showed the stability of FMT and the absence of well-defined drug excipient interaction. The XRD studies indicated the amorphous state of FMT in SDs. The drug release rate of all SDs formulation was found to be greater than the pure drug. Within one hour of dissolution studies, 99.43%, 92.5%, and 58.93% drug release were obtained, respectively, for PVP K-30, milk powder, and inulin. The first two were showing significantly higher release. SDs were also studied for bioavailability studies in-vivo in rats, which confirms that the SDs prepared by PVP K-30 and milk powder significantly enhancing the bioavailability of FMT. The maximum concentration of 15.05±2.45 μg/ml was achieved in 2 hours, and the area under the curve was found to be 33.78±7.3 μg. hour/ml. Therefore, the study results conclude that SDs of the FMT prepared by PVP K-30 successfully increases the dissolution and in-vivo bioavailability. Keywords – Solid dispersion, Second generation solid dispersions, Famotidine, In-vivo bioavailability, amorphous polymers, dissolution enhancement, solubility enhancement.

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.

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