scholarly journals FORMULATION AND OPTIMIZATION OF CURCUMIN SOLID DISPERSION PELLETS FOR IMPROVED SOLUBILITY

2019 ◽  
pp. 36-46
Author(s):  
SANJEEVANI DESHKAR ◽  
ARUN SATPUTE
Keyword(s):  
Solid Dispersion ◽  
Weight Ratio ◽  
Poloxamer 407 ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Dsc Studies ◽  
Poorly Soluble ◽  
Extrusion Spheronization

Objective: The present study was aimed at designing of solid dispersion based pellets of curcumin (Cu) for improving its solubility. Methods: Solid dispersion (SD) of Cu was prepared by the melt method using Poloxamer 407 (Pol 407) at a different weight ratio of Cu-Pol 407 (1:2, 1:3, 1:5, 1:7, 1:10). The solid dispersion was characterised by FTIR, SEM, DSC, XRD and evaluated for saturation solubility in water, drug content and in vitro dissolution. The pellets of Cu solid dispersion were prepared by extrusion spheronization technique and optimization was performed by 32full factorial design. The pellets were evaluated for size distribution, flow properties, hardness, disintegration and in vitro drug dissolution. Results: From the phase solubility analysis, Pol 407 was selected as a Solid dispersion carrier. The formation of Cu-SD by melt method using Pol 407, was confirmed from FTIR and DSC studies. XRD studies indicated a change of Cu from crystalline to amorphous form. There was a significant increase of Cu when formulated as SD compared to plain Cu. The optimization of extrusion spheronization process revealed the significant effect of Cu-Pol 407 ratio (p<0.0001) on in vitro dissolution of pellets. Higher Cu dissolution was obtained with Cu-SD pellets compared to plain Cu pellets. Conclusion: The present study demonstrated the potential of Cu-SD pellets in improving the solubility of poorly soluble Cu.

BEHAVIOURAL STUDY OF CYCLODEXTRIN INCLUSION COMPLEX ON ENHANCEMENT OF SOLUBILITY OF ACECLOFENAC

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (11) ◽  
pp. 19-23
Author(s):  
J Shaikh ◽  
◽  
S. V. Deshmane ◽  
R. N Purohit ◽  
K. R. Biyani
Keyword(s):  
Inclusion Complex ◽  
Solid Dispersion ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Solubility Study ◽  
Cyclodextrin Inclusion ◽  
Poorly Water Soluble ◽  
Cyclodextrin Inclusion Complex

The main objective of the present study was to enhance the solubility and dissolution rate of poorly water soluble aceclofenac using its solid dispersion with β-cyclodextrin. FTIR and DSC study was carried out to find out any incompatibility. The phase solubility of drug was carried out in 1, 2, 5, and 10% of β-cyclodextrin in distilled water. Kneading method and solvent evaporation method was use to prepared solid dispersion of aceclofenac and β-cyclodextrin. Different evaluation tests like solubility study in different solvents, PXRD and in vitro dissolution study of aceclofenac- β-cyclodextrin inclusion complex were carried out. The overall finding indicated that β-cyclodextrin is a desirable water soluble carrier, that helps in increasing solubility of drug. Due to its structural feature, β-cyclodextrin forms a good inclusion complex that decreases contact angle of drug with water molecules by increasing wetting properties. Hence, it can be concluded that, β-cyclodextrin is better water soluble carrier molecule in terms of its compatibility and increasing solubility behavior of poorly water soluble drug aceclofenac.

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.

IMPROVEMENT OF DISSOLUTION RATE OF FEBUXOSTAT USING HYBRID TECHNIQUE OF SPHERICAL CRYSTALLIZATION AND SOLID DISPERSION

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (09) ◽  
pp. 32-39
Author(s):  
D. B Tandel ◽  
◽  
P. A Shah ◽  
K. G. Patel ◽  
M. C Gohel ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Compatibility Study ◽  
Hybrid Technique ◽  
Spherical Crystallization ◽  
Spherical Agglomerates ◽  
Pvp K30 ◽  
Excipient Compatibility

The present study was carried out with an aim to improve dissolution rate of febuxostat (FBX, BCSclass II) drug. Spherical agglomerates were prepared by hybrid technique of spherical crystallization and solid dispersion using different ratios of FBX and polymer (PVP K30, HPMC E3LV and chitosan). Drug excipient compatibility study was evaluated by Fourier transform infrared spectroscopy and X-ray diffractometry. Scanning electron microscopy was used for measurement of size of agglomerate. In vitro dissolution study of prepared spherical agglomerates was compared with untreated FBX and marketed formulation in phosphate buffer pH 6.8. The ratio of drug to polymer also affected the drug dissolution results. Drug excipient compatibility study showed no interaction between FBX and PVP K30 (1:5) polymer. The use of PVP K30 (1:5) resulted in partial amorphization and improved drug dissolution. Direct compression method can be adopted in manufacturing to simplify the validation efforts. The performance of the formulated product was superior to the marketed product in the in vitro dissolution test.

scholarly journals Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 627
Author(s):  
Ahmad A. Shahba ◽  
Ahmad Y. Tashish ◽  
Fars K. Alanazi ◽  
Mohsin Kazi
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Negative Impact ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Dissolution Model ◽  
Dissolution Efficiency ◽  
Drug Free

The study aims to design a novel combination of drug-free solid self-nanoemulsifying drug delivery systems (S-SNEDDS) + solid dispersion (SD) to enhance cinnarizine (CN) dissolution at high pH environment caused by hypochlorhydria/achlorhydria. Drug-loaded and drug-free liquid SNEDDS were solidified using Neusilin® US2 at 1:1 and 1:2 ratios. Various CN-SDs were prepared using freeze drying and microwave technologies. The developed SDs were characterized by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD). In-vitro dissolution studies were conducted to evaluate CN formulations at pH 6.8. Drug-free S-SNEDDSs showed acceptable self-emulsification and powder flow properties. DSC and XRD showed that CN was successfully amorphized into SDs. The combination of drug-free S-SNEDDS + pure CN showed negligible drug dissolution due to poor CN migration into the formed nanoemulsion droplets. CN-SDs and drug-loaded S-SNEDDS showed only 4% and 23% dissolution efficiency (DE) while (drug-free S-SNEDDS + FD-SD) combination showed 880% and 160% enhancement of total drug release compared to uncombined SD and drug-loaded S-SNEDDS, respectively. (Drug-free S-SNEDDS + SD) combination offer a potential approach to overcome the negative impact of hypochlorhydria/achlorhydria on drug absorption by enhancing dissolution at elevated pH environments. In addition, the systems minimize the adverse effect of adsorbent on drug release.

scholarly journals ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF IBUPROFEN BY SOLID DISPERSION TECHNIQUE AND FORMULATION OF SUSTAINED RELEASE TABLETS CONTAINING THE OPTIMISED BATCH OF SOLID DISPERSION

2017 ◽  
pp. 37-44
Author(s):  
ABHIK KAR ◽  
ABDUL BAQUEE AHMED
Keyword(s):  
Sustained Release ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Poloxamer 407 ◽  
In Vitro Dissolution ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Sustained Release Tablets

Objective: The present study was aimed to enhance the solubility of poorly water soluble drug Ibuprofen using solid dispersion technique and to develop sustained release tablets containing solid dispersion granules of the optimized batch. Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, and anti-inflammatory propertiesMethods: Solid dispersions of Ibuprofen were prepared by using PEG 20000 and Poloxamer 407 in different weight ratios by fusion and solvent evaporation method. Drug-carrier physical mixtures were also prepared. Solid dispersions were characterized by saturation solubility, drug content, in vitro dissolution, FTIR and DSC analysis. Solid dispersion formulation, SDF9 (PEG 20000 and Poloxamer 407, 1:3:3) prepared by solvent evaporation method was considered as the optimized batch. Sustained release tablets containing the solid dispersion granules of the optimized batch were prepared by direct compression method using HPMC K100M at three concentrations (10%, 14%, 18% w/w). The prepared formulations were evaluated for hardness, thickness, weight variation, friability, in vitro dissolution studies and release kinetics modelling.Results: Solid dispersion formulation, SDF9showed 95.09% drug release in 60 min and considered as the optimized batch. Tablet formulation, FT3 (HPMC K100M 18% w/w) showed 96% drug release for 12 h.Conclusion: Solid dispersions of ibuprofen using a combination of PEG 20000 and poloxamer 407 by solvent evaporation method may result in higher aqueous solubility of the drug. Also sustained release tablets containing solid dispersion granules of ibuprofen, using HPMC K100M may be a promising approach to extend the release rate of the drug from the solid dispersion for 12 h.

Solubility enhancement of glipizide and development of its fast-dissolving oral film

2021 ◽  
Vol 16 ◽  
Author(s):  
Harshal Ashok Pawar ◽  
Mohd Saif Mohd Akram Momin
Keyword(s):  
Solid Dispersion ◽  
In Vitro Dissolution ◽  
Average Weight ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Solvent Evaporation Process ◽  
Tablet Dosage

Background: Difficulty in swallowing tablet dosage form is common among all ages people, especially old and pediatrics. Fast dissolving oral films (FDOFs) may represent an innovative dosage type that settles the issue of gulping and supply fast onset of action. Objective: The objective of the present investigation was to increase the solubility of poorly soluble Glipizide (BCS Class II) by solid dispersion technique and develop its FDOFs. Methods: A solvent evaporation process was used to make a solid dispersion of the Glipizide. The saturation solubility of glipizide and its solid dispersion was determined in a different solvent. For the film preparation, solvent casting method was chosen. The excipients were selected based on pre-formulation data. The composition of the film was optimized based on a trial-and-error basis using different concentrations of plasticizer. The average weight, thickness, disintegration time, tensile strength, surface pH, folding endurance, drug content, and in-vitro dissolution analysis of the films were all taken into consideration. Results: There was no incompatibility between drug / solid dispersion and the excipients. The solid dispersion of the glipizide showed improved solubility by almost 10 folds. Many of the formulated films disintegrated in less than 30 seconds. At the end of 5 minutes, the optimized film had released more than 90% of the compound. The prepared films were found to be stable at room temperature. Conclusion: The solubility of Glipizide was improved successfully by solubilization technique using soluplus. The FDOFs of the glipizide were successfully formulated using pullulan as polymer.

scholarly journals Bioavailability Enhancement of Ritonavir by Solid Dispersion Technique

2021 ◽  
Vol 11 (5) ◽  
pp. 52-56
Author(s):  
Teja Velupula ◽  
Gayathri Devi Amboru ◽  
Sneha Chowdary Gundapaneni ◽  
Bhavya Kadiyala ◽  
Phani Sreenidhi Kanakagiri ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Wave Number ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Dissolution Studies ◽  
Drug Content ◽  
Ft Ir ◽  
Dispersion Technique

Ritonavir is an antiretroviral agent used in the treatment of HIV-infection. It is a BCS class IV drug having poor aqueous solubility leading to poor bioavailability. Bioavailability is the amount of drug that enters the systemic circulation. The bioavailability is affected by various factors like solubility, dissolution and stability. In order to improve bioavailability, many techniques like solid dispersions, nanoparticles, liposomes, encapsulation methods were present. The main aim of this study is to improve the bioavailability of ritonavir with the help of Polyvinyl Pyrrolidone (PVP) K-30 by using solid dispersion technique. Different formulations were made with varied concentrations of polymer. Characterization of solid dispersion was done by phase solubility, drug content, Fourier transformed infrared spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC) and in-vitro dissolution studies.  From phase solubility studies that apparent solubility constant was found to be 42.227M-1. The drug content of the binary system of ritonavir and PVP was found to be ranging from 99.17% to 103.06%. %. FT-IR studies revealed that there was no drastic change in the wave number indicating polymer compatibility with drug. In-vitro dissolution studies proved that there was an increase in drug release of ritonavir with incremental ratios of polymer and F5 formulation has shown almost 95% of drug release. Keywords: Bioavailability, Solid dispersion, Polyvinyl pyrrolidine, Solvent evaporation, Dissolution.

scholarly journals FABRICATION AND EVALUATION OF SOLID DISPERSION CONTAINING GLIBENCLAMIDE

2018 ◽  
Vol 11 (8) ◽  
pp. 158
Author(s):  
Nikita Sehgal ◽  
Vishal Gupta N ◽  
Gowda Dv ◽  
Sivadasu P
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Amorphous State ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Stability Studies ◽  
Scanning Calorimetry ◽  
Dsc Studies

 Objective: The aim of the present study was to increase the dissolution rate of glibenclamide (GLIB) by molecular dispersion of drug in the polymeric matrix of Pluronic F-127.Methods: GLIB-loaded solid dispersions were formulated by fusion method. The formulated solid dispersions were characterized for scanning electron microscopy (SEM), X-ray diffractometry (XRD), differential scanning calorimetry (DSC), and evaluated for percentage yield, drug content, solubility, and in vitro dissolution profile, and stability studies were conducted as per International Conference on Harmonisation guidelines Q1A in stability chamber, both at intermediate and accelerated conditions.Results: Both XRD and DSC studies suggested that crystalline GLIB was converted to amorphous form after loading into carrier. SEM studies revealed that the prepared solid dispersions were in the form of irregular particles with the absence of crystalline material. Due to this conversion of crystalline to amorphous state, formulated solid dispersions had shown improved dissolution rate profile of GLIB and stability studies suggested that formulated solid dispersions showed no significant changes in appearance and also in drug content.Conclusion: Thus, from the obtained results, it can be concluded that dissolution profile of GLIB can be improved by formulating as solid dispersion.

scholarly journals Solubility and Dissolution Enhancement of Etoricoxib by Solid Dispersion Technique Using Sugar Carriers

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Abhisekh Das ◽  
Amit Kumar Nayak ◽  
Biswaranjan Mohanty ◽  
Satyabrata Panda
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Dsc Studies ◽  
Evaporation Technique ◽  
Physical Mixtures

The aim of the present study was to improve solubility and dissolution of the poorly aqueous soluble drug, etoricoxib by solvent evaporation technique using various sugar carriers, such as lactose, sucrose, and mannitol. Etoricoxib solid dispersions and their respective physical mixtures using lactose, sucrose, and mannitol were prepared in different ratios by solvent evaporation technique. The percent yield, drug content, saturation solubility, and in vitro dissolution of etoricoxib solid dispersions and physical mixtures were analyzed. Etoricoxib solid dispersions were characterized by FTIR spectroscopy, XRD, and DSC analysis. The FTIR spectroscopic analysis revealed the possibility of intermolecular hydrogen bonding in various solid dispersions. The XRD and DSC studies indicated the transformation of crystalline etoricoxib (in pure drug) to amorphous etoricoxib (in solid dispersions) by the solid dispersion technology. Both the aqueous solubility and dissolution of etoricoxib were observed in all etoricoxib solid dispersions as compared with pure etoricoxib and their physical mixtures. The in vitro dissolution studies exhibited improved dissolution in case of solid dispersion using lactose than the solid dispersions using both sucrose and mannitol. The in vitro dissolution of etoricoxib from these solid dispersions followed Hixson-Crowell model.

Influence of β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin on Enhancement of Solubility and Dissolution of Isradipine

2017 ◽  
Vol 10 (3) ◽  
pp. 3752-3757
Author(s):  
Narendar D ◽  
Ettireddy S
Keyword(s):  
Inclusion Complex ◽  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physical Stability ◽  
Molecular Complexes ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Phase Solubility ◽  
Cyclodextrin Complexation

The content of this investigation was to study the influence of β-cyclodextrin and hydroxy propyl-β-cyclodextrin complexation on enhancement of solubility and dissolution rate of isradipine. Based on preliminary phase solubility studies, solid complexes prepared by freeze drying method in 1:1 molar ratio were selected and characterized by DSC for confirmation of complex formation. Prepared solid dispersions were evaluated for drug content, solubility and in vitro dissolution. The physical stability of optimized formulation was studied at refrigerated and room temperature for 2 months. Solid state characterization of optimized complex performed by DSC and XRD studies.  Dissolution rate of isradipine was increased compared with pure drug and more with HP-β-CD inclusion complex than β-CD. DSC and XRD analyzes that drug was in amorphous form, when the drug was incorporated as isradipine β-CD and HP-β-CD inclusion complex. Stability studies resulted in low or no variations in the percentage of complexation efficiency suggesting good stability of molecular complexes. The results conclusively demonstrated that the enhancement of solubility and dissolution rate of isradipine by drug-cyclodextrin complexation was achieved.   

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