scholarly journals Solid Dispersions as a Technological Strategy to Improve the Bio-Performance of Antiparasitic Drugs with Limited Solubility

Proceedings ◽  
2020 ◽  
Vol 78 (1) ◽  
pp. 13
Author(s):  
Santiago N. Campos ◽  
Alicia G. Cid ◽  
Analía I. Romero ◽  
Mercedes Villegas ◽  
Cintia A. Briones Nieva ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Parasitic Infections ◽  
Dissolution Tests ◽  
Antiparasitic Drugs ◽  
Dissolution Efficiency ◽  
Time Required ◽  
Low Solubility ◽  
Initial Dissolution Rate

Albendazole (ABZ) and benznidazole (BZL) are drugs with low solubility used in parasitic infections treatment. In this research, solid dispersion (SD) technology was used to enhance ABZ and BZL performance by increasing their dissolution rate and solubility. SDs were prepared by the fusion method, employing Poloxamer 407 (P407) as carrier to disperse 32 of BZL or 50% w/w of ABZ. Furthermore, physical mixtures (PM) of P407 and either ABZ or BZL were also prepared, and then SDs and PMs were characterized. Dissolution tests of SDs, PMs and commercial formulations (CF) of ABZ and BZL were carried out and dissolution profiles were analyzed with the lumped mathematical model, which allowed parameters of pharmaceutical relevance to be obtained. The results indicated that ABZ SD presented an initial dissolution rate (IDR) 21-fold and 11-fold faster than PM and CF, respectively, while the IDR of BZL SD was 2.5-fold and 4.5-fold faster than PM and CF, respectively. For BZL formulations, the time required to reach 80% dissolution of the drug (t80%) was 4 (SD), 46 (PM), and 239 min (CF), while the dissolution efficiency (DE) at 30 min was 85 (DS), 71 (MF) and 65% (FC). For ABZ formulations, t80% was 2 (SD), value not reached (PM) and 40 min (CF), while the DE at 30 min was 85 (SD), 36 (MF) and 65% (CF). The SDs developed notably increased the dissolution rate, in consonance with the values obtained from the pharmaceutical parameters, which could lead to faster absorption and, consequently, increase the bioavailability of these drugs.

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.

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 APPLICATION OF SOLID DISPERSION TECHNIQUE IN SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF NATEGLINIDE

2017 ◽  
Vol 10 (11) ◽  
pp. 231
Author(s):  
Prasanthi Boddu ◽  
Venkata Lakshmi Cherakapu ◽  
Uma Devi Ponukumati
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
Immediate Release ◽  
Primary Objective ◽  
The Body ◽  
Sustained Effect ◽  
Component Solubility ◽  
Dispersion Technique ◽  
Dissolution Efficiency

  Objective: Nateglinide (NTG) is a potent short-acting biopharmaceutical classification system class II antidiabetic medication. The primary objective of the present investigation was to prepare and evaluate solid dispersions of NTG to enhance the component solubility and immediate release (IR) profile. The secondary objective was to formulate sustained release (SR) matrix layer of NTG for prolonging its effect in the body and to decrease oscillations in plasma concentration level.Methods: NTG (270 mg) SR layer was formulated using release retardant polymers such as Carbopol, ethyl cellulose (EC), hydroxy EC, hydroxypropyl methylcellulose (HPMC), Kollidon, and locust bean gum at concentrations of 15% and 30%. IR layer of NTG (60 mg) was formulated using drug: Polymer inclusion complexes (1:1 and 1:2) of β-cyclodextrin (CD), HP β-CD, polyvinylpyrrolidone (PVP) K-15, and PVP K-30 by physical mixing and kneading methods (KMs).Results: Among the all the carriers tested HP β-CD at 1:2 ratio prepared by KM (I3) gave highest enhancement of dissolution rate and dissolution efficiency with acceptable f1 (10.5) and f2 (51.0) values in comparison to marketed IR tablets (Starlix-60®). The SR formulation S12 was able to show a minimum amount of drug release (15%) within 1 hr comparatively, with a complete and sustained effect on drug release.Conclusion: Thus, HPMC K-100M at a concentration of 30% in the SR layer in combination with HP β-CD (1:2) solid dispersions in the IR layer may be used in the design of oral controlled drug delivery system for NTG. 

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.

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 The Effect of Cooling on the Degree of Crystallinity, Solid-State Properties, and Dissolution Rate of Multi-Component Hot-Melt Extruded Solid Dispersions

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 212
Author(s):  
Dean Hurley ◽  
Mark Davis ◽  
Gavin M. Walker ◽  
John G. Lyons ◽  
Clement L. Higginbotham
Keyword(s):  
Solid State ◽  
Dissolution Rate ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Poloxamer 407 ◽  
Degree Of Crystallinity ◽  
Scanning Calorimetry ◽  
Hot Melt ◽  
The Degree Of Crystallinity ◽  
Over Time

The effect of cooling on the degree of crystallinity, solid-state and dissolution properties of multi-component hot-melt extruded solid dispersions [SD] is of great interest for the successful formulation of amorphous SDs and is an area that is unreported, especially in the context of improving the stability of these specific systems. The thermal solid-state properties, degree of crystallinity, drug–polymer interactions, solubility and physical stability over time were investigated. X-ray powder diffraction [XRPD] and hyper differential scanning calorimetry [DSC] confirmed that indomethacin [INM] was converted to the amorphous state; however, the addition of poloxamer 407 [P407] had a significant effect on the degree of crystallinity and the solubility of the SD formulations. Spectroscopy studies identified the mechanism of interaction and solubility studies, showing a higher dissolution rate compared to amorphous and pure INM in pH 1.2 with a kinetic solubility of 20.63 µg/mL and 34.7 µg/mL after 3 and 24 h. XRPD confirmed that INM remained amorphous after 5 months stability testing in solid solutions with Poly(vinylpyrrolidone-co-vinyl acetate) [PVP VA64] and Plasdone S-630 [PL-S630]. Although cooling had a significant effect on the degree of crystallinity and on solubility of INM, the cooling method used did not have any significant effect on the amorphous stability of INM over time.

scholarly journals Formulation and Characterization of Nimodipine Nanoparticles for the Enhancement of solubility and dissolution rate

2021 ◽  
Vol 30 (2) ◽  
pp. 143-152
Author(s):  
Areej Wahhab Alhagiesa ◽  
Mowafaq M. Ghareeb
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Channel Blocker ◽  
Polymeric Nanoparticles ◽  
Poloxamer 407 ◽  
High Permeability ◽  
Freeze Dried ◽  
Dihydropyridine Calcium Channel Blocker ◽  
Low Solubility

Nimodipine (NMD) is a dihydropyridine calcium channel blocker useful for the prevention and treatment of delayed ischemic effects. It belongs to class ? drugs, which is characterized by low solubility and high permeability. This research aimed to prepare Nimodipine nanoparticles (NMD NPs) for the enhancement of solubility and dissolution rate. The formulation of nanoparticles was done by the solvent anti-solvent technique using either magnetic stirrer or bath sonicator for maintaining the motion of the antisolvent phase. Five different stabilizers were used to prepare NMD NPs( TPGS, Soluplus®, HPMC E5, PVP K90, and poloxamer 407). The selected formula F2, in which  Soluplus  has been utilized as a stabilizer, has a particle size (77 nm) and polydispersity index (PDI) (0.016). The formulas with the smallest particle size were freeze dried with the addition of 1 % w/w mannitol as cryoprotectant. The saturation solubility of NMD in the prepared nanoparticles was increased twenty four-folds, and the complete dissolution was achieved at 90 minutes compared with pure NMD, which reaches only 6%. The formation of hydrogen bonding between NMD and the polymer or the cryoprotectant, as confirmed by the FTIR study. In conclusion, the preparation of NMD as polymeric nanoparticles is a useful technique for enhancing the solubility and dissolution rate.

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 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

Effect of ZrO2 on the glass durability

2002 ◽  
Vol 713 ◽  
Author(s):  
M. Lobanova ◽  
A. Ledieu ◽  
P. Barboux ◽  
F. Devreux ◽  
O. Spalla ◽  
...  
Keyword(s):  
Experimental Data ◽  
Dissolution Rate ◽  
Pure Water ◽  
Final Concentration ◽  
Leaching Tests ◽  
Borosilicate Glasses ◽  
Silica Network ◽  
Dissolution Tests ◽  
Short Times ◽  
Initial Dissolution Rate

ABSTRACTBorosilicate glasses were prepared with the molar composition 70 SiO2-15 Na2O-15B2O3-n ZrO2 with n ranging from 0 to 10. The glasses were studied by conventional static dissolution tests of powders at 90°C in pure water and in buffered solutions for long times (months) and short times (minutes). During the first minutes of alteration in a buffered solution, sodium is rapidly leached until its loss becomes controlled by the silicon hydrolysis. The experimental data show that the introduction of zirconium drastically reduces the initial dissolution rate (Vo) of the glass. Zirconium strengthens the silica network but also strongly modifies the porous layer morphology. In the case of glasses with small Zr contents (less than 2%), the silica dissolution rate decreases but the formation of a passivating alteration layer is also delayed. As a result, small amounts of zirconium paradoxically decrease the loss of silica but increase the final loss of sodium and boron in the static leaching tests. Larger zirconium contents (above 5%) increase the durability of the glass regarding the initial dissolution rate and the final concentration of all elements.

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