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 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 Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

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.

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 Effect of Amphiphilic Graft Co-Polymer Carrier on Solubility and Dissolution Enhancement of Ambrisentan

2021 ◽  
pp. 329-338
Author(s):  
Rahul Radke ◽  
Neetesh K. Jain
Keyword(s):  
Ftir Spectroscopy ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Polymer Carrier ◽  
Dissolution Study

Aim: Ambrisentan is a endothelin type A selective receptor antagonist used in the management of pulmonary arterial hypertension. Ambrisentan is BCS Class II drug haves very poor solubility in water and shows incomplete absorption after oral administration. The present work was aimed to study the effect of amphiphilic graft co-polymer carrier on enhancement of solubility and dissolution rate of poorly water soluble drug ambrisentan. To improve the aqueous solubility of ambrisentan solid dispersion was formulated by using novel carrier amphiphilic graft co-polymer (Soluplus® ). Materials and Methods: Solid dispersion was prepared by kneading technique by utilizing various ratios of carrier. Obtained solid dispersions ware evaluated for solubility, percentage yield, drug content and in vitro dissolution study. Powder characterization was performed by infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD). Results: FTIR spectroscopy shows no interaction between drug and polymer. DSC study showed that endothermic peak of drug was completely disappeared in Solid dispersion suggesting complete miscibility of drug in Soluplus®. XRD study suggest the conversion of crystalline ambrisentan in to amorphous form. All solid dispersions prepared with Soluplus® as a carrier showed increase in solubility. Solubility of ambrisentan was found to be increased 7.17 fold in optimized SD formulation ASD5. In vitro dissolution study showed the faster drug release from SD formulation compare to its pure form. All solid dispersion formulation’s release more than 50% of drug in first 10 min. Conclusion: This study conclude that the preparation of amphiphilic graft co-polymer based solid dispersion prepared by kneading technique is found to be useful in enhancement the solubility and dissolution rate of ambrisentan.

scholarly journals Preparation and Evaluation of Silymarin-Loaded Solid Eutectic for Enhanced Anti-Inflammatory, Hepatoprotective Effect: In Vitro–In Vivo Prospect

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Abdulla Sherikar ◽  
Mohd Usman Mohd Siddique ◽  
Mahesh More ◽  
Sameer N. Goyal ◽  
Milan Milivojevic ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Biological Response ◽  
Eutectic Mixture ◽  
Fold Increase ◽  
In Vitro Dissolution ◽  
Anti Inflammatory ◽  
Pvp K30

Solubility of phytochemicals is a major concern for drug delivery, permeability, and their biological response. However, advancements in the novel formulation technologies have been helping to overcome these challenges. The applications of these newer technologies are easy for commercialization and high therapeutic outcomes compared to conventional formulations. Considering these facts, the present study is aimed to prepare a silymarin-loaded eutectic mixture with three different ratios of Polyvinylpyrrolidone K30 (PVP K30) and evaluating their anti-inflammatory, and hepatoprotective effects. The preliminary phytochemical and characterization of silymarin, physical mixture, and solid dispersions suggested and successfully confirmed the formation of solid dispersion of silymarin with PVP K30. It was found that the solubility of silymarin was increased by 5-fold compared to pure silymarin. Moreover, the in vitro dissolution displayed that 83% of silymarin released within 2 h with 2.8-fold increase in dissolution rate compared to pure silymarin. Also, the in vivo study suggested that the formulation significantly reduced the carbon tetrachloride- ( 0.8620 ± 0.05034 ∗ ∗ for 1 : 3 ratio), paracetamol- ( 0.7300 ± 0.01517 ∗ ∗ for 1 : 3 ratio), and ethanol- ( 0.8100 ± 0.04037 ∗ ∗ for 1 : 3 ratio) induced hepatotoxicity in rats. Silymarin solid dispersion was prepared using homogenization methods that have prominent anti-inflammatory effect ( 0.6520 ± 0.008602 ∗ ∗ with 8.33%) in carrageenan-induced rat paw model.

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

Formulation, Characterization and Solubility Enhancement of Manidipine Solid Dispersions

2019 ◽  
Vol 12 (2) ◽  
pp. 4453-4460
Author(s):  
Laxmi Raj A ◽  
Y. Shravan Kumar
Keyword(s):  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
X Ray Diffraction ◽  
Amorphous Form ◽  
X Ray ◽  
Solvent Evaporation Process

The study was aimed to formulate solid dispersions of Manidipine by using different novel carriers like Labrafac PG, Kolliwax RH 40, Soluplus, Kolliwax GMS II, Kolliphor EL and SLS in drug carrier ratio by using solvent evaporation method. The formulations were characterized for physical appearance, solubility and in vitro dissolution studies. The optimized formulation was characterized and Formulation SD13 was found to be optimized one based on the solubility, dissolution and other parameters using Kolliwax GMS II and SLS.  The drug release of the optimized formulation was found to be 99.41±5.38% within 90 min. Powder X-ray diffraction studies performed on solid dispersion showed that Manidipine existed in the amorphous form within the solid dispersion formulation fabricated using the solvent evaporation process. Additionally, scanning electron microscopy studies suggested the conversion of crystalline Manidipine to an amorphous form. Therefore, the solid dispersions using Kolliwax GMS II as hydrophilic carrier in the combination of SLS can be successfully used for improvement of solubility and dissolution of Manidipine.  

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