scholarly journals Solid Dispersion (Kneading) Technique: A Platform for Enhancement Dissolution Rate of Valsartan Poorly Water Soluble Drug

2020 ◽  
Vol 11 (01) ◽  
pp. 20-24
Author(s):  
Vinod T. Wagh ◽  
Ritu M. Gilhotra ◽  
Rajendra D. Wagh
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
X Ray Diffraction ◽  
Water Soluble Drug ◽  
Kneading Method ◽  
Differential Scanning Colorimetry ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The objective of this study was to the enhancement of dissolution rate of Valsartan. Using a solid dispersion (kneading) method with Kollidon and Povidone K30 as a carrier. Eight different drugs: Carrier ratios were prepared. Using factorial design taking 3 factors i.e., the concentration of Valsartan (x1), Kollidon (x2), and Povidone K30(x3). The enhancement of dissolution depends on the amount of carrier and an increase in the concentration of carrier. Enhancement of dissolution rate depends on reduce particle size of drug place on the surface of carrier and increased wettability of drug particle by carrier. Solid Dispersions prepared with Kollidon as a carrier in ratio 1:4 shows the enhancing dissolution in 30 mins to drug and Physical Mixture. Formulation evaluated by fourier-transform infrared spectroscopy, differential scanning colorimetry, X-ray diffraction, Scanning Electron Microscopy.

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

scholarly journals Preparation and Characterization of PEG4000 Palmitate/PEG8000 Palmitate-Solid Dispersion Containing the Poorly Water-Soluble Drug Andrographolide

2020 ◽  
Vol 2020 ◽  
pp. 1-7
Author(s):  
Qingyun Zeng ◽  
Liquan Ou ◽  
Guowei Zhao ◽  
Ping Cai ◽  
Zhenggen Liao ◽  
...  
Keyword(s):  
Thermal Stability ◽  
Molecular Weight ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Water Soluble ◽  
Carrier Material ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersion (SD) is the effective approach to improve the dissolution rate and bioavailability of class II drugs with low water solubility and high tissue permeability in the Biopharmaceutics Classification System. This study investigated the effects of polyethylene glycol (PEG) molecular weight in carrier material PEG palmitate on the properties of andrographolide (AG)-SD. We prepared SDs containing the poorly water-soluble drug AG by the freeze-drying method. The SDs were manufactured from two different polymers, PEG4000 palmitate and PEG8000 palmitate. The physicochemical properties of the AG-SDs were characterized by Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, dissolution testing, and so on. We found that AG-PEG4000 palmitate-SD and AG-PEG8000 palmitate-SD were similar in the surface morphology, specific surface area, and pore volume. Compared with the AG-PEG4000 palmitate-SD, the intermolecular interaction between PEG8000 palmitate and AG was stronger, and the thermal stability of AG-PEG8000 palmitate-SD was better. In the meanwhile, the AG relative crystallinity was lower and the AG dissolution rate was faster in AG-PEG8000 palmitate-SD. The results demonstrate that the increasing PEG molecular weight in the PEG palmitate can improve the compatibility between the poorly water-soluble drug and carrier material, which is beneficial to improve the SD thermal stability and increases the dissolution rate of poorly water-soluble drug in the SD.

scholarly journals Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

Drug Delivery ◽  
2007 ◽  
Vol 14 (1) ◽  
pp. 33-45 ◽  
Author(s):  
Rina J. Chokshi ◽  
Hossein Zia ◽  
Harpreet K. Sandhu ◽  
Navnit H. Shah ◽  
Waseem A. Malick
Keyword(s):  
Solid Solution ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Pros And Cons ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

scholarly journals RESEARCH AND DEVELOPMENT OF DIAZEPAM SOLID DISPERSION POWDER USING NATURAL POLYMERS

2018 ◽  
Vol 10 (5) ◽  
pp. 220
Author(s):  
Uditi Handa ◽  
Kamal Saroha
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Natural Polymers ◽  
Drug Content ◽  
Ftir Studies ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Pure Drug ◽  
Poorly Water Soluble Drug

Objective: The objective of this study was to enhance the solubility and dissolution rate of a poorly water-soluble drug by solid dispersion (SD) technique, in order to conduct an investigation of the effect of these natural hydrophilic polymers on release mechanism from SD.Methods: The SD of diazepam (DZM) were prepared by using modified sodium alginate (SA) and modified guar gum (GG) in different drug: polymer ratios (1:1 and 1:2) by using physical mixture method (PM) and fusion method (FM). Further, the formulations were characterized for calibration curve, Fourier transforms infrared spectroscopy (FTIR) studies, % age practical yield, drug content estimation, solubility studies, dissolution studies.Results: The pure drug and SD were characterized by pre and post-formulations studies. The %age practical yield ranged from 92.9±0.25 to 49±0.57%, and the drug content estimation ranged from 99.34±0.40 to 65.25±0.25 %. The FTIR studies shown that the compatibility between pure drug and natural polymers was stable. All the SD showed improved solubility as compared to the pure drug (PD). SD prepared with modified SA (1:2) by PM and FM shown the huge enhancement of solubility and dissolution rate of the DZM. This can be specific to the improvement in wettability and dispersibility, as well as enhances the drug amorphous fraction.Conclusion: On the basis of the research study, the SD technique shows the enhancement in the solubility of poorly water-soluble drug using natural polymers. SD containing natural polymers prepared with PM and FM shown the remarkable improvement in the release outline compared with PD, DZM.

DISSOLUTION ENHANECEMENT OF AN ANTIHYPERTENSIVE AGENT BY SOLID DISPERSION

2013 ◽  
pp. 21-24
Author(s):  
Keyword(s):  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
X Ray Diffraction ◽  
Peg 6000 ◽  
X Ray ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: To evaluate dissolution enhancement of IS, a poorly water-soluble drug, by PEG 6000-based solid dispersion and investigate mechanism of dissolution enhancement from the solid dispersion. Methods: Solid dispersion was prepared by melting method. Dissolution test was performed at pH 6.8. Powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FTIR) were used to investigate the drug crystallinity as well as the interaction between drug and polymer. Results: Dissolution rate of IS from the solid dispersion was significantly increased at pH 6.8 as compared to the pure drug. Drug crystallinity was reduced. FTIR showed the interaction between polymer and IS in the solid dispersion. Conclusions: PEG 6000 was successfully used to increase the dissolution of IS. Moreover, mechanism of the dissolution enhancement was fully explained in the study. Key words: poorly water-soluble drug, dissolution, solid dispersion.

scholarly journals Effect of Poloxamer on release of poorly water soluble drug Loratadine from solid dispersion: Kneading method

2015 ◽  
Vol 61 (01) ◽  
pp. 45-50 ◽  
Author(s):  
M. Mofizur Rahman ◽  
Mohammad Moniruzzaman ◽  
Sanjida Haque ◽  
M. A.K. Azad ◽  
Farjana Islam Aovi ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Water Soluble ◽  
Hydrophilic Polymers ◽  
Water Soluble Drug ◽  
Kneading Method ◽  
Dispersion Systems ◽  
Release Studies ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The main objective of the current study was to enhance the solubility and dissolution of poorly water soluble drug Loratadine (LOR) through formulation of solid dispersion systems (SDs) using hydrophilic polymers. SDs were prepared by kneading method using different drug-to-polymer ratios (1:3 and 1:5) with poloxomer 188 (samples DS1, DS2) and poloxomer 407 (samples DS3, DS4) as hydrophilic polymers. In vitro drug release studies were performed on prepared SDs (DS1-DS4) and compared to pure drug (LOR only, sample DS0). Prepared SDs showed significant improvement in the release profile compared to LOR.

Physical Stabilizing Effect of Biopolymers on Solid Dispersions Containing Indomethacin and Polyethylene Glycol

2012 ◽  
Vol 506 ◽  
pp. 307-310 ◽  
Author(s):  
Benchawan Chamsai ◽  
Pornsak Sriamornsak
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Water Soluble Drug ◽  
Stabilizing Effect ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersions of poorly water-soluble drug, indomethacin (IMC), and carriers at a ratio of 1:9 were prepared by melting method. The carriers used in this study were polyethylene glycol 4000 (PEG4000), hydroxypropyl methylcellulose (HPMC) and pectin. The solid dispersions obtained were characterized by powder x-ray diffractometry (PXRD) and dissolution studies. PXRD patterns showed that all solid dispersions led to amorphous products while their physical mixture still showed the crystalline state of drug. Crystalline drug was clearly detectable in solid dispersion products containing only IMC and PEG4000 after storage for 2 months. The formulations with biopolymer (i.e., HPMC, pectin or their combination) showed no drug crystal after storage. More than 80% of IMC dissolved within 5 minutes for all formulations after preparation while less than 40% of IMC dissolved, within 5 minutes, from the formulations containing IMC, PEG4000 and HPMC after storage for 2 months. The slower drug dissolution may be due to the gel-forming properties of HPMC as well as the agglomeration of the products after storage. The results suggested that either HPMC or pectin in solid dispersions can help to prevent the crystallization of amorphous IMC in solid dispersion, probably by a polymer anti-plasticizing effect. Pectin showed superior stabilizing effect with no retardation effect on drug dissolution.

scholarly journals COMPARISON AND CHARACTERIZATION OF INCLUSION COMPLEXES AND SOLID DISPERSIONS IN ENHANCEMENT OF DISSOLUTION RATE OF POORLY WATER SOLUBLE DRUG

2018 ◽  
Vol 10 (5) ◽  
pp. 173
Author(s):  
Radha Rani Earle ◽  
Rambabu Jammu ◽  
Lakshmi Usha ◽  
Ratna Kanth Lingam
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Peg 6000 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Objective: The purpose of the present study was to enhance solubility and dissolution characteristics of indomethacin by preparing inclusion complexes with hydroxypropyl β-cyclodextrin (HP β-CD) and solid dispersions with PEG 6000 to enhance its in vitro drug release and to further formulate it as a tabletMethods: Solid dispersions (SDs) and inclusion complexes (ICs) of Indomethacin with PEG 6000 and HP β-CD respectively were prepared to enhance the dissolution rate of this poorly water-soluble drug belonging to BCS class II. A comparison was made between two systems: solid dispersions with PEG 6000 obtained using melting and solvent evaporation technique, inclusion complexes with HP β-CD prepared by kneading technique. SDs were prepared in 1:1, 1:2, 1:3 and ICs in 1:0.25, 1:0.5, 1:1 w/w ratios of drug: polymer. Both the systems were characterized by FTIR, SEM, DSC, X-RD.Results: The dissolution of indomethacin increased with the increase in the concentration of the polymers. F4 and F9 formulations showed complete drug release in less than 30 min. Dissolution studies indicated that cyclodextrin complexes showed a better enhancement of dissolution rate when compared to solid dispersions. CDs were found to be more effective than PEGs at lower concentrations. These formulations were further compressed as tablets.Conclusion: The FTIR and DSC studies showed that no interactions existed between the drug and the polymer.

scholarly journals Solid Dispersion: Solubility Enhancement Technique of Poorly Water Soluble Drug

2020 ◽  
Vol 10 (1) ◽  
pp. 173-177 ◽  
Author(s):  
, Ikram ◽  
Kapil Kumar
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Inert Carrier ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersion is a technique which is widely and successfully applied to improve the solubility, dissolution rates and consequently the bioavailability of poorly soluble drugs. Dispersion of one or more active ingredients (hydrophobic) is done with an inert carrier (hydrophilic) at solid-state prepared by fusion method, solvent, and melting solvent method. In this review article, we have focused on the methods of preparation, advantages, disadvantages and characterization of the solid dispersions. Keywords: Solid dispersion; dissolution; solubility.

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