Physical stability of solid dispersions of the antiviral agent UC-781 with PEG 6000, Gelucire® 44/14 and PVP K30

2002 ◽  
Vol 244 (1-2) ◽  
pp. 87-98 ◽  
Author(s):  
F Damian ◽  
N Blaton ◽  
R Kinget ◽  
G Van den Mooter
Keyword(s):  
Solid Dispersions ◽  
Physical Stability ◽  
Antiviral Agent ◽  
Peg 6000 ◽  
Pvp K30

scholarly journals Impact Assessment of Different Polymers on Physicochemical Properties of Ibuprofen Loaded Solid Dispersions

2018 ◽  
Vol 17 (2) ◽  
pp. 183-190 ◽  
Author(s):  
Sonia Ferdousy ◽  
BK Sajeeb ◽  
Shahida Yeasmin ◽  
ABM Faroque
Keyword(s):  
Particle Size ◽  
Physicochemical Properties ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Particle Size Analysis ◽  
The Other ◽  
Size Analysis ◽  
Peg 6000 ◽  
Pregelatinized Starch ◽  
Pvp K30

In the present study, solid dispersions of ibuprofen were prepared to improve aqueous solubility of ibuprofen. A series of formulations were prepared where PEG 6000 with polymers named PVP K30, cross PVP, poloxamer 237, HPMC ASLF, pregelatinized starch, Na-CMC, Eudragit L100, and kollidon IR were used in different ratios. Among 41 formulations, solid dispersions of ibuprofen in PEG 6000 with each of PVP K30, poloxamer 237, and Na-CMC at ratio of 2:9:7 revealed improved solubility of 952.73 ± 1.31, 878.18 ± 0.97, and 1263.64 ± 1.58 μg/ml, respectively. The physicochemical properties of these preparations were ascertained by FTIR, SEM, DSC, and particle size analyses. FTIR spectrum showed absence of chemical interactions and physical compatibilities between ibuprofen and polymers were confirmed by DSC. Disappearance of individual surface properties in solid dispersions were revealed by SEM studies, which indicated the formation of effective preparations. On the other hand, particle size analysis showed reduction in particle size of ibuprofen from solid dispersions that demonstrated solubility enhancement of ibuprofen. The above studies suggested that solid dispersions of ibuprofen in PEG 6000 at ratios of 2:9:7 with each of PVP K30, poloxamer 237, and Na-CMC were found to be effective to improve aqueous solubility. Dhaka Univ. J. Pharm. Sci. 17(2): 183-190, 2018 (December)

Characterization and Physical Stability of Spray Dried Solid Dispersions of Probucol and PVP-K30

2008 ◽  
Vol 13 (5) ◽  
pp. 375-386 ◽  
Author(s):  
Pia Thybo ◽  
Betty L. Pedersen ◽  
Lars Hovgaard ◽  
Rene Holm ◽  
Anette Müllertz
Keyword(s):  
Solid Dispersions ◽  
Physical Stability ◽  
Pvp K30 ◽  
Spray Dried

Formulation and Optimization of Dolutegravir Fast Dissolving Tablets Using Various Solubility Enhancement Methods

2021 ◽  
Vol 11 (5) ◽  
Author(s):  
Srinivas Martha ◽  
singh Dr. Anoop
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Release Kinetics ◽  
Solid Dispersions ◽  
Antiviral Agent ◽  
Solvent Evaporation ◽  
Poloxamer 407 ◽  
Dissolution Profile ◽  
Peg 6000

Dolutegravir is a HIV-1 antiviral agent to control HIV/AIDS. In the present study Dolutegravir solid dispersion has been subjected to improve the solubility and dissolution rate performance by formulating as fast dissolving tablets, in which PEG 6000 and Poloxamer 407 were used as polymers. Solid dispersions of Dolutegravir were prepared with different carriers in different ratios of drug and carriers such as PEG 6000 and Poloxamer 407 (1:1, 1:2 and 1:3) by solvent evaporation and fusion method. The pre-compression and post-evaluation parameters were studied and the results were shown. All the results were within acceptable IP limits Finally, by comparing all the dissolution profile of solid dispersions , formulation F3 containing Dolutegravir + PEG 6000 (1:3) showed better results by solvent evaporation method at the end of 60 min with maximum drug release, hence it is selected as the best formulation. From the obtained optimized solid dispersion formulation, the fast dissolving tablets were prepared by using different concentrations of various super disintegrants. The in-vitro drug releases of the formulated Dolutegravir tablets were performed using a 6.8 pH Phosphate buffer as dissolution medium. The optimized DF3 formulation containing Sodium starch glycolate (SSG) (6% w/w) as super disintegrant, and it showed 98.04±1.9 % percentage drug release at 25 min. Characterization in solid-state were done by analytical methods such as UV-Visible, FT-IR studies. The optimized formulation followed first order release kinetics.

Physical stability of the amorphous state of loperamide and two fragment molecules in solid dispersions with the polymers PVP-K30 and PVP-VA64

2005 ◽  
Vol 25 (2-3) ◽  
pp. 313-320 ◽  
Author(s):  
Ilse Weuts ◽  
Dieter Kempen ◽  
Annelies Decorte ◽  
Geert Verreck ◽  
Jef Peeters ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Physical Stability ◽  
Amorphous State ◽  
Pvp K30

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.   

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

Sign in / Sign up

Export Citation Format

Share Document