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

Formulation Evaluation and Characterization of Fast Dissolving Tablets of Rofecoxib

2021 ◽  
pp. 60-64
Author(s):  
Preeti Mehra ◽  
Vishal Kapoor ◽  
Naveen Gupta ◽  
Dharmendra Singh Rajpoot ◽  
Neeraj Sharma
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Dissolution Profile ◽  
Major Drawback ◽  
Peg 4000 ◽  
Dissolution Efficiency ◽  
Pvp K30

Rofecoxib, a new non-steroidal anti-inflammatory agent mainly used for the treatment of osteoarthritis and rheumatoid arthritis. The major drawback of Rofecoxib is its very low water solubility, which results in poor bioavailability after oral administration. Hence, an attempt was made to formulate fast dissolving tablets of Rofecoxib. The solid dispersions of Rofecoxib were prepared with PEG-4000 and PVP K30 by solvent evaporation method. The characterization of prepared solid dispersions by FTIR, XRPD and DSC, which reveals lack of interaction with carriers and dictates amorphous state of solid dispersions. Solid dispersion of Rofecoxib with PVP K30 (1:6) showed maximum dissolution, therefore compressed into tablets by using microcrystalline cellulose, lactose and crosspovidone. The dissolution profile of developed fast dissolving tablets containing solid dispersion of Rofecoxib (1:6) was studied. The formulated formulations showed optimum dissolution efficiency.

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

scholarly journals A Novel Protocol Using Small-Scale Spray-Drying for the Efficient Screening of Solid Dispersions in Early Drug Development and Formulation, as a Straight Pathway from Screening to Manufacturing Stages

2018 ◽  
Vol 11 (3) ◽  
pp. 81
Author(s):  
Aymeric Ousset ◽  
Rosanna Chirico ◽  
Florent Robin ◽  
Martin Schubert ◽  
Pascal Somville ◽  
...  
Keyword(s):  
Spray Drying ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Physical Stability ◽  
Amorphous State ◽  
Amorphous Solid ◽  
Screening Strategy ◽  
Water Soluble ◽  
Small Scale ◽  
Absorption Window

This work describes a novel screening strategy that implements small-scale spray-drying in early development of binary amorphous solid dispersions (ASDs). The proposed methodology consists of a three-stage decision protocol in which small batches (20–100 mg) of spray-dried solid dispersions (SDSDs) are evaluated in terms of drug–polymer miscibility, physical stability and dissolution performance in bio-predictive conditions. The objectives are to select the adequate carrier and drug-loading (DL) for the manufacturing of robust SDSD; and the appropriate stabilizer dissolved in the liquid vehicle of SDSD suspensions, which constitutes the common dosage form used during non-clinical studies. This methodology was verified with CDP146, a poorly water soluble (<2 µg/mL) API combined with four enteric polymers and four stabilizers. CDP146/HPMCAS-LF 40:60 (w/w) and 10% (w/v) PVPVA were identified as the lead SDSD and the best performing stabilizer, respectively. Lead SDSD suspensions (1–50 mg/mL) were found to preserve complete amorphous state during 8 h and maintain supersaturation in simulated rat intestinal fluids during the absorption window. Therefore, the implementation of spray-drying as a small-scale screening approach allowed maximizing screening effectiveness with respect to very limited API amounts (735 mg) and time resources (9 days), while removing transfer steps between screening and manufacturing phases.

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.

scholarly journals Investigations on noval method for the formulation of solid dispersions part- I Formulation, characterization and selection

2017 ◽  
Vol 9 (3) ◽  
pp. 71
Author(s):  
Rakesh Kumar Sharma ◽  
Anil Kumar Middha
Keyword(s):  
Ir Spectroscopy ◽  
Solid Dispersions ◽  
Hydrophilic Polymers ◽  
Modulated Dsc ◽  
Dissolution Test ◽  
Stability Testing ◽  
Sustained Drug Release ◽  
Ft Ir ◽  
Pvp K30 ◽  
Ft Ir Spectroscopy

<p>The solid dispersions of indomethacin with hydrophilic polymers were prepared by lyophilization. The polymers used in the investigation were HPMC, PVP K30, CBR and PLF 127. The solubility and dissolution of indomethacin from prepared lyophilized solid dispersions were investigated in 0.1 N HCl, purified water and USP-NF dissolution media.  Out of fifteen lyophilized formulations from F1 to F15, five formulations F2, F5, F8, F12 and F14 showed highest solubility in purified water. Formulation F2, F8 failed to comply with the USP-NF dissolution test for indomethacin capsules. Formulation F14 showed maximum dissolution in the respective dissolution media within 60 min.  Sustained drug release was observed for 6 h with formulations F2 and F8 in USP-NF media. The formulations F2, F5, F8, F12 and F14 were characterized by modulated DSC and FT-IR spectroscopy. Some Formulations on stability testing were found physico-chemically stable at accelerated temperature conditions.</p>

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.

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