Dissolution Enhancement of Itraconazole by Hot-Melt Extrusion Alone and the Combination of Hot-Melt Extrusion and Rapid Freezing—Effect of Formulation and Processing Variables

2013 ◽  
Vol 11 (1) ◽  
pp. 186-196 ◽  
Author(s):  
Bo Lang ◽  
James W. McGinity ◽  
Robert O. Williams
Keyword(s):  
Hot Melt Extrusion ◽  
Dissolution Enhancement ◽  
Rapid Freezing ◽  
Melt Extrusion ◽  
Processing Variables ◽  
Hot Melt

scholarly journals SOLUBILITY AND DISSOLUTION ENHANCEMENT OF IVACAFTOR TABLETS BY USING SOLID DISPERSION TECHNIQUE OF HOT-MELT EXTRUSION - A DESIGN OF EXPERIMENTAL APPROACH

2019 ◽  
Vol 12 (1) ◽  
pp. 356
Author(s):  
Purnachandra Reddy Guntaka ◽  
Srinivas Lankalapalli
Keyword(s):  
Solid Dispersion ◽  
Ph Value ◽  
Hot Melt Extrusion ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Infrared Spectrometry ◽  
Lauryl Sulfate ◽  
Melt Extrusion ◽  
Structure Form ◽  
Hot Melt

Objective: The objective was to improve the solubility and dissolution of ivacaftor tablets by using solid dispersion (SD) technique.Methods: Ivacaftor is practically insoluble (<0.001 mg/mL) over pH value of 3.0–7.5 due to low solubility, and it shows poor bioavailability after oral administration. Therefore, SDs of Ivacaftor were prepared by SD technique of hot-melt extrusion (HME) by adding different polymers such as Soluplus, Hypromellose 5 cps, and Copovidone with surfactants sodium lauryl sulfate, poloxamer, and polysorbate 80 to enhance its solubility.Results: After the analysis of Fourier-transform infrared spectrometry, X-ray diffraction, and differential scanning calorimetry of SDs by HME shows a converted in crystalline structure form to an amorphous structure form of Ivacaftor. The results show that the formulation of Ivacaftor SDs by HMT has enhanced the solubility and dissolution of Ivacaftor.Conclusion: In the present study, the SDs of the poorly soluble drug substance Ivacaftor were successfully prepared using HME. The in vitro dissolution test shows a significant increase in dissolution rate of SDs prepared by HME (95%) in formulation FHM8 compared with plain Ivacaftor (9%) within 30 min.

scholarly journals Dissolution Enhancement of Raltegravir by Hot Melt Extrusion Technique

2018 ◽  
Vol 27 (1) ◽  
pp. 20-29A
Author(s):  
Ahmed S. Abdul Jabbar
Keyword(s):  
Solid Dispersion ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Dissolution Enhancement ◽  
Amorphous Solid Dispersion ◽  
Direct Compression ◽  
Compression Method ◽  
Melt Extrusion ◽  
Poorly Soluble ◽  
Hot Melt

The objective of the study to develop an amorphous solid dispersion for poorly soluble raltegravir by hot melt extrusion (HME) technique. A novel solubility improving agent plasdone  s630 was utilized. The HME raltegravir was formulated into tablet by direct compression method. The prepared tablets were assessed for all pre and post-compression parameters. The drug- excipients interaction was examined by FTIR and DSC. All formulas displayed complying with pharmacopoeial measures. The study reveals that formula prepared by utilizing drug and plasdone S630 at 1:1.5 proportion and span 20 at concentration about 30mg (trail-6) has given highest dissolution rate than contrasted with various formulas of raltegravir. Keywords: Hot melt extrusion, Raltegravir, Plasdone S630.

scholarly journals SOLUBILITY AND DISSOLUTION ENHANCEMENT OF IVACAFTOR TABLETS BY USING SOLID DISPERSION TECHNIQUE OF HOT-MELT EXTRUSION - A DESIGN OF EXPERIMENTAL APPROACH

2019 ◽  
Vol 12 (1) ◽  
pp. 356
Author(s):  
Purnachandra Reddy Guntaka ◽  
Srinivas Lankalapalli
Keyword(s):  
Solid Dispersion ◽  
Ph Value ◽  
Hot Melt Extrusion ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Infrared Spectrometry ◽  
Lauryl Sulfate ◽  
Melt Extrusion ◽  
Structure Form ◽  
Hot Melt

Objective: The objective was to improve the solubility and dissolution of ivacaftor tablets by using solid dispersion (SD) technique.Methods: Ivacaftor is practically insoluble (<0.001 mg/mL) over pH value of 3.0–7.5 due to low solubility, and it shows poor bioavailability after oral administration. Therefore, SDs of Ivacaftor were prepared by SD technique of hot-melt extrusion (HME) by adding different polymers such as Soluplus, Hypromellose 5 cps, and Copovidone with surfactants sodium lauryl sulfate, poloxamer, and polysorbate 80 to enhance its solubility.Results: After the analysis of Fourier-transform infrared spectrometry, X-ray diffraction, and differential scanning calorimetry of SDs by HME shows a converted in crystalline structure form to an amorphous structure form of Ivacaftor. The results show that the formulation of Ivacaftor SDs by HMT has enhanced the solubility and dissolution of Ivacaftor.Conclusion: In the present study, the SDs of the poorly soluble drug substance Ivacaftor were successfully prepared using HME. The in vitro dissolution test shows a significant increase in dissolution rate of SDs prepared by HME (95%) in formulation FHM8 compared with plain Ivacaftor (9%) within 30 min.

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