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 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.

Fenofibrate Solid Dispersion Processed by Hot-Melt Extrusion: Elevated Bioavailability and Its Cell Transport Mechanism

2019 ◽  
Vol 16 (6) ◽  
pp. 538-547 ◽  
Author(s):  
Ting Wen ◽  
Boyi Niu ◽  
Qiaoli Wu ◽  
Yixian Zhou ◽  
Xin Pan ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
In Vitro Dissolution ◽  
Amorphous Solid Dispersion ◽  
Dissolution Test ◽  
Melt Extrusion ◽  
Cell Transport ◽  
Hot Melt

Background: Fenofibrate (FNB) is an effective drug for the treatment of hypertriglyceridemia, hypercholesterolemia as well as mixed hyperlipidemia. However, due to its poor aqueous solubility, FNB has the problem of poor oral absorption followed by low bioavailability. Objective: The aim of this research was to construct FNB amorphous solid dispersion employing PVP VA64 as the carrier by hot-melt extrusion method, in order to improve the oral bioavailability. Additionally, the cell transport experiment was conducted to further investigate the mechanism of promoted osmotic absorption. Methods: The physical state of the obtained solid dispersion was characterized using SEM, DSC and XRD. Besides, in vitro Caco-2 cells were used to evaluate the cytotoxicity of the carrier and mimic gastrointestinal drug permeation. At last, in vitro dissolution test and in vivo bioavailability study were also carried out. Results: The prepared FNB solid dispersion was found to be an amorphous state after hot-melt extrusion process. In vitro cytotoxicity test on Caco-2 cells confirmed the excellent biocompatibility of the carrier PVP VA64. Besides, transwell cell transport assay and in vitro dissolution test revealed that FNB released from amorphous solid dispersion was equipped with an improved transmembrane transport and dissolution rate. Moreover, pharmacokinetic study in beagle dogs showed that comparing with commercial micronized product Lipanthyl®, the oral bioavailability of FNB solid dispersion was significantly enhanced (2.45 fold). Conclusion: In conclusion, PVP VA64 can be regarded as a promising polymer to enhance the bioavailability of poorly water-soluble drugs such as FNB processed by hot-melt extrusion. Besides, investigations on the mechanism of the enhanced penetration are expected to lay a foundation on the subsequent development of effective and practical solid dispersion.

scholarly journals Effect of Ultrafine Powderization and Solid Dispersion Formation via Hot-Melt Extrusion on Antioxidant, Anti-Inflammatory, and the Human Kv1.3 Channel Inhibitory Activities of Angelica gigas Nakai

2020 ◽  
Vol 2020 ◽  
pp. 1-11 ◽  
Author(s):  
Yunyao Jiang ◽  
Jingpei Piao ◽  
Nan Liu ◽  
Jincai Hou ◽  
Jianxun Liu ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Hot Melt Extrusion ◽  
Total Phenolic ◽  
No Production ◽  
Melt Extrusion ◽  
Angelica Gigas ◽  
Kv1.3 Channel ◽  
Ultrafine Grinding ◽  
Anti Inflammatory ◽  
Hot Melt

Angelica gigas Nakai (AGN) was first processed by ultrafine grinding technology and hot-melt extrusion (HME). The potential antioxidant and anti-inflammatory activities of AGN with a different process were compared, and the effect on the human Kv1.3 potassium channel was detected. The process of ultrafine powderization on AGN significantly increased the total phenolic and flavonoid contents, antioxidant activity, and DNA damage protective effect. On the contrary, AGN solid dispersion (AGN-SD) based on Soluplus® showed the highest inhibitory effect on NO production and the human Kv1.3 channel. In addition, AGN-SD inhibited the production of prostaglandin E2 and intracellular reactive oxygen species and the mRNA expression of inducible nitric oxide synthase, cyclooxygenase-2, interleukin 1β, and interleukin 6. Taken together, these results suggest that ultrafine powderization and solid dispersion formation via HME can significantly improve the biological activities of AGN. The results also suggested that ultrafine powderization and HME may be developed and applied in the pharmaceutical industry.

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