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.

scholarly journals Bio- Fortification of Angelica gigas Nakai Nano-Powder Using Bio-Polymer by Hot Melt Extrusion to Enhance the Bioaccessibility and Functionality of Nutraceutical Compounds

2019 ◽  
Vol 13 (1) ◽  
pp. 3
Author(s):  
Md Obyedul Kalam Azad ◽  
Wie Soo Kang ◽  
Jung Dae Lim ◽  
Cheol Ho Park
Keyword(s):  
Physicochemical Properties ◽  
Radical Scavenging ◽  
Hot Melt Extrusion ◽  
Total Phenolic ◽  
Melt Extrusion ◽  
Antioxidant Power ◽  
Angelica Gigas ◽  
Angelica Gigas Nakai ◽  
Nutraceutical Compounds ◽  
Hot Melt

Angelica gigas Nakai (AGN) is a popular traditional herbal medicine which has been used to alleviate various human diseases in Korea since ancient times. However, the low bioaccessibility of the nutraceutical compounds of AGN results in a poor water solubility, thereby limiting bioavailability. In this regard, a ternary AGN–biopolymer–plasticizer composite (AGNC) was developed to enhance the bioaccessibility of nutraceutical compounds from extrudate AGN formulations manufactured by hot melt extrusion (HME). The AGNC was prepared with extrudate AGN (EAGN) using different hydroxypropyl methylcellulose (HPMC) biopolymers (5% w/w) viz.: hypromellose phthalate (HP), hypromellose (AN), and hypromellose (CN) along with acetic acid (AA) (0.1 M, 20% w/v) as a plasticizer. The non-extrudate fresh AGN (FAGN) powder was used as a control. The physicochemical properties of the extrudate formulations and control were characterized by differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). DSC analysis showed a lower enthalpy (ΔH) (12.22 J/g) and lower glass transition temperature (Tg) (41 °C) in HP-AA-EAGN compared to the control. FTIR confirmed the physical crosslinking between AGN and biopolymer in the extrudate composite and demonstrated that some functional groups formed viz., -OH and -CH2. The obtained result also shows that the particle size was reduced by 341 nm, and solubility was increased by 65.5% in HP-AA-EAGN compared to the control (1499 nm, 29.4%, respectively). The bioaccessibility of the total phenolic content and the total flavonoids—including decursin (D) and decursinol angelate (DA)—were significantly higher in HP-AA-EAGN compared to the control. The 2,2-diphenyl-1 picryl hydrazyl (DPPH) free radical scavenging capacity and ferric reducing antioxidant power assay (FRAP) indicated that the HP-AA-EAGN formulation preserves a greater antioxidant profile than the other formulations. Finally, it is summarized that the addition of acidified HP biopolymer increased the bioaccessibility, functionality, and improved the physicochemical properties of nutraceutical compounds in the extrudate AGN formulation.

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.

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