Characterization of Physico-Mechanical Properties of Indomethacin and Polymers to Assess their Suitability for Hot-Melt Extrusion Processs as a Means to Manufacture Solid Dispersion/Solution**Mailing address of the place where the work was carried out, Hoffmann-La Roche, Inc., 340 Kingsland Street, Nutley, NJ, 07110.

2005 ◽  
Vol 94 (11) ◽  
pp. 2463-2474 ◽  
Author(s):  
Rina J. Chokshi ◽  
Harpreet K. Sandhu ◽  
Raman M. Iyer ◽  
Navnit H. Shah ◽  
A.Waseem Malick ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Solid Dispersion ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Mailing Address ◽  
Dispersion Solution ◽  
Hot Melt

scholarly journals IMPROVING SOLUBILITY AND DISSOLUTION OF A NATURAL PRODUCT APIGENIN VIA PREPARATION OF SOLID DISPERSION BY HOT MELT EXTRUSION

2021 ◽  
pp. 47-52
Author(s):  
SOFI N. STIANI ◽  
TAOFIK RUSDIANA ◽  
ANAS SUBARNAS
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Practical Method ◽  
Hot Melt Extrusion ◽  
Raw Material ◽  
Melt Extrusion ◽  
Scanning Calorimetry ◽  
Twin Screw ◽  
Hot Melt

Objective: Hot Melt Extrusion (HME) is one of the techniques for preparing a solid dispersion hydrophilic excipient known as a no solvents practical method to increase the solubility of drugs. Apigenin (APG) has properties that thermal stable with melting point 345-350 °C but very low solubility in the water around 1,35 µg/ml. The polymer is stable in the HME method are Soluplus and Kollidon VA 64. The study aims to optimize the kind of polymer in HME formulae to improve the solubility and dissolution rate of apigenin by solid dispersion using hot-melt extrusion. Methods: Apigenin 10–50% w/w and Kollidon®VA 64 or Soluplus® and combination of Kollidon®VA 64 and Soluplus® were mixed, and the resulting blends extruded using a twin-screw extruder (Teach-Line ZK25T). Characterization of apigenin extrudates conducted using scanning electron microscopy, thermogravimetric analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffractometry, and dissolution. Results: Solubility studies presented enhancement in apigenin of 10%/Soluplus®90%; 10% w/w apigenin/Kollidon®VA 64 (90%); and 33,3% w/w apigenin/Kollidon®VA 64 33,3% mix Soluplus® 33,3% increased more than 18,25; 16,18-and 8,52-fold in water, respectively. Furthermore dissolution studies showed enhancement in apigenin percent release of 10%/Soluplus®90%; 10% w/w apigenin/Kollidon®VA 64 90%; and 33,3% w/w apigenin/Kollidon®VA 64 33,3% mix Soluplus® 33,3% tablet apigenin HME up to 34,29%; 69,75% and 30,69%, respectively. Conclusion: The formulation of 10% w/w Apigenin and 90% Soluplus® using hot-melt extrusion able to increase water solubility approximately 18,25-fold than raw material apigenin.

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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