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 Formulation and Characterization of Solid Dispersion Prepared by Hot Melt Mixing: A Fast Screening Approach for Polymer Selection

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Arno A. Enose ◽  
Priya K. Dasan ◽  
H. Sivaramakrishnan ◽  
Sanket M. Shah
Keyword(s):  
Solid Dispersion ◽  
Hot Melt Extrusion ◽  
Extrusion Process ◽  
Melt Extrusion ◽  
Dynamic Vapor Sorption ◽  
Scanning Calorimetry ◽  
Melt Mixing ◽  
Predictive Tool ◽  
Evaporation Technique ◽  
Hot Melt

Solid dispersion is molecular dispersion of drug in a polymer matrix which leads to improved solubility and hence better bioavailability. Solvent evaporation technique was employed to prepare films of different combinations of polymers, plasticizer, and a modal drug sulindac to narrow down on a few polymer-plasticizer-sulindac combinations. The sulindac-polymer-plasticizer combination that was stable with good film forming properties was processed by hot melt mixing, a technique close to hot melt extrusion, to predict its behavior in a hot melt extrusion process. Hot melt mixing is not a substitute to hot melt extrusion but is an aid in predicting the formation of molecularly dispersed form of a given set of drug-polymer-plasticizer combination in a hot melt extrusion process. The formulations were characterized by advanced techniques like optical microscopy, differential scanning calorimetry, hot stage microscopy, dynamic vapor sorption, and X-ray diffraction. Subsequently, the best drug-polymer-plasticizer combination obtained by hot melt mixing was subjected to hot melt extrusion process to validate the usefulness of hot melt mixing as a predictive tool in hot melt extrusion process.

scholarly journals Preliminary Development of Solid Dispersion for an Insoluble Compound ZL006 by Miniaturized Hot Melt Extrusion

2019 ◽  
Vol 01 (01) ◽  
pp. e11-e21
Author(s):  
Lijun Zhang ◽  
Hansen Luan ◽  
Weiyue Lu ◽  
Hao Wang
Keyword(s):  
Solid Dispersion ◽  
Scale Up ◽  
Hot Melt Extrusion ◽  
Minimal Amount ◽  
Melt Extrusion ◽  
Scanning Calorimetry ◽  
Modulated Differential Scanning Calorimetry ◽  
Hydrogen Bond Formation ◽  
Hot Melt

AbstractThe purpose of this study was to develop a solid dispersion (SD) by miniaturized hot-melt extrusion (HME) for an insoluble molecule ZL006 which showed potency of increasing leukocytes. A preliminary formulation screening was conducted using solvent evaporation method. The selected SD formulation was further optimized and scaled up using a miniaturized twin-screw extruder. Solid-state characterizations of the scale-up SD and its corresponding physical mixture (PM) were performed by X-ray powder diffraction (XRPD), modulated differential scanning calorimetry (mDSC), and Fourier's transform infrared spectroscopy (FTIR). XRPD and mDSC results indicated the formation of amorphous SD. FTIR spectrum indicated the possible hydrogen bond formation between the compound and the excipient. A discriminating non-sink condition micro-dissolution of SD showed the fast release of ZL006 which was approximately two-fold and three-fold of dissolution of PM and pure crystalline compound, respectively. The preliminary in vivo pharmacokinetics (PK) study in rats showed 71% oral bioavailability from the SD, while the bioavailability of ZL006 conventional suspension was less than 1%. Thus, an SD formulation for ZL006 with improved solubility and bioavailability was developed by miniaturized HME with minimal amount of compound at early preclinical stage, which could enable the preclinical evaluation.

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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