scholarly journals Application of the combination of ball-milling and hot-melt extrusion in the development of an amorphous solid dispersion of a poorly water-soluble drug with high melting point

RSC Advances ◽  
2019 ◽  
Vol 9 (39) ◽  
pp. 22263-22273 ◽  
Author(s):  
Wenling Fan ◽  
Wenjing Zhu ◽  
Xinyi Zhang ◽  
Yan Xu ◽  
Liuqing Di
Keyword(s):  
Melting Point ◽  
Amorphous Solid ◽  
Water Soluble ◽  
Amorphous Solid Dispersion ◽  
High Melting ◽  
High Melting Point ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Hot Melt ◽  
Poorly Water Soluble Drug

The aim of the study was to develop an amorphous solid dispersion of a poorly water-soluble drug with high melting point by ball milling and hot melt extrusion as a co-processing method.

scholarly journals Orodispersible Polymer Films with the Poorly Water-Soluble Drug, Olanzapine: Hot-Melt Pneumatic Extrusion for Single-Process 3D Printing

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 692 ◽  
Author(s):  
Hui-Won Cho ◽  
Seung-Hoon Baek ◽  
Beom-Jin Lee ◽  
Hyo-Eon Jin
Keyword(s):  
3D Printing ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Fused Deposition ◽  
Water Soluble Drug ◽  
Single Process ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Hot Melt ◽  
Poorly Water Soluble Drug

Amorphous solid dispersions (ASDs) improve the oral delivery of poorly water-soluble drugs. ASDs of olanzapine (OLZ), which have a high melting point and low solubility, are performed using a complicated process. Three-dimensional (3D) printing based on hot-melt pneumatic extrusion (HMPE) is a simplified method for producing ASDs. Unlike general 3D printing, printlet extrusion is possible without the preparation of drug-loaded filaments. By heating powder blends, direct fused deposition modeling (FDM) printing through a nozzle is possible, and this step produces ASDs of drugs. In this study, we developed orodispersible films (ODFs) loaded with OLZ as a poorly water-soluble drug. Various ratios of film-forming polymers and plasticizers were investigated to enhance the printability and optimize the printing temperature. Scanning electron microscopy (SEM) showed the surface morphology of the film for the optimization of the polymer carrier ratios. Differential scanning calorimetry (DSC) was used to evaluate thermal properties. Powder X-ray diffraction (PXRD) confirmed the physical form of the drug during printing. The 3D printed ODF formulations successfully loaded ASDs of OLZ using HMPE. Our ODFs showed fast disintegration patterns within 22 s, and rapidly dissolved and reached up to 88% dissolution within 5 min in the dissolution test. ODFs fabricated using HMPE in a single process of 3D printing increased the dissolution rates of the poorly water-soluble drug, which could be a suitable formulation for fast drug absorption. Moreover, this new technology showed prompt fabrication feasibility of various formulations and ASD formation of poorly water-soluble drugs as a single process. The immediate dissolution within a few minutes of ODFs with OLZ, an atypical antipsychotic, is preferred for drug compliance and administration convenience.

Controlled Release of a Poorly Water-Soluble Drug from Hot-Melt Extrudates Containing Acrylic Polymers

2006 ◽  
Vol 32 (5) ◽  
pp. 569-583 ◽  
Author(s):  
Yucun Zhu ◽  
Navnit H. Shah ◽  
A. Waseem Malick ◽  
Martin H. Infeld ◽  
James W. McGinity
Keyword(s):  
Controlled Release ◽  
Water Soluble ◽  
Acrylic Polymers ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Hot Melt ◽  
Poorly Water Soluble Drug

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

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