Application of Melt Extrusion in the Development of a Physically and Chemically Stable High-Energy Amorphous Solid Dispersion of a Poorly Water-Soluble Drug

2008 ◽  
Vol 5 (6) ◽  
pp. 994-1002 ◽  
Author(s):  
Jay P. Lakshman ◽  
Yu Cao ◽  
James Kowalski ◽  
Abu T. M. Serajuddin
Keyword(s):  
Solid Dispersion ◽  
Amorphous Solid ◽  
High Energy ◽  
Water Soluble ◽  
Amorphous Solid Dispersion ◽  
Melt Extrusion ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

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.

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.

scholarly journals Preparation and Characterization of PEG4000 Palmitate/PEG8000 Palmitate-Solid Dispersion Containing the Poorly Water-Soluble Drug Andrographolide

2020 ◽  
Vol 2020 ◽  
pp. 1-7
Author(s):  
Qingyun Zeng ◽  
Liquan Ou ◽  
Guowei Zhao ◽  
Ping Cai ◽  
Zhenggen Liao ◽  
...  
Keyword(s):  
Thermal Stability ◽  
Molecular Weight ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Water Soluble ◽  
Carrier Material ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersion (SD) is the effective approach to improve the dissolution rate and bioavailability of class II drugs with low water solubility and high tissue permeability in the Biopharmaceutics Classification System. This study investigated the effects of polyethylene glycol (PEG) molecular weight in carrier material PEG palmitate on the properties of andrographolide (AG)-SD. We prepared SDs containing the poorly water-soluble drug AG by the freeze-drying method. The SDs were manufactured from two different polymers, PEG4000 palmitate and PEG8000 palmitate. The physicochemical properties of the AG-SDs were characterized by Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, dissolution testing, and so on. We found that AG-PEG4000 palmitate-SD and AG-PEG8000 palmitate-SD were similar in the surface morphology, specific surface area, and pore volume. Compared with the AG-PEG4000 palmitate-SD, the intermolecular interaction between PEG8000 palmitate and AG was stronger, and the thermal stability of AG-PEG8000 palmitate-SD was better. In the meanwhile, the AG relative crystallinity was lower and the AG dissolution rate was faster in AG-PEG8000 palmitate-SD. The results demonstrate that the increasing PEG molecular weight in the PEG palmitate can improve the compatibility between the poorly water-soluble drug and carrier material, which is beneficial to improve the SD thermal stability and increases the dissolution rate of poorly water-soluble drug in the SD.

In Vitro-In Vivo Correlation for Solid Dispersion of a Poorly Water-Soluble Drug Efonidipine Hydrochloride

2020 ◽  
Vol 21 (5) ◽  
Author(s):  
Xu Cheng ◽  
Jianlong Gao ◽  
Jiaqi Li ◽  
Gang Cheng ◽  
Meijuan Zou ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Bioavailability of a Poorly Water-Soluble Drug from Tablet and Solid Dispersion in Humans

1991 ◽  
Vol 80 (7) ◽  
pp. 712-714 ◽  
Author(s):  
Pai-Chang Sheen ◽  
Soo-Il Kim ◽  
John J. Petillo ◽  
Abu T.M. Serajuddin
Keyword(s):  
Solid Dispersion ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

scholarly journals Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

Drug Delivery ◽  
2007 ◽  
Vol 14 (1) ◽  
pp. 33-45 ◽  
Author(s):  
Rina J. Chokshi ◽  
Hossein Zia ◽  
Harpreet K. Sandhu ◽  
Navnit H. Shah ◽  
Waseem A. Malick
Keyword(s):  
Solid Solution ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Pros And Cons ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

scholarly journals RESEARCH AND DEVELOPMENT OF DIAZEPAM SOLID DISPERSION POWDER USING NATURAL POLYMERS

2018 ◽  
Vol 10 (5) ◽  
pp. 220
Author(s):  
Uditi Handa ◽  
Kamal Saroha
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Natural Polymers ◽  
Drug Content ◽  
Ftir Studies ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Pure Drug ◽  
Poorly Water Soluble Drug

Objective: The objective of this study was to enhance the solubility and dissolution rate of a poorly water-soluble drug by solid dispersion (SD) technique, in order to conduct an investigation of the effect of these natural hydrophilic polymers on release mechanism from SD.Methods: The SD of diazepam (DZM) were prepared by using modified sodium alginate (SA) and modified guar gum (GG) in different drug: polymer ratios (1:1 and 1:2) by using physical mixture method (PM) and fusion method (FM). Further, the formulations were characterized for calibration curve, Fourier transforms infrared spectroscopy (FTIR) studies, % age practical yield, drug content estimation, solubility studies, dissolution studies.Results: The pure drug and SD were characterized by pre and post-formulations studies. The %age practical yield ranged from 92.9±0.25 to 49±0.57%, and the drug content estimation ranged from 99.34±0.40 to 65.25±0.25 %. The FTIR studies shown that the compatibility between pure drug and natural polymers was stable. All the SD showed improved solubility as compared to the pure drug (PD). SD prepared with modified SA (1:2) by PM and FM shown the huge enhancement of solubility and dissolution rate of the DZM. This can be specific to the improvement in wettability and dispersibility, as well as enhances the drug amorphous fraction.Conclusion: On the basis of the research study, the SD technique shows the enhancement in the solubility of poorly water-soluble drug using natural polymers. SD containing natural polymers prepared with PM and FM shown the remarkable improvement in the release outline compared with PD, DZM.

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