To crush or not to crush: A brief review of novel tablets and capsules prepared from nanocrystal and amorphous solid dispersion technologies

2020 ◽  
Author(s):  
Elizabeth Uttaro ◽  
Madhu Pudipeddi ◽  
Anne Schweighardt ◽  
Fang Zhao
Keyword(s):  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Healthcare Providers ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersion ◽  
Accurate Information ◽  
Drug Products ◽  
Development Pipeline ◽  
New Formulation

Abstract Purpose To educate healthcare professionals regarding the risks of manipulating drug products formulated via nanocrystal or amorphous solid dispersion technologies. Summary Recent pharmaceutics innovations such as nanocrystals and amorphous solid dispersions have been used successfully to improve oral bioavailability of drugs. Over 30 drug products based on these technologies have been approved by the Food and Drug Administration, and more are in the development pipeline. While these products are similar in appearance to traditional tablets or capsules, they should not be crushed or suspended in liquid vehicles. Such manipulations can compromise the integrity of the formulation and subsequently alter the oral bioavailability. It is alarming that the majority of these products are not included in the Institute for Safe Medication Practices (ISMP) “Do Not Crush” list. A summary drug table is presented in this article to provide accurate information for pharmacists and other healthcare providers. Conclusion Novel formulations of tablets and capsules are being used to increase the oral bioavailability of certain drugs. Crushing these products can significantly alter product performance and clinical outcomes. We encourage ISMP to add these drug products to the Do Not Crush list due to wide use of this list throughout healthcare. In the meantime, pharmacists should be mindful of the new formulation technologies and advocate for the proper use of these drug products.

scholarly journals Enhanced Oral Bioavailability of Resveratrol by Using Neutralized Eudragit E Solid Dispersion Prepared via Spray Drying

Antioxidants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 90
Author(s):  
Eun-Sol Ha ◽  
Du Hyung Choi ◽  
In-hwan Baek ◽  
Heejun Park ◽  
Min-Soo Kim
Keyword(s):  
Spray Drying ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Pharmaceutical Products ◽  
In Vitro Dissolution ◽  
Dependent Manner ◽  
Amorphous Solid Dispersions ◽  
Eudragit E

In this study, we designed amorphous solid dispersions based on Eudragit E/HCl (neutralized Eudragit E using hydrochloric acid) to maximize the dissolution of trans-resveratrol. Solid-state characterization of amorphous solid dispersions of trans-resveratrol was performed using powder X-ray diffraction, scanning electron microscopy, and particle size measurements. In addition, an in vitro dissolution study and an in vivo pharmacokinetic study in rats were carried out. Among the tested polymers, Eudragit E/HCl was the most effective solid dispersion for the solubilization of trans-resveratrol. Eudragit E/HCl significantly inhibited the precipitation of trans-resveratrol in a pH 1.2 dissolution medium in a dose-dependent manner. The amorphous Eudragit E/HCl solid dispersion at a trans-resveratrol/polymer ratio of 10/90 exhibited a high degree of supersaturation without trans-resveratrol precipitation for at least 48 h by the formation of Eudragit E/HCl micelles. In rats, the absolute oral bioavailability (F%) of trans-resveratrol from Eudragit E/HCl solid dispersion (10/90) was estimated to be 40%. Therefore, trans-resveratrol-loaded Eudragit E/HCl solid dispersions prepared by spray drying offer a promising formulation strategy with high oral bioavailability for developing high-quality health supplements, nutraceutical, and pharmaceutical products.

scholarly journals Silymarin-solid dispersions: Characterization and influence of preparation methods on dissolution

2010 ◽  
Vol 60 (4) ◽  
pp. 427-443 ◽  
Author(s):  
Dalwadi Sonali ◽  
Soni Tejal ◽  
Thakkar Vaishali ◽  
Gandhi Tejal
Keyword(s):  
Spray Drying ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Precipitation Method ◽  
Amorphous Solid Dispersion ◽  
Preparation Methods ◽  
Hydrogen Bond Formation ◽  
Pure Drug ◽  
Co Precipitation

Silymarin-solid dispersions: Characterization and influence of preparation methods on dissolution The influence of preparation methodology of silymarin solid dispersions using a hydrophilic polymer on the dissolution performance of silymarin was investigated. Silymarin solid dispersions were prepared using HPMC E 15LV by kneading, spray drying and co-precipitation methods and characterized by FTIR, DSC, XRPD and SEM. Dissolution profiles were compared by statistical and model independent methods. The FTIR and DSC studies revealed weak hydrogen bond formation between the drug and polymer, while XRPD and SEM confirmed the amorphous nature of the drug in co-precipitated solid dispersion. Enhanced dissolution compared to pure drug was found in the following order: co-precipitation > spray drying > kneading methodology (p < 0.05). All preparation methods enhanced silymarin dissolution from solid dispersions of different characteristics. The co-precipitation method proved to be best and provided a stable amorphous solid dispersion with 2.5 improved dissolution compared to the pure drug.

Effect of supersaturation on the oral bioavailability of paclitaxel/polymer amorphous solid dispersion

2018 ◽  
Vol 9 (1) ◽  
pp. 344-356 ◽  
Author(s):  
Linlin Miao ◽  
Yuheng Liang ◽  
Wenli Pan ◽  
Jingxin Gou ◽  
Tian Yin ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersion
Sign in / Sign up

Export Citation Format

Share Document