scholarly journals Enhancing the Poor Flow and Tableting Problems of High Drug-Loading Formulation of Canagliflozin Using Continuous Green Granulation Process and Design-of-Experiment Approach

2020 ◽  
Vol 13 (12) ◽  
pp. 473
Author(s):  
Bjad K. Almutairy ◽  
El-Sayed Khafagy ◽  
Ahmed Alalaiwe ◽  
Mohammed F. Aldawsari ◽  
Saad M. Alshahrani ◽  
...  

Maximization of drug-loading can significantly reduce the size of dosage form and consequently decrease the cost of manufacture. In this research, two challenges were addressed: poor flow and tableting problems of high-drug loading (>70%) formulation of canagliflozin (CNG), by adopting the moisture-activated dry granulation (MADG) process. In this method, heating and drying steps were omitted so, called green granulation process. A 32 full-factorial design was performed for optimization of key process variables, namely the granulation fluid level (X1) and the wet massing time (X2). Granulation of CNG was carried out in the presence of polyvinylpyrrolidone, and the prepared granules were compressed into tablets. Regression analysis demonstrated the significant (p ≤ 0.05) effect of X1 and X2 on properties of granules and corresponding tablets, with pronounced impact of X1. Additionally, marked improvement of granules’ properties and tableting of CNG were observed. Furthermore, the optimized process conditions that produced good flow properties of granules and acceptable tablets were high level of granulation fluid (3.41% w/w) and short wet massing time (1.0 min). Finally, the MADG process gives the opportunity to ameliorate the poor flow and tableting problems of CNG with lower amounts of excipients, which are important for successful development of uniform dosage unit.

2016 ◽  
Vol 23 (6) ◽  
pp. 587-595 ◽  
Author(s):  
Preetanshu Pandey ◽  
Christopher Levins ◽  
Steve Pafiakis ◽  
Brian Zacour ◽  
Dilbir S. Bindra ◽  
...  

2018 ◽  
Author(s):  
Robert Luxenhofer ◽  
Michael M Lübtow ◽  
Lukas Hahn ◽  
Thomas Lorson ◽  
Rainer Schobert

Many natural compounds with interesting biomedical properties share one physicochemical property, namely a low water solubility. Polymer micelles are, among others, a popular means to solubilize hydrophobic compounds. The specific molecular interactions between the polymers and the hydrophobic drugs are diverse and recently it has been discussed that macromolecular engineering can be used to optimize drug loaded micelles. Specifically, π-π stacking between small molecules and polymers has been discussed as an important interaction that can be employed to increase drug loading and formulation stability. Here, we test this hypothesis using four different polymer amphiphiles with varying aromatic content and various natural products that also contain different relative amounts of aromatic moieties. While in the case of paclitaxel, having the lowest relative content of aromatic moieties, the drug loading decreases with increasing relative aromatic amount in the polymer, the drug loading of curcumin, having a much higher relative aromatic content, is increased. Interestingly, the loading using schizandrin A, a dibenzo[a,c]cyclooctadiene lignan with intermediate relative aromatic content is not influenced significantly by the aromatic content of the polymers employed. The very high drug loading, long term stability, the ability to form stable highly loaded binary coformulations in different drug combinations, small sized formulations and amorphous structures in all cases, corroborate earlier reports that poly(2-oxazoline) based micelles exhibit an extraordinarily high drug loading and are promising candidates for further biomedical applications. The presented results underline that the interaction between the polymers and the incorporated small molecules are complex and must be investigated in every specific case.<br>


2019 ◽  
Vol 233 ◽  
pp. 230-235 ◽  
Author(s):  
Li-li Lu ◽  
Wen-ya Xiong ◽  
Jun-bin Ma ◽  
Tian-fang Gao ◽  
Si-yuan Peng ◽  
...  

2021 ◽  
Vol 266 ◽  
pp. 118122
Author(s):  
Tianxing Chen ◽  
Yuan Yang ◽  
Hui Peng ◽  
Andrew K. Whittaker ◽  
Yao Li ◽  
...  

2021 ◽  
Vol 147 ◽  
pp. 110286
Author(s):  
Christian E. Ziegler ◽  
Moritz Graf ◽  
Sebastian Beck ◽  
Achim M. Goepferich

2010 ◽  
Vol 132 (12) ◽  
pp. 4259-4265 ◽  
Author(s):  
Youqing Shen ◽  
Erlei Jin ◽  
Bo Zhang ◽  
Caitlin J. Murphy ◽  
Meihua Sui ◽  
...  

2017 ◽  
Vol 533 (1) ◽  
pp. 73-83 ◽  
Author(s):  
Jie Hou ◽  
Chunlei Guo ◽  
Yuzhi Shi ◽  
Ergang Liu ◽  
Weibing Dong ◽  
...  

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