Our vertical twin screw micro extrusion technology could also be used to improve the bioavailability of other drugs being considered as treatments for COVID19

24 Apr 2020

Impressive results from Stage 2 trials at Rondol to reformulate hydroxychloroquine (HCQ) and optimize its dosing

 

After careful screening we selected BASF Soluplus as the matrix polymer. Our data demonstrates that by selecting a 70% Soluplus - 30% HCQ sulphate blend premixed for 15 mms and utilising an "ultra light mixing" screw profile and a maximum extrusion temperature close to the melt point of  HCQ sulphate on our vertical extruder, we can significantly reduce the crystallinity of HCQ within the blend (minimum of 20%).

 

The reduced crystallinity should result in improved dissolution performance and thus improved bioavailability and lower dosing of HCQ  to treat COVID19. 

 

Furthermore, we achieved this reduction in crystallinity at a screw speed of a 200 RPM allowing for high throughput manufacturing of HCQ pellets, which can be used to manufacture either tablets or capsules for oral administration.  

 

We of course await the results of the WHO Solidarity clinical trial assessing HCQ as a treatment for COVID19.  

 

In the meantime we are happy to share and discuss our results with whomever is interested in the development and manufacture of improved formulations and/or increased production of hydroxychloroquine.  

 

Our vertical twin screw micro extrusion technology could also be used to improve the bioavailability of other drugs being considered as treatments for COVID19, especially those where there are toxicity issues and where the initial required dosing is estimated to be high.

 

Also the next stage of our research will assess the stability and dissolution profile of the HCQ pellets and we hope to have further data for consideration for academic publication by the end of June.

 

Huge thank you to all teams who have contributed their experience, time and money to these results at BASF Pharma Solutions, University of Birmingham School of Pharmacy, Institut Jean Lamour, Queens University Belfast, Region Grand Est, Rondol Industrie and Sanofi Active Ingredients.

 

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