Advanced search
Start date

Evaluation of the degradation products of Ritonavir antiretroviral drug during hot extrusion process (HME)

Grant number: 19/22048-1
Support Opportunities:Scholarships abroad - Research Internship - Doctorate
Effective date (Start): January 31, 2020
Effective date (End): January 30, 2021
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Analytical Chemistry
Principal Investigator:Renato Lajarim Carneiro
Grantee:Benedito Roberto de Alvarenga Junior
Supervisor: Lynne Taylor
Host Institution: Centro de Ciências Exatas e de Tecnologia (CCET). Universidade Federal de São Carlos (UFSCAR). São Carlos , SP, Brazil
Research place: Purdue University, United States  
Associated to the scholarship:17/13095-0 - Experimental design applied to forced degradation of Nitazoxanide and Sofosbuvir pharmaceutical drugs, BP.DR


Human Immunodeficiency Virus (HIV) is one the major global public health issue that targets the immune system, destroying the function of immune cells. The infected individuals gradually become susceptible to wide range of infections. In this context, ritonavir is a pharmaceutical drug against HIV that acts as a protease inhibitor interfering in the reproductive cycle of the virus. However, ritonavir is a class IV drug in the Biopharmaceutical Classification System (BCS), presenting low solubility and bioavailability. In some formulations, ritonavir is presented as solution using ethanol/water. To overcome this issue, hot-melt extrusion technology rises as an effective processing technique used to increase the solubility of poorly water-soluble pharmaceutical drugs. However, degradation products can be generated during the HME process due to the high temperatures, oxidation processes, and reactions catalyzed by metallic interfaces. The understanding of degradation kinetics and degradation products is very important to minimize their production and ensure an effective and safe drug product. The goal of this work is to enhance the solubility and bioavailability of pharmaceutical drug ritonavir using hot-melt extrusion technique and evaluate the degradation products generated during the process, as well as the influence of the variables of the HME in the degradation of the API. Analytical methods (Liquid Chromatography-LC, Mass Spectrometry-MS, and Nuclear Magnet Resonance-NMR), and Quality by Design concepts will be applied to obtain a final product with desired quality. (AU)

News published in Agência FAPESP Newsletter about the scholarship:
Articles published in other media outlets (0 total):
More itemsLess items

Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
MOSESON, DANA E.; JORDAN, MADISON A.; SHAH, DISHAN D.; CORUM, ISAAC D.; ALVARENGA, JR., BENEDITO R.; TAYLOR, LYNNE S.. Application and limitations of thermogravimetric analysis to delineate the hot melt extrusion chemical stability processing window. International Journal of Pharmaceutics, v. 590, . (19/22048-1)
DE ALVARENGA, JR., BENEDITO ROBERTO; MOSESON, DANA E.; CARNEIRO, RENATO LAJARIM; TAYLOR, LYNNE S.. Impact of Polymer Type on Thermal Degradation of Amorphous Solid Dispersions Containing Ritonavir. MOLECULAR PHARMACEUTICS, . (19/22048-1, 17/13095-0)

Please report errors in scientific publications list by writing to: