Lopinavir/ritonavir, a new galenic oral formulation from commercial solid form, fine-tuned by nuclear magnetic resonance spectroscopy

European Journal of Hospital Pharmacy. Science and Practice
Ielizza DesideriFederica Balzano

Abstract

The lopinavir/ritonavir combination is one of the first antiretroviral drugs to be used in the treatment of COVID-19. In incapacitated patients, such as those in intensive care, an oral liquid formulation is needed. In Italy a marketed formulation is available, but only by importing it from other European countries. A galenic oral formulation prepared in the hospital pharmacy from lopinavir/ritonavir tablets was fine-tuned, evaluating the content of the active pharmaceutical ingredient (API) and stability of the formulation by using nuclear magnetic resonance (NMR) spectroscopy. To overcome the insolubility of lopinavir/ritonavir in water, ethanol and glycerol have been used as additional excipients. To define the best excipient proportion and best preparation method, three different formulations (ethanol 7.1-7.5%, glycerol 6-15%, and water) and two different preparation procedures (two step vs one step) have been studied. Each formulation has been compared with Kaletra oral solution (lopinavir 80 mg/mL, ritonavir 20 mg/mL) by NMR spectroscopy. API content and stability were measured. The presence of ethanol and glycerol as co-solvents is crucial both to improve solubilisation and promote the stability of the oral form. In the ...Continue Reading

References

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Jul 29, 2021·Infection Prevention in Practice·M TobaiqyN Helmi

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Methods Mentioned

BETA
nuclear magnetic resonance
NMR
1

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