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Int. J. Mol. Sci. 2019, 20(7), 1718; https://doi.org/10.3390/ijms20071718

Development and Palatability Assessment of Norvir® (Ritonavir) 100 mg Powder for Pediatric Population

1
AbbVie Inc., North Chicago, IL 60064, USA
2
Senopsys LLC, Woburn, MA 01801, USA
*
Author to whom correspondence should be addressed.
Received: 25 February 2019 / Revised: 29 March 2019 / Accepted: 3 April 2019 / Published: 6 April 2019
(This article belongs to the Special Issue Paediatric Formulation: Design and Development)
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Abstract

Norvir® (ritonavir) is a Biopharmaceutical Classification System Class IV compound with poor solubility in water (~5 µg/mL) and limited oral bioavailability. Early stage development efforts were focused on an oral solution (OS) which provided reasonable bioavailability but exhibited taste-masking challenges and required the use of solvents with potential pediatric toxicity. Norvir® oral powder, 100 mg (NOP) was developed to replace OS. The objective of this study is to provide an overview of the development of NOP and palatability assessment strategy. Palatability of NOP was assessed using the flavor profile method: (1) As an aqueous suspension dose/response and (2) evaluation with foods. The dose/response sensory analysis indicated that NOP has strong intensity bitterness and burnt aromatics (3 on the 0–3 flavor profile scale) at the clinical dose (100 mg/10 mL) and the recognition threshold was determined to be 0.3 mg/10 mL. To improve palatability, 100 mg/10 mL NOP aqueous suspension was evaluated with foods. Consuming foods high in fat and/or sugar content after NOP administration successfully reduced bitterness to a 1.5 intensity. In summary, NOP provides dose flexibility, enhanced stability, eliminated solvents, and maintains consistent bioavailability, with reduced bitterness and improved palatability via administration with common food products. View Full-Text
Keywords: Norvir®; ritonavir; poorly soluble compound; pediatric; palatability assessment; bioavailability; flavor profile Norvir®; ritonavir; poorly soluble compound; pediatric; palatability assessment; bioavailability; flavor profile
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Morris, J.B.; Tisi, D.A.; Tan, D.C.T.; Worthington, J.H. Development and Palatability Assessment of Norvir® (Ritonavir) 100 mg Powder for Pediatric Population. Int. J. Mol. Sci. 2019, 20, 1718.

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