Flavoring systems for pharmaceutical compositions and methods of making such compositions

Abstract

A flavoring system for a liquid pharmaceutical composition and pharmaceutical compositions containing such flavoring systems are disclosed. Flavoring systems of the invention include at least one sweetening agent, at least two flavored ingredients, and at least one flavor modifier selected from the group consisting of citric acid, sodium citrate, sodium chloride, and mixtures thereof. At least two of the flavored ingredients are selected from the group consisting of a vanilla flavored ingredient, a peppermint flavored ingredient, a menthol flavored ingredient, a cotton candy flavored ingredient, and mixtures thereof. The one or more sweetening agents comprise glycerin, monoammonium glycyrrhizinate, saccharin sodium, acesulfame potassium, high fructose corn syrup, and / or mixtures thereof. Pharmaceutical compositions of the invention include a flavoring system of the invention, a solvent system, and at least one pharmaceutically active agent, such as lopinavir or derivatives thereof, ritonavir or derivatives thereof, or mixtures thereof. Methods for making such liquid pharmaceutical compositions are also disclosed.

Description

[0001] This application claims priority to the provisional application Ser. No. 60 / 230,095 Filed on Sep. 5, 2000.FIELD OF THE INVENTION [0002] This invention relates to flavoring systems for pharmaceutical compositions, pharmaceutical compositions containing such flavoring systems, and methods of making such compositions. In particular, this invention is related to flavoring systems for liquid pharmaceutical compositions containing ritonavir or derivatives thereof, lopinavir or derivatives thereof, and mixtures of any of the above. The invention is also directed toward pharmaceutical compositions containing the flavoring systems of the invention and toward methods of making these pharmaceutical compositions. BACKGROUND OF THE INVENTION [0003] The pharmaceutically active agents lopinavir and ritonavir are well known inhibitors of the Human Immunodeficiency Virus (HIV), which is the causative organism of Acquired Immunodeficiency Syndrome (AIDS). Both ritonavir and lopinavir inhibit H...

AI Technical Summary

Benefits of technology

[0006] In general, Applicants have discovered that by increasing the number and type of ingredients in flavoring systems for liquid pharmaceutical compositions containing pharmaceutically active agents, such as lopinavir and ritonavir, the taste of pharmaceutical compositions containing these agents is improved. Flavoring systems of the invention generally contain two or more flavored ingredients, one or more sweetening agents, and one or more flavor modifiers selected from the group consisting of sodium citrate, sodium chloride, citric acid and mixtures thereof. Preferably two or more and most preferably all of the ingredients identified in the previous sentence are included as flavor modifiers in flavoring systems of the invention. The total amount of flavor modifiers included in flavoring systems of the invention is at least about 0.10% by weight and not greater than about 1.0% by weight based upon the total pharmaceutical composition containing such flavoring system. Most preferably, all of these flavor modifiers are included in the flavoring system in the following amounts by weight: sodium citrate in an amount of about 0.20%, sodium chloride in an amount of about 0.35%, and citric acid in an amount of about 0.11% based upon the total weight of the pharmaceutical composition. Unless otherwise stated herein, all weights are based upon the total weight of the pharmaceutical composition.

Problems solved by technology

Although much progress has been made toward treating AIDS, none of the current treatments have proven to be totally effective in reversing the disease.

In addition, many of the pharmaceutically active agents useful in treating AIDS have a bitter taste that discourages patients from complying with their drug taking regimen.