Topical Antiviral Formulations

Abstract

The present invention relates to formulations of nucleotide reverse transcriptase inhibitors (N(t)RTIs), preferably [2-(6-Amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid (tenofovir, PMPA), or a physiologically functional derivative thereof, suitable for topical application and their use in the prevention of HIV infections.

Description

FIELD OF THE INVENTION [0001] The invention relates generally to formulations of compounds with antiviral activity and more specifically with anti-HIV properties. BACKGROUND OF THE INVENTION [0002] Human immunodeficiency virus (HIV) infection and related diseases are a major public health problem worldwide. One approach to the problem of HIV / AIDS is to reduce the risk of transmission of HIV and thus reduce the number of individuals who become newly infected. Even when treatments or cures become available, prevention of infections in the initial instance will likely remain as the first line of defense. For medical, psychological, and economic reasons, it is preferable to prevent the initial infection, rather than treating, individuals with AIDS. [0003] Education in regard to sexually transmitted diseases (STDs), their modes of transmission, and so-called “safe-sex” techniques has shown some promise in reducing the risks of STD transmission through sexual activity. Screening of the bl...

AI Technical Summary

Benefits of technology

[0007] This invention generally relates to compositions and methods which prevent and / or reduce the risk of transmission of HIV through sexual activity. Although it is mainly directed at heterosexual conduct (i.e., male / female vaginal intercourse), the compositions of this invention may also be used by parties engaged in other types of sexual conduct. For example, the compositions of this invention could be used by parties engaged in anal intercourse (male / female or male / male); compositions of this invention intended to be used in anal intercourse are preferably modified to adjust the buffering capacity to pH values normally found in the rectum and by altering the lubricity of the formulation.

[0009] If desired, flavorants, scents, fragrances, and colorants may be incorporated into the composition so long as they do not interfere with the safety or efficacy of the composition. Indeed, incorporation of such flavorants, scents, fragrances, and colorants into the compositions of this invention may increase the probability that the composition will be used during sexual activity.

[0010] One advantage of the present method is that it can be used for protection during a wide variety of sexual activities (vaginal or anal) by heterosexuals, bisexuals, and homosexuals. Another advantage of the present method of reducing the transmission of HIV is that this method may be implemented and / or used most easily by the party being penetrated. Thus, a woman may use the present method to protect herself (as well as her partner) with or without the partner's knowledge of the method being used. Moreover, the partner would not be required to rely on his or her partner's claim of being AIDS-free or agreement to use condoms for protection. Either or both sexual parties (especially the female participant) could initiate and implement the use of the present method. Preferably the method is used before the sexual activity and most preferably both before and after the sexual activity. Moreover, the compositions of this invention offer the added benefit that they are also useful in the prevention and / or treatment of bacterial vaginosis.

Problems solved by technology

Human immunodeficiency virus (HIV) infection and related diseases are a major public health problem worldwide.

Even with their known effectiveness in preventing STDs, current safe-sex techniques are not always used, or are not always used properly, for many reasons (e.g. carelessness, lack of knowledge, improper techniques, cultural barriers, unplanned or spontaneous sexual activity, and the like).

Moreover, even when used, safe-sex techniques (except perhaps abstinence) are not always effective.

However, there is no formulation that is totally effective against HIV.

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