Pharmaceutical emulsions for retroviral protease inhibitors

Abstract

The present invention provides an emulsion formulation with high oral bioavailability containing lecithin as an emulsifier and solubilizing agent to achieve a high loading of the pyranone compound of formula I.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application is a continuation of U.S. pending application Ser. No. 09 / 532 196, filed Mar. 22, 2000, which in turn claims the benefit of the following provisional application: U.S. Ser. No. 60 / 127,026, filed Mar. 31, 1999, under 35 USC § 119(e)(1).FIELD OF THE INVENTION [0002] The present invention relates to novel pharmaceutical compositions in the form of emulsions with high oral bioavailability and prolonged blood levels for compounds which are inhibitors of retroviral protease. In particular, the composition is a safe emulsion formulation comprising a HIV protease inhibitor, an oil component, an emulsifying agent consisting of lecithin and solvents for pediatric patients. BACKGROUND OF THE INVENTION [0003] It has recently been discovered that certain pyranone compounds inhibit retroviral protease and thus they are useful for treating patients infected with human immunodeficiency virus (HIV) which results in acquired immunodefici...

AI Technical Summary

Benefits of technology

[0018] Another object of the present invention is to provide a safe pediatric formulation for HIV infected infants or small children who are especially vulnerable to the side effects of synthetic surfactants.

[0019] A further object of the present invention is to provide an emulsion formulation containing a high drug load of the pyranone compound of formula I for convenient administration which also has high oral bioavailability.

[0020] A still further object of the present invention is to provide an emulsion formulation which is capable of producing a prolonged blood level curve indicating sustained release.

[0021] The objects of the present invention have been accomplished in that the present invention provides an emulsion formulation containing natural, nontoxic lecithin as an emulsifier while at the same time allows a high loading of the pyranone compound of formula I. This novel formulation also achieves the desired high oral bioavailability and produces a prolonged blood level curve

Problems solved by technology

However, these formulations require synthetic surfactants as emulsifiers to stabilize the compositions.

Unfortunately, the catalog of suitable synthetic surfactants is limited.

Therefore, they have the potential for sustained release and high trough levels in the clinic.

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