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Pharmaceutical emulsions for retroviral protease inhibitors

a protease inhibitor and emulsion technology, applied in the field of pharmaceutical compositions, can solve the problems of high trough level in the clinic, limited synthetic surfactant catalog, and potential for sustained releas

Inactive Publication Date: 2005-12-15
BOEHRINGER INGELHEIM INT GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a safe pharmaceutical composition for HIV infected patients that includes a pyranone compound of formula I. The composition is in the form of an emulsion formulation containing a high drug load of the pyranone compound of formula I, which has high oral bioavailability and produces a prolonged blood level curve indicating sustained release. The emulsion formulation contains natural, nontoxic lecithin as an emulsifier and allows for a high loading of the pyranone compound of formula I. The invention also provides a safe pediatric formulation for HIV infected infants or small children who are vulnerable to the side effects of synthetic surfactants. The technical effects of the invention include improved safety and effectiveness of the pyranone compound of formula I for the treatment of HIV infection.

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.

Method used

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  • Pharmaceutical emulsions for retroviral protease inhibitors
  • Pharmaceutical emulsions for retroviral protease inhibitors
  • Pharmaceutical emulsions for retroviral protease inhibitors

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0050]

ComponentWeight (mg)Compound of Formula I60Miglyol 812200Propylene Glycol100Lecithin20Na Deoxycholate0.5glycerine24Methyl paraben1.8Propyl paraben0.2Waterq.s.

example 2

[0051]

ComponentWeight (mg)Compound of Formula I60GDO / GMO (8:2)200Propylene Glycol100Lecithin20Na Deoxycholate0.5glycerine2.4Methyl paraben1.8Propyl paraben0.2Waterq.s.

example 3

[0052]

ComponentWeight (mg)Compound of Formula I60Miglyol 812200Propylene Glycol100Lecithin20Na Deoxycholate0.5glycerine24Methyl paraben1.8Propyl paraben0.2Waterq.s.

[0053] The examples 1 and 3 are the same formulation but different particle sizes

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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...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/107A61K9/48A61K31/445
CPCA61K9/1075A61K31/445A61K9/4858
Inventor WANG, YOUMINMOROZOWICH, WALTER
Owner BOEHRINGER INGELHEIM INT GMBH
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