Amorphous efavirenz and the production thereof

Inactive Publication Date: 2007-02-01
ISP INVESTMENTS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010] The use of a solvent/non-solvent blend system has been found to provide additional benefits beyond the benefits obtained with a solvent only system. This solvent/non-solvent approach can produce a spray dried powder of lower residual solvent content and smaller particle size. A further consequence of this engineered particle morphology is the increase in bulk powder density. Increased powder density is an important attribute for many applications. The extent of polymer collapse—and therefore the net effect on the spray dried powder properties—depends on the polymer solvation factors, such as the initial ratio of solvent to non-solvent, the polymer chemical structure and the polymer molecular weight. In addition to reducing residual solvent content and increasing density, the primary polymer may be paired with the solvent/non-solvent system in order to affect not only the morphology of the particle, but a

Problems solved by technology

Eventually, the solvent composition is insuf

Method used

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  • Amorphous efavirenz and the production thereof
  • Amorphous efavirenz and the production thereof
  • Amorphous efavirenz and the production thereof

Examples

Experimental program
Comparison scheme
Effect test

example # 1

A. Example #1

[0081] 1. Efavirenz was spray dried with polyvinylpyrrolidone (PVP) (Plasdone® K-29 / 32, ISP) from 100% dichloromethane in the ratio 3 efavirenz: 1 PVP. Dichloromethane is a solvent for both efavirenz and PVP. [0082] 2. Analysis of efavirenz crystallinity by differential scanning calorimetry (DSC) (Q1000®, TA Instruments) showed the complete absence of an efavirenz melt endotherm. The spray dried powder contained only completely amorphous efavirenz (FIG. 1).

example # 2

B. Example #2

[0083] The efavirenz composition of Example #1 was placed on storage at 20° C. and 40° C. After 196 days of storage the sample show no amount of efavirenz crystallinity and contained only completely amorphous efavirenz at both storage temperatures (FIG. 2).

example # 3

C. Example #3

[0084] 1. Efavirenz was spray dried with polyvinylpyrrolidone-co-vinyl acetate (PVP-VA) (Plasdone® S-630, ISP) in the ratio 3 efavirenz:1 PVP-VA from 100% acetone. Acetone is a solvent for both efavirenz and PVP-VA. [0085] 2. Analysis of efavirenz crystallinity by DSC (Q1000®, TA Instruments) showed the complete absence of an efavirenz melt endotherm. The spray dried powder contained only completely amorphous efavirenz (FIG. 3).

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Abstract

Efavirenz compositions of enhanced bioavailability are described that contain efavirenz with at least one solubility-enhancing polymer. Described methods to produce the bioenhanced products comprise solvent spray drying. One aspect of the method includes the steps of providing a mixture comprising efavirenz, a solubility-enhancing polymer and a single solvent, a solvent blend or solvent/non-solvent blend removing and then evaporating the mixture to form amorphous efavirenz.

Description

REFERENCE TO RELATED APPLICATION [0001] This application claims the benefit of U.S. Pat. App. No. 60 / 703,374, filed Jul. 28, 2005, the contents of which are hereby incorporated by reference.BACKGROUND OF THE INVENTION [0002] The present invention is directed to compositions containing amorphous efavirenz and methods for producing amorphous efavirenz. More particularly, the present invention relates to compositions and methods for preparing amorphous efavirenz utilizing at least one solubility-enhancing polymer. In accordance with one embodiment, the efavirenz is dissolved in a solvent containing the polymer. In yet another embodiment, a blend of solvent / non-solvent for the polymer is employed. The amorphous efavirenz product can be produced by any method suitable to the composition. When necessary, solvent can be removed from compositions to yield the amorphous efavirenz product. In one further development of the invention, efavirenz-polymer-solvent (or a solvent / non-solvent blend) ...

Claims

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Application Information

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IPC IPC(8): A61K31/538A61K9/14
CPCA61K9/1617A61K9/1635A61K31/538A61K31/536A61K9/4866A61P9/00A61P31/18
Inventor DONEY, JOHN ALFRED
Owner ISP INVESTMENTS INC
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