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Pharmaceutical composition for improved administration of HIV gp41-derived peptides,And its use in therapy

A composition and medicine technology, applied in the field of pharmaceutical compositions, can solve problems such as undisclosed

Inactive Publication Date: 2008-12-24
TRIMERIS INC (US)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, a drug containing a solution consisting of a mixture of a synthetic peptide (HIV fusion inhibitor) and a polyol such as PEG at a final concentration of not less than 5% by weight (e.g., weight / volume percentage) and not more than 75% by weight The composition has not been disclosed so far

Method used

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  • Pharmaceutical composition for improved administration of HIV gp41-derived peptides,And its use in therapy
  • Pharmaceutical composition for improved administration of HIV gp41-derived peptides,And its use in therapy

Examples

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Embodiment 1

[0026]In this example, a pharmaceutical composition according to the present invention is described, wherein T1249 (SEQ ID NO: 5, see US Patent No. 6,258,752) is used in several specific examples. However, it is understood (shown by the examples herein) that synthetic peptides other than T1249 (SEQ ID NO: 5) can be used in the pharmaceutical composition according to the invention, especially since such synthetic peptides (HIV fusion inhibiting peptides) share structural, biochemical, and functional characteristics. More specifically, these synthetic peptides all contain coiled-coil repeats of 7, which facilitate soluble intermolecular interactions in aqueous solutions containing the polyols described in detail in this application. Other shared structural, biochemical, and functional features include, but are not limited to, amino acid sequences containing one or more leucine zipper motifs, coiled-coil propensity, oligomerization propensity, and ability to inhibit transmission ...

Embodiment 2

[0040] In this example, illustrated is the unexpected effect that the use of the pharmaceutical composition as an injection solution according to the present invention can be obtained from the incidence and intensity when compared with previously known formulations of pharmaceutical compositions containing synthetic peptides. Reduced injection site reactions. Injection site reactions can be determined experimentally by administering the pharmaceutical composition to be tested in the form of an injectable aqueous formulation to rabbits by the subcutaneous route using standard models for injection site reactions known in the art. Typically, the injectable aqueous formulation, as a unit dose, will be injected at 4-5 sites per animal. Table 4 shows that when using an aqueous formulation containing about 100 mg of synthetic peptide but no polyol ("Formulation C"), the difference was observed when using an aqueous formulation containing approximately 100 mg of synthetic peptide and ...

Embodiment 3

[0052] From the narration of the present application, it is clear to those skilled in the art that due to the similarity in structure, function, and composition of such HIV fusion inhibitor peptides (as previously described in detail herein), the pharmaceutical composition according to the present invention can be It is composed of any one or more HIV fusion inhibitor peptides (for example, the concentration is not lower than 70mg / ml, more preferably not lower than 100mg / ml) and the final concentration is not lower than 10% and not higher than the weight of the pharmaceutical composition A solution composed of 50% polyol mixture is used as an injectable solution formulation. In that regard, T20 (SEQ ID NO: 4) was used as a synthetic peptide to be included in the pharmaceutical composition according to the present invention. Table 6 shows another illustrative example of a pharmaceutical composition according to the invention. This embodiment of the pharmaceutical composition c...

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Abstract

The present invention provides a pharmaceutical composition comprising a solution consisting of a mixture of a synthetic peptide and a polyol at a final concentration of not less than 70 mg / ml; wherein the synthetic peptide is an HIV fusion inhibitor, and wherein the final concentration of the polyol is Not less than 5% by weight and not more than 75% by weight of the pharmaceutical composition. Also provided is a unit dose pharmaceutical composition containing a synthetic peptide comprising an aqueous formulation consisting of a mixture of a synthetic peptide and a polyol at a final concentration of not less than 70 mg / ml; wherein the synthetic peptide is an HIV fusion inhibitor, and Wherein the final concentration of the polyol is not lower than 5% by weight and not higher than 75% by weight of the pharmaceutical composition. Further provided is a method of treating HIV infection by administering a pharmaceutical composition of the invention to an HIV-infected individual.

Description

technical field [0001] The present invention relates to a pharmaceutical composition composed of a mixture of a polymer and a synthetic peptide derived from HIV gp41. More particularly, the present invention comprises a pharmaceutical composition comprising a mixture of a polyol and a synthetic peptide having an amino acid sequence derived from the HR1 or HR2 region of HIV gp41. Background technique [0002] It is now known that cells can be infected by HIV through a fusion process that occurs between the cell membrane and the viral membrane. The generally accepted model for this process is that the viral coat glycoprotein complex (gp120 / gp41) binds to cell surface receptors on the target cell membrane. Following gp120 binding to cellular receptors (e.g., CD4 binding to chemokine co-receptors such as CCR-5 or CXCR-4), a conformational change within the gp120 / gp41 complex is induced allowing gp41 to insert into the target cell membrane and regulate membrane fusion . [000...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/74A61K38/00A61K39/00A61K39/12A61K39/21A61K47/30A61K47/32A61K47/34A61P31/18A61K47/10
Inventor 杰·邸大卫·海尔曼布赖恩·布雷
Owner TRIMERIS INC (US)