Pharmaceutical Compositions

a technology of compositions and pharmaceuticals, applied in the field of compounded drugs, can solve the problems of multiple drug resistant strains of hiv, patient non-compliance, and well-known patient non-compliance, and achieve the effect of reducing the burden of medication (pill) or difficulty in patient compliance, and maintaining the efficacy of therapy

Inactive Publication Date: 2013-07-04
VIIV HEALTHCARE CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0079]The parenteral pharmaceutical composition comprising compound (I) of the present invention is long-acting. Accordingly, the composition is useful for the treatment or prevention of HIV infection with administration at long time intervals, compared with conventional compositions or with other compounds similar to compound (I) in chemical structure. The compositions of the present invention can be intermittently administered to a patient, e.g., once per week, once per month, once per every 2 months, or one per every 3 months. Therefore, the compositions of the present invention and an administration by subcutaneous (SC) or intramuscular (IM) injection using the same c...

Problems solved by technology

Patient non-compliance is a well known problem accompanying the complex HIV treatment regimens.
Patient non-compliance is a crit...

Method used

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  • Pharmaceutical Compositions
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Examples

Experimental program
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Effect test

example 1

Pharmaceutical Composition

[0081]

TABLE 1Composition of a compound of formula (I) Injectable SuspensionQuantityComponent(mg / mL)FunctionCompound of Formula (I)200.0ActiveMannitol45.0Tonicity agentPolysorbate 2020.0Wetting agentPolyethylene Glycol (PEG) 335020.0StabilizerWater for InjectionQS to 1.0 mLSolvent

[0082]Manufacturing Process

[0083]A compound of formula (I), mannitol, polysorbate 20, PEG 3350, and water for injection were compounded and milled using a wet bead mill. The resulting suspension was filled into 3 mL, USP Type I glass vials at a fill volume of 1.5 mL, the vials are stoppered and sealed, and then terminally sterilized by gamma irradiation.

example 2

Particle Size

[0084]A sample of a compound of formula (I) injectable suspension prepared by the process as described in Example 1 was irradiated by gamma irradiation at 29.9-31.5 kGy dose. The milling time was 5 hours. The particle size determined by laser diffraction technique is the following:

[0085]×10=75 nm

[0086]×50=157 nm

[0087]×90=646 nm

[0088]×50 of less than 200 nm was achieved.

example 3

Gamma Irradiation

[0089]A sample of a compound of formula (I) injectable suspension prepared by the process as described in Example 1 was irradiated by gamma irradiation at 29.9-31.5 kGy dose. Samples pre gamma irradiation and post gamma irradiation were tested for drug related impurities by HPLC.

Total Drug Related Impurities, % area / areaPre Gamma Irradiation0.19Post Gamma Irradiation0.16

[0090]The formulation is stable upon gamma irradiation.

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Abstract

The present Invention relates to pharmaceutical compositions of (3S,11aR)-N-[(2,4-difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide, useful in the treatment or prevention of Human Immunodeficiency Virus (HIV) infections.

Description

BACKGROUND OF THE INVENTION[0001]WO 2006 / 116764 discloses a class of compounds useful in the treatment of HIV infection and AIDS. There is a continuing need for pharmaceutical compositions suitable for treatment over a long period of time. We have discovered pharmaceutical compositions of (3S,11aR)-N-[(2,4-difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide that are long-acting and therefore suitable for administration to patients in the treatment of HIV infections.[0002]Patient non-compliance is a well known problem accompanying the complex HIV treatment regimens. Patient non-compliance is a critical problem in the treatment of HIV because such non-compliance may lead to the emergence of multiple-drug resistant strains of HIV.[0003]The present invention addresses the issue of non-compliance by formulating (3S,11aR)-N-[(2,4-difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-oxazolo[3...

Claims

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Application Information

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IPC IPC(8): A61K31/4985A61K31/505
CPCA61K31/505A61K31/4985A61P31/00A61P31/18A61K9/16
Inventor MUNDHRA, DEEPAK B.PAN, RENNAN
Owner VIIV HEALTHCARE CO
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