Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF5 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text describes a new compound (I) that can be used to treat or prevent HIV infection. This compound is designed to be long-acting, meaning it can be administered less frequently than traditional medications. This reduces the burden of pill-taking and improves patient compliance. In the examples provided, the compound is shown to be effective in reducing the amount of HIV in the body and maintaining therapy's effectiveness over a longer period of time. The compound can be administered through a subcutaneous or intramuscular injection.

Problems solved by technology

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.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Pharmaceutical Compositions
  • Pharmaceutical Compositions
  • Pharmaceutical Compositions

Examples

Experimental program
Comparison scheme
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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Fractionaaaaaaaaaa
Fractionaaaaaaaaaa
Timeaaaaaaaaaa
Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/4985A61K31/505
CPCA61K31/505A61K31/4985A61P31/00A61P31/18A61K9/16
Inventor MUNDHRA, DEEPAK B.PAN, RENNAN
Owner VIIV HEALTHCARE CO
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com