Pharmaceutical composition, preparation and uses thereof

A technology of composition and medicine, applied in the field of pharmaceutical composition, preparation and use

Inactive Publication Date: 2016-03-16
キュラダイムソシエテパールアクシオンサンプリフィエ
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] It is evident from the prior art and despite the long-standing pharmaceutical demand that compounds (including therapeutic, prophylactic and diagnostic compounds) t

Method used

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  • Pharmaceutical composition, preparation and uses thereof
  • Pharmaceutical composition, preparation and uses thereof
  • Pharmaceutical composition, preparation and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Example 1: Synthesis of liposomes as biocompatible nanoparticle n°1

[0079] Preparation of liposomes using the lipid membrane rehydration method:

[0080] a) Lipids were dissolved in chloroform. Chloroform was finally evaporated under nitrogen flow. Rehydration of the lipid film was performed at 50° C. with HEPES 20 mM pH 7.4 and NaCl 140 mM so that the lipid concentration was 5 mM.

[0081] The following lipid compositions were used to prepare charged liposomes: DPPC (dipalmitoylphosphatidylcholine): 86% moles; MPPC (monopalmitoylphosphatidylcholine): 10% moles; DSPE-PEG (di Stearoylphosphatidylethanolamine-[methoxy(polyethylene glycol)-2000]): 4 mole%.

[0082] b) Six thawing cycles were then performed by successively placing the sample in liquid nitrogen and in a water bath regulated at 50°C.

[0083] c) Under controlled temperature and pressure, using a hot barrel extruder (LIPEX TM extruder, NorthernLipids) to calibrate the size of the liposomes. In all case...

Embodiment 2

[0087] Example 2: A method that allows for a dose reduction of at least 10% of a therapeutic compound to be administered in a subject with equivalent efficacy in said subject.

[0088] The pharmaceutical composition according to claim 1 is administered in xenografted nude mice in such a manner that said pharmaceutical composition comprises biocompatible nanoparticles and is capable of generating electrons and / or when exposed to ionizing radiation such as X-rays or high-energy photon-activatable oxide nanoparticles for anti-cancer therapy (used as "the compound" or "drug compound"):

[0089] a) administering biocompatible nanoparticle to each nude mouse (by intravenous injection);

[0090] b) between greater than 5 minutes and 72 hours after step a), administer (by intravenous injection) the therapeutic compound in each mouse of step a) at a dose lower (10%) than the currently used dose;

[0091] c) Measuring the concentration of the therapeutic compound in blood or plasma sam...

Embodiment 3

[0094] Example 3: Synthesis of liposomes as biocompatible nanoparticle n ° 2

[0095] Preparation of liposomes using the lipid membrane rehydration method:

[0096] a) Lipids were dissolved in chloroform. Chloroform was finally evaporated under nitrogen flow. Rehydration of the lipid film was performed at 60° C. with HEPES 20 mM pH 7.4 and NaCl 140 mM so that the lipid concentration was 25 mM.

[0097] The following lipid compositions were used to prepare charged liposomes: DPPC (dipalmitoylphosphatidylcholine) 62% moles; HSPC (hydrogenated soybean phosphatidylcholine) 20% moles; CHOL (cholesterol) 16% moles ; POPS (1-palmitoyl-2-oleoylphosphatidylserine) 1% mole; DSPE-PEG (distearoylphosphatidylethanolamine-[methoxy(polyethylene glycol)-2000]) 1% mole.

[0098] b) Six thawing cycles were then carried out by successively placing the sample in liquid nitrogen and in a water bath regulated at 60°C.

[0099] c) Under controlled temperature and pressure, using a hot barrel ext...

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Abstract

The present invention relates to a pharmaceutical composition comprising the combination of (i) a biocompatible nanoparticle and of (ii) a pharmaceutical compound of interest, to be administered to a subject in need of such a compound of interest, wherein the nanoparticle potentiates the compound of interest efficiency. The longest dimension of the biocompatible nanoparticle is typically between about 4 and about 500 nm, and its absolute surface charge value is of at least 10 m V (|10 m V|). The invention also relates to such a composition for use for administering the compound of interest in a subject in need thereof, wherein the nanoparticle and the compound of interest are to be administered in said subject between more than 5 minutes and about 72 hours one from each other.

Description

technical field [0001] The present invention relates to a pharmaceutical composition comprising a combination of (i) biocompatible nanoparticles and (ii) a compound of interest to be administered to a subject in need of such a compound, wherein the nanoparticles enhance Efficacy of the compound. Biocompatible nanoparticle typically has a longest dimension of about 4 to about 500 nm and an absolute surface charge value of at least 10 mV (|10 mV|). [0002] The present invention also relates to such compositions for administering a compound of interest to a subject in need thereof, wherein the nanoparticles and the compound of interest are administered sequentially in said subject, usually separated by more than 5° from each other. minutes to about 72 hours. [0003] The combined and usually sequential administration of the biocompatible nanoparticle and the target compound to a subject maintains the drug of the target compound when compared to the drug benefit and toxicity in...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K9/127A61K9/14A61K9/00
CPCA61K9/5115A61K31/704A61K9/1271A61K9/0014A61K9/14Y10S977/773A61K9/127A61P35/00A61P41/00
Inventor 阿格尼丝·波迪艾尔劳伦特·莱维马里-艾迪斯·梅尔奥德蕾·达尔蒙马蒂厄·热尔曼
Owner キュラダイムソシエテパールアクシオンサンプリフィエ
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