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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) that cannot be effectively used in patients because of their unacceptable toxicity or because of their unfavorable pharmacokinetic parameters Improvement is still an issue

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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