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Nanoparticle dispersion containing lactam compound

A technology of lactam compounds and nanoparticles, which can be used in medical preparations containing active ingredients, organic active ingredients, drug combinations, etc., and can solve problems such as limiting the maximum dose of medicinal active ingredients.

Inactive Publication Date: 2009-04-22
ELAN PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of polyoxyethylated castor oil may have drawbacks such as the possibility of limiting the maximum dose of the pharmaceutically active ingredient administered to the patient

Method used

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  • Nanoparticle dispersion containing lactam compound
  • Nanoparticle dispersion containing lactam compound
  • Nanoparticle dispersion containing lactam compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

Example 1 - containing 5% by weight of lactam compound Ia and 2% by weight of Pluronic TM Preparation of Nanoparticle Dispersion of F108 Surfactant

[0085] Prepare 5% by weight Pluronic in deionized water TM A stock solution of F 108 surfactant (BASF Corp.) was filtered through a 0.2 micron filter. to NanoMill in the order listed TM The following materials were added to the jacketed 10-mL milling chamber of the -01 mill (Elan Pharma International Limited, Ireland): 5.43 g of 0.5 mm polystyrene milling media, 0.233 g of the lactam compound of formula Ia , 1.865mL of filtered containing 5% by weight Pluronic TM A solution of F108 surfactant, and 2.563 mL of deionized water. Assemble the mill and equilibrate the milling chamber to a temperature of 4°C-5°C by means of a circulating constant temperature water bath. The contents were milled for 2 minutes at 1800 rpm, then 43 minutes at 5500 rpm. The resulting nanoparticle dispersion was separated from the polystyrene millin...

Embodiment 2

Example 2 - Preparation of nanoparticle dispersion containing 10% by weight of lactam compound Ia, 1.8% by weight of polyvinylpyrrolidone (PVP) and 0.2% by weight of sodium deoxycholate

[0086] A stock solution of 4% by weight PVP (-10,000MW) and 0.4% by weight sodium deoxycholate was prepared in water for injection and filtered through a 0.45 micron filter. to NanoMill in the order listed TM -01 The following were added to the jacketed 50-mL milling chamber of the mill: 26.1 g of 0.5 mm polystyrene milling media, 2.25 g of the lactam compound of Formula Ia, 10.1 g of filtered PVP K13-19 Polymer stock solution and 10.1 g of filtered sodium deoxycholate stock solution. Assemble the mill and equilibrate the milling chamber to a temperature of 4°C-5°C by means of a circulating constant temperature water bath. The contents were milled for 2 minutes at 1800 rpm, then 58 minutes at 2930 rpm. The resulting nanoparticle dispersion was separated from the polystyrene milling beads by...

Embodiment 3

Example 3 - containing 5% by weight of lactam compound Ia and 2% by weight of Pluronic TM Preparation of Nanoparticle Dispersion of F108 Surfactant

[0089] Prepare 5% by weight Pluronic in Water for Injection TM A stock solution of F108 surfactant was filtered through a 0.22 micron filter. to NanoMill in the order listed TM In the jacketed 100-mL milling chamber of the -01 mill, the following were added: 48.86 g of 0.5 mm polystyrene milling media, 2.11 g of the lactam compound of Formula Ia, 16.78 g of 5% by weight Pluronic TMA filtered solution of F108 surfactant and 23.05 g of WFI. Assemble the mill and equilibrate the milling chamber to a temperature of 4°C-5°C by means of a circulating constant temperature water bath. The contents were milled for 2 minutes at 1800 rpm, then 88 minutes at 2140 rpm. The resulting nanoparticle dispersion was separated from the polystyrene milling beads by aspiration into a 3-mL Sub-Q syringe fitted with a 26 gauge 5 / 8 inch needle and ...

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Abstract

Disclosed is a nanoparticle dispersion comprising nanoparticles dispersed in an aqueous medium in the presence of at least one stabilizer. The nanoparticles comprise at least lactam compound of formula (I): wherein R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, and Q are defined herein. A method is provided of the parenteral administration of the nanoparticle dispersion as a treatment for cancer or another proliferative disease. Also, a solid nanoparticulate composition comprising the nanoparticles of the lactam compound, and a method of administration are disclosed.

Description

field of invention [0001] The present invention generally relates to compositions comprising nanoparticles of one or more lactam compounds. These compositions are suitable for the treatment of tumors. Methods of using these compositions to treat cancer or other proliferative diseases are also provided. Background of the invention [0002] Epoxypolytubulin is a macrolide compound used in the pharmaceutical field. For example, epoxy polytubulin A and B are naturally occurring compounds that can be isolated from certain microorganisms and have the structure: Epoxy Polytubulin A R=H epoxy polytubulin B R = methyl [0003] Epoxypolytubulin is known to produce microtubule-stabilizing effects similar to and thus exhibit cytotoxic activity against rapidly proliferating cells e.g. arising in cancer or other hyperproliferative cellular diseases (see Angew. Chem. Int. Ed. Engl., Vol. 35, No. 13 / 14 1996 and D.M. Bollag, Exp. Opin. Invest. Drugs, 6(7):867-873, 1997). [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/427A61K9/00A61K9/14A61K9/51
CPCA61K9/0019A61K9/145A61K9/146A61K31/427A61P1/00A61P1/16A61P11/02A61P13/12A61P17/00A61P17/06A61P19/02A61P19/10A61P21/00A61P25/16A61P25/28A61P27/02A61P31/12A61P35/00A61P7/06A61P9/06A61P9/10A61P3/10
Inventor M·K·弗兰基尼T·A·哈比E·利弗塞奇
Owner ELAN PHARM INC