Nanoparticulate clopidogrel and aspirin combination formulations

A technology of granular clopidogrel and clopidogrel, applied in the field of nanoparticle clopidogrel and aspirin combined preparation, can solve problems such as difficult bioavailability

Inactive Publication Date: 2008-08-06
ELAN PHRMA INT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because clopidogrel is practically insoluble in water, it may not have significant bioavailability

Method used

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  • Nanoparticulate clopidogrel and aspirin combination formulations
  • Nanoparticulate clopidogrel and aspirin combination formulations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0184] The purpose of this example is to illustrate how to prepare the nanoparticulate clopidogrel / aspirin composition.

[0185] Aqueous dispersions of clopidogrel bisulfate can be combined with one or more surface stabilizers, followed by incorporation in NanoMill(R) 0.01 (NanoMill Systems, King of Prussia, PA; see eg US Pat. No. 6,431,478) for milling in a 10 ml chamber. The composition may be milled at a speed of 2500 for a suitable period of time, such as about 60 minutes.

[0186] The milled composition can be harvested and analyzed via microscopy. For example, Lecia DM5 000B and Lecia CTR 5000 light sources (Laboratory Instruments and Supplies Ltd., Ashbourne Co., Meath, Ireland) can be used for microscopy. Microscopic examination may reveal the presence of discrete clopidogrel nanoparticles.

[0187] The particle size of crushed clopidogrel microparticles was also measured in Milli Q Water with a Horiba LA-910 Particle Sizer (ParticularScience, Hatton Derbyshire, Eng...

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Abstract

The present invention relates to compositions comprising nanoparticulate clopidogrel and aspirin combinations or salts or derivatives thereof, which have improved clopidogrel bioavailability. The nanoparticulate clopidogrel microparticles and optionally the nanoparticulate aspirin microparticles of the composition have an effective average particle size of less than about 2000 nm, which is used for the prevention and treatment of lesions caused by platelet aggregation. Clopidogrel and aspirin microparticles can also be formulated as a controlled release polymer coated delivery system or a matrix delivery system.

Description

[0001] Cross references to related patent applications [0002] This application claims the benefit of US Patent Provisional Application No. 60 / 689,930, filed June 12, 2005, under 35 U.S.C. §119(e), which is incorporated herein by reference. field of invention [0003] In general, the present invention relates to compounds and compositions useful in the prevention and treatment of pathological conditions caused by platelet aggregation. More particularly, the present invention relates to nanoparticulate clopidogrel, or a salt or derivative thereof, in combination with aspirin (optionally in nanoparticulate form) (also referred to herein as "nanoparticle clopidogrel and aspirin combination") and compositions comprising the same Compositions. The effective average particle size of the nanoparticulate clopidogrel and optionally aspirin in the combination composition can be less than about 2000 nm. Clopidogrel and / or aspirin microparticles may also be coated with any of a variet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4365A61K31/60A61P9/10
CPCA61K9/145A61K9/146A61K9/2077A61K9/5084A61K31/4365A61K31/4743A61K31/60A61K45/06A61P7/02A61P9/00A61P9/10A61K2300/00B82B3/00H01J1/30
Inventor S·詹金斯G·G·利弗西奇
Owner ELAN PHRMA INT LTD
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