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Nanoparticulate formulations of docetaxel and analogues thereof

A docetaxel and nanoparticle technology, which is applied in the fields of prostate cancer, lung cancer, ovarian cancer, and breast cancer treatment, can solve the problem of no description of docetaxel nanoparticle preparation, etc., and achieve the effect of rapid drug dissolution

Inactive Publication Date: 2008-04-09
ELAN PHRMA INT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

None of these patents describe nanoparticulate formulations of docetaxel or its analogs

Method used

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  • Nanoparticulate formulations of docetaxel and analogues thereof
  • Nanoparticulate formulations of docetaxel and analogues thereof
  • Nanoparticulate formulations of docetaxel and analogues thereof

Examples

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preparation example Construction

[0160] The preparation of povidone polymers results in polymers containing molecules of unequal chain length, and therefore of different molecular weights. The average molecular weight for each particular commercially available grade varies. Because it is difficult to directly determine the molecular weight of polymers, the most widely used method for classifying various molecular weights is the K-value method based on viscosity measurements. The K values ​​for the various grades of povidone polymers have a function representing the average molecular weight, which is obtained from viscosity measurements and calculated according to Fikentscher's formula.

[0161] The average weight (Mw) of molecular weights is determined by methods that measure the weight of individual molecules, such as light scattering. Table 1 provides molecular weight data for several commercially available povidone polymers, all of which are soluble.

[0162]While applicants do not wish to be bound by a ...

Embodiment 1

[0260] The purpose of this example was to prepare a nanoparticulate anhydrous docetaxel formulation.

[0261] Figure 1 shows a light micrograph of unmilled Docetaxel (anhydrous) (Camida Ltd.), showing that conventional non-nanoparticulate Docetaxel (anhydrous) has an average particle size of 212,060 nm, D50 is 175,530nm and D90 is 435,810nm.

[0262] Aqueous dispersion of 5% (w / w) Docetaxel (Camida Ltd.) with 1.25% (w / w) polyvinylpyrrolidone (PVP) K17 and 0.25% (w / w) sodium deoxycholate merge. Then to NanoMill _ 0.01 of this mixture was added to a 10 ml chamber (NanoMill Systems, King of Prussia, PA; see US Pat. No. 6,431,478), along with a 220 micron PolyMill _ Grinding media (Dow Chemical) (89% media loading). The mixture was milled at 2500 rpm for 180 minutes.

[0263] After milling, the particle size of the milled docetaxel particles was then measured in deionized distilled water using a Horiba LA 910 particle size analyzer. The mean particle size of the milled docet...

Embodiment 2

[0266] The purpose of this example was to prepare a nanoparticulate anhydrous docetaxel formulation.

[0267] Aqueous dispersion of 5% (w / w) anhydrous docetaxel with 1.25% (w / w) Tween _ 80 and 0.1% (w / w) lecithin were combined. Then in NanoMill _ 0.01 in a 10 ml chamber (NanoMill Systems, King of Prussia, PA), along with a 220 micron PolyMill _ Grinding media (Dow Chemical) (89% media loading) milled the mixture together. The mixture was milled at 5500 rpm for 60 minutes.

[0268] After milling, the particle size of the milled docetaxel particles was then measured in deionized distilled water using a Horiba LA 910 particle size analyzer. The mean particle size of the milled docetaxel particles was 166 nm, with a D50 of 147 nm and a D90 of 242 nm. Figure 3 shows a light micrograph of milled docetaxel.

[0269] This result indicates that stable nanoparticulate docetaxel formulations were successfully prepared with an average particle size of 166 nm.

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Abstract

Described are nanoparticulate docetaxel or analogue thereof compositions. The compositions, which comprise a nanoparticulate docetaxel or analogue thereof and at least one surface stabilizer, can be used in the treatment of cancer.

Description

technical field [0001] The present invention relates to a nanoparticulate composition of docetaxel and its analogs, a preparation method of the composition, and the nanoparticulate composition in the treatment of cancer, especially breast cancer, ovarian cancer, and prostate cancer. and use in lung cancer. Background technique [0002] A. Background on docetaxel and its analogs [0003] Diterpenes taxoids or taxanes are compounds that inhibit cell growth by preventing cell division and include docetaxel and paclitaxel. They are also known as antimitotic or antimicrotubule agents or mitotic inhibitors. [0004] Diterpene taxane-based compositions with anti-tumor and anti-leukemia activity and their uses are described in US Patent 5,438,072. US Patent 6,624,317 relates to the preparation of diterpene taxane conjugates for use in cancer therapy. The structure and numbering of the taxane ring system is shown in Figure 1A of Magnus US Patent 5,508,447 ("Magnus Patent"). The ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50
CPCA61K9/0019A61K9/146A61K31/337A61K9/145A61P35/00A61P35/02A61K9/50A61K9/08B82Y5/00
Inventor G·利沃赛德S·詹金斯E·利沃赛德
Owner ELAN PHRMA INT LTD
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