Taxane particles and their use

Patent metadata

Field	Value
Publication number	US-9814685-B2
Application number	US-201615174505-A
Country	US
Kind code	B2
Filing date	Jun 6, 2016
Priority date	Jun 4, 2015
Publication date	Nov 14, 2017
Grant date	Nov 14, 2017

Abstract

Compositions are provided that include having at least 95% by weight of a taxane, or a pharmaceutically acceptable salt thereof, where the particles have a mean bulk density between about 0.050 g/cm 3 and about 0.15 g/cm 3 , and/or a specific surface area (SSA) of at least 18 m 2 /g, 20 m 2 /g, 25 m 2 /g, 30 m 2 /g, 32 m 2 /g, 34 m 2 /g, or 35 m 2 /g. Methods for making and using such compositions are also provided.

First claim

We claim:

1. A composition, comprising particles including at least 95% by weight of a taxane selected from the group consisting of paclitaxel and docetaxel, or a pharmaceutically acceptable salt thereof, wherein the particles have one or both of the following characteristics:
(i) a mean bulk density between about 0.050 g/cm 3 and about 0.15 g/cm 3 , and/or
(ii) have a specific surface area (SSA) of at least 18 m 2 /g; and
wherein the taxane particles include both agglomerated taxane particles and non-agglomerated taxane particles.

2. The composition of claim 1 , wherein the taxane is paclitaxel or a pharmaceutically acceptable salt thereof, and wherein the particles have a mean bulk density between about 0.050 g/cm 3 and about 0.12 g/cm 3 .

3. The composition of claim 1 , wherein the paclitaxel particles have a specific surface area (SSA) of at least 18 m 2 /g.

4. The composition of claim 1 , wherein the taxane is paclitaxel or a pharmaceutically acceptable salt thereof, and wherein the paclitaxel particles have a SSA of between about 22 m 2 /g and about 40 m 2 /g.

5. The composition of claim 2 , wherein at least 40% (w/w) of the paclitaxel is dissolved in 30 minutes or less in a solution of 50% methanol/50% water (v/v) at 37° and pH 7.0 in a USP II paddle apparatus operating at 75 RPM.

6. The composition of claim 1 , wherein the taxane is docetaxel or a pharmaceutically acceptable salt thereof, and wherein the particles have a mean bulk density between about 0.050 g/cm 3 and about 0.12 g/cm 3 .

7. The composition of claim 1 , wherein the taxane is docetaxel or a pharmaceutically acceptable salt thereof, and wherein the docetaxel particles have a SSA of at least 18 m 2 /g.

8. The composition of claim 7 , wherein the docetaxel particles have a SSA of between about 40 m 2 /g and about 50 m 2 /g.

9. The composition of claim 6 , wherein at least 20% (w/w) of the docetaxel is dissolved in 30 minutes or less in a solution of 15% methanol/85% water (v/v) at 37° and pH 7.0 in a USP II paddle apparatus operating at 75 RPM.

10. A composition, comprising:
(a) particles including at least 95% by weight of paclitaxel, wherein at least 40% (w/w) of the paclitaxel is dissolved in 30 minutes or less in a solution of 50% methanol/50% water (v/v) at 37° and pH 7.0 in a USP II paddle apparatus operating at 75 RPM, wherein the particles include both agglomerated paclitaxel particles and non-agglomerated paclitaxel particles; or
(b) at least 95% by weight of docetaxel, wherein at least 20% (w/w) of the docetaxel is dissolved in 30 minutes or less in a solution of 15% methanol/85% water (v/v) at 37° and pH 7.0 in a USP II paddle apparatus operating at 75 RPM, wherein the particles include both agglomerated paclitaxel particles and non-agglomerated paclitaxel particles.

11. The composition of claim 1 , wherein the particles have a mean particle size of between about 0.4 μm and about 1.2 μm.

12. The composition of claim 1 , wherein the composition comprises a suspension further comprising a pharmaceutically acceptable aqueous carrier.

13. The composition of claim 1 , wherein the particles comprise at least 98% by weight of the compound.

14. A method for treating a tumor, comprising administering to a subject with a tumor an amount effective to treat the tumor of the composition of claim 1 .

15. The method of claim 14 , wherein the tumor is selected from the group consisting of a breast tumor, an ovarian tumor, a lung tumor, a bladder tumor, a prostate tumor, a bone tumor, a stomach tumor and a pancreatic tumor.

16. The method of claim 14 , wherein the subject is a human subject.

17. The composition of claim 3 , wherein the particles have a mean particle size of between about 0.4 μm and about 1.2 μm.

18. The composition of claim 7 , wherein the particles have a mean particle size of between about 0.4 μm and about 1.2 μm.

Assignees

• Crititech Inc

Inventors

• Baltezor Michael
• Farthing Joseph
• Sittenauer Jake
• Espinosa Jahna
• Campbell Samuel
• Mcclorey Matthew
• Fischer Julia K
• Williams Mark D
• Clapp Gary E

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• B01J2/04

  in a gaseous medium {(if combined with suspending the material in a gas, e.g. fluidised beds B01J2/16)} · CPC title

• B01J3/008

  Processes carried out under supercritical conditions · CPC title

• A61K9/10 Primary

  Dispersions; Emulsions · CPC title

• B05B13/0278

  Arrangement or mounting of spray heads (B05B13/0207 takes precedence) · CPC title