US2012138056A1PendingUtilityA1

Dry powder composition comprising co-jet milled particles for pulmonary inhalation

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Assignee: MORTON DAVIDPriority: Sep 15, 2003Filed: Dec 27, 2011Published: Jun 7, 2012
Est. expirySep 15, 2023(expired)· nominal 20-yr term from priority
Inventors:David Alexander Vodden MortonJohn Staniforth
A61K 9/16A61K 9/0075A61K 31/5513A61K 31/473A61K 31/55A61K 9/1623A61K 9/008A61K 9/1694A61K 9/1617A61K 31/727B02C 19/06A61K 9/50
62
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Claims

Abstract

The present invention relates to particles and to methods of making particles. In particular, the invention relates to methods of making composite active particles comprising a pharmaceutically active material for pulmonary inhalation, the method comprising a jet milling process.

Claims

exact text as granted — not AI-modified
1 . A method for making composite active particles for pulmonary inhalation, the method comprising the step of jet milling active particles in the presence of particles of additive material. 
     
     
         2 . A method as claimed in  claim 1 , wherein the additive material is selected from the group consisting of: an amino acid, a metal stearate and a phospholipid. 
     
     
         3 . A method as claimed in  claim 2 , wherein the additive material is selected from the group consisting of: leucine, isoleucine, lysine, valine, methionine, phenylalanine, and a combination of any of the foregoing. 
     
     
         4 . A method as claimed in  claim 3 , wherein the additive material comprises one of the following: leucine and L leucine. 
     
     
         5 . A method as claimed in  claim 2 , wherein the additive material comprises magnesium stearate. 
     
     
         6 . A method as claimed in  claim 2 , wherein the additive material comprises lecithin. 
     
     
         7 . A method as claimed in  claim 1 , wherein the step of jet milling is carried out at an inlet pressure of between 0.1 and 3 bar. 
     
     
         8 . A method as claimed in  claim 1 , wherein the step of jet milling is carried out at an inlet pressure of between 3 and 12 bar. 
     
     
         9 . A method as claimed in  claim 1 , wherein at least 90% by volume of the active particles are less than 20 μm in diameter prior to the step of jet milling. 
     
     
         10 . A method as claimed in  claim 1 , wherein at least 90% by volume of the additive particles are less than 20 μm in diameter prior to the step of jet milling. 
     
     
         11 . A method as claimed in  claim 1 , wherein the step of jet milling is carried out at temperatures below room temperature. 
     
     
         12 . A method as claimed in  claim 11 , wherein the step of jet milling is carried out at a temperature below 10° C. 
     
     
         13 . A method as claimed in  claim 1 , wherein the step of jet milling further comprises jet milling carrier particles with the active particles and the particles of additive material. 
     
     
         14 . A method as claimed in  claim 13 , wherein the carrier particles have a particle size of at least 20 μm. 
     
     
         15 . A method as claimed in  claim 13 , wherein the carrier particles have a particle size of less than 30 μm. 
     
     
         16 . A pharmaceutical composition comprising composite active particles prepared in accordance with the method as claimed in  claim 1 . 
     
     
         17 . The pharmaceutical composition of  claim 16 , wherein said composition is for pulmonary inhalation. 
     
     
         18 . The pharmaceutical composition of  claim 16 , wherein the additive material forms a coating on the surface of the composite particles. 
     
     
         19 . The pharmaceutical composition of  claim 18 , wherein the coating is a discontinuous coating. 
     
     
         20 . The pharmaceutical composition of  claim 18 , wherein the coating of additive material is not more than 1 μm in thickness. 
     
     
         21 . The pharmaceutical composition of  claim 16 , wherein said composite active particles have an MMAD of not more than 10 μm. 
     
     
         22 . The pharmaceutical composition of  claim 21 , wherein said composite active particles have an MMAD of not more than 5 μm. 
     
     
         23 . The pharmaceutical composition of  claim 16 , wherein at least 90% by weight of the composite active particles have a diameter of not more than 10 μm. 
     
     
         24 . The pharmaceutical composition of  claim 23 , wherein at least 90% by weight of the particles have a diameter of not more than 5 μm. 
     
     
         25 - 26 . (canceled) 
     
     
         27 . A composition as claimed in  claim 16 , wherein the composition is a dry powder composition. 
     
     
         28 . A composition as claimed in  claim 16 , wherein the composition further comprises carrier particles. 
     
     
         29 . A composition as claimed in,  claim 16 , wherein the composition has a FPF(ED) of at least 70%. 
     
     
         30 . A composition as claimed in  claim 29 , wherein the FPF(ED) is at least 80%. 
     
     
         31 . A composition as claimed in  claim 16 , wherein the composition has a FPF(MD) of at least 60%. 
     
     
         32 . A composition as claimed in  claim 29 , wherein the FPF(MD) is at least 70%. 
     
     
         33 . A dry powder inhaler containing a composition as claimed in  claim 16 . 
     
     
         34 . (canceled) 
     
     
         35 . A method as claims in  claim 1 , wherein the step of jet milling active particles is carried out in the presence of particles of additive material and one of the following: air, compressible gas and fluid. 
     
     
         36 . A method according to  claim 11 , wherein the step of jet milling is carried out at a temperature below 0° C. 
     
     
         37 . A method as claimed in  claim 13 , wherein the carrier particles have a particle size of less than 20 μm. 
     
     
         38 . A method as claimed in  claim 13 , wherein the carrier particles have a particle size of less than 10 μm. 
     
     
         39 . A pharmaceutical composition as claimed in  claim 21 , wherein said composite active particles have an MMAD of not more than 1 μm. 
     
     
         40 . A pharmaceutical composition as claimed in  claim 23 , wherein at least 90% by weight of the particles have a diameter of not more than 1 μm. 
     
     
         41 . A composition as claimed in  claim 29 , wherein the FPF(ED) is at least 90%. 
     
     
         42 . A composition as claimed in  claim 29 , wherein the FPF(MD) is at least 85%.

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