US2016158150A1PendingUtilityA1

Manufacture of Pharmaceutical Compositions

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Assignee: VECTURA LTDPriority: Sep 15, 2003Filed: Dec 15, 2015Published: Jun 9, 2016
Est. expirySep 15, 2023(expired)· nominal 20-yr term from priority
Inventors:David Alexander Vodden MortonJohn Staniforth
A61K 31/55A61K 9/1623A61K 9/50A61K 9/16A61K 31/473A61K 31/5513A61K 9/0075A61K 31/727B02C 19/06A61K 9/008A61K 9/1617A61K 9/1694
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 use in a pharmaceutical composition for pulmonary inhalation, the method comprising jet milling active particles in the presence of particles of additive material and, optionally, air or a compressible gas or fluid. 
     
     
         2 . A method as claimed in  claim 1 , wherein the additive material comprises an amino acid, a metal stearate or a phospholipid. 
     
     
         3 . A method as claimed in  claim 2 , wherein the additive material comprises one or more of leucine, isoleucine, lysine, valine, methionine, phenylalanine. 
     
     
         4 . A method as claimed in  claim 3 , wherein the additive material comprises leucine and preferably 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 any one of the preceding claims, wherein the jet milling is carried out at an inlet pressure of between 0.1 and 3 bar. 
     
     
         8 . A method as claimed in any one of  claims 1 - 6 , wherein the jet milling is carried out at an inlet pressure of between 3 and 12 bar. 
     
     
         9 . A method as claimed in any one of the preceding claims, wherein at least 90% by volume of the active particles are less than 20 μm in diameter prior to jet milling. 
     
     
         10 . A method as claimed in any one of the preceding claims, wherein at least 90% by volume of the additive particles are less than 20 μm in diameter prior to jet milling. 
     
     
         11 . A method as claimed in any one of the preceding claims, wherein jet milling is carried out at temperatures below room temperature. 
     
     
         12 . A method as claimed in  claim 11 , wherein jet milling is carried out at a temperature below 10° C. and preferably below 0° C. 
     
     
         13 . A method as claimed in any one of the preceding claims, wherein carrier particles are also jet milled 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, preferably less than 20 μm and more preferably less than 10 μm. 
     
     
         16 . Composite active particles for use in a pharmaceutical composition made using a method as claimed in any one of the preceding claims. 
     
     
         17 . Composite active particles as claimed in  claim 16 , for pulmonary inhalation. 
     
     
         18 . Composite active particles as claimed in either of  claims 16  and  17 , wherein the additive material forms a coating on the surface of the additive particles. 
     
     
         19 . Composite active particles as claimed in  claim 18 , wherein the coating is a discontinuous coating. 
     
     
         20 . Composite active particles as claimed in either of  claims 18  and  19 , wherein the coating of additive material is not more than 1 μm in thickness. 
     
     
         21 . Composite active particles as claimed in any one of  claims 16 - 20 , having an MMAD of not more than 10 μm. 
     
     
         22 . Composite active particles as claimed in  claim 21 , having an MMAD of not more than 5 μm, not more than 3 μm, not more than 2 μm, or not more than 1 μm. 
     
     
         23 . Composite active particles as claimed in any one of  claims 16 - 22 , wherein at least 90% by weight of the composite active particles have a diameter of not more than 10 μm. 
     
     
         24 . Composite active particles as claimed in  claim 23 , wherein at least 90% by weight of the particles have a diameter of not more than 5 μm, not more than 3 μm, or not more than 1 μm. 
     
     
         25 . A pharmaceutical composition comprising composite active particles as claimed in any one of  claims 16 - 24 . 
     
     
         26 . A composition as claimed in  claim 25 , wherein the composition is for pulmonary inhalation. 
     
     
         27 . A composition as claimed in either of  claims 25  and  26 , wherein the composition is a dry powder composition. 
     
     
         28 . A composition as claimed in  claim 27 , wherein the composition further comprises carrier particles. 
     
     
         29 . A composition as claimed in any one of  claims 25 - 28 , 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%, at least 85%, or at least 90%. 
     
     
         31 . A composition as claimed in any one of  claims 25 - 28 , 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%, at least 80%, or at least 85%. 
     
     
         33 . A dry powder inhaler containing a composition as claimed in any one of  claims 25 - 32 . 
     
     
         34 . Use of an additive material as a milling aid in the jet milling of an active material.

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