Processes for making lactose utilizing pre-classification techniques and pharmaceutical formulations formed therefrom

Patent metadata

Field	Value
Publication number	US-9365905-B2
Application number	US-81589006-A
Country	US
Kind code	B2
Filing date	Feb 6, 2006
Priority date	Feb 10, 2005
Publication date	Jun 14, 2016
Grant date	Jun 14, 2016

Abstract

A process for forming lactose suitable for use in a pharmaceutical formulation comprises providing a plurality of lactose particles containing no more than 10% w/w of lactose particles having a volume average particle size of about 70 microns or less; milling the plurality of lactose particles to yield a plurality of milled lactose particles with an average particle size, (D50), ranging from about 50 microns to about 100 microns; and classifying the plurality of milled lactose particles into at least two fractions comprising a fine fraction and a coarse fraction wherein the fine fraction has an average particle size, (D50), ranging from about 3 microns to about 50 microns, and the coarse fraction has an average particle size, (D50), ranging from about 40 microns to about 250 microns.

First claim

That which is claimed is:

1. A process for forming lactose composition suitable for use in a pharmaceutical formulation, said process comprising:
providing a plurality of lactose particles containing no more than 10% w/w of lactose particles having a volume average particle size of about 70 microns or less, wherein said plurality of lactose particles are present as crystalline lactose;
milling the plurality of lactose particles to yield a plurality of milled lactose particles with an average particle size, (D50), ranging from about 50 microns to about 100 microns;
classifying said plurality of milled lactose particles into at least two fractions comprising a fine fraction and a coarse fraction wherein the fine fraction has an average particle size, (D50), ranging from 10 microns to 30 microns, and the coarse fraction has an average particle size, (D50), ranging from about 40 microns to about 250 microns; and
combining a portion of the coarse fraction with a portion of the fine fraction to form a lactose composition consisting of the fine fraction and the coarse fraction;

wherein said step of providing a plurality of lactose particles containing no more than 10% w/w of lactose particles having a volume average particle size of about 70 microns or less comprises obtaining said plurality of lactose particles by classifying crystalline lactose into two fractions comprising: (i) a fine fraction and (ii) said plurality of lactose particles containing no more than 10% w/w of lactose particles having a volume average particle size of about 70 microns or less.

2. The process according to claim 1 , wherein the lactose is selected from the group consisting of anhydrous lactose, lactose monohydrate, and combinations thereof.

3. The process according to claim 1 , further comprising combining at least one medicament with a lactose composition to form a pharmaceutical formulation, the lactose composition comprising from 0 to 100 percent by weight of the coarse fraction and from 0 to 100 percent by weight of the fine fraction.

4. The process according to claim 1 , further comprising combining the lactose composition with at least one medicament to form a pharmaceutical formulation.

5. The process according to claim 1 , further comprising combining: (i) from 0 to 100 percent by weight of the coarse fraction, (ii) from 0 to 100 percent by weight of the fine fraction, and (iii) at least one medicament to form a pharmaceutical formulation.

6. The process according to claim 3 , wherein the pharmaceutical formulation is a dry powder pharmaceutical formulation suitable for inhalation.

7. The process according to claim 3 , wherein the at least one medicament comprises at least one beta agonist.

8. The process according to claim 7 , wherein the at least one beta agonist comprises salmeterol xinafoate.

9. The process according to claim 7 , wherein the at least one beta agonist comprises salbutamol sulphate.

10. The process according to claim 3 , wherein the at least one medicament comprises at least one anti-inflammatory steroid.

11. The process according to claim 10 , wherein the at least one anti-inflammatory steroid comprises fluticasone propionate.

12. The process according to claim 3 , wherein the at least one medicament comprises at least one beta agonist and at least one anti-inflammatory steroid.

13. The process according to claim 12 , wherein the at least one beta agonist comprises salmeterol xinafoate and the at least one anti-inflammatory steroid comprises fluticasone propionate.

14. The process according to claim 3 , wherein the at least one medicament is selected from the group consisting of albuterol sulphate, salmeterol xinafoate, fluticasone propionate, beclomethasone dipropionate, and combinations thereof.

15. The process according to claim 3 , wherein said pharmaceutical formulation further comprises at least one additional excipient.

Assignees

• Newman Stephen
• Damhuis Rudolf Johannes
• Dmv Fonterra Excipients Technology Gmbh
• Glaxo Group Ltd

Inventors

• Newman Stephen
• Damhuis Rudolf Johannes

Classifications

• A61P11/00

  Drugs for disorders of the respiratory system · CPC title

• C07H3/00

  Compounds containing only hydrogen atoms and saccharide radicals having only carbon, hydrogen, and oxygen atoms (preparation by hydrolysis of di-or polysaccharides C13; separation or purification of sucrose, glucose, fructose, lactose or maltose C13) · CPC title

• A61K9/0075

  for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles · CPC title

• C13K5/00 Primary

  Lactose · CPC title

• A61K31/715

  Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters · CPC title