Details for Patent: 9,345,664

Title:	Process for preparing a medicament
Abstract:	The present invention provides a process for preparing a particulate medicament that has greater homogeneity and a lower adhesion between the particles of the active ingredient and the carrier. The process comprises the steps of: (a) combining a pharmaceutically active ingredient in the form of an agglomerate of primary particles having an agglomerate particle size such that the agglomerate is capable of passing through a sieve having a mesh of 50-3000 .mu.m with a pharmaceutically acceptable particulate carrier, and (b) mixing the resultant material in a mixer to break up the agglomerate into primary particles dispersed in the pharmaceutically acceptable particulate carrier such that 90% or more of the pharmaceutically active ingredient exists as primary particles having a particle size of 50 .mu.m or less.
Inventor(s):	Zeng; Xian-Ming (Surrey, GB), Tee; Sean Kee (London, GB)
Assignee:	NORTON HEALTHCARE LTD (GB)
Filing Date:	Sep 01, 2004
Application Number:	10/594,473
Claims:	1. A process for preparing a dry powder inhaler containing an inhalable medicament comprising the steps of: (a) forming a plurality of loose agglomerates of a pharmaceutically active ingredient by passing the pharmaceutically active ingredient through a sieve having a mesh of 50-3000 .mu.m, wherein the loose agglomerates are not spheronized; (b) combining the plurality of loose agglomerates obtained from step (a) with a pharmaceutically acceptable particulate carrier; (c) mixing the resultant material from step (b) in a mixer outside of an inhaler to break up the loose agglomerates into primary particles of the pharmaceutically active ingredient and to disperse the primary particles in the pharmaceutically acceptable particulate carrier such that 90% or more of the pharmaceutically active ingredient has a particle size of 50 .mu.m or less to provide the inhalable medicament; and (d) filling the inhalable medicament from step (c) into the reservoir of a dry powder inhaler. 2. A process as claimed in claim 1, wherein the sieve used in step (a) has a mesh of 250-1000 .mu.m. 3. A process as claimed in claim 1, wherein the pharmaceutically active ingredient is an anti-inflammatory steroid and/or a bronchodilator. 4. A process as claimed in claim 1, wherein the pharmaceutically active ingredient is budesonide, formoterol or etiprednol. 5. A process as claimed in claim 1, wherein the pharmaceutically acceptable particulate carrier is lactose. 6. A process as claimed in claim 5, wherein the pharmaceutically acceptable particulate carrier is alpha-lactose monohydrate. 7. A process as claimed in claim 1, wherein the reservoir is the reservoir of a multidose dry powder inhaler. 8. A process as claimed in claim 1, wherein the reservoir is defined by a capsule. 9. A process as claimed in claim 8, wherein the capsule, when filled, contains a unit dose of active ingredient. 10. A process as claimed in claim 1, wherein the carrier is a classified carrier that is passed through a mesh with a mesh size of 90 .mu.m and collected on a mesh with a mesh size of 63 .mu.m. 11. A process as claimed in claim 1, wherein 90% or more of the pharmaceutically active ingredient in the inhalable medicament provided by step (c) has a particle size of 20 .mu.m or less. 12. A process as claimed in claim 11, wherein 90% or more of the pharmaceutically active ingredient in the inhalable medicament provided by step (c) has a particle size of 10 .mu.m or less. 13. A process as claimed in claim 11, wherein 95% or more of the pharmaceutically active ingredient in the inhalable medicament provided by step (c) has a particle size of between about 0.5-5 .mu.m. 14. A process as claimed in claim 5, wherein the particle size of lactose is between 40 and 150 .mu.m. 15. A process as claimed in claim 14, wherein the particle size of lactose is between 40 and 90 .mu.m. 16. A process for preparing a dry powder inhaler containing an inhalable medicament comprising the steps of: (a) forming a plurality of loose agglomerates of a pharmaceutically active ingredient by passing the pharmaceutically active ingredient through a sieve having a mesh of 50-3000 .mu.m, wherein the loose agglomerates are not spheronized; (b) combining the plurality of loose agglomerates obtained from step (a) with a pharmaceutically acceptable particulate carrier; (c) mixing the resultant material from step (b) in a mixer outside of an inhaler to break up the loose agglomerates into primary particles of the pharmaceutically active ingredient and to disperse the primary particles in the pharmaceutically acceptable particulate carrier such that 90% or more of the pharmaceutically active ingredient has a particle size of 50 .mu.m or less to provide the inhalable medicament and such that the pharmaceutically active ingredient has a low adhesion with and is dispersed homogeneously in the pharmaceutically acceptable particulate carrier such that drug recovery from each of a plurality of samples taken from the medicament has a relative standard deviation from the mean of less than or equal to 5%; and (d) filling the inhalable medicament from step (c) into the reservoir of a dry powder inhaler.