You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 29, 2024

Claims for Patent: 8,435,567


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 8,435,567
Title:Pharmaceutical compositions of hydrophobic surface-modified active substance microparticles for inhalation
Abstract: The invention provides microparticles for use in a pharmaceutical composition for Pulmonary administration, each microparticle comprising a particle of an active substance having, on its surface, particles of a hydrophobic material suitable for delaying the dissolution of the active substance. The invention also provides a method for making the microparticles.
Inventor(s): Staniforth; John Nicholas (Bath, GB), Harris; Haggis (Bristol, GB), Morton; David Alexander Vodden (Bath, GB), Bannister; Robin (Essex, GB)
Assignee: Vectura Limited (Chippenham, GB)
Application Number:13/269,025
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,435,567
Patent Claims: 1. Microparticles for use in a pharmaceutical composition for pulmonary administration, comprising particles of an active substance having, on their surfaces, particles of a hydrophobic material suitable for promoting the dispersal of the active particles on actuation of an inhaler and suitable for delaying the dissolution of the active substance, wherein the hydrophobic material comprises one or more materials selected from the group consisting of hydrophobic amino acids, metal stearates, a C.sub.10 to C.sub.22 carboxylic acid, phospholipids, and derivatives thereof.

2. The microparticles according to claim 1, wherein the hydrophobic material comprises a C.sub.10 to C.sub.22 carboxylic acid, which may be linear or branched, saturated or unsaturated, or a derivative thereof.

3. The microparticles according to claim 1, wherein the hydrophobic material comprises magnesium stearate.

4. The microparticles according to claim 1, wherein the hydrophobic material comprises a phospholipid.

5. The microparticles according to claim 1, which comprise not more than 90% of the hydrophobic material based on the total weight of the microparticles.

6. The microparticles according to claim 1, having a mass median aerodynamic diameter of not more than 10 .mu.m.

7. The microparticles as claimed in claim 1, which are in the form of agglomerated microparticles.

8. The microparticles as claimed in claim 1, which have at least a partial coating of a film-forming material.

9. The microparticles as claimed in claim 1, being such that, upon inhalation of the microparticles, the active substance exerts its pharmaceutical effect over a period greater by at least 20% than the period over which the active substance exerts its pharmaceutical effect when inhaled alone.

10. The microparticles as claimed in claim l, having a rate of dissolution no greater than 80% of the rate of dissolution of particles of the active substance.

11. The microparticles as claimed in claim 1, comprising an effective amount of an antimuscarinic agent, .beta.-agonist, leukotriene receptor antagonist or steroid.

12. The microparticles as claimed in claim 1, in which the particles of hydrophobic material are present as a coating on the surface of the particles of active substance.

13. The microparticles as claimed in claim 12, in which the coating is a discontinuous coating.

14. The microparticles as claimed in claim 1, which are suitable for use in a powder for use in a dry powder inhaler.

15. A composition for inhalation, comprising microparticles as claimed in claim 1.

16. The composition as claimed in claim 15, which is a dry powder and is suitable for use in a dry powder inhaler.

17. The composition as claimed in claim 15, which comprises a propellant and is suitable for use in a pressurised metered dose inhaler.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.