.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 8,101,160

« Back to Dashboard

Details for Patent: 8,101,160

Title:Formulations for use in inhaler devices
Abstract: A formulation for use in an inhaler device comprises carrier particles having a diameter of at least 50 .mu.m and a mass median diameter of at least 175 .mu.m; fine particles of an excipient material having a mass median aerodynamic diameter of not more than 20 .mu.m; and active particles. The formulation has excellent flowability even at relatively high contents of fine particles.
Inventor(s): Staniforth; John Nicholas (Bath, GB), Morton; David Alexander Vodden (Bath, GB)
Assignee: Vectura Limited (GB)
Filing Date:Apr 17, 2001
Application Number:10/257,883
Claims:1. A formulation for use in an inhaler device, comprising carrier particles in the form of an agglomerate consisting of a plurality of crystals fused to one another, wherein the carrier particles have a diameter of at least 50 .mu.m and a mass median aerodynamic diameter of at least 175 .mu.m and a fissured surface in which the fissures between the crystals of the agglomerate are at least 20 .mu.m wide and at least 20 .mu.m deep; fine particles consisting of an excipient material consisting of one or more crystalline sugars and having a mass median aerodynamic diameter of not more than 20 .mu.m; and active particles; wherein the fine excipient particles are present in an amount of from not less than 5% by weight based on the total weight of the formulation, to 50% by weight based on the total weight of the carrier particles, fine excipient particles and active particles.

2. A formulation according to claim 1, in which the mass median diameter of the carrier particles is at least 200 .mu.m.

3. A formulation according to claim 1, in which the mass median aerodynamic diameter of the fine excipient particles is not more than 15 .mu.m.

4. A formulation according to claim 3, in which the mass median aerodynamic diameter of the fine excipient particles is not more than 10 .mu.m.

5. A formulation according to claim 1, in which the carrier particles and the fine excipient particles are of the same material.

6. A formulation according to claim 1, in which at least the carrier particles are of a crystalline sugar.

7. A formulation according to claim 6, in which the carrier particles are of dextrose or lactose.

8. A formulation according to claim 7, in which the carrier particles are of lactose.

9. A formulation according to claim 1, in which the fine excipient particles are of dextrose or lactose.

10. A formulation according to claim 9, in which the fine excipient particles are of lactose.

11. A formulation according to claim 1, in which the carrier particles are of a crystalline sugar having a tapped density not exceeding 0.75 g/cm.sup.3.

12. A formulation according to claim 1, in which the carrier particles have a tapped density not exceeding 0.70 g/cm.sup.3.

13. A formulation according to claim 1, in which the carrier particles have a bulk density as measured by mercury intrusion porosimetry of not exceeding 0.6 g/cm3.

14. A formulation according to claim 1, in which the carrier particles are obtainable by a wet granulation process.

15. A formulation according to claim 1, in which the carrier particles are dendritic spherulites.

16. A formulation according to claim 1, which contains up to 90% by weight of active particles and fine excipient particles, based on the total weight of active particles, fine excipient particles and carrier particles.

17. A formulation according to claim 16, which contains up to 50% by weight of active particles and fine excipient particles, based on the total weight of active particles, fine excipient particles and carrier particles.

18. A formulation according to claim 17, which contains up to 20% by weight of active particles and fine excipient particles, based on the total weight of active particles, fine excipient particles and carrier particles.

19. A formulation according to claim 1, in which the active particles are present in an amount of from 0.01 to 90% by weight, based on the total weight of active particles and fine excipient particles.

20. A formulation according to claim 19, in which the active particles are present in an amount of from 0.1 to 50% by weight, based on the total weight of active particles and fine excipient particles.

21. A formulation according to claim 1, which contains up to 20% by weight of active particles, based on the total weight of the formulation.

22. A formulation according to claim 1, which comprises at least 50% by weight carrier particles, based on the total weight of the formulation.

23. A formulation according to claim 22, which comprises at least 70% by weight carrier particles, based on the total weight of the formulation.

24. A formulation according to claim 1, wherein the fine excipient particles are present in an amount of from not less than 5% by weight based on the total weight of the formulation up to 20% by weight based on the total weight of the formulation.

25. A formulation according to claim 24, in which the fine excipient particles are present in an amount of from not less than 5% by weight based on the total weight of the formulation up to 15% by weight based on the total weight of the formulation.

26. A formulation according to claim 1, which contains at least 20% by weight, based on the total weight of the formulation, of particles of diameter less than 20 .mu.m.

27. A formulation according to claim 1, in which the active particles comprise an agent having therapeutic activity when delivered into the lung.

28. A formulation according to claim 27, in which the active particles comprise a therapeutically active agent for the prevention or treatment of respiratory disease.

29. A formulation according to claim 1, in which the active particles comprise one or more active agents selected from .beta.2-agonists, ipratropium bromide, steroids, cromones and leukotriene receptor antagonists.

30. A formulation according to claim 27, in which the active particles comprise a therapeutically active agent for systemic use.

31. A formulation according to claim 27, in which the active particles comprise one or more agents selected from peptides, polypeptides, proteins and DNA fragments.

32. A formulation according to claim 31, in which the active particles comprise insulin.

33. A formulation according to claim 1, comprising more than 5% by weight, based on the total weight of the formulation, of particles of aerodynamic diameter less than 20 .mu.m, the formulation having a flowability index of 12 mm or less.

34. A formulation according to claim 33, which comprises more than 10% by weight particles of aerodynamic diameter less than 20 .mu.m.

35. A formulation according to claim 1, comprising: from 5 to 90% by weight carrier particles having a diameter of at least 50 .mu.m and a mass median diameter of at least 175 .mu.m; from 0.01 to 80% by weight of a therapeutically active agent; from 9 to 50% by weight of particles of fine excipient material; in each case, by weight, based on the total weight of the carrier particles, active agent and fine excipient material.

36. An inhaler device comprising a formulation according to claim 1.

37. A device according to claim 36, which is a dry powder inhaler.

38. A device according to claim 37, which is a pressurised metered dose inhaler.

39. A method of manufacturing a formulation according to claim 1, comprising mixing the fine excipient particles with the carrier particles and the active particles.

40. The formulation of claim 1 which has a flowability index of 12 mm or less.

41. The formulation of claim 1, wherein each carrier particle contains at least three lactose primary crystals of the tomahawk shape.

42. A formulation as claimed in claim 1, wherein the crystals of the agglomerate are fused to one another by solid bridges.
« Back to Dashboard

For more information try a trial or see the database preview and plans and 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 verifification 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.

`abc