Systemic administration of a therapeutic preparation

• US 5,506,203 A
• Filed: 06/23/1994
• Issued: 04/09/1996
• Est. Priority Date: 06/24/1993
• Status: Expired due to Term

• Current Assignee: Astrazeneca AB (Astrazeneca PLC)
• Original Assignee: Ab Astra
• Inventors: Backstrom, Kjell G. E., Johansson, Ann C. B., Dahlback, Carl M. O., Edman, Peter
• Primary Examiner(s): Schain, Howard E.
• Assistant Examiner(s): Prickril, Benet
• Application Number:
  US08/265,371
• Time in Patent Office: 656 Days
• Field of Search: 514/3, 514/4, 530/303
• US Class Current: 424/489
• CPC Class Codes: A61K 38/28 Insulins
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 9/0075 for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
• CPC Class Codes: A61K 9/145 with organic compounds

Abstract

A method of treating a patient in need of insulin treatment, including the steps of introducing into the lower respiratory tract of the patient an effective amount of a therapeutic preparation in the form of a dry powder containing (a) insulin and (b) an enhancer compound which enhances the absorption of insulin in the lungs of the patient.

Claims

1. A method of treating a patient in need of insulin treatment, comprising introducing into the lower respiratory tract of said patient an effective amount of a dry powder formulation comprising active compounds (a) insulin and (b) an enhancer which enhances the absorption of insulin in the lower respiratory tract of said patient, said dry powder formulation being suitable for inhalation.

2. The method of claim 1, wherein at least 50% of the total mass of said active compounds in said powder, at the point of introduction into the respiratory system of said patient, consists of particles having a diameter of about 10 microns or less.

3. The method of claim 2, wherein said powder is supplied as agglomerates of said particles of said active compounds contained in an inhaler device, said agglomerates being substantially deagglomerated prior to entry into the respiratory system of said patient.

4. The method of claim 2, wherein the dry powder formulation is supplied in an inhaler device as an ordered mixture of (i) particles of active compounds having a diameter of about 10 microns or less and (ii) particles of a carrier substance.

5. The method of claim 3, wherein said particles are inhaled by said patient from said inhaler device, said agglomerates being substantially deagglomerated by air turbulence in said inhaler device.

6. The method of claim 2, wherein said patient inhales said powder from a single-dose, dry powder inhaler device.

7. The method of claim 1, wherein said insulin is human insulin.

8. The method of claim 1, wherein said enhancer is a surfactant.

9. The method of claim 1, wherein said enhancer is a salt of a fatty acid, a bile salt or a phospholipid.

10. The method of claim 8, wherein said enhancer is a salt of a fatty acid, said fatty acid having 10-14 carbon atoms.

11. The method of claim 10, wherein said fatty acid has 10 carbon atoms.

12. The method of claim 9, wherein said enhancer is a sodium, potassium, or organic amine salt of said fatty acid.

13. The method of claim 12, wherein said fatty acid is capric acid.

14. The method of claim 12, wherein said enhancer is sodium caprate.

15. The method of claim 1, wherein the ratio of insulin to enhancer in said powder is between about 9:

1 and about 1;

1.

16. The method of claim 1, wherein at least 50% of the total mass of said active compounds is in the form of particles which have a diameter of 10 microns or less, or of agglomerates of said particles.

17. A method of treating a patient in need of insulin treatment, comprising introducing into the lower repiratory tract of the patient a dry powder pharmaceutical preparation comprising active compounds (a) insulin and (b) an enhancer which enhances the systemic absorption of insulin in the lower respiratory tract of said patient, said preparation being in the form of a dry powder in which at least 50% of the total mass of active compounds consists of particles having a diameter of about 10 microns or less, wherein the plasma pharmacokinetics of said insulin delivered by said method more closely resemble the plasma pharmacokinetics of endogenous insulin secreted by a healthy individual in response to a glucose challenge, than do the plasma pharmacokinetics of human insulin delivered by subcutaneous injection.

18. The method of claim 17, wherein the enhancer is a surfactant.

19. The method of claim 17, wherein the enhancer is a salt of a fatty acid.

20. The method of claim 17, wherein the enhancer is sodium caprate.