Method for altering drug pharmacokinetics based on medical delivery platform

• US 9,242,052 B2
• Filed: 03/17/2014
• Issued: 01/26/2016
• Est. Priority Date: 06/29/2000
• Status: Expired due to Term

• Current Assignee: Becton, Dickinson & Co
• Original Assignee: Becton, Dickinson & Co
• Inventors: Pettis, Ronald J, Harvey, Noel G, Down, James A
• Primary Examiner(s): BOUCHELLE, LAURA A
• Application Number:
  US14/215,271
• Publication Number:
  US 20140200547A1
• Time in Patent Office: 680 Days
• US Class Current: 1/1
• CPC Class Codes: A61K 38/28 Insulins
• CPC Class Codes: A61K 38/29 Parathyroid hormone, i.e. parathormone; Parathyroid hormone-related peptides
• CPC Class Codes: A61M 2037/0038 having a channel at the side surface
• CPC Class Codes: A61M 2037/0061 Methods for using microneedles
• CPC Class Codes: A61M 37/0015 by using microneedles
• CPC Class Codes: A61M 5/158 Needles for infusions; Accessories therefor, e.g. for inserting infusion needles, or for holding them on the body
• CPC Class Codes: A61M 5/32 Needles; Details of needles pertaining to their connection with syringe or hub infusion needles A61M5/158; Accessories for bringing the needle into, or holding the needle on, the body A61M5/42, A61M5/46 take precedence; guide needles for catheters A61M25/065; Devices for protection of needles apparatus specially adapted for cleaning or sterilising needles A61M5/001
• CPC Class Codes: A61M 5/3286 Needle tip design, e.g. for improved penetration
• CPC Class Codes: A61M 5/3291 Shafts with additional lateral openings
• CPC Class Codes: A61M 5/3295 Multiple needle devices, e.g. a plurality of needles arranged coaxially or in parallel
• CPC Class Codes: A61M 5/46 having means for controlling depth of insertion
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics

Abstract

A method for directly delivering whereby a substance is introduced into an intradermal space within mammalian skin which involves administering the substance through at least one small gauge hollow needle having an outlet with an exposed height between 0 and 1 mm. The outlet is inserted into the skin to a depth of between 0.3 mm and 2 mm such that the delivery of the substance occurs at a depth between 0.3 mm and 2 mm.

Claims

1. A method for administration of a drug to a human subject, comprising delivering the drug through the lumen of a hollow needle into an intradermal compartment of the human subject'"'"'s skin, which method comprises

(a) inserting the needle into the subject'"'"'s skin so that the needle penetrates the intradermal compartment, and the needle'"'"'s outlet depth and exposed height of the outlet are located within the intradermal compartment, wherein the outlet has an exposed height of 0 to about 1 mm;

and

(b) delivering the drug through the lumen of the needle with the application of pressure in an amount effective to control the rate of delivery of the drug,

so that the drug is delivered through the lumen of the needle into the intradermal compartment and distributed systemically exhibiting any one of the following improved pharmacokinetic parameters as compared to subcutaneous delivery;

(i) a higher maximum plasma concentration and a higher bioavailability;

(ii) a higher maximum plasma concentration and a decreased time to elicit a minimally detectable blood or plasma concentration;

(iii) a higher bioavailability and a decreased time to elicit a minimally detectable blood or plasma concentration;

(iv) a higher bioavailability and decreased time to maximal plasma concentration;

or

(v) a decreased time to elicit a minimally detectable blood or plasma concentration and decreased time to maximal plasma concentration;

wherein the drug is a small molecule, a macromolecule, or a monoclonal antibody.

2. The method of claim 1, wherein the needle is selected from the group consisting of microneedles, catheter needles, and injection needles.

3. The method of claim 1, wherein a single needle is inserted.

4. The method of claim 1, wherein multiple needles are inserted.

5. The method of claim 1, wherein the drug is administered as a solution delivered by pressure directly on the solution.

6. The method of claim 1, wherein the needle has a length from about 0.5 to about 1.7 mm.

7. The method of claim 1, wherein the needle'"'"'s outlet depth is between about 0.3 mm to 2 mm when the needle is inserted.

8. The method of claim 1, wherein the outlet has an exposed height of 0 mm.

9. The method of claim 1, wherein the delivery rate is controlled by spacing of multiple needles.

10. The method of claim 1, wherein the improved pharmacokinetic parameters are a higher maximum plasma concentration and a higher bioavailability.

11. The method of claim 1, wherein the improved pharmacokinetic parameters are a higher maximum plasma concentration and a decreased time to elicit a minimally detectable blood or plasma concentration.

12. The method of claim 1, wherein the improved pharmacokinetic parameters are a higher bioavailability and a decreased time to elicit a minimally detectable blood or plasma concentration.

13. The method of claim 1, wherein the improved pharmacokinetic parameters are a higher bioavailability and decreased time to maximal plasma concentration.

14. The method of claim 1, wherein the improved pharmacokinetic parameters are a decreased time to elicit a minimally detectable blood or plasma concentration and decreased time to maximal plasma concentration.

15. The method of claim 1, wherein the drug is a small molecule.

16. The method of claim 15, wherein the small molecule is butorphanol, a COX-II inhibitor, a dermatological agent, dihydroergotamine, a dopamine agonist, a dopamine antagonist, granisetron, metoclopramide, midazolam, an agent for the common cold, an anti-addiction agent, an anti-allergy agent, an anti-emetic, an anti-obesity agent, an anti-osteoporotic agent, an anti-infective, an analgesic, an anesthetic, an anorexic agent, an anti-arthritic agent, an anti-asthmatic agent, an anti-convulsant, an anti-depressant, an anti-diabetic agent, an anti-histamine, an anti-inflammatory agent, an antimigraine preparation, an anti-motion sickness preparation, an anti-nauseant, an anti-neoplastic agent, an anti-parkinsonism drug, an anti-pruritic, an anti-psychotic, an anti-pyretic, an anti-cholinergic, a benzodiazepine antagonist, a vasodilator, a bone stimulating agent, a central nervous system stimulant, a hormone, a hypnotic, an immunosuppressive, a muscle relaxant, a parasympatholytic, a parasympathomimetric, a prostaglandin, a psychostimulant, a sedative, or a tranquilizer.

17. The method of claim 1, wherein the drug is a macromolecule.

18. The method of claim 17, wherein the macromolecule is inulin, adrenocorticotropic hormone (ACTH), luteinizing hormone-releasing hormone, growth hormone-releasing hormone, cholecystokinin, parathyroid hormone or fragments thereof, thyroid releasing hormone or analogs thereof, secretin, alpha-1 anti-trypsin, an anti-angiogenesis agent, calcitonin or analogs thereof, ceredase, enkephalins or other opioid peptides, epidermal growth factors, erythropoietin or analogs thereof, follicle stimulating hormone, granulocyte colony-stimulating factor (G-CSF), glucagon, granulocyte-macrophage colony-stimulating factor (GM-CSF), growth hormone or analogs thereof, a growth hormone antagonist, hirudin or analogs thereof, IgE suppressor, insulin, insulinotropin or analogs thereof, insulin-like growth factor, interferon, interleukin, luteinizing hormone, luteinizing hormone releasing hormone or analogs thereof, heparins, low molecular weight heparin, or macrophage colony-stimulating factor (M-CSF).

19. The method of claim 1, wherein the drug is a monoclonal antibody.

20. The method of claim 19, wherein the monoclonal antibody is a peglyated antibody, a pegylated protein or a protein modified with hydrophilic or hydrophobic polymers or additional functional groups, a fusion protein, or a single chain antibody fragment.