Apparatus and method for transdermal delivery of desmopressin

• US 20060093658A1
• Filed: 10/25/2005
• Published: 05/04/2006
• Est. Priority Date: 10/26/2004
• Status: Abandoned Application

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Sathyan, Gayatri, Gupta, Suneel, Daddona, Peter, Cormier, Michel J.N., Weyers, Richard, Staehr, Peter, Ameri, Mahmound
• Application Number:
  US11/259,010
• Publication Number:
  US 20060093658A1
• Time in Patent Office: Days
• US Class Current: 424/448
• CPC Class Codes: A61K 9/0021 Intradermal administration, e.g. through microneedle arrays, needleless injectors mechanical aspects A61M
• CPC Class Codes: A61M 2037/0023 Drug applicators using microneedles
• CPC Class Codes: A61M 2037/0061 Methods for using microneedles
• CPC Class Codes: A61M 37/0015 by using microneedles

Abstract

An apparatus and method for transdermally delivering desmopressin comprising a delivery system having a microprojection member (or system) that includes a plurality of microprojections (or array thereof) that are adapted to pierce through the stratum corneum into the underlying epidermis layer, or epidermis and dermis layers. In one embodiment, the desmopressin is contained in a biocompatible coating that is applied to the microprojection member.

Claims

1. A delivery system for transdermally delivering desmopressin to a patient, comprising:

a microprojection member having a plurality of microprojections that are adapted to pierce the stratum corneum of the patient; and

a biocompatible coating disposed on said microprojection member, said coating being formed from a coating formulation having desmopressin disposed therein.

2. The delivery system of claim 1, wherein said coating is disposed on at least one of said plurality of microprojections.

3. The delivery system of claim 1, wherein said coating formulation comprises an aqueous formulation.

4. The delivery system of claim 1, wherein said coating formulation comprises a non-aqueous formulation.

5. The delivery system of claim 1, wherein said desmopressin is selected from the group consisting of desmopressin, arginine vasopressin, vasopressin analogs and combinations thereof.

6. The delivery system of claim 5, wherein said desmopressin is selected from the group consisting of active fragments, degradation products, salts, simple derivatives and combinations thereof of desmopressin, arginine vasopressin and vasopressin analogs.

7. The delivery system of claim 6, wherein said desmopressin is desmopressin.

8. The delivery system of claim 1, wherein desmopressin comprises in the range of approximately 1-30 wt. % of said coating formulation.

9. The delivery system of claim 1, wherein desmopressin comprises in the range of 1 μ

g-2000 μ

g of said biocompatible coating.

10. The delivery system of claim 1, wherein the pH of said coating formulation is below approximately pH 8.

11. The delivery system of claim 1, wherein said coating formulation includes at least one buffer selected from the group consisting of ascorbic acid, citric acid, succinic acid, glycolic acid, gluconic acid, glucuronic acid, lactic acid, malic acid, pyruvic acid, tartaric acid, tartronic acid, fumaric acid, maleic acid, phosphoric acid, tricarbally acid, malonic acid, adipic acid, citraconic acid, glutaratic acid, itaconic acid, mesaconic acid, citramalic acid, dimethylopropionic acid, tiglic acid, glyceric acid, methacrylic acid, isocrotonic acid, β

-hydroxybutyric acid, crotonic acid, angelic acid, hydracrylic acid, aspartic acid, glutamic acid, glycine and mixtures thereof.

12. The delivery system of claim 1, wherein said coating formulation includes at least one surfactant selected from the group consisting of sodium lauroamphoacetate, sodium dodecyl sulfate (SDS), cetylpyridinium chloride (CPC), dodecyltrimethyl ammonium chloride (TMAC), benzalkonium, chloride, polysorbates, sorbitan derivatives, alkoxylated alcohols and mixtures thereof.

13. The delivery device of claim 1, wherein said coating formulation includes at least one polymeric material having amphiphilic properties.

14. The delivery system of claim 1, wherein said coating formulation includes a hydrophilic polymer selected from the following group consisting of hydroxyethyl starch, dextran, poly(vinyl alcohol), poly(ethylene oxide), poly(2-hydroxyethyl-methacrylate), poly(n-vinyl pyrolidone), polyethylene glycol and mixtures thereof.

15. The delivery system of claim 1, wherein said coating formulation includes a biocompatible carrier selected from the group consisting of human albumin, bioengineered human albumin, polyglutamic acid, polyaspartic acid, polyhistidine, pentosan polysulfate, polyamino acids, sucrose, trehalose, melezitose, raffinose, stachyose, mannitol and like sugar alcohols.

16. The delivery system of claim 1, wherein said coating formulation includes a stabilizing agent selected from the group consisting of a non-reducing sugar, a polysaccharide and a reducing sugar.

17. The delivery system of claim 1, wherein said coating formulation includes at least one vasoconstrictor selected from the group consisting of amidephrine, cafaminol, cyclopentaimine, deoxyepinephrine, epinephrine, felypressin, indanzoline, metizoline, midodrine, naphazoline, nordefrin, octodrine, ornipressin, oxymethazoline, phenylephrine, phenylethanolamine, phenylpropanolamine, propylhexedrine, pseudoephedrine, tetrahydrozoline, tramazoline, tuaminoheptane, tymazoline, vasopressin, xylometazoline, and mixtures thereof.

18. The delivery system of claim 1, wherein said coating formulation includes at least one pathway patency modulator selected from the group consisting of osmotic agents, zwitterionic compounds, anti-inflammatory agents and anticoagulants.

19. The delivery system of claim 1, wherein said coating formulation has a viscosity in the range of approximately 3-500 centipose.

20. The delivery system of claim 1, wherein the thickness of said biocompatible coating is less than approximately 25 microns.

28. The delivery system of claim 1 wherein the patient is a child.

30. The delivery system of claim 1 wherein the patient is an adult.

32. The delivery system of claim 1 wherein the patient is a geriatric patient.

21. A method of transdermally delivering desmopressin to a patient, comprising the steps of:

providing a microprojection member having a plurality of microprojections, said microprojection member having a coating disposed thereon, said coating including desmopressin;

applying said microprojection member to a skin site of said patient, whereby said plurality of microprojections pierce the stratum corneum and deliver said desmopressin to said patient; and

removing said microprojection member from said skin site.

22. The method of claim 21, wherein said microprojection member remains applied to said skin site for a period of time in the range of 5 sec. to 24 hrs.

23. The method of claim 21, wherein said desmopressin is selected from the group consisting of desmopressin, arginine vasopressin, vasopressin analogs and combinations thereof.

24. The method of claim 21, wherein said desmopressin is selected from the group consisting of active fragments, degradation products, salts, simple derivatives and combinations thereof of desmopressin, arginine vasopressin and vasopressin analogs.

25. The method of claim 21, wherein said desmopressin is desmopressin.

26. The method of claim 21, wherein said desmopressin comprises in the range of approximately 1 μ

g-2000 μ

g of said biocompatible coating.

27. The method of claim 21, wherein said delivery of said desmopressin exhibits improved pharmacokinetics compared to the pharmacokinetic characteristics of intravenous or subcutaneous delivery.

29. The method of claim 21, wherein the patient is a child.

31. The method of claim 21, wherein the patient is an adult.

33. The method of claim 21, wherein the patient is a geriatric patient.