Solid dose delivery vehicle and methods of making same

• US 6,565,871 B2
• Filed: 08/31/2001
• Issued: 05/20/2003
• Est. Priority Date: 12/02/1994
• Status: Expired due to Fees

• Current Assignee: QDose Limited
• Original Assignee: Elan Drug Delivery Ltd (Philip Morris Limited)
• Inventors: Colaco, Camilo, Roser, Bruce J., Blair, Julian, Kampinga, Jaap
• Primary Examiner(s): Azpuru, Carlos A.
• Application Number:
  US09/945,180
• Publication Number:
  US 20020012687A1
• Time in Patent Office: 627 Days
• Field of Search: 424/45, 424/46, 424/78.04, 424/423, 424/427, 424/430, 424/434, 424/436, 424/449
• US Class Current: 424/423
• CPC Class Codes: A61K 9/0021 Intradermal administration, e.g. through microneedle arrays, needleless injectors mechanical aspects A61M
• CPC Class Codes: A61K 9/145 with organic compounds
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The present invention encompasses a solid dose delivery vehicle for ballistic administration of a bioactive material to subcutaneous and intradermal tissue, the delivery vehicle being sized and shaped for penetrating the epidermis. The delivery vehicle further comprises a stabilizing polyol glass loaded with the bioactive material and capable of releasing the bioactive material in situ. The present invention further includes methods of making and using the solid dose of the invention.

Claims

1. A therapeutic composition in solid dose form comprising a therapeutic agent, a stabilizing polyol, and a physiologically acceptable salt;

wherein said salt is present in an amount sufficient to effect a loss of water from the composition so that at ambient humidity the vapor pressure of water of crystallisation is at least 14 mm Hg at 20 C. and wherein said solid dose form is a glass.

2. The composition, according to claim 1, which comprises a salt selected from the group consisting of ammonium chloride, ammonium orthophosphate, ammonium sulfate, barium chloride dihydrate, calcium lactate pentahydrate, copper sulfate pentahydrate, magnesium salicylate tetrahydrate, magnesium sulfate heptahydrate, potassium bisulfate, potassium bromide, potassium chromate, potassium dihydrogen orthophosphate, sodium acetate trihydrate, sodium bromoiridate dodecahydrate, sodium carbonate decahydrate, sodium fluoride, sodium hydrogen orthophosphate dodecahydrate, sodium metaperiodate trihydrate, sodium metaphosphate trihydrate, sodium metaphosphate hexahydrate, sodium sulfite heptahydrate, sodium sulfate heptahydrate, sodium sulfate decahydrate, sodium thiosulfate pentahydrate, and zinc sulfate heptahydrate.

3. The composition, according to claim 1, wherein said polypol is a carbohydrate.

4. The composition, according to claim 3, wherein said carbohydrate is selected from the group consisting of monosaccharides, disaccharides, trisaccharides, and oligosaccharides.

5. The composition, according to claim 4, wherein said polyol is trehalose.

6. The composition, according to claim 4, wherein said polyol stabilizes the therapeutic agent during processing and/or storage.

7. The composition, according to claim 1, wherein said therapeutic agent is stable in the presence of elevated temperature or organic solvents.

8. The composition, according to claim 1, wherein the solid dose is suitable for pulmonary, topical, ocular, GI, rectal, vaginal, transmucosal, transermal, intradermal or subcutaneous administration.

9. The composition, according to claim 1, wherein said therapeutic agent is a bioactive material.

10. The composition, according to claim 9, wherein said bioactive material is a peptide or protein.

11. The composition, according to claim 1, wherein said therapeutic agent is an immunogen.

12. The composition, according to claim 1, wherein said therapeutic agent is prophylactic for use as a vaccine.

13. The composition, according to claim 1, wherein said therapeutic agent comprises an antigen and an adjuvant.

14. A therapeutic composition in solid dose form comprising a therapeutic agent, a polyol, and a physiologically acceptable salt;

wherein said therapeutic composition is a powder and wherein said salt is present in an amount sufficient to prevent clumping of the powder.

15. The composition, according to claim 14, which comprises a salt selected from the group consisting of ammonium chloride, ammonium orthophosphate, ammonium sulfate, barium chloride dihydrate, calcium lactate pentahydrate, copper sulfate pentahydrate, magnesium salicylate tetrahydrate, magnesium sulfate heptahydrate, potassium bisulfate, potassium bromide, potassium chromate, potassium dihydrogen orthophosphate, sodium acetate trihydrate, sodium bromoiridate dodecahydrate, sodium carbonate decahydrate, sodium fluoride, sodium hydrogen orthophosphate dodecahydrate, sodium metaperiodate trihydrate, sodium metaphosphate trihydrate, sodium metaphosphate hexahydrate, sodium sulfite heptahydrate, sodium sulfate heptahydrate, sodium sulfate decahydrate, sodium thiosulfate pentahydrate, and zinc sulfate heptahydrate.

16. The composition, according to claim 14, wherein said polyol is a stabilizing polyol.

17. The composition, according to claim 16, wherein said polyol is a carbohydrate.

18. The composition, according to claim 17, wherein said carbohydrate is selected from the group consisting of monosaccharides, disaccharides, trisaccharides, and oligosaccharides.

19. The composition, according to claim 16, wherein said polyol is trehalose.

20. The composition, according to claim 16, wherein said polyol stabilizes the therapeutic agent during processing and/or storage.

21. The composition, according to claim 14, wherein said therapeutic agent is stable in the presence of elevated temperature or organic solvents.

22. The composition, according to claim 14, wherein the solid dose is suitable for pulmonary, topical, ocular, GI, rectal, vaginal, transmucosal, transermal, intradermal or subcutaneous administration.

23. The composition, according to claim 14, wherein said therapeutic agent is a bioactive material.

24. The composition, according to claim 22, wherein said bioactive material is a peptide or protein.

25. The composition, according to claim 14, wherein said therapeutic agent is an immunogen.

26. The composition, according to claim 14, wherein said therapeutic agent is prophylactic for use as a vaccine.

27. The composition, according to claim 14, wherein said therapeutic agent comprises an antigen and an adjuvant.