Transmucosal formulations of low molecular weight peptide drugs

• US 5,204,108 A
• Filed: 04/09/1990
• Issued: 04/20/1993
• Est. Priority Date: 10/10/1987
• Status: Expired due to Term

• Current Assignee: West Pharmaceutical Services Drug Delivery & Clinical Research Centre Ltd
• Original Assignee: Danbiosyst UK Ltd
• Inventors: Illum, Lisbeth
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Azpuru, Carlos
• Application Number:
  US07/469,443
• Time in Patent Office: 1,107 Days
• Field of Search: 424/435, 424/436, 424/434, 424/489, 424/490, 424/491, 424/492, 424/494, 424/718
• US Class Current: 424/434
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/1658 Proteins, e.g. albumin, gelatin

Abstract

A drug delivery composition comprising a plurality of microspheres and active drug associated with each microsphere, the drug being for systemic delivery and having a maximum molecular weight of 6000, and the composition being substantially free of an enhancer. The microspheres may be of starch, gelatin or albumin. Suitable drugs include peptides, such as insulin, and antigenic vaccine ingredients. The compositions are suitable for delivery across a mucosal surface such as the vagina, eye or nose.

Claims

1. A drug delivery composition which is suitable for transmucosal delivery and which comprises a plurality of microspheres adapted to gel in contact with the mucosal surface and active drug associated with each microsphere, the composition being substantially free of an enhancer, characterised in that the drug is for systemic delivery and is a peptide having a maximum molecular weight of 6000, and the microspheres comprise starch, gelatin, collagen or dextran.

2. A drug delivery composition as claimed in claim 1 in which the microspheres are starch microspheres of an average diameter of between 10 and 100 μ

m.

3. A drug delivery composition as claimed in claim 1 wherein the microsphere material is at least partially cross-linked.

4. A drug delivery composition as claimed in claim 1 wherein the microspheres are formed from the active drug itself.

5. A drug delivery composition as claimed in claim 1 wherein the microspheres are suitable for administration to the vagina.

6. A drug delivery composition as claimed in claim 1 wherein the microspheres are suitable for administration to the eye.

7. A drug delivery composition as claimed in claim 1 wherein the microspheres are suitable for delivery to the nasal mucosa.

8. A drug delivery composition as claimed in claim 1 and which is a vaccine.

9. A drug delivery composition according to claim 1 wherein the peptide has a molecular weight of at least 1000.

10. A drug delivery composition as claimed in claim 1 wherein the peptide is insulin or a calcitonin.

11. A drug delivery composition as claimed in claim 1 wherein the drug is associated with the microspheres by being incorporated therein.

12. A drug delivery composition as claimed in claim 11 wherein the drug is incorporated into the microspheres during preparation of the microspheres.

13. A drug delivery composition as claimed in claim 11 wherein the drug is incorporated into the microspheres after preparation of the microspheres.