Preparation comprising exanatide for delivery into a lumen of the intestinal tract
Embodiments of the invention provide swallowable devices, preparations and methods for delivering drugs and other therapeutic agents within the GI tract. Many embodiments provide a swallowable device for delivering the agents. Particular embodiments provide a swallowable device such as a capsule for delivering drugs into the intestinal wall or other GI lumen. Embodiments also provide various drug preparations that are configured to be contained within the capsule, advanced from the capsule into the intestinal wall and degrade to release the drug into the bloodstream to produce a therapeutic effect. The preparation can be operably coupled to delivery means having a first configuration where the preparation is contained in the capsule and a second configuration where the preparation is advanced out of the capsule into the intestinal wall. Embodiments of the invention are particularly useful for the delivery of drugs which are poorly absorbed, tolerated and/or degraded within the GI tract.
1. A therapeutic preparation comprising a exenatide, the preparation shaped as a solid tissue penetrating member having a pointed end, the preparation configured to be contained in a swallowable enclosure having a tubular shape with curved ends and to be released from the enclosure to penetrate and be inserted into a gastro-intestinal (GI) wall of a patient after oral ingestion of the enclosure by the application of force upon the preparation, wherein upon insertion into the GI wall, the preparation releases exenatide into the blood stream of the patient.
2. The preparation of claim 1 , wherein the preparation is adapted for insertion into a wall of the patient's small intestine.
3. The preparation of claim 1 , wherein the preparation is adapted for insertion into a wall of the patient's stomach.
4. The preparation of claim 1 , wherein the preparation is adapted to be operably coupled to a delivery means having a first configuration and a second configuration, the preparation being contained within the enclosure in the first configuration and advanced out of the capsule and into the GI wall in the second configuration.
5. The preparation of claim 4 , wherein the delivery means comprises a least one expandable balloon having an expanded and a non-expanded state and the first configuration is the non-expanded state and the second configuration is the expanded state.
6. The preparation of claim 4 , wherein the delivery means comprises a spring.
7. The preparation of claim 1 , wherein the preparation comprises a biodegradable material which degrades within the intestinal wall to release exenatide into the blood stream.
8. The preparation of claim 7 , wherein the biodegradable material comprises poly(lactic-co-glycolic acid) (PLGA), a sugar or maltose.
9. The preparation of claim 1 , wherein the preparation comprises at least one pharmaceutical excipient.
10. The preparation of claim 9 , wherein the at least one pharmaceutical excipient comprises at least one of a binder, a preservative, or a disintegrant.
11. The preparation of claim 10 , wherein the binder comprises polyethylene glycol (PEG).
12. The preparation of claim 1 , wherein a dose of exenatide in the preparation is in a range of about 1 to 20 μg.
13. The preparation of claim 12 , wherein a dose of exenatide in the preparation is in a range of about 1 to 10 μg.
14. The preparation of claim 13 , wherein a dose of exenatide in the preparation is in a range of about 4 to 8 μg.
15. The preparation of claim 1 , wherein a weight percent of exenatide in the tissue penetrating member comprises between about 0.1 to 1%.
16. The preparation of claim 1 , wherein the tissue penetrating member includes a retaining feature for retaining the tissue penetrating member within the GI wall after insertion.
17. The preparation of claim 1 , wherein the tissue penetrating member includes a shaped section in which the exenatide is contained.
18. The preparation of claim 17 , wherein the shaped section has a cylinder or pellet shape.
19. The preparation of claim 1 , wherein the tissue penetrating member has sufficient stiffness to be advanced completely into the intestinal wall by the application of a force to the tissue penetrating member.
20. The preparation of claim 1 , wherein the preparation is configured to produce a long-term release of exenatide.
21. The preparation of claim 20 , wherein the long term release of exanatide has a t½ in range of about 6 to 24 hours.
22. The preparation of claim 1 , wherein the preparation comprises a therapeutically effective dose of another therapeutic agent for the treatment of diabetes or another glucose regulation disorder.
23. The preparation of claim 22 , wherein the other therapeutic agent comprises a therapeutically effective dose of insulin.
24. The preparation of claim 23 , wherein a dose of insulin in the preparation is in a range from about 1 to 50 units of insulin or about 4 to 9 units of insulin.
25. The preparation of claim 22 , wherein the other therapeutic agent comprises metformin.
26. The preparation of claim 25 , wherein a dose of exenatide and a dose of metformin in the preparation are matched to control a blood glucose level of a patient without injecting incretin into the patient.
27. A therapeutic preparation comprising a therapeutically effective dose exenatide for the control of a blood glucose level in a patient having diabetes or other blood glucose regulation disorder, the preparation shaped as a solid tissue penetrating member having a pointed end, the preparation configured to be contained in a swallowable enclosure having a tubular shape with curved ends and to be released from the enclosure to penetrate and be inserted into a gastro-intestinal (GI) wall of the patient after oral ingestion of the enclosure, wherein upon insertion into the GI wall, the preparation releases exenatide into the blood stream of the patient to control the blood glucose level in the patient.
28. The preparation of claim 27 , wherein the patient's blood glucose level is controlled within a normal physiologic range.
29. The preparation of claim 27 , wherein a dose of exenatide in the preparation is in a range of about 1 to 20 μg.