# US 10,864,254 B2 · Method of delivering gonadotropin releasing hormone or an analogue thereof into a lumen of the intestinal tract using a swallowable drug delivery device

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- Number: US 10,864,254 B2
- Document ID: US10864254B2
- Status: Granted
- Kind: B2
- Application number: 16/400,707
- Filed: 2019-05-01
- Published: 2019-12-26
- Granted: 2020-12-15
- Earliest claimed: 2010-12-23
- Assignees: Rani Therapeutics, LLC
- Applicants: Rani Therapeutics, LLC
- Inventors: Mir Imran
- Web page: https://patentgrep.com/patent/US10864254B2

## CPC

- A61K 38/22: Hormones (derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin A61K38/33, e.g. corticotropin A61K38/35)
- A61K 9/0009: {involving or responsive to electricity, magnetism or acoustic waves; Galenical aspects of sonophoresis, iontophoresis, electroporation or electroosmosis}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/0065: {Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus}
- A61K 9/4891: {Coated capsules; Multilayered drug free capsule shells (with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004)}
- A61K 38/09: Luteinising hormone-releasing hormone [LHRH] {, i.e. Gonadotropin-releasing hormone [GnRH]}; Related peptides
- A61M 5/00: Devices for bringing media into the body in a subcutaneous, intra-vascular or intramuscular way; Accessories therefor, e.g. filling or cleaning devices, arm rests (tube connectors, tube couplings, valves or branch units, specially adapted for medical use A61M39/00; containers specially adapted for medical or pharmaceutical purposes A61J1/00)
- A61M 25/10: Balloon catheters ({A61M25/0125 takes precedence; embolectomy A61B17/22032; retractors A61B17/02;} inflatable balloons for placing stents or stent-grafts A61F2/958 {; stomach balloons for treatment of obesity A61F5/0003; oesophagal tubes A61J15/00})
- A61M 37/0015: {by using microneedles}
- A61M 31/002: {Devices for releasing a drug at a continuous and controlled rate for a prolonged period of time (artificial gland structures or devices A61F2/022; intra-uterine contraceptive devices A61F6/14; tampons for introducing into the vagina A61F13/20, A61L15/00; suppositories or bougies for intra-vaginal or intra-uterine application A61K9/02; physical forms of medicinal preparations for sustained or differential drug release A61K9/20, A61K9/50)}
- A61M 2037/0023: {Drug applicators using microneedles}
- A61M 2037/0061: {Methods for using microneedles}
- A61M 2210/1042: Alimentary tract (A61M2210/0618 takes precedence)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61M: DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY (introducing media into or onto the bodies of animals A61D7/00; means for inserting tampons A61F13/26; devices for administering food or medicines orally A61J; containers for collecting, storing or administering blood or medical fluids A61J1/05); DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY (surgery A61B; chemical aspects of surgical articles A61L); DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR {(Electrotherapy, e.g. producing anaesthesia by the use of alternating or intermittent currents A61N1/36021)}

## Abstract

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.

## Claims

### Claim 1

A method for delivering gonadotropin releasing hormone (GnRH) or GnRH analogue to a patient in need thereof, the method comprising:
swallowing an enclosure having an interior, a delivery means, and a GnRH or GnRH analogue (GGA) preparation coupled to the delivery means, the GGA preparation comprising a therapeutically effective dose of GGA, the delivery means having a first configuration and a second configuration, the preparation being contained within the interior in the first configuration and advanced out of the interior and into a gastro-intestinal (GI) lumen wall in the second configuration so as to deliver the GGA preparation into the GI lumen wall, the enclosure protecting the GGA preparation from degradation by GI fluids, the GGA preparation supplied in the enclosure in a solid or semi-solid form with a pointed shape which can be delivered from the enclosure into the wall of GI lumen by the application of force on the preparation; and
triggering the delivery means responsive to a condition in the GI lumen to deliver the GGA preparation from the enclosure into the wall of the GI lumen.

### Claim 2 (depends on 1)

The method of claim 1, wherein the GI lumen is the small intestine.

### Claim 3 (depends on 1)

The method of claim 1, wherein the GI lumen is the stomach.

### Claim 4 (depends on 1)

The method of claim 1, wherein the condition is a selected pH.

### Claim 5 (depends on 4)

The method of claim 4, wherein the pH is above about 7.1.

### Claim 6 (depends on 1)

The method of claim 1, wherein a weight percent of GnRH or GnRH analogue in the preparation is in a range between about 2 to 15%.

### Claim 7 (depends on 1)

The method of claim 1, wherein a dose of GnRH or GnRH analogue in the preparation is in a range from about 0.1 to 2.0 mg.

### Claim 8 (depends on 7)

The method of claim 7, wherein a dose of GnRH or GnRH analogue in the preparation is in a range from about 0.2 to 1.0 mg.

### Claim 9 (depends on 7)

The method of claim 7, wherein a dose of GnRH or GnRH analogue in the preparation is in a range from about 0.3 to 1.5 mg.

### Claim 10 (depends on 1)

The method of claim 1, wherein the GGA preparation comprises at least one pharmaceutical excipient.

### Claim 11 (depends on 10)

The method of claim 10, wherein the at least one pharmaceutical excipient comprises at least one of a binder, a preservative or a disintegrant.

### Claim 12 (depends on 1)

The method of claim 1, further comprising retaining the GGA preparation within the GI lumen wall after insertion.

### Claim 13 (depends on 12)

The method of claim 12, wherein retaining comprises anchoring a portion of the GGA preparation in GI lumen wall tissue.

### Claim 14 (depends on 1)

The method of claim 1, wherein delivering the GGA preparation comprises applying a force to the GGA preparation.

### Claim 15 (depends on 14)

The method of claim 14, wherein the GGA preparation is advanced completely into the GI lumen wall by such application of force.

### Claim 16 (depends on 14)

The method of claim 14, wherein the GGA preparation is advanced through the GI lumen wall by such application of force.

### Claim 17 (depends on 14)

The method of claim 14, wherein the force is a mechanical force applied to a surface of GGA preparation.

### Claim 18 (depends on 1)

The method of claim 1, wherein the GnRH analogue is leuprorelin.

### Claim 19 (depends on 18)

The method of claim 18, wherein a dose of leuprorelin in the preparation is in a range from about 0.1 to 2 mg.

### Claim 20 (depends on 19)

The method of claim 19, wherein, a dose of leuprorelin in the preparation is in a range from about 0.2 to 1.0 mg.