Intranasal 0.15% and 0.24% testosterone gel formulations and use thereof for treating anorgasmia or hypoactive sexual desire disorder

• US 10,111,888 B2
• Filed: 10/23/2015
• Issued: 10/30/2018
• Est. Priority Date: 05/13/2011
• Status: Active Grant

• Current Assignee: Acerus Biopharma, Inc.
• Original Assignee: Acerus Biopharma, Inc.
• Inventors: Kreppner, Wayne, Fogarty, Siobhan, Oberegger, Werner, Maes, Paul Jose Pierre Marie
• Primary Examiner(s): Shiao, Rei Tsang
• Application Number:
  US14/922,070
• Publication Number:
  US 20160271144A1
• Time in Patent Office: 1,103 Days
• Field of Search: 514170
• CPC Class Codes: A61K 31/568 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61P 15/10 for impotence

Abstract

The present invention relates to lower dosage strength pernasal testosterone gel formulations for intranasal administration and treatment methods for using the lower dosage strength pernasal testosterone gel formulations for treating a female subject with anorgasmia and/or hypoactive sexual desire disorder.

Claims

1. A method of treating a female for anorgasmia, said method comprising:

(a) depositing an intranasal testosterone gel in an amount of between about 50 microliters and 150 microliters in each nasal cavity of each nostril of the female onto a mucosal membrane on an outer external nasal wall, opposite the nasal septum, preferably at about the middle to about the upper section of the outer external nasal wall and just under the cartilage section of the outer external nasal wall, to nasally deliver to the subject the intranasal testosterone gel to effectively treat the anorgasmia, wherein the testosterone gel comprises;

(i) about 0.15% testosterone by weight of the intranasal testosterone gel, wherein the testosterone has a particle size of greater than 10 μ

m to prevent the testosterone particles from entering the respiratory tract following said nasal deposition; and

(ii) a pharmaceutically acceptable vehicle; and

(b) squeezing or rubbing the exterior of the nose of the female following said nasal deposition to contact the nasally deposited intranasal testosterone gel with the nasal septum mucosal membrane within the nasal cavity, so that at least a portion of the deposited intranasal testosterone gel remains in contact with the mucosal membranes on the outer nasal wall and the nasal septum within the nasal cavity for sustained release of the testosterone from the intranasal testosterone gel over dose life.

2. The method of claim 1, wherein the intranasal testosterone gel is in an amount of about 100 microliters.

3. The method of claim 1, wherein said nasal deposition comprises depositing the intranasal testosterone gel into the nose of the female once or twice daily on demand.

4. The method of claim 1, wherein said nasal deposition comprises depositing the intranasal testosterone gel into the nose of the female at least once daily.

5. The method of claim 1, wherein said nasal deposition comprises depositing the intranasal testosterone gel into the nose of the female at least twice daily.

6. The method of claim 1, wherein the intranasal testosterone gel comprises:

(a) 0.15% testosterone,

(b) 91.85% castor oil,

(c) 4.0% oleoyl polyoxylglycerides, and

(d) 4.0% colloidal silicon dioxide.

7. A method of treating a female for hypoactive sexual desire disorder (HSDD), said method comprising:

(a) depositing an intranasal testosterone gel in an amount of between about 50 microliters and 150 microliters in each nasal cavity of each nostril of the female onto a mucosal membrane on an outer external nasal wall, opposite the nasal septum, preferably at about the middle to about the upper section of the outer external nasal wall and just under the cartilage section of the outer external nasal wall, to nasally deliver to the subject the intranasal testosterone gel to effectively treat the HSDD, wherein the testosterone gel comprises;

(i) about 0.15% testosterone by weight of the intranasal testosterone gel, wherein the testosterone has a particle size of greater than 10 μ

m to prevent the testosterone particles from entering the respiratory tract following said nasal deposition; and

(ii) a pharmaceutically acceptable vehicle; and

(b) squeezing or rubbing the exterior of the nose of the female following said nasal deposition to contact the nasally deposited intranasal testosterone gel with the nasal septum mucosal membrane within the nasal cavity, so that at least a portion of the deposited intranasal testosterone gel remains in contact with the mucosal membranes on the outer nasal wall and the nasal septum within the nasal cavity for sustained release of the testosterone from the intranasal testosterone gel over dose life.

8. The method of claim 7, wherein the intranasal testosterone gel is in an amount of about 100 microliters.

9. The method of claim 7, wherein said nasal deposition comprises depositing the intranasal testosterone gel into the nose of the female once or twice daily on demand.

10. The method of claim 7, wherein said nasal deposition comprises depositing the intranasal testosterone gel into the nose of the female at least once daily.

11. The method of claim 7, wherein said nasal deposition comprises depositing the intranasal testosterone gel into the nose of the female at least twice daily.

12. The method of claim 7, wherein the intranasal testosterone gel comprises:

(a) 0.15% testosterone,

(b) 91.85% castor oil,

(c) 4.0% oleoyl polyoxylglycerides, and

(d) 4.0% colloidal silicon dioxide.