Water-Immiscible Materials as Vehicles for Drug Delivery

• US 20100286121A1
• Filed: 10/22/2008
• Published: 11/11/2010
• Est. Priority Date: 11/05/2007
• Status: Abandoned Application

• Current Assignee: Bausch & Lomb Incorporated (Bausch Health Cos., Inc.)
• Original Assignee: Bausch & Lomb Incorporated (Bausch Health Cos., Inc.)
• Inventors: Coffey, Martin J., Rohrs, Brian R.
• Application Number:
  US12/741,266
• Publication Number:
  US 20100286121A1
• Time in Patent Office: Days
• US Class Current: 514/211.15
• CPC Class Codes: A61K 31/4709 Non-condensed quinolines and containing further heterocyclic rings
• CPC Class Codes: A61K 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• 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 9/0019 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
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/02 Ophthalmic agents

Abstract

A pharmaceutical composition includes at least one pharmaceutical component and at least one water-immiscible material. The pharmaceutical component is more soluble in the water-immiscible material than in water. The pharmaceutical composition is suitable for ocular administration.

Claims

1. An ophthalmic pharmaceutical composition consisting essentially of:

at least one pharmaceutical component;

at least one water-immiscible material; and

optionally a viscosity-modifying compound;

wherein the pharmaceutical component has a Formula I, II, II, IV, V, or VI, and the pharmaceutical component has a solubility in water of less than about 0.1 mg/g measured at a pH of about 7.4 and at 25°

C., and the pharmaceutical component and the water-immiscible material are combined to form at least one mixture suitable for formulation for ocular administration.

2. The composition of claim 1, wherein the pharmaceutical component is solubilizable in the water-immiscible material in an amount of at least about 0.1 mg/g.

4. The composition of claim 1, wherein the water-immiscible material is selected from the group consisting of castor oil, corn oil, mineral oil, miglyol, benzyl benzoate, polycaprolactone, poly(caprolactone) triol, ethyl oleate, vitamin A, α

-tocopherol (vitamin E), medium-chain triglyceride, long-chain triglyceride, and combinations thereof.

6. The composition of claim 1, wherein the pharmaceutical component represents between 0.01% and 50%, and the water-immiscible material represents between 99.99% and 50%, based upon the total weight of the composition.

7. The composition of claim 1, wherein the pharmaceutical component represents between 0.1% and 25% of the total weight of the composition

8. The composition of claim 1, wherein the composition is a suspension containing particles of the pharmaceutical component in the water-immiscible material.

9. The composition of claim 8, wherein the particles of the pharmaceutical component have a particle site of between about 0.01 μ

m to about 1 μ

m in diameter.

10. The composition of claim 1, wherein the composition provides a sustained-release, controlled release, or extended release of the pharmaceutical component over a period of 90 days or greater at a target tissue.

3. (canceled)

5. (canceled)

11. (canceled)

12. (canceled)

13. (canceled)

14. (canceled)

15. A method of providing extended availability of a pharmaceutical component in an ocular environment of a subject for an extended treatment of an ocular disorder in said subject, the method comprising:

administering to said ocular environment ophthalmic pharmaceutical composition consisting essentially of;

at least one pharmaceutical component;

at least one water-immiscible material; and

optionally a viscosity-modifying compound;

wherein the pharmaceutical component has Formula I, II, III, IV, V, or VI, and the pharmaceutical component has a solubility in water of less than about 0.1 mg/g measured at a pH of about 7.4 and at 25°

C., and the pharmaceutical component and the water-immiscible material are combined to form at least one mixture suitable for formulation for ocular administration.

16. The method of claim 15, wherein the mixture is injected into a vitreous humor of the ocular environment.

17. The method of claim 15, wherein the mixture is injected into a subconjunctiva of the ocular environment.

18. The method of claim 15, wherein said ocular disorder is selected from the group consisting of diabetic retinopathy, diabetic macular edema, cystoid macular edema, age macular degeneration (including the wet and dry form), optic neuritis, retinitis, chorioretinitis, intermediate and posterior uveitis, choroidal neovascuralization, and combinations thereof;

and said pharmaceutical component comprises a therapeutic agent for said ocular disorder.

19. (canceled)