Formulation for lipophilic agents

• US 7,148,211 B2
• Filed: 09/18/2002
• Issued: 12/12/2006
• Est. Priority Date: 09/18/2002
• Status: Expired due to Term

• Current Assignee: Genzyme Corporation (Sanofi )
• Original Assignee: Genzyme Corporation (Sanofi )
• Inventors: LeVan, Leon W., Goldensoph, Creighton Reed, Driscoll, Jeffrey W., Mazess, Richard B.
• Primary Examiner(s): Padmanabhan, Sreeni
• Assistant Examiner(s): MITCHELL, GREGORY W
• Application Number:
  US10/247,765
• Publication Number:
  US 20040053894A1
• Time in Patent Office: 1,546 Days
• Field of Search: 514/167, 514/168
• US Class Current: 514/168
• CPC Class Codes: A61K 31/592 9,10-Secoergostane derivatives, e.g. ergocalciferol, i.e. vitamin D2
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• 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: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/18 for pancreatic disorders, e.g. pancreatic enzymes
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/02 Nutrients, e.g. vitamins, minerals
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 5/18 of the parathyroid hormones

Abstract

The invention relates to pharmaceutical formulations of lipophilic therapeutic agents in which such agents are solubilized in largely aqueous vehicles, and processes for preparing and using the same.

Claims

1. A parenteral formulation, comprising a lipophilic drug which is doxercalciferol, a non-ionic solubilizer which is polysorbate 20 present at a concentration of about 0.05% to about 5% w/w, a lipophilic antioxidant which is butylated hydroxytoluene (BHT) present at a concentration of about 20 to about 2000 ppm, an optional agent which is ethanol present at a concentration of 0 to 30% w/w, and an aqueous vehicle.

2. A formulation as set forth in claim 1, wherein the optional agent is present in a concentration of 0% to about 10% w/w.

3. A formulalion as set forth in claim 1, wherein the optional agent is present in a concentration of about 1% to about 3% w/w.

4. A formulation as set forth in claim 1, wherein the non-ionic solubilizer includes 0.5%–

2.5% w/w polysorbate 20, the lipophilic antioxidant includes 20 ppm BHT and the optional agent includes 2.5% w/w ethanol.

5. A formulation as set forth in claim 1, wherein the doxercalciferol is present at a concentration of 2–

10 μ

g/mL.

6. A parenteral formulation suitable for treatment of secondary hyperparathyroidism comprising 2–

10 μ

g/mL of doxercalciferol 0.5%–

2.5% w/w polysorbate 20, 20 ppm BHT and 2.5% w/w ethanol.