US2006183722A1PendingUtilityA1

Formulation for lipophilic agents

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Assignee: GENZYME CORPPriority: Sep 18, 2002Filed: Apr 20, 2006Published: Aug 17, 2006
Est. expirySep 18, 2022(expired)· nominal 20-yr term from priority
Inventors:Richard B. MazessJeffrey DriscollCreighton Reed GoldensophLeon W. Levan
A61P 5/18A61P 31/12A61P 5/00A61P 35/00A61P 25/24A61P 31/04A61P 29/00A61P 25/22A61P 3/02A61P 25/04A61P 25/20A61K 47/26A61K 31/592A61P 15/00A61P 1/18A61P 17/06A61K 47/10A61P 13/08A61P 1/00A61K 9/0019A61K 9/00A61K 31/59
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Claims

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

exact text as granted — not AI-modified
1 . A formulation, comprising a vitamin D compound; a non-ionic solubilizer selected from the group consisting of polyoxyalkylenes, polysorbate 20, fatty acid esters of glycerol, cyclodextrins, dextrans, and fatty alcohol ethers of oligoglucosides; a lipophilic antioxidant selected from the group consisting of butylated hydroxytoluene (BHT), lipoic acid, lycopene, lutein, lycophyll, xanthophyll, carotene, zeaxanthin, vitamin E and esters thereof; and an aqueous vehicle.  
   
   
       2 . A formulation as set forth in  claim 1 , wherein the lipophilic antioxidant is present in a concentration of 20 to 2000 ppm.  
   
   
       3 . A formulation as set forth in  claim 1 , wherein the non-ionic solubilizer is present in a concentration of 0.05 to 5% w/w.  
   
   
       4 . A formulation as set forth in  claim 1 , wherein the formulation is suitable for parenteral administration.  
   
   
       5 . A formulation as set forth in  claim 1 , further comprising an optional agent which is an organic solvent, a preservative or both.  
   
   
       6 . A formulation as set forth in  claim 5 , wherein the optional agent includes benzyl alcohol and ethanol.  
   
   
       7 . A formulation as set forth in  claim 6 , wherein the optional agent includes ethanol.  
   
   
       8 . A formulation as set forth in  claim 6 , wherein the optional agent includes benzyl alcohol.  
   
   
       9 . A formulation as set forth in  claim 6 , wherein the optional agent is present in a concentration of 0 to 30% w/w.  
   
   
       10 . A formulation as set forth in  claim 9 , wherein the optional agent is present in a concentration of 0% to about 10% w/w.  
   
   
       11 . A formulation as set forth in  claim 10 , wherein the optional agent is present in a concentration of about 1% to about 3% w/w.  
   
   
       12 . The formulation of  claim 1 , wherein the vitamin D compound is selected from the group consisting of 1α,24-dihydroxyvitamin D 2 , 1α,24-dihydroxyvitamin D 4 , 1α,25-dihydroxyvitamin D 3 , 1α-hydroxyvitamin D 3 , 1α,25-dihydroxyvitamin D 2 , 1α,25-dihydroxyvitamin D 4 , and 1α,24,25-dihydroxyvitamin D 2 , seocalcitol, calcipotriol, maxacalcitol, falecalcitriol, paricalcitol.  
   
   
       13 . The formulation of  claim 12  wherein the vitamin D is 1α,24-dihydroxyvitamin D 2 .  
   
   
       14 . The formulation of  claim 12  wherein the vitamin D is 1α,24-dihydroxyvitamin D 4 .  
   
   
       15 . The formulation of  claim 12  wherein the vitamin D is 1α,25-dihydroxyvitamin D 3 .  
   
   
       16 . The formulation of  claim 12  wherein the vitamin D is 1α-hydroxyvitamin D 3 .  
   
   
       17 . The formulation of  claim 12  wherein the vitamin D is 1α,25-dihydroxyvitamin D 2 .  
   
   
       18 . The formulation of  claim 12  wherein the vitamin D is 1α,25-dihydroxyvitamin D 4 .  
   
   
       19 . The formulation of  claim 12  wherein the vitamin D is 1α,24,25-dihydroxyvitamin D 2 .  
   
   
       20 . The formulation of  claim 12  wherein the vitamin D is seocalcitol.  
   
   
       21 . The formulation of  claim 12  wherein the vitamin D is calcipotriol.  
   
   
       22 . The formulation of  claim 12  wherein the vitamin D is maxacalcitol.  
   
   
       23 . The formulation of  claim 12  wherein the vitamin D is falecalcitriol.  
   
   
       24 . The formulation of  claim 12  wherein the vitamin D is paricalcitol.  
   
   
       25 . The formulation of  claim 1 , wherein the vitamin D compound is a previtamin D compound selected from the group consisting of 1α-hydroxyprevitamin D 2 , 1α,24-dihydroxyprevitamin D 2 , 1α,25-dihydroxyprevitamin D 2 , 24-hydroxyprevitamin D 2 , 1α-hydroxyprevitamin D 3  and 1α,25-dihydroxyprevitamin D 3 .  
   
   
       26 . A parenteral formulation, comprising a vitamin D compound, 0.05 to 5% w/w of a non-ionic solublizer non-ionic selected from the group consisting of polyoxyalkylenes, polysorbate 20, fatty acid esters of glycerol, cyclodextrins, dextrans, and fatty alcohol ethers of oligoglucosides; and 20 to 2000 ppm of a lipophilic antioxidant selected from the group consisting of butylated hydroxytoluene (BHT), lipoic acid, lycopene, lutein, lycophyll, xanthophyll, carotene, zeaxanthin, vitamin E and esters thereof.  
   
   
       27 . A formulation as set forth in  claim 26 , further comprising an optional agent.  
   
   
       28 . A formulation as set forth in  claim 27 , 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.  
   
   
       29 . A formulation as set forth in  claim 27 , 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 benzyl alcohol.  
   
   
       30 . The formulation of  claim 26 , wherein the vitamin D compound is selected from the group consisting of 1α,24-dihydroxyvitamin D 2 , 1α,24-dihydroxyvitamin D 4 , 1α,25-dihydroxyvitamin D 3 , 1α-hydroxyvitamin D 3 , 1α,25-dihydroxyvitamin D 2 , 1α,25-dihydroxyvitamin D 4 , and 1α,24,25-dihydroxyvitamin D 2 , seocalcitol, calcipotriol, maxacalcitol, falecalcitriol, paricalcitol.  
   
   
       31 . The formulation of  claim 30  wherein the vitamin D is 1α,24-dihydroxyvitamin D 2 .  
   
   
       32 . The formulation of  claim 30  wherein the vitamin D is 1α,24-dihydroxyvitamin D 4 .  
   
   
       33 . The formulation of  claim 30  wherein the vitamin D is 1α,25-dihydroxyvitamin D 3 .  
   
   
       34 . The formulation of  claim 30  wherein the vitamin D is 1α-hydroxyvitamin D 3 .  
   
   
       35 . The formulation of  claim 30  wherein the vitamin D is 1α,25-dihydroxyvitamin D 2 .  
   
   
       36 . The formulation of  claim 30  wherein the vitamin D is 1α,25-dihydroxyvitamin D 4 .  
   
   
       37 . The formulation of  claim 30  wherein the vitamin D is 1α,24,25-dihydroxyvitamin D 2 .  
   
   
       38 . The formulation of  claim 30  wherein the vitamin D is seocalcitol.  
   
   
       39 . The formulation of  claim 30  wherein the vitamin D is calcipotriol.  
   
   
       40 . The formulation of  claim 30  wherein the vitamin D is maxacalcitol.  
   
   
       41 . The formulation of  claim 30  wherein the vitamin D is falecalcitriol.  
   
   
       42 . The formulation of  claim 30  wherein the vitamin D is paricalcitol.  
   
   
       43 . The formulation of  claim 26 , wherein the vitamin D compound is a previtamin D compound selected from the group consisting of 1α-hydroxyprevitamin D 2 , 1α,24-dihydroxyprevitamin D 2 , 1α,25-dihydroxyprevitamin D 2 , 24-hydroxyprevitamin D 2 , 1α-hydroxyprevitamin D 3  and 1α,25-dihydroxyprevitamin D 3 .  
   
   
       44 . The formulation as set forth in  claim 26 , wherein the vitamin D compound is present at a concentration of 2-10 μg/mL.  
   
   
       45 . The formulation as set forth in  claim 26 , wherein the vitamin D compound is present at a concentration of 10-100 μg/mL.

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