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US 2026/0097044 A1Published application
Ion pair liquid crystal formulations for long-acting injectables of poorly soluble drugs
AssigneeFORDOZ Pharma Corp.
InventorsYuan Chen, Sydney Ugwu, Yiwen Wang, James He
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Abstract
This application discloses a method to solubilize poorly soluble drugs in a liquid crystal vehicle for long-acting injectables. Poorly soluble acidic drugs-hydrophobic basic compounds ion pairs are incorporated into liquid crystal vehicles to solubilize and slowly release the drug after parenteral administration. Ion pairs such as Meloxicam-Dodecylamine, Sulfadiazine-Dodecylamine, Methotrexate-Dodecylamine, Levothyroxine-Dodecylamine, Meloxicam-Tridodecylamine, and Meloxicam-Bupivacaine are incorporated into liquid crystal vehicles to solubilize and control release the drugs.
Claims25
A composition comprising:
- a) a liquid crystal comprising a drug-drug ion pair or drug-excipient ion pair wherein the ion pair is a Lewis acid-base interaction;
- b) about 5 wt. % to about 99 wt. % of one or more phospholipids;
- c) 0 wt. % to about 80 wt. % percent of one or more low hydrophilic-lipophilic balance (HLB) lipids wherein the low HLB lipids exhibit an HLB value of 12 or less and are not a phospholipid;
- d) 0 wt. % to about 99 wt. % of one or more bio-tolerant organic solvents;
- and
- e) 0 wt. % to about 50 wt. % of a release adjuster
- wherein a drug in the liquid crystal comprises about 0.1 wt. % to about 20 wt. % of the composition.
4 more elements
A composition comprising:
- a) a liquid crystal comprising a drug-drug ion pair or drug-excipient ion pair wherein the ion pair is a Lewis acid-base interaction and the ion pair is selected from:
- (i) at least one acidic drug selected from the group consisting of etodolac, diflunisal, mefenamic acid, cataflam, indomethacin, piroxicam, meloxicam, oxaprozin, fenoprofen, salsalate, cetecoxib, nabumetone, sulindac, and ketoprofen, sulfadiazine, methotrexate, levothyroxine, and mixtures thereof and a basic drug selected from the group consisting of bupivacaine, ropivacaine, lidocaine, procaine, chloroprocaine, tetracaine, cocaine, benzocaine, and mixtures thereof or (ii) at least one acidic drug selected from the group consisting of etodolac, diflunisal, mefenamic acid, cataflam, indomethacin, piroxicam, meloxicam, oxaprozin, fenoprofen, salsalate, cetecoxib, nabumetone, sulindac, and ketoprofen, sulfadiazine, methotrexate, levothyroxine, and mixtures thereof and a basic amine excipient selected from the group consisting of amine is selected from the group consisting of dodecylamine, tridodecylamine, didodecylamine, n-octylamine, di-n-octylamine, tri-n-octylamine, n-hexylamine, tri-n-hexylamine, di-n-hexylamine and mixtures thereof;
- b) about 10 wt. % to about 85 wt. % of one or more unsaturated phosphocholines selected from the group consisting of egg phosphocholine, soy phosphocholine, dioleoylphosohcholine, and mixtures thereof;
- c) about 5 wt. % to about 60 wt. % percent of one or more low hydrophilic-lipophilic balance (HLB) lipids wherein the low HLB lipids exhibit an HLB value of 12 or less, are not a phospholipid and are selected from the group consisting of glyceryl dioleate, glyceryl monololeate, oleic acid, castor oil, sesame oil, sunflower oil, and mixtures thereof;
- d) about 5 wt. % to about 60 wt. % of one or more bio-tolerant organic solvents selected from the group consisting of methanol, ethanol, isopropanol, n-butanol, t-butanol, benzyl alcohol, benzyl benzoate, N-methyl-2-pyrrolidone (NMP), polyethylene glycol 400 (PEG400), propylene glycol (PG), dimethylsulfoxide (DMSO), dimethylacetamide (DMAC), water, and mixtures thereof;
- and
- e) 0 wt. % to about 50 wt. % of a release adjuster
- wherein a drug in the liquid crystal comprises about 0.1 wt. % to about 20 wt. % of the composition.
5 more elements
Dependencies are inferred from the claim text.