# US 9,750,812 B2 · Lipid based pharmaceutical preparations for oral and topical application; their compositions, methods, and uses thereof

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- Number: US 9,750,812 B2
- Document ID: US9750812B2
- Status: Granted
- Kind: B2
- Application number: 13/120,127
- Filed: 2009-09-25
- Published: 2011-09-01
- Granted: 2017-09-05
- Earliest claimed: 2008-09-27
- Assignees: Jina Pharmaceuticals, Inc.
- Applicants: Shoukath M. Ali; Ateeq Ahmad; Moghis U. Ahmad; Saifuddin Sheikh; Imran Ahmad
- Inventors: Shoukath M. Ali; Ateeq Ahmad; Moghis U. Ahmad; Saifuddin Sheikh; Imran Ahmad
- Web page: https://patentgrep.com/patent/US9750812B2

## CPC

- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- A61K 8/14: Liposomes; Vesicles
- A61K 8/4953: {containing pyrimidine ring derivatives, e.g. minoxidil}
- A61K 8/63: Steroids; Derivatives thereof
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/10: Dispersions; Emulsions
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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)
- A61P 17/14: for baldness or alopecia
- A61Q 7/00: Preparations for affecting hair growth
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present invention relates to the topical and oral delivery of a composition comprising one or more active agents for treating a disease or symptoms in a subject. In some embodiments, the present invention comprises a composition comprising at least one active compound, e.g., finasteride or minoxidil, and one or more lipids. In some embodiments, the present invention relates to composition and method of preparation for treating androgenic alopecia (AGA), prevention of hair loss and female hirsutism. In some embodiment, the present invention comprises finasteride and at least one lipid component for the treatment of benign prostatic hyperplasia. In some embodiment, the present invention comprises tacrolimus or amphotericin B and at least one lipid component for the treatment of skin or eye related diseases. The present invention provides a method of preparation of a composition comprising at least one active compound and at least one lipid and administering the composition to a subject by oral or topical delivery. In certain embodiments the subject is a mammal. In certain preferred embodiment, the subject is human.

## Claims

### Claim 1

A lipid composition comprising at least two active compounds dissolved in a non-toxic solvent-water system, wherein the composition comprises:
effective amounts of finasteride and minoxidil; and
a lipid or mixture of lipids
in a non-toxic solvent-water system, wherein the composition is a clear lipidic solution obtainable by mixing dissolved active compound and a lipid or mixture of lipids together in said non-toxic solvent-water system to produce said clear lipid solution.

### Claim 2 (depends on 1)

The lipid composition of claim 1, wherein said lipid or mixture of lipids is selected from the group consisting of egg phosphatidylcholine (EPC), egg phosphatidylglycerol (EPG), soy phosphatidylcholine (SPC), hydrogenated soy phosphatidylcholine (HSPC), dimyristoylphosphatidylcholine (DMPC), dimyristoylphosphatidylglycerol (DMPG), dipalmitoylphosohatidylcholine (DPPC), disteroylphosphatidylglycerol (DSPG), dipalmitoylphosphatidylglycerol (DMPG), phosphatidylethanolamines, phosphatidylserine, phosphatidylinositol, phosphatidic acid, cholesterol (Chol), cholesterol sulfate and its salts (CS), cholesterol hemisuccinate and its salts (Chems), cholesterol phosphate and its salts (CP), cholesterylphosphocholine, hydroxycholesterol derivatives, amino cholesterol derivatives, cholesteryl succinate, cholesteryl oleate, polyethylene glycol derivatives of cholesterol (cholesterol-PEG), coprostanol, cholestanol, cholestane, cholic acid, cortisol, corticosterone, hydrocortisone, and calciferol; guggulsterol, guggul sulfate and its salts, guggul laurate, guggulsterol derivatives containing long chain or short chain, saturated or unsaturated fatty acids, gugguloleate, guggul myristate, monoglycerides, diglycerides, triglycerides, carbohydrate-based lipids selected from a group consisting of galactolipid, mannolipid, galactolecithin, fatty acids selected from a group consisting of saturated or unsaturated fatty acids having a chain length of C4-C34, long chain alcohols selected from a group consisting of saturated or unsaturated alcohols having a chain length of C5-C34, and pegylated derivatives of a phospholipid selected from the group consisting of pegylated derivatives of distearoylphosphatidylglycerol, dipalmitoylphosphatidylglycerol, dimyristoylphosphatidylglycerol, and dioleoylphosphatidylglycerol.

### Claim 3 (depends on 1)

The lipid composition of claim 1, wherein the composition further comprises polyethylene glycol (PEG) having an average molecular weight ranging from about 200-20,000.

### Claim 4 (depends on 1)

The lipid composition of claim 1, further comprising an active compound selected from the group consisting of Duasteride, Amphotericin B, and Tacrolimus.

### Claim 5 (depends on 1)

The lipid composition of claim 1, wherein the non-toxic solvent-water system comprises at least one alcohol, said alcohol selected from the group consisting of ethanol, propyl alcohol, isopropyl alcohol, propylene glycol, and butanol.

### Claim 6 (depends on 1)

The lipid composition of claim 1, wherein the non-toxic solvent-water system comprises at least one oil selected from the group consisting of soybean oil, vegetable oil, olive oil, coconut oil, sunflower oil, almond oil, canola oil, sesame seed oil, peanut oil, corn oil, and cod oil.

### Claim 7 (depends on 1)

The lipid composition of claim 1, wherein said composition in a suitable vehicle for administration, wherein said vehicle is water or aqueous buffer comprising one or more non-toxic solvents selected from a group consisting of ethanol, propyl alcohol, isopropyl alcohol, propylene glycol, and butanol.

### Claim 8 (depends on 1)

The lipid composition of claim 1, wherein said composition comprises finasteride, minoxidil, soy phosphatidylcholine and 70% isopropyl alcohol in water.

### Claim 9 (depends on 1)

The lipid composition of claim 1, wherein said composition comprises finasteride, minoxidil, and soy phosphatidylcholine in propylene glycol.

### Claim 10 (depends on 1)

The lipid composition of claim 1, wherein said composition comprises finasteride, minoxidil, and soy phosphatidylcholine in propylene glycol-isopropyl alcohol-water solution.

### Claim 11 (depends on 1)

The lipid composition of claim 1, wherein said composition comprises tacrolimus, cholesteryl sulfate, and soy phosphatidylcholine in isopropanol or ethanol.

### Claim 12 (depends on 1)

The lipid composition of claim 1, wherein said composition comprises amphotericin B, cholesteryl sulfate, and soy phosphatidylcholine in isopropanol or ethanol.