# US 11,026,934 B2 · Topical retinoid compositions

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- Number: US 11,026,934 B2
- Document ID: US11026934B2
- Status: Granted
- Kind: B2
- Application number: 16/369,320
- Filed: 2019-03-29
- Published: 2019-07-25
- Granted: 2021-06-08
- Earliest claimed: 2015-07-13
- Assignees: Dr. Reddy's Laboratories, Inc.
- Applicants: Dr. Reddy's Laboratories Ltd.
- Inventors: Sateesh Kandavilli; Franklin Okumu; Manish M. Bankar; Sujit Kumar Dolai
- Web page: https://patentgrep.com/patent/US11026934B2

## CPC

- A61K 31/4436: containing a heterocyclic ring having sulfur as a ring hetero atom
- A61C 19/00: Dental auxiliary appliances (dental chairs or accessories therefor, working stands whether or not combined with chairs A61G15/00)
- A61C 19/08: combined with anaesthetising implements (dental hypodermic syringes A61M5/00)
- A61K 8/49: containing heterocyclic compounds
- A61K 8/671: {Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal}
- A61K 8/678: {Tocopherol, i.e. vitamin E}
- 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 9/122: {Foams; Dry foams (edible foams A61K9/0056)}
- A61K 31/355: Tocopherols, e.g. vitamin E
- A61K 31/7004: Monosaccharides having only carbon, hydrogen and oxygen atoms
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/10: Anti-acne agents
- A61Q 19/00: Preparations for care of the skin
- A61Q 19/02: for chemically bleaching or whitening the skin
- A61Q 19/08: Anti-ageing preparations
- A61Q 19/10: Washing or bathing preparations
- A61K 8/498: {having 6-membered rings or their condensed derivatives, e.g. coumarin}
- 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)
- A61C: DENTISTRY; APPARATUS OR METHODS FOR ORAL OR DENTAL HYGIENE (non-driven toothbrushes A46B; {tongue scrapers A61B17/24;} preparations for dentistry A61K6/00; preparations for cleaning the teeth or mouth A61K8/00, A61Q11/00)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

The present application relates to topical compositions. In particular, the present application relates to a topical composition comprising retinoid as active agent, and pharmaceutically acceptable excipient(s), and a process of preparing such compositions. Further, the present application relates to method of using topical compositions for the treatment of skin disorders such as acne, rosacea, psoriasis etc.

## Claims

### Claim 1

A topical lotion composition, comprising:
a) a retinoid compound;
b) an oil phase comprising one or more water immiscible substances;
c) a hydrophilic phase comprising water;
d) a thickener;
e) one or more dermatologically acceptable excipient; and
f) one or more surfactants in the range from about 0.01% w/w to about 10% w/w of the total weight of the composition;
wherein the composition is free of propellant, and wherein the composition has pH from about 4 to about 7; wherein the composition excludes peanut oil.

### Claim 2 (depends on 1)

The topical composition of claim 1, wherein said retinoid compound is selected from tretinoin, isotretinoin, acitretin, tazarotene, and adapalene.

### Claim 3 (depends on 1)

The topical composition of claim 1, wherein the retinoid compound is tazarotene.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the retinoid compound is tretinoin.

### Claim 5 (depends on 1)

The topical composition of claim 1, wherein the retinoid compound is suspended in the composition.

### Claim 6 (depends on 1)

The topical composition of claim 1, wherein the particle size of the retinoid compound is less than about 50 microns.

### Claim 7 (depends on 1)

The topical composition of claim 1, wherein the composition comprises at least about 60% w/w water based on the total weight of the composition.

### Claim 8 (depends on 1)

The topical composition of claim 1, wherein D90 globule size of oil phase is at least 2 microns and less than about 50 microns.

### Claim 9 (depends on 1)

The topical composition of claim 1, wherein the thickener is selected from carbomers, polyvinyl pyrrolidone, locust gum, polyvinyl alcohol, cross-linked polyacrylate polymer, guar gum, locust bean gum, polysaccharides, cellulose polymers and any combinations thereof.

### Claim 10 (depends on 9)

The topical composition of claim 9, wherein the thickener comprises a carbomer.

### Claim 11 (depends on 1)

A method of treating the skin disorder comprising: administering the topical composition of claim 1, to a patient in need thereof, wherein the skin disorder is selected from acne vulgaris, rosacea, atopic dermatitis, skin wrinkles, facial mottle, hyperpigmentation, hypopigmentation, photo aging, papule, pustule, psoriasis, nodulocystic acne lesion and lentigo.

### Claim 12

A topical lotion composition comprising:
a) tretinoin or a pharmaceutically acceptable salt thereof;
b) at least one thickener comprising carbomer;
c) at least one preservative selected from the group consisting of benzyl alcohol, methylparaben, and combinations thereof;
d) an antioxidant comprising butylated hydroxytoluene;
e) a moisturizer comprising glycerin;
f) an emollient comprising mineral oil;
g) a pH adjusting agent comprising trolamine;
h) water; and
i) one or more surfactants in the range from about 0.01% w/w to about 10% w/w of the total weight of the composition, wherein the one or more surfactants have a hydrophilic/lipophilic balance (HLB) of more than 10, and wherein the composition excludes surfactants selected from cetyl alcohol and stearyl alcohol;
wherein the composition is free of propellant, and wherein the composition has pH from about 4 to about 7.

### Claim 13 (depends on 12)

The topical composition of claim 12, wherein the retinoid compound is suspended in the composition.

### Claim 14 (depends on 12)

The topical composition of claim 12, wherein the particle size of the retinoid compound is less than about 50 microns.

### Claim 15 (depends on 12)

The topical composition of claim 12, wherein the composition comprises at least about 60% w/w water based on the total weight of the composition.

### Claim 16 (depends on 12)

The topical composition of claim 12, wherein D90 globule size of oil phase is at least 2 microns and less than about 50 microns.

### Claim 17 (depends on 12)

The topical composition of claim 12, wherein the thickener is the range of from 0.01% to 2%.

### Claim 18 (depends on 12)

The topical composition of claim 12, wherein the composition has viscosity in the range of from about 1000 cps to about 50,000 cps, when measured by Brookfield DV-II pro Viscometer with low viscosity spindle no. 4 at 20 rpm.

### Claim 19 (depends on 12)

A method of treating the skin disorder comprising: administering the topical composition of claim 12, to a patient in need thereof, wherein the skin disorder is selected from acne vulgaris, rosacea, atopic dermatitis, skin wrinkles, facial mottle, hyperpigmentation, hypopigmentation, photo aging, papule, pustule, psoriasis, nodulocystic acne lesion and lentigo.

### Claim 20 (depends on 1)

The topical composition of claim 1, wherein the thickener is the range of from 0.01% to 2%.

### Claim 21

A topical lotion composition comprising:
a) a retinoid compound;
b) an oil phase comprising one or more water immiscible substances;
c) a hydrophilic phase comprising water;
d) a thickener; and
e) one or more dermatologically acceptable excipient;
wherein the composition is free of propellant;
wherein the thickener is selected from carbomers, polyvinyl pyrrolidone, locust gum, polyvinyl alcohol, cross-linked polyacrylate polymer, guar gum, locust bean gum, polysaccharides, cellulose polymers and any combinations thereof;
wherein the composition excludes peanut oil; and
wherein a substantial amount of retinoid compound is in hydrophilic phase.

### Claim 22

A topical lotion composition comprising:
a) tazarotene or a pharmaceutically acceptable salt thereof;
b) at least one thickener comprising carbomer;
c) at least one preservative selected from the group consisting of, methylparaben, propylparaben, and combinations thereof;
d) a chelating agent;
e) an emollient comprising mineral oil;
f) a pH adjusting agent; and
g) water;
wherein the composition is free of propellant;
wherein the composition excludes peanut oil; and
wherein a substantial amount of retinoid compound is in hydrophilic phase.

### Claim 23 (depends on 22)

The topical composition of claim 22, wherein the thickener is the range of from 0.01% to 2%.

### Claim 24 (depends on 22)

The composition of claim 22, wherein the pH adjusting agent comprises sodium hydroxide.

### Claim 25 (depends on 22)

The composition of claim 22, and further comprising one or more surfactants hydrophilic/lipophilic balance (HLB) of more than 10, and wherein the composition excludes surfactants selected from cetyl alcohol and stearyl alcohol.

### Claim 26 (depends on 1)

The composition of claim 1, and further comprising at least one preservative selected from the group consisting of benzyl alcohol, methylparaben, propylparaben, and mixtures thereof.

### Claim 27 (depends on 1)

The composition of claim 1, and further comprising a preservative comprising methylparaben.

### Claim 28 (depends on 1)

The composition of claim 1, and further comprising an emollient.

### Claim 29 (depends on 28)

The composition of claim 28, wherein the emollient comprises mineral oil.

### Claim 30 (depends on 1)

The composition of claim 1, and wherein the one or more surfactants have a hydrophilic/lipophilic balance (HLB) of more than 10, and wherein the composition excludes surfactants selected from cetyl alcohol and stearyl alcohol.

### Claim 31 (depends on 12)

The composition of claim 12, and further comprising an emollient.

### Claim 32 (depends on 31)

The composition of claim 31, wherein the emollient comprises mineral oil.

### Claim 33 (depends on 12)

The composition of claim 12, wherein the composition excludes peanut oil.

### Claim 34 (depends on 21)

The composition of claim 21, and further comprising at least one preservative selected from the group consisting of benzyl alcohol, methylparaben, propylparaben, and mixtures thereof.

### Claim 35 (depends on 21)

The composition of claim 21, and further comprising a preservative comprising methylparaben.

### Claim 36 (depends on 21)

The composition of claim 21, and further comprising an emollient.

### Claim 37 (depends on 36)

The composition of claim 36, wherein the emollient comprises mineral oil.

### Claim 38 (depends on 21)

The composition of claim 21, and further comprising one or more surfactants having a hydrophilic/lipophilic balance (HLB) of more than 10, and wherein the composition excludes surfactants selected from cetyl alcohol and stearyl alcohol.

### Claim 39 (depends on 1)

The composition of claim 1, wherein the composition has a viscosity in the range of from about 1000 cps to about 50,000 cps, when measured by Brookfield DV-II pro Viscometer with low viscosity spindle no. 4 at 20 rpm.

### Claim 40 (depends on 21)

The composition of claim 21, wherein the composition has a viscosity in the range of from about 1000 cps to about 50,000 cps, when measured by Brookfield DV-II pro Viscometer with low viscosity spindle no. 4 at 20 rpm.

### Claim 41 (depends on 22)

The composition of claim 22, wherein the composition has a viscosity in the range of from about 1000 cps to about 50,000 cps, when measured by Brookfield DV-II pro Viscometer with low viscosity spindle no. 4 at 20 rpm.