Topical pharmaceutical composition of acitretin

Patent metadata

Field	Value
Publication number	US-10342774-B2
Application number	US-201816100736-A
Country	US
Kind code	B2
Filing date	Aug 10, 2018
Priority date	Oct 31, 2013
Publication date	Jul 9, 2019
Grant date	Jul 9, 2019

Abstract

The present invention relates to a topical pharmaceutical composition comprising acitretin and a process for its preparation. It also relates to a method of treating skin disorders by administering said topical pharmaceutical composition.

First claim

We claim:

1. A stable topical pharmaceutical composition of acitretin comprising a therapeutically effective amount of acitretin from about 0.02% w/w to about 0.2% w/w based on the total weight of the composition and one or more gelling agents.

2. The stable topical pharmaceutical composition of claim 1 , wherein the gelling agent is present in an amount from about 0.05% w/w to about 10% w/w based on the total weight of the composition.

3. The stable topical pharmaceutical composition of claim 1 , wherein the gelling agent is selected from the group comprising carboxyvinyl polymers, natural gums, cellulose derivatives, acrylates, alginic acid-propylene glycol ester, polyoxyethylene-polyoxypropylene copolymers, polyvinyl pyrrolidone, polyethylene glycol, polyethylene oxide, polyvinyl alcohol, silicon dioxide, and mixtures thereof.

4. The stable topical pharmaceutical composition of claim 3 , wherein the gelling agent is a carboxyvinyl polymer.

5. The stable topical pharmaceutical composition of claim 1 , wherein the composition further comprises a solvent, a co-solvent, percutaneous absorption enhancers, antioxidants, preservatives, chelating agents, surfactants, pH-adjusting agents, humectants, fragrances, and mixtures thereof.

6. The stable topical pharmaceutical composition of claim 5 , wherein the solvent is selected from the group comprising water, white soft paraffin, light liquid paraffin, heavy liquid paraffin, mineral oil, hydrocarbon oil, ester oil, triglyceride oil, oil of plant origin, oil of animal origin, unsaturated or polyunsaturated oil, essential oil, silicone oil, and mixtures thereof.

7. The stable topical pharmaceutical composition of claim 6 , wherein the solvent is water.

8. The stable topical pharmaceutical composition of claim 5 , wherein the co-solvent is selected from the group comprising diethylene glycol monoethyl ether, propylene glycol, polyethylene glycol, glycerin, dimethyl isosorbide, isopropyl myristate, isopropyl palmitate, isopropyl stearate, ethyl oleate, capric acid, lauric acid, myristic acid, oleic acid, linoleic acid, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, and mixtures thereof.

9. The stable topical pharmaceutical composition of claim 8 , wherein the co-solvent is a combination of diethylene glycol monoethyl ether, dimethyl isosorbide; and polysorbate 80.

10. The stable topical pharmaceutical composition of claim 9 , wherein diethylene glycol monoethyl ether is present in a range of about 20% to about 30% w/w based on the total weight of the composition.

11. The stable topical pharmaceutical composition of claim 9 , wherein dimethyl isosorbide is present in a range of about 1% to about 10% w/w based on the total weight of the composition.

12. The stable topical pharmaceutical composition of claim 9 , wherein polysorbate 80 is present in a range of about 0.1% to about 5% w/w based on the total weight of the composition.

13. A stable topical pharmaceutical composition effective for treating psoriasis comprising from about 0.02% w/w to about 0.2% w/w of acitretin based on total weight of the composition, wherein the composition exhibits reduced skin irritancy in comparison to marketed tazorotene 0.1% gel using a Rhino Mouse Model.

Assignees

• Sun Pharmaceutical Ind Ltd

Inventors

• Venkateshwaran Rathinasabapathy
• Jain Vikas
• Dubey Vaibhav
• Madan Sumit
• Arora Vinod Kumar
• Rao Rajesh

Classifications

• A61K47/26

  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 title

• A61K9/0014

  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) · CPC title

• A61K31/202 Primary

  having three or more double bonds, e.g. linolenic (eicosanoids, e.g. leukotrienes A61K31/557) · CPC title

• A61K47/32

  Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} · CPC title

• A61K9/06

  Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} · CPC title