# US 9,750,711 B2 · Low dose oral pharmaceutical composition of isotretinoin

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- Number: US 9,750,711 B2
- Document ID: US9750711B2
- Status: Granted
- Kind: B2
- Application number: 15/444,571
- Filed: 2017-02-28
- Published: 2017-06-15
- Granted: 2017-09-05
- Earliest claimed: 2014-10-01
- Assignees: Sun Pharmaceutical Industries Limited
- Applicants: Sun Pharmaceutical Industries Limited
- Inventors: Harish Kumar Madan; Rathinasabapathy Venkateshwaran; Sumit Madan; Ravi Kochhar
- Web page: https://patentgrep.com/patent/US9750711B2

## CPC

- A61K 31/203: Retinoic acids {; Salts thereof}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/148: {with compounds of unknown constitution, e.g. material from plants or animals (with oils, fats, waxes, shellac A61K9/145)}
- A61K 9/4858: {Organic compounds}
- A61K 9/4875: {Compounds of unknown constitution, e.g. material from plants or animals (oils, fats, waxes, shellac A61K9/4858)}
- 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)

## Abstract

The present invention provides a low dose oral pharmaceutical composition of isotretinoin having reduced food effect, in particular no food effect. The present invention further relates to a process for preparing the oral pharmaceutical composition of the present invention.

## Claims

### Claim 1

An oral pharmaceutical composition in the form of a capsule comprising isotretinoin and a pharmaceutically acceptable excipient, wherein the composition has a mean Cmax value in the range of about 9 ng/mL/mg to about 40 ng/mL/mg when administered in a dose of about 0.4 mg/kg to about 1.6 mg/kg of the body weight in a human subjects under fasting conditions.

### Claim 2 (depends on 1)

The oral pharmaceutical composition in the form of a capsule of isotretinoin according to claim 1 wherein the composition has AUC0-t in the range of about 125 ng·h/mL/mg to about 500 ng·h/mL/mg under fasting condition.

### Claim 3 (depends on 2)

The oral pharmaceutical composition in the form of a capsule of isotretinoin according to claim 2 wherein composition exhibits mean fed/fasted ratio of AUC0-t value of about 0.9 to about 1.40.

### Claim 4 (depends on 1)

The oral pharmaceutical composition in the form of a capsule composition according to claim 1 wherein the composition is in the form of a dispersion which is further filled into the capsules.

### Claim 5 (depends on 1)

The oral pharmaceutical composition in the form of a capsule composition according to claim 1 wherein the isotretinoin is micronized and has D90 less than 30 μm.

### Claim 6 (depends on 1)

The oral pharmaceutical composition in the form of a capsule composition according to claim 1 wherein the isotretinoin is present in an amount of about 5.5% to about 15% based on the total weight of the composition.

### Claim 7 (depends on 1)

The oral pharmaceutical composition in the form of a capsule composition according to claim 1 wherein the composition further comprises a surfactant.

### Claim 8 (depends on 7)

The oral pharmaceutical composition in the form of a capsule composition according to claim 7 wherein the surfactant is selected from the group consisting of anionic, cationic or non-ionic surfactants, sorbitan fatty acid esters; polysorbates; mononylphenyl ethers of polyethyleneglycols; dioctyl sodium sulfosuccinate, sodium lauryl sulphate, lecithin, fatty acid esters of propylene glycol, fatty acid esters of glycerol, poloxamers, and mixtures thereof.

### Claim 9 (depends on 1)

The oral pharmaceutical composition in the form of a capsule according to claim 1, wherein the composition releases not less than 50% of isotretinoin in 15 minutes when measured in United States Pharmacopeia (USP) type II dissolution apparatus, paddle at 75 rpm, in 900 mL of pH 7.4 phosphate buffer with 70 mg/L pancreatin and 4.5% LDAO as 30% solution with spiral coated sinker.