Pharmaceutical compositions comprising isotretinoin and processes for preparation and uses thereof
Inventors
Anvekar, Ashish • Vishnubhotla, Nagaprasad • Jana, Arun
Assignees
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Publication Number
US-12016830-B2
Publication Date
2024-06-25
Expiration Date
Abstract
The present invention provides a high-dose oral pharmaceutical composition and high drug loading of isotretinoin with low fill-weight, and smaller size capsules, and methods of preparation and use thereof.
Core Innovation
The invention relates to a capsule dosage form and a preparation method for a high dose oral pharmaceutical composition comprising isotretinoin or a pharmaceutically acceptable salt or ester thereof and at least one pharmaceutically acceptable excipient. The capsule dosage form includes a pharmaceutical composition containing at least 30 mg isotretinoin, wherein the size of the capsule is 1 to 4.
A core aspect of the disclosed capsule dosage form is the combination of isotretinoin with pharmaceutically acceptable excipients in a formulation suitable for high dose delivery while using small capsule sizes. Excipient components can include oily or lipid vehicle components, surfactants, co-surfactants, antioxidants, and optional co-solvents, together with capsule constraints such as small capsule size (1 to 4).
The disclosure further provides a preparation process for the high dose oral pharmaceutical composition. The process includes heating a mixture of oil, surfactant and co-surfactant, dissolving antioxidants to the mixture and then cooling to room temperature, dispersing isotretinoin under stirring, and optionally adding a co-solvent and optionally milling. The filled hard gelatin capsule is then banded using a gelatin banding solution prepared by soaking gelatin in water and adding polysorbate 80.
Claims Coverage
The document provides two independent claims: one directed to a capsule dosage form and one directed to a method for preparing a high dose oral pharmaceutical composition. The inventive features emphasize a small capsule size with at least 30 mg isotretinoin in a capsule dosage form containing a pharmaceutical excipient, and a staged preparation workflow followed by hard gelatin capsule banding with a gelatin banding solution.
High dose isotretinoin capsule dosage form with small capsule size
A capsule dosage form comprising a pharmaceutical composition comprising at least 30 mg of isotretinoin or a pharmaceutically acceptable salt or ester thereof and a pharmaceutically acceptable excipient, wherein the size of the capsule is 1 to 4.
Staged preparation and gelatin banding for high dose oral isotretinoin composition
A method for the preparation of a high dose oral pharmaceutical composition comprising isotretinoin or a pharmaceutically acceptable salt or ester thereof and at least one pharmaceutical excipient, comprising heating a mixture of oil, surfactant and co-surfactant; dissolving antioxidants and then cooling to room temperature; dispersing isotretinoin under stirring; optionally adding a co-solvent; optionally milling; filling the mixture into hard gelatin capsule; preparing a gelatin banding solution by soaking gelatin in water and adding polysorbate 80; and banding the filled capsule with banding solution.
Overall, the claims cover a high dose isotretinoin capsule dosage form using a small capsule size (1 to 4) with at least 30 mg isotretinoin plus a pharmaceutically acceptable excipient, and a staged formulation workflow followed by hard gelatin capsule banding using a gelatin banding solution prepared with soaked gelatin and polysorbate 80.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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