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-12527750-B2
Publication Date
2026-01-20
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 high-dose oral isotretinoin capsule composition designed for smaller capsule sizes and reduced fill weight while maintaining required quality attributes. The capsule composition includes isotretinoin or a pharmaceutically acceptable salt or ester of isotretinoin, an oily/lipid vehicle, a surfactant, a co-surfactant, and antioxidants, and the concentration of isotretinoin in the composition is at least 20% w/w.
The formulation is characterized by high isotretinoin concentration and defined ratios and fill constraints to achieve high-dose and high drug load performance in capsule form. It further specifies capsule fill volume limits and isotretinoin concentration ranges, along with acceptable particle size distribution parameters using D10/D50/D90.
The invention also defines stability and impurity/related-substance constraints for the capsule composition. Storage stability is described using ICH conditions at defined temperatures and relative humidities for at least three months, and impurity criteria include total related substances at or below 1.5% and specific impurities such as tretinoin and impurity G. The partial content also reports pharmacokinetic comparison data versus ABSORICA® alongside dissolution and clinical PK studies.
Claims Coverage
Independent claim clm-00001 covers one inventive feature centered on a capsule composition with an isotretinoin concentration of at least 20% w/w, together with an oily/lipid vehicle, a surfactant, a co-surfactant, and antioxidants. Dependent claims add further constraints including fill volume limits, surfactant concentration ranges, storage stability at defined ICH conditions for at least three months, and impurity/related-substance limits including specific impurity identities.
High concentration isotretinoin capsule composition with oily/lipid vehicle and dual surface-active components
A capsule composition comprising isotretinoin or a pharmaceutically acceptable salt or ester thereof, an oily/lipid vehicle, a surfactant, a co-surfactant, and antioxidant(s), wherein the concentration of isotretinoin in the composition is at least 20% w/w.
The independent coverage is anchored on a capsule composition that combines isotretinoin or its salt/ester with an oily/lipid vehicle, a surfactant, a co-surfactant, and antioxidants, while meeting an isotretinoin concentration of at least 20% w/w. Dependent claims further narrow the formulation space with capsule fill volume limits, surfactant concentration ranges, storage stability duration under defined temperature and relative humidity, and impurity/related-substance criteria with particular impurities.
Stated Advantages
Designed for smaller capsule sizes and reduced fill weight while maintaining required quality attributes.
High-dose and high drug load performance in capsule form.
Documented Applications
Oral isotretinoin capsule composition.
Pharmacokinetic comparison data, dissolution, and clinical PK studies versus ABSORICA®.
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