Pharmaceutical composition for oral administration comprising high concentration taxane
Inventors
Lee, In-Hyun • Son, Min-hee • Park, Yeong-Taek • LEE, Han-Koo
Assignees
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Publication Number
US-11020370-B2
Publication Date
2021-06-01
Expiration Date
Abstract
The present invention provides a pharmaceutical composition for oral administration, comprising (a) 4 to 40% by weight of a taxane, (b) 10 to 30% by weight of a medium chain triglyceride, (c) 30 to 70% by weight of monooleoyl glycerol, (d) 5 to 30% by weight of a surfactant, and (e) 10 to 30% by weight of polyoxyl glyceryl fatty acid ester and a process for preparing the same.
Core Innovation
The invention relates to an oral high-concentration taxane formulation comprising paclitaxel or docetaxel and defined lipid and surfactant components, where the formulation is present as a clear solution suitable for filling in soft capsules. The formulation includes a specified amount of medium chain triglyceride selected from listed triglycerides, and a specified amount of monooleoyl glycerol. The formulation further includes specific surfactant and solubilizing components intended to maintain clarity and avoid precipitation.
The formulation includes polyoxyethylene(80) sorbitan monooleate as a surfactant and includes polyoxyl glyceryl fatty acid ester selected from caprylocaproyl polyoxyl glyceride, lauroyl polyoxyl glyceride, and stearoyl polyoxyl glyceride. The inclusion of polyoxyl glyceryl fatty acid ester in combination with the medium chain triglyceride and monooleoyl glycerol in the claimed composition ranges provides a clear, precipitate-free high-concentration solution. Comparative examples describe opaque dispersions and white precipitate when alternative compositions are used.
Soft gelatin capsules are described as being filled with the clear solution, with the document including stability information for capsules over a storage period. The stability and appearance of the filled soft capsules are supported by qualitative appearance figures and data comparing clear solutions against comparative dispersions that show precipitates. The described formulation is positioned to enable high-concentration oral taxane dosing in a capsule form while maintaining a clear appearance.
Claims Coverage
The independent claim covers a soft capsule filled with a clear solution comprising five components—paclitaxel or docetaxel, a defined medium chain triglyceride, monooleoyl glycerol, polyoxyethylene(80) sorbitan monooleate as a surfactant, and a defined polyoxyl glyceryl fatty acid ester—each with specific weight ranges. Dependent claims further refine the specific polyoxyl glyceryl fatty acid ester members and narrow ingredient percentage ranges simultaneously.
A soft capsule filled with a clear solution
A soft capsule filled with a clear solution consisting of paclitaxel or docetaxel (4 to 40% by weight), a medium chain triglyceride selected from the listed group (10 to 30% by weight), monooleoyl glycerol (30 to 70% by weight), polyoxyethylene(80) sorbitan monooleate as a surfactant (5 to 30% by weight), and polyoxyl glyceryl fatty acid ester selected from the listed group (10 to 30% by weight).
Using polyoxyl glyceryl fatty acid ester polyoxyl-32 variants
The soft capsule of claim 1 wherein the polyoxyl glyceryl fatty acid ester is selected from caprylocaproyl polyoxyl-32 glyceride, lauroyl polyoxyl-32 glyceride, and stearoyl polyoxyl-32 glyceride.
Tightening multiple ingredient weight ranges simultaneously
A composition defined by specific weight percentages of paclitaxel or docetaxel (4 to 25%), a medium chain triglyceride (10 to 20%), monooleoyl glycerol (40 to 60%), polyoxyethylene(80) sorbitan monooleate (10 to 25%), and a polyoxyl glyceryl fatty acid ester (10 to 20%).
Overall claim coverage centers on a soft capsule containing a clear, precipitate-free high-concentration solution of paclitaxel or docetaxel achieved by using specified ranges of medium chain triglyceride and monooleoyl glycerol together with polyoxyethylene(80) sorbitan monooleate and a defined polyoxyl glyceryl fatty acid ester, further refined by selecting polyoxyl-32 variants and narrowing composition ranges.
Stated Advantages
Provides a clear, precipitate-free high-concentration solution suitable for soft capsule filling.
Capsules maintain clear appearance over the documented stability period (reported as 6 months).
Documented Applications
Oral high-concentration taxane formulations where paclitaxel or docetaxel is provided in soft capsules as a clear solution.
Soft gelatin capsule filling for paclitaxel or docetaxel compositions using the claimed lipid/surfactant system.
Stability assessment of the filled soft capsules over 6 months, including qualitative appearance evaluation.
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