Pharmaceutical composition for oral administration comprising taxane
Inventors
Lee, In-Hyun • Son, Min-hee • Park, Yeong-Taek • LEE, Seul-Ae • LEE, Han-Koo
Assignees
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Publication Number
US-10653663-B2
Publication Date
2020-05-19
Expiration Date
Abstract
Provided is a pharmaceutical composition for oral administration, including (a) a taxane, (b) a medium chain triglyceride, (c) an oleoyl glycerol complex having 30 to 65% by weight of monooleoyl glycerol contents; 15 to 50% by weight of dioleoyl glycerol contents; and 2 to 20% by weight of trioleoyl glycerol contents, (d) a surfactant, and optionally (e) polyoxyl glyceryl fatty acid ester and a process for preparing the same.
Core Innovation
The invention relates to an oral pharmaceutical composition comprising paclitaxel or docetaxel, a medium chain triglyceride, and an oleoyl glycerol complex. The oleoyl glycerol complex contains monooleoyl glycerol, dioleoyl glycerol, and trioleoyl glycerol in specified weight fraction ranges, and the composition further comprises a surfactant selected from specified groups, optionally accompanied by polyoxyl glyceryl fatty acid ester.
The pharmaceutical composition is defined to be a clear solution form at room temperature and is changed to a clear solution form when allowed to stand at room temperature after being stored at 4°C. The formulation is characterized as essentially consisting of the stated percentages of paclitaxel or docetaxel, medium chain triglyceride, oleoyl glycerol complex, and the specified surfactant.
The disclosed examples and comparative observations indicate that the temperature-dependent appearance behavior is a key aspect of the composition. The document describes comparison with a monoolein condition showing different appearance changes, and it further reports clear solution formation behavior after cold storage followed by standing at room temperature.
Claims Coverage
The partial content provides one independent claim (clm-00001). The claim includes inventive features centered on the specific composition percentages and the temperature/appearance requirement for a clear solution form after storage at 4°C and standing at room temperature, with dependent claims further refining component ranges and the medium chain triglyceride selection.
Clear-solution oral taxane composition with defined oleoyl glycerol complex fractions
A pharmaceutical composition for oral administration consisting essentially of paclitaxel or docetaxel; a medium chain triglyceride; an oleoyl glycerol complex having 30 to 65% by weight of monooleoyl glycerol contents, 15 to 50% by weight of dioleoyl glycerol contents, and 2 to 20% by weight of trioleoyl glycerol contents; and a surfactant selected from polyoxyethylene-polyoxypropylene block copolymer, sorbitan ester, polyoxyethylene sorbitan, and polyoxyethylene ether, where the pharmaceutical composition is in a clear solution form at room temperature and is changed to a clear solution form when allowed to stand at room temperature after being stored at 4°C.
Across the independent claim and its dependent refinements, the coverage is directed to an oral paclitaxel/docetaxel composition with an oleoyl glycerol complex defined by specific monooleoyl/dioleoyl/trioleoyl glycerol weight fraction ranges, plus a specified surfactant, combined with a clear-solution temperature/standing requirement after cold storage. Dependent claims further constrain the oleoyl glycerol complex component ranges and restrict the medium chain triglyceride to selected named compounds.
Stated Advantages
Maintains a clear solution form at room temperature and after being stored at 4°C followed by standing at room temperature.
Enables changing to a clear solution form after cold storage followed by standing at room temperature.
Documented Applications
Oral administration of paclitaxel or docetaxel as a pharmaceutical composition.
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