Dual-Release HDAC Composition for Sustained Cancer Pretreatment
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing methods for administering HDAC inhibitors as pretreatment for cancer are inefficient and do not effectively maintain the required plasma concentration for an extended period, hindering the full potential of cancer pretreatment.
Innovation Solution
A pharmaceutical composition comprising HDAC inhibitors in both immediate and extended release formulations, with 70-90% in the immediate release and the remainder in the extended release, ensuring rapid attainment and sustained plasma concentration for at least 48 hours.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If only immediate release formulation is used, then rapid plasma concentration attainment is achieved, but plasma concentration cannot be maintained for extended period
Solution Approach 1:
The patent combines immediate release and extended release formulations into a single pharmaceutical composition. The immediate release portion rapidly delivers the HDAC inhibitor to achieve therapeutic plasma concentration quickly, while the extended release portion maintains this concentration over an extended period (at least 48 hours), resolving the contradiction between rapid attainment and sustained maintenance of plasma concentration.
Solution Approach 2:
The pharmaceutical composition uses a composite formulation approach, integrating two different release mechanisms (immediate and extended release) into one product. This composite structure allows the composition to exhibit both rapid initial release characteristics and prolonged sustained release characteristics, simultaneously achieving fast plasma concentration attainment and long-duration maintenance.
2Speed
If high dose of HDAC inhibitor is administered, then desired plasma concentration is reached quickly, but side effects increase
Solution Approach 1:
The extended release formulation provides continuous, controlled delivery of the HDAC inhibitor, maintaining therapeutic plasma concentration without requiring high initial doses. This continuous action at optimized levels achieves the desired effect while avoiding the peak concentration-related side effects that would result from high-dose immediate release administration.
Solution Approach 2:
The patent changes the release rate parameter of the HDAC inhibitor by using a dual formulation system. Instead of a single high-dose immediate release that causes side effects, the composition releases the drug at two different rates: a higher initial rate for rapid attainment followed by a controlled sustained rate for maintenance, thereby achieving therapeutic effect without excessive peak concentrations.
3Duration of action of moving object
If multiple administrations are required to maintain plasma concentration, then extended coverage is achieved, but treatment complexity increases
Solution Approach 1:
By merging immediate release and extended release formulations into a single pharmaceutical composition, the patent eliminates the need for multiple separate administrations. Patients receive one dose that provides both rapid plasma concentration attainment and sustained maintenance for at least 48 hours, significantly simplifying the treatment regimen while maintaining therapeutic effectiveness.
Data Source
Figure 1A
Figure 1B~1C
Figure 1D
AI summary
The present invention relates to a pharmaceutical composition comprising an HDAC inhibitor, a pharmaceutically acceptable acid or salt thereof or a mixture of the acid and salt, provided both in a immediate release form and in an extended release form wherein 70-90 weight % of the HDAC inhibitor is provided in the immediate release form and the remainder of the HDAC inhibitor is provided in the extended release form.. In further aspects the present invention relates to a kit comprising a number of doses of an HDAC inhibitor, a pharmaceutically acceptable acid or salt thereof or a mixture of the acid and salt thereof provided both in an immediate release form and in an extended release form. In still further aspects the present invention relates to an HDAC inhibitor, a pharmaceutically acceptable acid or salt thereof or a mixture of the acid and salt, provided in both an immediate release form and an extended release form, for use in a method of pretreating cancer, and a method of pretreating cancer using said HDAC inhibitor provided both in said immediate release form and said extended release form. Further aspects relate to combination treatment of cancer and to a dispenser for a blister pack.