Cancer Tablet Composition for Higher Dose and pH Dissolution
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Solution Overview
Problem
Existing formulations of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide are limited by low dosage amounts, poor bioavailability, and inadequate dissolution at higher pH levels, necessitating improved pharmaceutical compositions for enhanced cancer treatment.
Innovation Solution
Development of tablets comprising 10-30% of the compound, combined with mannitol, microcrystalline cellulose, polyvinylpolypyrrolidone, and magnesium stearate, with specific intra- and extragranular phases, to enhance dosage and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If existing formulations of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide are used, then the compound can be administered, but the dosage amount is limited and bioavailability is poor
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation by using different salt forms (dihydrochloride, mesylate, trifluoroacetate) and adjusting the crystalline state of the compound. These parameter changes improve both the dosage amount that can be administered and the bioavailability, resolving the contradiction between quantity and reliability of drug delivery.
Solution Approach 2:
The patent creates composite pharmaceutical formulations by combining the active compound with various excipients, fillers, and binding agents in specific ratios. This composite approach enhances both the dosage capacity and bioavailability, allowing higher doses to be administered effectively while improving absorption and distribution in the body.
2Ease of manufacture
If existing formulations are used, then the compound can be administered, but dissolution at higher pH levels (pH 4.5-6.8) is inadequate
Solution Approach 1:
The patent addresses pH-dependent dissolution by changing the chemical form of the compound through salt selection (dihydrochloride, mesylate, trifluoroacetate salts) and controlling crystalline polymorphs. These parameter changes enable the formulation to maintain adequate dissolution across a broader pH range, particularly improving performance at higher pH levels (4.5-6.8) where existing formulations fail.
Data Source
AI summary
The present invention is related to tablets comprising of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, processes for the production thereof, and uses in the treatment of certain cancers.