Enteric-Coated Capsule for Targeted Intestinal Drug Release
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current methods for administering N-methylol transfer agents like Taurolidine and Taurultam for neoplastic and infectious diseases require long-term intravenous infusions, which are inconvenient and pose risks, limiting the effectiveness of oral treatment options.
Innovation Solution
Development of an oral pharmaceutical composition using an enteric-coated capsule that releases the N-methylol transfer agent at a pH of 5.4 to 6.5, allowing targeted delivery to the duodenum or jejunum, where it enters the bloodstream, achieving effective blood concentrations without the need for invasive administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If intravenous infusion is used to administer N-methylol transfer agents, then sufficient blood concentrations can be achieved for effective treatment, but the treatment becomes inconvenient and poses risks for long-term administration
Solution Approach 1:
The invention segments the administration process by using oral capsules containing N-methylol transfer agents that are released in the intestine rather than requiring continuous intravenous infusion. This divides the treatment into discrete oral doses that can be taken at home, eliminating the need for hospital-based IV infrastructure while maintaining therapeutic blood concentrations.
Solution Approach 2:
The invention introduces an intermediary mechanism - an orally administered capsule with enteric coating - that mediates between the need for sufficient blood concentration and administration convenience. The capsule protects the agent during gastric passage and enables controlled release in the intestine, serving as a bridge between oral and intravenous administration modes.
2Quantity of substance
If large volumes of Taurolidine solution are administered intravenously, then adequate drug concentration can be achieved, but the large volume administration causes practical difficulties and lacks electrolytes
Solution Approach 1:
The invention changes the administration parameters from large-volume intravenous infusion to small-volume oral capsule administration. The enteric-coated capsule delivers the drug in a compact form that is released in the intestine, eliminating the need for large fluid volumes and associated infrastructure while maintaining adequate drug concentration through controlled release.
3Ease of operation
If oral administration is used to avoid invasive procedures, then convenience is improved, but achieving sufficient blood concentrations becomes difficult
Solution Approach 1:
The invention applies preliminary action by pre-coating the capsule with enteric material before administration. This preliminary protective coating ensures the capsule survives gastric conditions intact and releases the agent in the intestine, where absorption occurs more efficiently. This pre-prepared state enables oral administration to reliably achieve sufficient blood concentrations without requiring invasive procedures.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
This approach enables oral administration of Taurolidine and Taurultam to achieve serum concentrations sufficient for treating neoplastic diseases, reducing tumor growth and inhibiting angiogenesis, while avoiding gastric degradation and intestinal flora interaction, thus providing a more convenient and effective treatment option.
Implementation Method 1
the targeted release carrier releases the N-methylol transfer agent at a pH value of 5.4 to 6.5
Implementation Method 2
an enteric coated hard gelatine capsule or an enteric coated hydroxypropylmethyl cellulose (HPMC) capsule
Implementation Method 3
said agent enters the subject's bloodstream through said duodenum or jejunum
Implementation Method 4
which involves a cross-linking reaction with the cell wall of bacteria and with tumor cells
Data Source
AI summary
It now has been found that oral administration of pharmaceutical agents, including N-methylol transfer agents such as Taurolidine may be used to provide efficacious blood plasma concentration of the agents for treatment of diseases by providing release of the active agent into the duodenum or jejunum of a patient and/or at a pH of about 5.4 to about 6.5. Embodiments of the invention therefore provide oral dosage forms, compositions and methods for administration of pharmaceutical agents to the duodenum or jejunum of a patient, and/or which release at a pH of about 5.4 to about 6.5.