Oral Suspension of Alkylating Agents for Stability and Palatability
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Solution Overview
Problem
Current oral solid dosage forms of antineoplastic alkylating agents are difficult for patients to swallow, especially post-surgery, and injectable forms are inconvenient for frequent administration, with alkylating agents also having a bitter taste and stability issues in liquid formulations.
Innovation Solution
Development of a flavored oral liquid suspension composition of antineoplastic alkylating agents with improved stability and palatability, using a combination of Temozolomide as the active ingredient along with antioxidants, preservatives, surfactants, sweeteners, and flavoring agents, stabilized by medium chain triglycerides and colloidal silicone dioxide, to mask the bitter taste and ensure bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oral solid dosage forms are used, then stability is maintained, but patient compliance deteriorates due to difficulty in swallowing
Solution Approach 1:
The patent transforms the physical state of the medication from solid capsules to liquid suspension form. This parameter change allows the drug to be administered orally without swallowing difficulties while maintaining stability through specific formulation techniques including use of antioxidants and pH control
Solution Approach 2:
The patent creates a composite liquid formulation combining Temozolomide with multiple excipients including suspending agents, antioxidants, pH adjusters, and flavoring agents. This composite approach ensures both stability and improved patient compliance through enhanced palatability and ease of administration
2Ease of operation
If injectable forms are used, then patient compliance improves for liquid administration, but device complexity and medical staff requirement increase
Solution Approach 1:
The patent develops a self-administerable oral liquid suspension that patients can take at home without requiring hospitalization or medical staff intervention. The formulation is designed for direct oral administration, eliminating the need for injection equipment and professional administration
3Reliability
If solid dosage forms are used, then stability is maintained, but taste masking becomes difficult
Solution Approach 1:
The patent introduces flavoring agents and sweeteners as intermediary substances that mask the bitter taste of Temozolomide. These additives act as mediators between the drug and patient's taste receptors, hiding the unpleasant taste while the drug maintains its therapeutic effect
Solution Approach 2:
The patent changes the physical form from solid to liquid suspension, which allows for better incorporation of flavoring agents and sweeteners. The liquid medium enables more effective taste masking compared to solid dosage forms
Data Source
AI summary
The present invention provides pharmaceutical composition of antineoplastic alkylating agent in oral suspension dosage form. The oral suspension composition comprises of alkylating agent with other pharmaceutical excipients such as vehicle, preservative, antioxidant, suspending agent, surfactant, sweetener and flavouring agent. The present invention is an oral suspension having improved stability and palatability. The present invention also provides oral solution with flavor that has masked bitter taste of the drug. Further, the present invention also provides a process for preparation thereof.