Drotaverine Controlled-Release Formulation for Degradation-Stable Dosing
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Solution Overview
Problem
Existing formulations of Drotaverine are susceptible to oxidative and hydrolytic degradation, and there is a need for a controlled release formulation that provides stable, prolonged drug delivery to improve patient compliance and reduce dosing frequency.
Innovation Solution
Development of controlled release formulations of Drotaverine or its salts using polymers and acidifying agents, which release the drug in a biphasic manner, ensuring immediate and sustained release over 12-24 hours, reducing the dosing frequency to once or twice a day.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If drotaverine is formulated as a controlled release formulation, then the duration of action is extended, but the manufacturing precision requirements increase
Solution Approach 1:
The patent changes the physical-chemical parameters of drotaverine by forming salts with specific counterions (e.g., drotaverine hydrochloride, drotaverine sulfate) and adjusting the crystalline structure through controlled crystallization processes. This allows extended duration of action while maintaining manufacturability through standardized pharmaceutical techniques.
Solution Approach 2:
The patent creates composite formulations by combining drotaverine with specific excipients and using controlled release matrices (such as hydrophilic matrices or coated tablets). These composite structures enable extended duration of action through controlled drug release while following conventional manufacturing protocols.
2Loss of time
If drotaverine is formulated as a controlled release formulation, then the frequency of administration is reduced, but the device complexity increases
Solution Approach 1:
The patent segments the drug release mechanism into distinct phases (initial release and sustained release) using multi-layer tablet structures or core-coating systems. This segmentation achieves reduced administration frequency through controlled release while maintaining relatively simple manufacturing processes using conventional tablet pressing and coating techniques.
Solution Approach 2:
The patent introduces intermediary substances (excipients, coating materials, or matrix components) that mediate between the drotaverine and the body. These intermediaries control the release rate and extend duration of action without requiring complex delivery systems, using instead standard pharmaceutical excipients and coating materials.
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
The formulations achieve uniform plasma levels, reduce pill burden, and improve patient compliance by maintaining therapeutic effects for extended periods with reduced side effects.
Implementation Method 1
Controlled release formulations comprising drotaverine or salt thereof. The controlled release formulation provides sustained release of the active substance over an extended period, thereby reducing the frequency of administration.
Implementation Method 2
The controlled release formulation provides sustained release of the active substance over an extended period, thereby reducing the frequency of administration and helping to maintain plasma concentrations within a specific range.
Data Source
Figure 1
AI summary
The present invention provides controlled release formulations comprising Drotaverine or salt thereof or similar active agents which are prone to oxidative/hydrolytic degradation. The invention provides once or twice a day controlled release formulations of Drotaverine or salt thereof which avoids fluctuations of plasma levels, reduces pill burden and side effects owing to simplified dosage schedule, thereby improving patient compliance. The invention also provides methods of preparation of controlled release formulations of Drotaverine or salt thereof. The invention further provides controlled-release formulations of Drotaverine or salt thereof for treating at least one symptom of gastrointestinal, biliary, urological and gynecological disorders characterized by spastic conditions of smooth muscles in a subject.