Metastin Derivative Sustained-Release via Copolymer Matrix
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Solution Overview
Problem
Current sustained-release formulations for metastin derivatives are inadequate in reducing side effects, improving patient convenience, and maintaining prolonged medicinal effects, as they require frequent dosing and have instability issues.
Innovation Solution
A sustained-release formulation comprising a metastin derivative or its salt combined with a lactic acid-glycolic acid copolymer of specific molecular weight and composition, produced using a W/O/W emulsion method, which slowly releases the compound over an extended period, enhancing stability and reducing administration frequency.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If a sustained-release formulation is developed to reduce administration frequency, then patient convenience is improved, but formulation stability and release control become more difficult to achieve
Solution Approach 1:
The patent uses a composite material system consisting of a metastin derivative encapsulated within a lactic acid-glycolic acid copolymer matrix. This composite structure allows the formulation to maintain stability during storage while providing controlled sustained release over time, resolving the contradiction between ease of operation and reliability.
Solution Approach 2:
The patent optimizes specific parameters including the molecular weight of the lactic acid-glycolic acid copolymer (5,000-40,000) and the glycolic acid content (greater than 0 wt% and 60 wt% or less) to achieve the desired balance between formulation stability and sustained release performance, reducing administration frequency while maintaining reliability.
2Duration of action of moving object
If a sustained-release formulation is developed to maintain prolonged medicinal effects, then dosage frequency is reduced, but the complexity of achieving controlled release increases
Solution Approach 1:
The lactic acid-glycolic acid copolymer composite provides inherent controlled release properties through its biodegradable matrix structure, extending medicinal effect duration without requiring complex release mechanisms or additional components.
Solution Approach 2:
By controlling the molecular weight (5,000-40,000) and glycolic acid content (greater than 0 wt% and 60 wt% or less) of the copolymer, the patent achieves optimized controlled release profiles that extend medication duration while keeping the formulation relatively simple.
3Reliability
If high dosage amount is used to achieve medicinal effect, then therapeutic efficacy is improved, but side effects increase
Solution Approach 1:
The sustained-release formulation provides continuous release of the metastin derivative over an extended period, maintaining therapeutic blood concentrations without requiring high peak dosages that would cause side effects. This continuous action ensures reliable therapeutic efficacy at lower overall dosage amounts.
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 formulation achieves stable and prolonged release of the metastin derivative, improving patient convenience by reducing dosing frequency and maintaining effective blood concentrations for an extended duration, while minimizing side effects.
Implementation Method 1
a sustained-release formulation comprising a compound represented by Formula: Ac-D-Tyr-Hyp-Asn-Thr-Phe-AzaGly-Leu-Arg(Me)-Trp-NH2 (I) or a salt thereof and a lactic acid-glycolic acid copolymer having a weight average molecular weight of 5,000 to 40,000 or a salt thereof
Implementation Method 2
lactic acid-glycolic acid copolymer having a weight average molecular weight of 5,000 to 40,000
Implementation Method 3
produced by a method using a W/O/W emulsion
Implementation Method 4
subjecting the W/O/W emulsion to an in-water-drying method
Data Source
AI summary
The present invention relates to a sustained-release formulation comprising a metastin derivative and a lactic acid-glycolic acid copolymer having a weight average molecular weight of about 5,000 to about 40,000 or a salt thereof. The sustained-release formulation of the present invention slowly and stably release compound (I) or a salt thereof for a long time and exerts a medicinal effect of compound (I) or a salt thereof for a long time. Furthermore, the sustained-release formulation of the present invention, which improves patient's convenience by reducing the number of administration times, is an excellent formulation as a clinical medicine.