Bioabsorbable Pharmaceutical Formulation Sustained Drug Release
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Solution Overview
Problem
Current bioabsorbable pharmaceutical formulations fail to sustain the release of effective drug components for an extended period, often leading to rapid release after administration, which limits the duration and effectiveness of the drug's therapeutic action.
Innovation Solution
A bioabsorbable pharmaceutical formulation utilizing a lactic acid-glycolic acid copolymer with specific molecular weight fractions, allowing for controlled release of drugs like Luteinizing Hormone-Releasing Hormone (LH-RH) over a month to three months, maintaining therapeutic levels and minimizing side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If a conventional biodegradable polymer is used as a release sustaining base material, then the formulation is bioabsorbable and can be degraded in the body, but the drug component is released rapidly just after administration and cannot be sustained for at least a month at a defined rate
Solution Approach 1:
The patent applies parameter changes by precisely controlling the molecular weight distribution parameters of the lactic acid-glycolic acid copolymer. Specifically, it sets the weight-average molecular weight between 5,000-30,000 and the polydispersity index (weight-average/number-average molecular weight ratio) between 1.05-2.0. These parameter optimizations enable the polymer to provide sustained drug release for at least one month while maintaining reliable controlled release performance, resolving the contradiction between release duration and release control reliability.
Solution Approach 2:
The patent uses a lactic acid-glycolic acid copolymer as a composite material with specific compositional ratios. By adjusting the lactic acid content (50-95 wt%) and glycolic acid content (50-5 wt%), the formulation achieves both bioabsorbability and sustained drug release capability. The copolymer structure combines the advantages of both monomers to create a material that degrades at a controlled rate while maintaining structural integrity for sustained release.
2Quantity of substance
If the drug is released rapidly after administration, then the initial therapeutic effect is achieved, but the total dosage must be increased and side effects increase to maintain therapeutic levels over time
Solution Approach 1:
The patent implements continuity of useful action through sustained drug release over at least one month. The optimized copolymer formulation maintains a steady release rate, ensuring continuous therapeutic action without large fluctuations in drug concentration. This continuous release pattern reduces the need for repeated high-dose administrations, thereby lowering total dosage requirements and minimizing side effects associated with peak concentration fluctuations.
3Ease of operation
If the number of administrations is reduced, then patient compliance improves and treatment convenience increases, but maintaining therapeutic levels becomes more difficult without sustained release
Solution Approach 1:
The patent applies preliminary action by formulating the drug in advance with a sustained-release copolymer matrix that is designed to release the drug over an extended period. This pre-engineered formulation ensures that a single administration provides therapeutic effects lasting at least one month, eliminating the need for frequent re-administrations and improving patient compliance without compromising therapeutic efficacy.
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 ensures a sustained release of the drug at a defined rate, maintaining therapeutic efficacy while reducing the frequency and amount of drug administration, thereby minimizing side effects and optimizing drug utilization.
Implementation Method 1
a lactic acid-glycolic acid copolymer which has become famous as a biodegradable polymer compound... excellent as a biodegradable release-sustaining base material
Data Source
AI summary
A bioabsorbable release-sustaining pharmaceutical formulation using a biodegradable release-sustaining base material which can prevent an effective component drug from being released too rapidly just after administration of the formulation and then allow continued release of the drug for at least one month at a defined rate, is provided. For the biodegradable release-sustaining base material, a lactic acid-glycolic acid copolymer (PLGA) with an adjusted distribution in molecular weight is used.