Lanreotide Sustained Release Composition Optimizing Solubility
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Solution Overview
Problem
Current extended release formulations of lanreotide for treating conditions like acromegaly and neuroendocrine tumors require frequent administration, causing inconvenience and discomfort to patients, and there is a need for a formulation that provides sustained release for more than two months with high doses while maintaining a convenient injection volume.
Innovation Solution
A pharmaceutical composition comprising lanreotide as the active ingredient, a hydrosoluble co-solvent such as N-methyl-2-pyrrolidone, propylene glycol, or glycofurol, and a pH modifier, formulated to achieve a sustained release for at least two months with a high dose of lanreotide (e.g., 120 or 360 mg) in a volume of 2 mL or less, by optimizing solubility and injectability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If the amount of injected pharmaceutical active ingredient is increased to extend the duration of treatment for more than one month, then the duration of action is improved, but the injected volume increases causing discomfort to the patient
Solution Approach 1:
The patent changes the concentration parameter of lanreotide in the formulation, achieving high dose (120, 240 or 360 mg) in a small volume (≤2 mL) by optimizing the pharmaceutical composition parameters including co-solvent selection and pH adjustment
Solution Approach 2:
The patent uses a composite pharmaceutical formulation combining lanreotide with specific co-solvents (NMP, propylene glycol, glycofurol) and pH modifiers to create a sustained-release composition that maintains high drug concentration in minimal volume
2Reliability
If repeated injections are administered to maintain therapeutic levels, then the therapeutic efficacy is improved, but the inconvenience and discomfort to the patient increases
Solution Approach 1:
The patent implements excessive action by providing a single injection that delivers more than sufficient therapeutic dose (120, 240 or 360 mg) designed to last for at least 2 months, eliminating the need for repeated injections and thereby improving patient convenience while maintaining reliable therapeutic effect
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 composition enables a sustained release of lanreotide for up to two months with a high dose in a minimal injection volume, reducing patient discomfort and frequency of administration, while maintaining therapeutic efficacy.
Implementation Method 1
a hydrosoluble co-solvent present in a concentration ranging from 10 to 25 % by weight relative to the total weight of the composition, and selected from N-methyl-2-pyrrolidone (NMP), propylene glycol, glycerol, low molecular weight polyethylene glycols (PEG), glycofurol, ethanol
Data Source
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AI summary
The present invention relates to a pharmaceutical composition for a sustained release of lanreotide, in particular for a sustained release compatible with therapeutic treatments for at least 2 months. The pharmaceutical compositions are particularly useful for the treatment of diseases lanreotide is indicated for.