Ginseng Extract Oral Preparation Dissolution
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Solution Overview
Problem
Natural product extracts, such as ginseng extracts, face challenges with low solubility and disintegrability in water, leading to poor bioavailability and effectiveness in oral preparations due to their low solubility and aggregation in water-based solvents.
Innovation Solution
An oral preparation comprising a solubilizer mixture of poloxamer and polyethylene glycol, a water-insoluble diluent like dicalcium phosphate, a lubricant such as silicon dioxide, and a disintegrant like crospovidone, which improves the solubility and dispersibility of the natural product extract, specifically processed ginseng extract, enhancing its dissolution rate and disintegrability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If natural product extract is used in oral preparation, then therapeutic effects are provided, but dissolution rate and disintegrability are poor due to low solubility in water
Solution Approach 1:
The patent uses solubilizing agents (poloxamer 407, polyethylene glycol 4000) as intermediaries to bridge the gap between water-soluble oral preparation matrix and water-insoluble natural product extract (ginseng extract). These solubilizing agents form micellar structures that encapsulate the hydrophobic ginseng saponins, enabling them to dissolve in the aqueous environment of the oral preparation while maintaining their therapeutic activity.
Solution Approach 2:
The patent changes the physical-chemical parameters of the natural product extract by controlling the saponin content (60-80% of total extract) and using enzymatic hydrolysis to convert insoluble ginseng saponins into more soluble forms. This parameter optimization transforms the extract from poorly soluble to adequately soluble in the oral preparation medium, resolving the dissolution rate issue while preserving therapeutic effects.
2Reliability
If natural product extract is used in oral preparation, then therapeutic effects are provided, but disintegrability is poor due to aggregation in water-based solvents
Solution Approach 1:
The patent employs disintegrating agents (sodium starch glycolate, crospovidone) as intermediaries that create physical separation between aggregated natural product extract particles. These agents absorb water and expand, mechanically breaking apart aggregates and facilitating disintegration of the oral preparation, thereby improving the release of therapeutic compounds without altering their structure or activity.
Solution Approach 2:
The patent utilizes porous excipients (dicalcium phosphate, cellulose) that create a porous matrix structure in the oral preparation. This porous structure prevents dense aggregation of the natural product extract, allowing water penetration and facilitating rapid disintegration. The porous architecture provides channels for fluid penetration and maintains physical separation of extract particles, resolving the aggregation issue while preserving 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 oral preparation significantly increases the bioavailability of the natural product extract by enhancing its dissolution rate and disintegrability, ensuring the extract is disintegrated within 5 minutes and maintaining stability during storage, with a dissolution rate of 85% or more within 60 minutes.
Implementation Method 1
the solubilizer is a mixture of a poloxamer and polyethylene glycol (PEG), the poloxamer and polyethylene glycol being mixed at a weight ratio of 1-10:1-10
Implementation Method 2
the disintegrant is at least one selected from the group consisting of crospovidone and sodium croscamellose
Data Source
Figure 1(A)~2(B)
Figure 3(A)~4(B)
Figure 5~6(B)
AI summary
The present invention relates to an oral preparation having an improved dissolution rate and disintegration properties for a natural substance extract, the oral preparation comprising poloxamer, as a solubilizer, and a water-insoluble diluent as main components in a processed ginseng extract, which is a representative natural substance extract, which contains increased amounts of ginsenoside Rg3 and Rh2 components which are trace amounts of ginsenoside components, and a configuration of additionally mixing-in a lubricant, a water-soluble diluent and a disintegrating agent has been confirmed, and in the oral preparation produced by said confirmed configuration, improvement in the dissolution rate and disintegration properties of the processed ginseng extract has been confirmed, and the maintaining of the improved dissolution rate and disintegration properties even during long-term storage has been confirmed, and thus the natural substance extract-containing preparation having an improved dissolution rate and disintegration properties of the present invention may be used to increase the bioavailability of the natural substance extract, and thus the preparation is expected to be usable for the development of an oral preparation having an increased physiological effect.