Piceatannol-3'-O-beta-D-glucopyranoside Formulation for Microcirculation Block
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Solution Overview
Problem
Current treatments for microcirculation block, such as cardiovascular and cerebrovascular diseases, often have limited effectiveness, significant side effects, and target specific organs rather than the entire microcirculatory system, making them inadequate for comprehensive treatment and prevention.
Innovation Solution
A pharmaceutical formulation comprising piceatannol-3'-o-β-d-glucopyranoside and gastrodin or water-soluble cyclodextrin derivatives is developed to improve microcirculation by enhancing solubility and bioavailability, addressing the poor solubility issues of piceatannol-3'-o-β-d-glucopyranoside, which is then used to treat microcirculation block induced by various causes including brain microvascular injury and ischemic reperfusion injury.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If current medicines for microcirculation block are used, then specific organ symptoms are targeted, but the treatment is limited to specific parts and does not address the whole microcirculatory system
Solution Approach 1:
The patent applies universality by developing a pharmaceutical composition that can treat microcirculation block across multiple organs and systems simultaneously. The composition is designed to improve microcirculation in the brain, heart, kidneys, and other organs through a single administration, rather than requiring organ-specific treatments. This multi-functional approach addresses the limitation of current medicines that target only specific organs.
2Reliability
If current medicines for microcirculation block are used, then some symptoms are treated, but they have strong toxic and side effects
Solution Approach 1:
The patent applies parameter changes by modifying the chemical parameters of the active ingredients through combination with gastrodin and water-soluble cyclodextrin derivatives. This changes the pharmacokinetic parameters including solubility, bioavailability, and toxicity profile. The composition achieves better therapeutic effectiveness while reducing toxic side effects through these parameter modifications.
3Reliability
If piceatannol-3'-o-β-d-glucopyranoside is used alone, then therapeutic effect is achieved, but solubility is poor limiting formulation and absorption
Solution Approach 1:
The patent applies the intermediary principle by introducing gastrodin and water-soluble cyclodextrin derivatives as mediator substances. These intermediaries enhance the solubility and bioavailability of piceatannol-3'-o-β-d-glucopyranoside without compromising its therapeutic effect. The mediators facilitate better formulation and absorption, resolving the contradiction between therapeutic effectiveness and ease of manufacture.
4Reliability
If early stage microcirculation block is treated, then prevention is possible, but symptoms are not obvious making it easy to overlook
Solution Approach 1:
The patent applies preliminary action by providing a pharmaceutical composition that can be administered in the early stages of microcirculation block before severe symptoms develop. The composition prevents progression to more serious conditions by improving microcirculation function proactively. The broad-spectrum action of the composition allows it to address subtle early-stage changes that are difficult to detect, enabling prevention before obvious symptoms appear.
Data Source
AI summary
Disclosed is an application of piceatannol-3'-O-β-D-glucopyranoside in the preparation of medicaments for improving microcirculation block. The medicaments comprise piceatannol-3'-O-β-D-glucopyranoside of formula (I) as active ingredients: and one or more pharmaceutically acceptable additives, especially of gastrodin and/or water soluble cyclodextrin derivatives, or PEG400 and mannitol. The invention also discloses applications of piceatannol-3'-O-β-D-glucopyranoside as active ingredients in the preparation of medicaments for improving block induced by brain microvascular injury and/or block induced by ischemical reperfusion injury and/or block induced by leucocyte adherence and/or block induced by peroxides. The invention tests the effects of medicaments by tail intravenous injection with Kunming normal mice and model mice with microcirculation block induced artificially. The capillary vessel net and the shrinkage of arteriole and venule are observed under microcirculation microscope. The test shows that: the medicament has obvious expansion effect on blood vessels of the normal mice, can evidently antagonize the shrinkage of arteriole and venule and the reduction of the open number of capillary vessel net of the model mice with microcirculation block, and can obviously confront the blood flow slowing.