Inhaled Magnesium Isoglycyrrhizinate for Bioavailability and Low Aggregation
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Solution Overview
Problem
Current treatments for chronic obstructive pulmonary disease (COPD) and chronic viral hepatitis lack effective preparations that can improve bioavailability and reduce side effects, while existing inhaled preparations face challenges with drug aggregation and absorption issues.
Innovation Solution
Development of an inhaled preparation of magnesium isoglycyrrhizinate with controlled particle size (0.5-10 um) and suitable carriers (ground/sieved/fine lactose) to enhance pulmonary deposition and systemic absorption, and a liquid preparation for nebulizers with isotonicity and pH adjustment for improved bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If intravenous injection of magnesium isoglycyrrhizinate is used to treat chronic viral hepatitis, then timely treatment effect is achieved, but patient compliance deteriorates due to infusion reactions, vascular stimulation and phlebitis
Solution Approach 1:
The patent changes the administration route from intravenous injection to inhaled preparation, fundamentally altering the delivery parameter. The inhaled preparation delivers magnesium isoglycyrrhizinate directly to the lungs where it is rapidly absorbed into the bloodstream, achieving timely treatment effect while avoiding infusion reactions, vascular stimulation and phlebitis associated with intravenous administration
Solution Approach 2:
The patent introduces the lungs as an intermediary organ for drug absorption. Instead of direct intravenous injection, the drug is inhaled and absorbed through the pulmonary alveoli, which serve as a mediator to deliver the drug systemically while bypassing the problematic intravenous administration route and its associated side effects
2Loss of time
If oral administration of diammonium glycyrrhizinate is used for sequential therapy, then hospitalization time is reduced, but bioavailability deteriorates leading to low therapeutic effect
Solution Approach 1:
The patent changes the administration route from oral to inhaled, fundamentally altering the delivery parameter. The inhaled preparation achieves rapid pulmonary absorption and high systemic bioavailability, overcoming the low bioavailability of oral administration while still allowing outpatient treatment and reduced hospitalization time
Solution Approach 2:
The patent utilizes the pneumatic mechanism of inhalation to deliver the drug directly to the pulmonary alveoli. The inhaled preparation is delivered as an aerosol or vapor that condenses in the lungs, utilizing respiratory mechanics to achieve rapid absorption and high bioavailability without the limitations of oral administration
3Reliability
If inhaled preparation with fine particles is used to improve pulmonary deposition, then bioavailability is enhanced, but drug aggregation occurs during preparation and storage
Solution Approach 1:
The patent introduces lactose as an intermediary carrier material. The magnesium isoglycyryhizinate is mixed with lactose in specific ratios (1:5 to 1:20), and the lactose acts as a spacer that prevents direct contact and aggregation of the drug particles, maintaining stability while enabling fine particle size for high pulmonary deposition and bioavailability
Solution Approach 2:
The patent applies different properties to different components of the inhaled preparation. The drug particles are micronized to fine sizes (0.5-5 μm) for high pulmonary deposition, while the lactose carrier maintains larger particle sizes and specific physical properties that prevent aggregation. This local differentiation of particle properties resolves the contradiction between fine particle requirements and aggregation prevention
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 inhaled preparation significantly enhances bioavailability, reduces side effects, and effectively treats COPD and hepatitis by delivering magnesium isoglycyrrhizinate directly to the lungs, improving patient compliance and reducing treatment costs.
Implementation Method 1
enhance pulmonary deposition and systemic absorption
Data Source
AI summary
The present invention belongs to the field of medicine, relates to an inhaled preparation of isoglycyrrhizic acid or a salt thereof, and in particular relates to an inhaled preparation of magnesium isoglycyrrhizinate and the use thereof in preparing drugs for treating respiratory system diseases.